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DE102004028751A1 - New 4-heterocyclyl-1-acyl-piperidine derivatives, useful e.g. for treating headache, diabetes and cardiovascular disease, are antagonists of calcitonin-gene related peptide - Google Patents

New 4-heterocyclyl-1-acyl-piperidine derivatives, useful e.g. for treating headache, diabetes and cardiovascular disease, are antagonists of calcitonin-gene related peptide Download PDF

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DE102004028751A1
DE102004028751A1 DE200410028751 DE102004028751A DE102004028751A1 DE 102004028751 A1 DE102004028751 A1 DE 102004028751A1 DE 200410028751 DE200410028751 DE 200410028751 DE 102004028751 A DE102004028751 A DE 102004028751A DE 102004028751 A1 DE102004028751 A1 DE 102004028751A1
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oxo
piperidin
ylmethyl
dihydro
tetrahydro
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Philipp Dr. Lustenberger
Stephan Georg Dr. Mueller
Klaus Dr. Rudolf
Dirk Dr. Stenkamp
Gerhard Schaenzle
Kirsten Dr. Arndt
Henri Dr. Doods
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Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals Inc
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Boehringer Ingelheim Pharmaceuticals Inc
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Priority to PCT/EP2005/002082 priority patent/WO2005084672A1/en
Priority to EP05715592A priority patent/EP1722792A1/en
Priority to US11/073,341 priority patent/US7205294B2/en
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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Abstract

Die vorliegende Erfindung betrifft substituierte Piperidine der allgemeinen Formel,

Figure 00000001
in der A, B, D, E,..., R1, R2 und X wie im Anspruch 1 definiert sind, deren Tautomere, deren Diastereomere, deren Enantiomere, deren Gemische und deren Salze, insbesondere deren physiologisch verträgliche Salze mit anorganischen oder organischen Säuren oder Basen, welche wertvolle pharmakologische Eigenschaften aufweisen, insbesondere CGRP-antagonistische Eigenschaften, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung.The present invention relates to substituted piperidines of the general formula
Figure 00000001
in which A, B, D, E, ..., R 1 , R 2 and X are as defined in claim 1, their tautomers, their diastereomers, their enantiomers, their mixtures and their salts, in particular their physiologically acceptable salts with inorganic or organic acids or bases which have valuable pharmacological properties, in particular CGRP-antagonistic properties, medicaments containing these compounds, their use and processes for their preparation.

Description

Gegenstand der vorliegenden Erfindung sind ausgewählte CGRP-Antagonisten der allgemeinen Formel

Figure 00010001
deren Tautomere, deren Diastereomere, deren Enantiomere, deren Hydrate, deren Gemische und deren Salze sowie die Hydrate der Salze, insbesondere deren physiologisch verträgliche Salze mit anorganischen oder organischen Säuren, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung.The present invention relates to selected CGRP antagonists of the general formula
Figure 00010001
their tautomers, their diastereomers, their enantiomers, their hydrates, their mixtures and their salts, and the hydrates of the salts, in particular their physiologically acceptable salts with inorganic or organic acids, medicaments containing these compounds, their use and processes for their preparation.

In der obigen allgemeinen Formel bedeuten in einer ersten Ausführungsform
A ein Stickstoff- oder Sauerstoffatom oder eine CH-Gruppe,
B ein Stickstoffatom, eine CH- oder eine Carbonyl-Gruppe,
D ein Wasserstoffatom oder eine Methylgruppe,
E ein Wasserstoff-, Fluor- Chlor- oder Bromatom, eine Methyl-, Ethyl- oder Trifluormethylgruppe,
X eine Methylen- oder NH-Gruppe,
---- eine Einfachbindung, wenn A ein Sauerstoffatom darstellt, oder
R1 einen Rest der Formel

Figure 00020001
und
R2 einen Rest der Formel
Figure 00020002
In the above general formula, in a first embodiment
A is a nitrogen or oxygen atom or a CH group,
B is a nitrogen atom, a CH or a carbonyl group,
D is a hydrogen atom or a methyl group,
E is a hydrogen, fluorine, chlorine or bromine atom, a methyl, ethyl or trifluoromethyl group,
X is a methylene or NH group,
---- a single bond, if A represents an oxygen atom, or
R 1 is a radical of the formula
Figure 00020001
and
R 2 is a radical of the formula
Figure 00020002

Eine zweite Ausführungsform der vorliegenden Erfindung umfasst diejenigen Verbindungen der allgemeinen Formel I, in denen
die Kombination von A, B, D, E und ---- eine Gruppe der Formel

Figure 00030001
R1 einen Rest der Formel
Figure 00040001
und
R2 einen Rest der Formel
Figure 00040002
deren Tautomere, deren Diastereomere, deren Enantiomere, deren Hydrate, deren Gemische und deren Salze sowie die Hydrate der Salze.A second embodiment of the present invention comprises those compounds of general formula I in which
the combination of A, B, D, E and ---- a group of the formula
Figure 00030001
R 1 is a radical of the formula
Figure 00040001
and
R 2 is a radical of the formula
Figure 00040002
their tautomers, their diastereomers, their enantiomers, their hydrates, their mixtures and their salts, and the hydrates of the salts.

Beispielsweise seien folgende bevorzugte Verbindungen der allgemeinen Formel I erwähnt:

  • (1) 1-1,4'-Bipiperidinyl-1'-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (2) 2-(1H-Indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (3) 1-4,4'-Bipiperidinyl-1-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (4) 1-(4-Dimethylamino-piperidin-1-yl)-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (5) (S)-2-(1H-Indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (6) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (7) 2-(1H-Indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (8) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (9) 2-(1H-Indazol-5-ylmethyl)-1-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (10) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (11) 2-(1H-Indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (12) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-butan-1,4- dion,
  • (13) 1-[4-(4-fluor-phenyl)-piperazin-1-yl]-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (14) 1-[4-(4-fluor-phenyl)-piperidin-1-yl]-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (15) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-pyridin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (16) (1'-{2-(1H-Indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butyryl}-4,4'-bipiperidinyl-1-yl)-essigsäure-methylester,
  • (17) 2-(1H-Indazol-5-ylmethyl)-1-(1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (18) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (19) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (20) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (21) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(4-dimethylamino-piperidin-1-yl)-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (22) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (23) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (24) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (25) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (26) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (27) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (28) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-2-oxo-ethyl}-amid,
  • (29) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-ethyl]-amid,
  • (30) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperazin-1-yl]-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (31) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperidin-1-yl]-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (32) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-pyridin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (33) [1'-(3-(1H-Indazol-5-yl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionyl)-4,4'-bipiperidinyl-1-yl]-essigsäure-methylester,
  • (34) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-(1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl)-2-oxo- ethyl]-amid,
  • (35) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (36) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (37) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (38) 1-(4-Dimethylamino-piperidin-1-yl)-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (39) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (40) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (41) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (42) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (43) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (44) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (45) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (46) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-butan-1,4-dion,
  • (47) 1-[4-(4-fluor-phenyl)-piperazin-1-yl]-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (48) 1-[4-(4-fluor-phenyl)-piperidin-1-yl]-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (49) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-pyridin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (50) (1'-{2-(7-Methyl-1H-indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butyryl}-4,4'-bipiperidinyl-1-yl)-essigsäure-methylester,
  • (51) 1-(1'-Methanesulfonyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (52) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (53) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (54) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (55) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(4-dimethylamino-piperidin-1-yl)-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (56) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1- yl]-2-oxo-ethyl}-amid,
  • (57) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (58) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (59) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (60) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (61) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (62) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-2-oxo-ethyl}-amid,
  • (63) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-ethyl]-amid,
  • (64) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperazin-1-yl]-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (65) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperidin-1-yl]-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (66) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-pyridin-4-yl-piperazin-1-yl)- ethyl]-amid,
  • (67) [1'-(3-(7-Methyl-1H-indazol-5-yl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionyl)-4,4'-bipiperidinyl-1-yl]-essigsäure-methylester,
  • (68) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (69) 2-(1H-Indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (70) 1-4,4'-Bipiperidinyl-1-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (71) 2-(1H-Indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (72) 2-(1H-Indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (73) 2-(1H-Indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (74) 2-(1H-Indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (75) 1-1,4'-Bipiperidinyl-1'-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (76) 1-(4-Dimethylamino-piperidin-1-yl)-2-(1H-indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (77) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (78) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (79) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo- ethyl}-amid,
  • (80) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (81) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (82) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (83) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (84) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (85) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (86) 1-4,4'-Bipiperidinyl-1-yl-2-(7-ethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (87) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (88) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (89) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (90) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (91) 2-(7-Chlor-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (92) 1-4,4'-Bipiperidinyl-1-yl-2-(7-chlor-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (93) 2-(7-Chlor-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (94) 2-(7-Chlor-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (95) 2-(7-chlor-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (96) 2-(7-Chlor-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (97) 2-(7-Brom-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (98) 1-4,4'-Bipiperidinyl-1-yl-2-(7-brom-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (99) 2-(7-Brom-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (100) 2-(7-Brom-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (101) 2-(7-Brom-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (102) 2-(7-Brom-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (103) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
  • (104) 1-4,4'-Bipiperidinyl-1-yl-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
  • (105) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (106) 4-[4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
  • (107) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
  • (108) 4-[4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
  • (109) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(1-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (110) 1-4,4'-Bipiperidinyl-1-yl-2-(1-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (111) 2-(1-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (112) 2-(1-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (113) 2-(1-Methyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (114) 2-(1-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (115) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (116) 1-4,4'-Bipiperidinyl-1-yl-2-(1,7-dimethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (117) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (118) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (119) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (120) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (121) 2-(1H-Benzotriazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (122) 2-(1H-Benzotriazol-5-ylmethyl)-1-4,4'-bipiperidinyl-1-yl-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (123) 2-(1H-Benzotriazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (124) 2-(1H-Benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (125) 2-(1H-Benzotriazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (126) 2-(1H-Benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (127) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (128) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-1H-benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (129) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (130) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (131) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (132) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (133) 2-(1H-Indol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (134) 1-4,4'-Bipiperidinyl-1-yl-2-(1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (135) 2-(1H-Indol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (136) 2-(1H-Indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3- yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (137) 2-(1H-Indol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (138) 2-(1H-Indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (139) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (140) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (141) 2-(7-Methyl-1H-indol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (142) 2-(7-Methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (143) 2-(7-Methyl-1H-indol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (144) 2-(7-Methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (145) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-ethyl-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (146) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-ethyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (147) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-ethyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (148) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-ethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (149) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-ethyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (150) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-ethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (151) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-chlor-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (152) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-chlor-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (153) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-chlor-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (154) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-chlor-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (155) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-chlor-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (156) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-chlor-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (157) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-brom-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (158) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-brom-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (159) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-brom-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (160) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-brom-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (161) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-brom-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (162) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-brom-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (163) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
  • (164) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
  • (165) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
  • (166) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
  • (167) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
  • (168) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
  • (169) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (170) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (171) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1-methyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (172) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (173) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1-methyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (174) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (175) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (176) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (177) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (178) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (179) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (180) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (181) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (182) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure (1-(1H-benzotriazol-5-ylmethyl)-2-4,4'-bipiperidinyl-1-yl-2-oxo-ethyl]-amid,
  • (183) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-benzotriazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (184) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (185) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-benzotriazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (186) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (187) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (188) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (189) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)- piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (190) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (191) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (192) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (193) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (194) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1H-indol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (195) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (196) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (197) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (198) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (199) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (200) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (201) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (202) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (203) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (204) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (205) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (206) 1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (207) 1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (208) 2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (209) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (210) 2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (211) 1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (212) 1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (213) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (214) 1-4,4'-Bipiperidinyl-1-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (215) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (216) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (217) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (218) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (219) 1-1,4'-Bipiperidinyl-1'-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (220) 1-(4-Dimethylamino-piperidin-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (221) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (222) 1-4,4'-Bipiperidinyl-1-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (223) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (224) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (225) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (226) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (227) 1-1,4'-Bipiperidinyl-1'-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (228) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(4-dimethylamino-piperidin-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (229) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (230) 1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (231) 1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (232) 2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-di hydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (233) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (234) 2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (235) 1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (236) 1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (237) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (238) 1-4,4'-Bipiperidinyl-1-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (239) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (240) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (241) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (242) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)- butan-1,4-dion,
  • (243) 1-1,4'-Bipiperidinyl-1'-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl)-butan-1,4-dion,
  • (244) 1-(4-Dimethylamino-piperidin-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (245) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (246) 1-4,4'-Bipiperidinyl-1-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (247) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (248) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (249) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (250) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (251) 1-1,4'-Bipiperidinyl-1'-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (252) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(4-dimethylamino-piperidin-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin- 1-yl]-butan-1,4-dion,
  • (253) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (254) 1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (255) 1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (256) 2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (257) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (258) 2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (259) 1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (260) 1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (261) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (262) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]- butan-1,4-dion,
  • (263) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (264) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (265) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (266) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (267) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (268) 1-(4-Dimethylamino-piperidin-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (269) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (270) 1-4,4'-Bipiperidinyl-1-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (271) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (272) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl- piperidin-1-yl)-butan-1,4-dion,
  • (273) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (274) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (275) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (276) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(4-dimethylamino-piperidin-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (277) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (278) 1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (279) 1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (280) 2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (281) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (282) 2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)- butan-1,4-dion,
  • (283) 1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (284) 1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (285) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (286) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (287) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (288) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (289) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (290) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (291) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (292) 1-(4-Dimethylamino-piperidin-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)- piperidin-1-yl]-butan-1,4-dion,
  • (293) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (294) 1-4,4'-Bipiperidinyl-1-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (295) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (296) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (297) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (298) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
  • (299) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (300) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(4-dimethylamino-piperidin-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (301) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (302) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)- ethyl]-amid,
  • (303) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (304) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (305) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (306) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (307) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (308) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (309) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (310) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (311) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
  • (312) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin- 1-yl-piperidin-1-yl)-ethyl]-amid,
  • (313) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (314) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (315) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (316) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (317) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (318) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (319) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (320) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (321) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (322) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin- 4-yl-piperazin-1-yl)-ethyl]-amid,
  • (323) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (324) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-dimethylaminopiperidin-1-yl)-2-oxo-ethyl]-amid,
  • (325) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (326) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (327) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (328) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (329) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (330) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (331) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
  • (332) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol- 6-ylmethyl)-ethyl]-amid,
  • (333) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (334) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (335) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (336) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (337) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (338) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (339) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure(2-1,4'-bipiperidinyl-1'-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (340) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (341) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (342) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)- 2-oxo-ethyl]-amid,
  • (343) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (344) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (345) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (346) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (347) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
  • (348) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-dimethylamino-piperidin-1-yl)-2-oxo-ethyl]-amid,
  • (349) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (350) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (351) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (352) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperazin-1-yl- piperidin-1-yl)-ethyl]-amid,
  • (353) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (354) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (355) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (356) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (357) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl)-amid,
  • (358) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (359) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (360) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (361) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (362) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4- piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (363) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (364) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (365) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (366) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (367) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (368) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (369) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (370) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (371) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (372) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-dimethyl amino-piperidin-1-yl)-2-oxo-ethyl]-amid,
  • (373) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (374) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (375) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (376) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (377) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (378) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (379) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (380) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
  • (381) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (382) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl methyl)-2-oxo-ethyl]-amid,
  • (383) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methylpiperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (384) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazal-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (385) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (386) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (387) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (388) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (389) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
  • (390) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (391) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
  • (392) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-pipera zin-1-yl-piperidin-1-yl)-ethyl]-amid,
  • (393) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
  • (394) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
  • (395) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
  • (396) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-dimethylamino-piperidin-1-yl)-2-oxo-ethyl]-amid,
  • (397) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidin-1-yl]-1-(4-pyrrolidin-1-yl-piperidin-1-yl)-butan-1,4-dion,
  • (398) 4-(2-Oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carbonsäure-[1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-pyrrolidin-1-yl-piperidin-1-yl)-ethyl]-amid,
deren Tautomere, deren Diastereomere, deren Enantiomere, deren Hydrate, deren Gemische und deren Salze sowie die Hydrate der Salze.For example, the following preferred compounds of general formula I may be mentioned:
  • (1) 1-1,4'-bipiperidinyl-1'-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (2) 2- (1H-Indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (3) 1-4,4'-bipiperidinyl-1-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (4) 1- (4-Dimethylamino-piperidin-1-yl) -2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (5) (S) -2- (1H-Indazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (6) 2- (1H-Indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 yl] 1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (7) 2- (1H-Indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (8) 2- (1H-Indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 yl] -1- (4-piperi din-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (9) 2- (1H-Indazol-5-ylmethyl) -1- [4- (4-methyl-perhydro-1,4-diazepin-1-yl) -piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (10) 2- (1H-Indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1] yl] -1- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (11) 2- (1H-indazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (12) 2- (1H-Indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1] yl] -1- (4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -butane-1,4-dione,
  • (13) 1- [4- (4-fluoro-phenyl) -piperazin-1-yl] -2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (14) 1- [4- (4-fluoro-phenyl) -piperidin-1-yl] -2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (15) 2- (1H-Indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1] yl] -1- (4-pyridin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (16) (1 '- {2- (1H-Indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine] 3-yl) -piperidin-1-yl] -butyryl} -4,4'-bipiperidinyl-1-yl) -acetic acid methylester,
  • (17) 2- (1H-Indazol-5-ylmethyl) -1- (1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (18) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (19) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2 - (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (20) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (21) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (22) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2 - [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (23) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2 -oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (24) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2 - [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (25) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2 -oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (26) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2 - [4- (4-methyl-perhydro-1,4-diazepin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (27) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2 -oxo-2- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (28) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2 - [4- (1-methyl-piperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -2-oxo-ethyl} -amide,
  • (29) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2 -oxo-2- (4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -ethyl] -amide,
  • (30) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -] piperazin-1-yl] -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (31) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -] piperidin-1-yl] -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (32) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2 -oxo-2- (4-pyridin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (33) [1 '- (3- (1H-Indazol-5-yl) -2 - {[4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) -piperidine-1-carbonyl] -amine o} -propionyl) -4,4'-bipiperidinyl-1-yl] -acetic acid methylester,
  • (34) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2 - (1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (35) 1-1,4'-bipiperidinyl-1'-yl-2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (36) 1- (1'-Methyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (37) 1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (38) 1- (4-Dimethylamino-piperidin-1-yl) -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (39) 2- (7-Methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (40) 2- (7-Methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (41) 2- (7-Methyl-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (42) 2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (43) 2- (7-Methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-perhydro-1,4-diazepin-1-yl) -piperidin-1-yl] -4 - [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (44) 2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (45) 2- (7-Methyl-1H-indazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -4 - [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (46) 2- (7-Methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4- piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -butan-1,4-dione,
  • (47) 1- [4- (4-fluoro-phenyl) -piperazin-1-yl] -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (48) 1- [4- (4-fluoro-phenyl) -piperidin-1-yl] -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (49) 2- (7-Methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-pyridin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (50) (1 '- {2- (7-methyl-1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) -piperidin-1-yl] -butyryl} -4,4'-bipiperidinyl-1-yl) -acetic acid methylester,
  • (51) 1- (1'-Methanesulfonyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (52) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (53) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'- bipiperidinyl-1-yl) -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (54) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (55) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (56) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazole-5-) ylmethyl) -2- [4- (4-methyl-1-piperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (57) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazole-5- ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (58) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazole-5-) ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (59) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazole-5- ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (60) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazol-5-) ylmethyl) -2- [4- (4-methyl-perhydro-1,4-diazepin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (61) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazole-5-one] ylmethyl) -2-oxo-2- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (62) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazole-5- ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -2-oxo-ethyl} -amide,
  • (63) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazole-5- ylmethyl) -2-oxo-2- (4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -ethyl] -amide,
  • (64) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -] piperazin-1-yl] -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (65) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -] piperidin-1-yl] -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (66) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazole-5-one] ylmethyl) -2-oxo-2- (4-pyridin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (67) [1 '- (3- (7-Methyl-1H-indazol-5-yl) -2 - {[4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine -3-yl) -piperidine-1-carbonyl] -amino} -propionyl) -4,4'-bipiperidinyl-1-yl] -acetic acid methylester,
  • (68) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methanesulfonyl-4,4'- bipiperidinyl-1-yl) -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (69) 2- (1H-Indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (5-oxo-3-phenyl-4 , 5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (70) 1-4,4'-bipiperidinyl-1-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1, 2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (71) 2- (1H-Indazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (72) 2- (1H-Indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine 1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (73) 2- (1H-Indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (74) 2- (1H-Indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine 1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (75) 1-1,4'-bipiperidinyl-1'-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1 , 2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (76) 1- (4-Dimethylamino-piperidin-1-yl) -2- (1H-indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1 , 2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (77) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (78) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-one yl-1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (79) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -2-oxoethyl} -amide,
  • (80) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (81) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (82) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (83) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1 ' -yl-1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (84) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidine-1-) yl) -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (85) 2- (7-Ethyl-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (86) 1-4,4'-bipiperidinyl-1-yl-2- (7-ethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (87) 2- (7-Ethyl-1H-indazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (88) 2- (7-Ethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (89) 2- (7-Ethyl-1H-indazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -piperazin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (90) 2- (7-Ethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (91) 2- (7-Chloro-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1yl] -butan-1,4-dione,
  • (92) 1-4,4'-bipiperidinyl-1-yl-2- (7-chloro-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (93) 2- (7-Chloro-1H-indazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (94) 2- (7-chloro-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (95) 2- (7-chloro-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (96) 2- (7-chloro-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (97) 2- (7-Bromo-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (98) 1-4,4'-bipiperidinyl-1-yl-2- (7-bromo-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (99) 2- (7-bromo-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (100) 2- (7-Bromo-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (101) 2- (7-Bromo-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (102) 2- (7-Bromo-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (103) 1- (1'-Methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) piperidin-1-yl] -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
  • (104) 1-4,4'-bipiperidinyl-1-yl-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
  • (105) 2- (7-Methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (106) 4- [4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazine-1) yl-piperidin-1-yl) -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
  • (107) 1- [4- (1-Methylpiperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepine-3-yl) -piperidin-1-yl] -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
  • (108) 4- [4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidine-4-) yl-piperazin-1-yl) -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
  • (109) 1- (1'-Methyl-4,4'-bipiperidinyl-1-yl) -2- (1-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (110) 1-4,4'-bipiperidinyl-1-yl-2- (1-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (111) 2- (1-Methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (112) 2- (1-Methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (113) 2- (1-Methyl-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (114) 2- (1-Methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (115) 2- (1,7-Dimethyl-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo -1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (116) 1-4,4'-bipiperidinyl-1-yl-2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4, 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (117) 2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (118) 2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (119) 2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (120) 2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (121) 2- (1H-Benzotriazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (122) 2- (1H-Benzotriazol-5-ylmethyl) -1,4,4'-bipiperidinyl-1-yl-4- [4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (123) 2- (1H-Benzotriazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (124) 2- (1H-Benzotriazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1] yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (125) 2- (1H-Benzotriazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (126) 2- (1H-Benzotriazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1] yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (127) 2- (7-Methyl-1H-benzotriazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (128) 1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-1H-benzotriazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (129) 2- (7-Methyl-1H-benzotriazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (130) 2- (7-Methyl-1H-benzotriazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (131) 2- (7-Methyl-1H-benzotriazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (132) 2- (7-Methyl-1H-benzotriazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (133) 2- (1H-Indol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (134) 1-4,4'-bipiperidinyl-1-yl-2- (1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (135) 2- (1H-Indol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (136) 2- (1H-Indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (137) 2- (1H-Indol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -piperazin-1-yl] -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (138) 2- (1H-Indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (139) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (140) 1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (141) 2- (7-Methyl-1H-indol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (142) 2- (7-Methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (143) 2- (7-Methyl-1H-indol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (144) 2- (7-Methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (145) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-ethyl-1H-indazole-5- ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (146) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (7-ethyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (147) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-ethyl-1H-indazole-5- ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (148) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-ethyl-1H-indazole-5- ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (149) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-ethyl-1H-indazole-5- ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (150) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-ethyl-1H-indazole-5- ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (151) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-1H-indazole-5- ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (152) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (7-chloro-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (153) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-1H-indazole-5- ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (154) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-1H-indazole-5- ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (155) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-1H-indazole-5- ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (156) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-1H-indazole-5- ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (157) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-bromo-1H-indazole-5- ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (158) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (7-bromo-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (159) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-bromo-1H-indazole-5- ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (160) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-bromo-1H-indazole-5- ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (161) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-bromo-1H-indazole-5- ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (162) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-bromo-1H-indazole-5- ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (163) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'- bipiperidinyl-1-yl) -2-oxo-1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
  • (164) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 2-oxo-1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
  • (165) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazine-1 -yl) piperidin-1-yl] -2-oxo-1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
  • (166) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-2- (4-pipera zin-1-yl-piperidin-1-yl) -1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
  • (167) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidine-4 yl) piperazin-1-yl] -2-oxo-1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
  • (168) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-2- (4-piperidine-4-) yl-piperazin-1-yl) -1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
  • (169) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'- bipiperidinyl-1-yl) -1- (1-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (170) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (1-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (171) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1-methyl-1H-indazole-5-) ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (172) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1-methyl-1H-indazole-5-one] ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (173) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1-methyl-1H-indazole-5- ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (174) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1-methyl-1H-indazole-5-one] ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (175) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1,7-dimethyl-1H-indazole) 5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (176) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (1,7-dimethyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (177) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1,7-dimethyl-1H-indazole) 5-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (178) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1,7-dimethyl-1H-indazole) 5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (179) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1,7-dimethyl-1H-indazole) 5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (180) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1,7-dimethyl-1H-indazole) 5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (181) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-ylmethyl) -2 - (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (182) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid (1- (1H-benzotriazol-5-ylmethyl) -2 -4,4'-bipiperidinyl-1-yl-2-oxo-ethyl] -amide,
  • (183) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-benzotriazol-5-ylmethyl) -2 - [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (184) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-ylmethyl) -2 -oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (185) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-benzotriazol-5-ylmethyl) -2 - [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (186) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-ylmethyl) -2 -oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (187) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-benzotriazole-5- ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (188) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (7-methyl-1H-benzotriazole-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (189) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-benzotriazole-5- ylmethyl) -2- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (190) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-benzotriazole-5- ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (191) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-benzotriazole-5- ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (192) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-benzotriazole-5- ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (193) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indol-5-ylmethyl) -2 - (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (194) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (1H-indol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (195) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indol-5-ylmethyl) -2 - [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (196) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indol-5-yl thyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (197) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indol-5-ylmethyl) -2 - [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (198) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indol-5-ylmethyl) -2 -oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (199) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'- bipiperidinyl-1-yl) -1- (7-methyl-1H-indol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (200) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (7-methyl-1H-indol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (201) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indole-5-) ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (202) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indole-5-) ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (203) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indole-5-) ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (204) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indole-5-) ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (205) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (206) 1-4,4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (207) 1- [4- (4-Methylpiperazin-1-yl) -piperidin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [ 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (208) 2- (2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (209) 1- [4- (1-Methylpiperidin-4-yl) piperazin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [ 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (210) 2- (2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (211) 1-1,4'-bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2 , 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (212) 1- (4-Dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (213) 1- (1'-Methyl-4,4'-bipiperidinyl-1-yl) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [ 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (214) 1-4,4'-bipiperidinyl-1-yl-2- (4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -4- [4- (2-yl) oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (215) 2- (4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (216) 2- (4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepine-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (217) 2- (4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (218) 2- (4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepine-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (219) 1-1,4'-Bipiperidinyl-1'-yl-2- (4- methyl-2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl) -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (220) 1- (4-Dimethylamino-piperidin-1-yl) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo -1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (221) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [ 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (222) 1-4,4'-bipiperidinyl-1-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo) 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (223) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (224) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepine-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (225) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (226) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepine-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (227) 1-1,4'-Bipiperidinyl-1'-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo -1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (228) 2- (4-Chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (4-dimethylamino-piperidin-1-yl) -4- [4- (2-oxo -1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (229) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (230) 1-4,4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl) 4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (231) 1- [4- (4-Methylpiperazin-1-yl) -piperidin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [ 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (232) 2- (2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4- triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (233) 1- [4- (1-Methylpiperidin-4-yl) piperazin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [ 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (234) 2- (2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazole -1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (235) 1-1,4'-Bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl -4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (236) 1- (4-Dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (237) 1- (1'-Methyl-4,4'-bipiperidinyl-1-yl) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [ 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (238) 1-4,4'-bipiperidinyl-1-yl-2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5- oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (239) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (240) 2- (4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2 , 4-triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (241) 2- (4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -piperazin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (242) 2- (4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2 , 4-triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione,
  • (243) 1-1,4'-Bipiperidinyl-1'-yl-2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl) -4- [4- (5 -oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl) -butan-1,4-dione,
  • (244) 1- (4-Dimethylamino-piperidin-1-yl) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo -3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (245) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [ 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (246) 1-4,4'-bipiperidinyl-1-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo) 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (247) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (248) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2 , 4-triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (249) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (250) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2 , 4-triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (251) 1-1,4'-Bipiperidinyl-1'-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo -3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (252) 2- (4-Chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (4-dimethylamino-piperidin-1-yl) -4- [4- (5-oxo 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione,
  • (253) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (254) 1-4,4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (255) 1- [4- (4-Methylpiperazin-1-yl) -piperidin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4 - [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (256) 2- (2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine -3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (257) 1- [4- (1-Methylpiperidin-4-yl) piperazin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4 - [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (258) 2- (2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine -3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (259) 1-1,4'-Bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (260) 1- (4-Dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (261) 1- (1'-Methyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4 - [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (262) 1-4,4'-Bipiperidinyl-1-yl-2- (7-methyl-2-oxo-2,3-dihydro-1 H -benzimidazol-5-ylmethyl) -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione,
  • (263) 2- (7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidine-1 yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (264) 2- (7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (265) 2- (7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazine-1] yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (266) 2- (7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (267) 1-1,4'-bipiperidinyl-1'-yl-2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (268) 1- (4-Dimethylamino-piperidin-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (269) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4 - [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (270) 1-4,4'-bipiperidinyl-1-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (271) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidine-1] yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (272) 2- (7-Chloro-2-oxo-2,3-dihydro-1 H -benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butane-1,4-dione,
  • (273) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazine-1] yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (274) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (275) 1-1,4'-bipiperidinyl-1'-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (276) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (4-dimethylamino-piperidin-1-yl) -4- [4- (2 oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (277) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (278) 1-4,4'-Bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-1 H -benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-) phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (279) 1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4 - (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione;
  • (280) 2- (2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4 triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (281) 1- [4- (1-Methylpiperidin-4-yl) piperazin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4 - [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (282) 2- (2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4 -triazol-1-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione,
  • (283) 1-1,4'-Bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (284) 1- (4-Dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (285) 1- (1'-Methyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4 - [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (286) 1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5- oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (287) 2- (7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidine-1] yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione .
  • (288) 2- (7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1 , 2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (289) 2- (7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazine-1] yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione .
  • (290) 2- (7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1 , 2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (291) 1-1,4'-bipiperidinyl-1'-yl-2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5 -oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (292) 1- (4-Dimethylamino-piperidin-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5 oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione,
  • (293) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4 - [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (294) 1-4,4'-bipiperidinyl-1-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5- oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (295) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidine-1] yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione .
  • (296) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1 , 2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (297) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazine-1] yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione .
  • (298) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1 , 2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
  • (299) 1-1,4'-Bipiperidinyl-1'-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo- 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (300) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (4-dimethylamino-piperidin-1-yl) -4- [4- (5 -oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
  • (301) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'- bipiperidinyl-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (302) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (303) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazine-1 -yl) piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (304) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (305) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidine-4 yl) piperazin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (306) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (307) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (308) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (309) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'- bipiperidinyl-1-yl) -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (310) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (311) 2- (4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
  • (312) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (313) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (4-methyl-2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (314) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (315) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (316) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (317) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (318) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (319) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo-2,3-dihydro benzoxazol-6-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (320) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (321) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (322) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (323) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl -1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (324) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2- (4-dimethylaminopiperidine-1-yl) -2-oxo-ethyl] -amide,
  • (325) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4 '-bipiperidinyl-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (326) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-one yl-2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (327) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazine -1-yl) piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (328) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (329) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidine -4-yl) piperazine-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (330) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (331) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1 ' -yl-2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (332) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidine-1-) yl) -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
  • (333) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4 '-bipiperidinyl-1-yl) -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (334) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-one yl-1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (335) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4-methyl-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (336) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (337) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4-methyl-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (338) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (339) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid (2-1,4'-bipiperidinyl-1'-yl 1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (340) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidine-1-) yl) -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (341) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (342) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-one yl-1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (343) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (344) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (345) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (346) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (347) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1 ' -yl-1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
  • (348) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -2- (4-dimethylamino-piperidin-1-yl) -2-oxo-ethyl] -amide,
  • (349) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'- bipiperidinyl-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (350) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (351) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazine-1 -yl) piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (352) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (353) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidine-4 yl) piperazin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (354) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (355) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (356) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (357) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'- bipiperidinyl-1-yl) -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl) -amide,
  • (358) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (359) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo-2,3-dihydro -1H-benzimidazol-5-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (360) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (361) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (362) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (363) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (364) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (365) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (366) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl] 1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (367) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (368) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (369) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (370) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (371) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl -1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (372) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-dimethylamino-piperidin-1-yl) -2-oxo-ethyl] -amide,
  • (373) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4 '-bipiperidinyl-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (374) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-one yl-2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (375) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazine -1-yl) piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (376) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (377) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidine -4-yl) piperazine-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (378) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (379) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl 2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (380) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidine-1-) yl) -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
  • (381) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4 '-bipiperidinyl-1-yl) -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (382) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-one yl-1- (7-methyl-2-oxo-2,3-dihydro-1 H -benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (383) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (384) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo) 2,3-dihydro-1H-benzimidazal-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (385) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (386) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (387) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1 ' -yl-1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (388) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidine-1-) yl) -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (389) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
  • (390) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-one yl-1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (391) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
  • (392) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
  • (393) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
  • (394) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
  • (395) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1 ' -yl-1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
  • (396) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-dimethylamino-piperidin-1-yl) -2-oxo-ethyl] -amide,
  • (397) 2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydrobenzo [d] [1,3] diazepin-3-yl) piperidin-1-yl] -1- (4-pyrrolidin-1-yl-piperidin-1-yl) -butan-1,4-dione,
  • (398) 4- (2-Oxo-1,2,4,5-tetrahydro-benzo [d] [1,3] diazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazole) 5-ylmethyl) -2-oxo-2- (4-pyrrolidin-1-yl-piperidin-1-yl) -ethyl] -amide,
their tautomers, their diastereomers, their enantiomers, their hydrates, their mixtures and their salts, and the hydrates of the salts.

Die Verbindungen der allgemeinen Formel (I) werden nach prinzipiell bekannten Methoden hergestellt. Die folgenden Verfahren haben sich zur Herstellung der erfindungsgemäßen Verbindungen der allgemeinen Formel (I) besonders bewährt:

  • (a) Zur Herstellung von Verbindungen der allgemeinen Formel (I), in der X die NH-Gruppe bedeutet und A, B, D, E, ----, R1 und R2 wie eingangs erwähnt definiert sind: Umsetzung von Piperidinen der allgemeinen Formel
    Figure 00430001
    in der R1 wie eingangs erwähnt definiert ist, mit Kohlensäurederivaten der allgemeinen Formel
    Figure 00430002
    in der G eine nucleofuge Gruppe, bevorzugt die Phenoxy-, 1H-Imidazol-1-yl-, 1H-1,2,4-Triazol-1-yl-, Trichlormethoxy- oder die 2,5-Dioxopyrrolidin-1-yloxy-Gruppe bedeutet, und mit primären Aminen der allgemeinen Formel
    Figure 00430003
    in der A, B, D, E, ---- und R2 wie eingangs erwähnt definiert ist, mit der Maßgabe, dass diese Gruppen keine weitere freie primäre oder sekundäre aliphatische Aminofunktion enthalten.
The compounds of general formula (I) are prepared by methods known in principle. The following processes have proven particularly suitable for the preparation of the compounds of general formula (I) according to the invention:
  • (A) For the preparation of compounds of the general formula (I) in which X is the NH group and A, B, D, E, ----, R 1 and R 2 are defined as mentioned above: reaction of piperidines the general formula
    Figure 00430001
    in which R 1 is defined as mentioned above, with carbonic acid derivatives of the general formula
    Figure 00430002
    in the G is a nucleofugic group, preferably the phenoxy, 1H-imidazol-1-yl, 1H-1,2,4-triazol-1-yl, trichloromethoxy or the 2,5-dioxopyrrolidin-1-yloxy- Group means, and with primary amines of the general formula
    Figure 00430003
    in which A, B, D, E, ---- and R 2 are defined as mentioned above, with the proviso that these groups contain no further free primary or secondary aliphatic amino function.

Die im Prinzip zweistufigen Reaktionen werden in der Regel als Eintopfverfahren durchgeführt, und zwar bevorzugt in der Weise, dass man in der ersten Stufe eine der beiden Komponenten (III) oder (V) mit äquimolaren Mengen des Kohlensäurederivates der allgemeinen Formel (IV) in einem geeigneten Lösungsmittel bei tieferer Temperatur zur Reaktion bringt, anschließend wenigstens äquimolare Mengen der anderen Komponente (III) oder (V) zugibt und die Umsetzung bei höherer Temperatur beendet. Die Umsetzungen mit Bis-(trichlormethyl)-carbonat werden bevorzugt in Gegenwart von wenigstens 2 Äquivalenten (bezogen auf Bis-(trichlormethyl)-carbonat) einer tertiären Base, beispielsweise von Triethylamin, N-Ethyldiisopropylamin, Pyridin, 1,5-Diaza-bicyclo-[4,3,0]-non-5-en, 1,4-Diazabicyclo[2,2,2]octan oder 1,8-Diazabicyclo-[5,4,0]-un-dec-7-en, durchgeführt. Als Lösungsmittel, die wasserfrei sein sollten, kommen beispielsweise Tetrahydrofuran, Dioxan, Dimethylformamid, Dimethylacetamid, N-Methyl-2-pyrrolidon, 1,3-Dimethyl-2-imidazolidinon oder Acetonitril in Betracht, bei Verwendung von Bis-(trichlormethyl)-carbonat als Carbonylkomponente werden wasserfreie Chlorkohlenwasserstoffe, beispielsweise Dichlormethan, 1,2-Dichlorethan oder Trichlorethylen, bevorzugt. Die Reaktionstemperaturen liegen für die erste Reaktionsstufe zwischen –30°C und +25°C, bevorzugt –5°C und +10°C, für die zweite Reaktionsstufe zwischen +15°C und der Siedetemperatur des verwendeten Lösungsmittels, bevorzugt zwischen +20°C und +70°C (Siehe auch: H. A. Staab und W. Rohr, "Synthesen mit heterocyclischen Amiden (Azoliden)", Neuere Methoden der Präparativen Organischen Chemie, Band V, S. 53-93, Verlag Chemie, Weinheim/Bergstr., 1967; P. Majer und R.S. Randad, J. Org. Chem. 59, S. 1937-1938 (1994); K. Takeda, Y. Akagi, A. Saiki, T. Sukahara und H. Ogura, Tetrahedron Letters 24 (42), 4569-4572 (1983)).

  • (b) Zur Herstellung von Verbindungen der allgemeinen Formel (I), in der X die Methylengruppe bedeutet und A, B, D, E, ----, R1 und R2 wie eingangs erwähnt definiert sind, mit der Maßgabe, dass diese Gruppen keine weitere freie primäre oder sekundäre aliphatische Aminofunktion enthalten: Kupplung einer Carbonsäure der allgemeinen Formel
    Figure 00450001
    in der A, B, D, E, ---- und R2 wie eingangs erwähnt definiert sind, mit einem Piperidin der allgemeinen Formel
    Figure 00450002
    in der R1 die eingangs erwähnten Bedeutungen besitzt.
The two-stage reactions in principle are generally carried out as a one-pot process, preferably in such a way that in the first stage one of the two components (III) or (V) with equimolar amounts of the carbonic acid derivative of the general formula (IV) in a brings appropriate solvent at a lower temperature to the reaction, then at least equimolar amounts of the other component (III) or (V) is added and the reaction is terminated at a higher temperature. The reactions with bis (trichloromethyl) carbonate are preferably in the presence of at least 2 equivalents (based on bis (trichloromethyl) carbonate) of a tertiary base, for example of triethylamine, N-ethyldiisopropylamine, pyridine, 1,5-diaza-bicyclo - [4,3,0] -non-5-ene, 1,4-diazabicyclo [2,2,2] octane or 1,8-diazabicyclo [5,4,0] -un-dec-7-ene , carried out. Suitable solvents which should be anhydrous, for example, tetrahydrofuran, dioxane, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, 1,3-dimethyl-2-imidazolidinone or acetonitrile into consideration when using bis (trichloromethyl) carbonate Anhydrous chlorohydrocarbons, for example dichloromethane, 1,2-dichloroethane or trichlorethylene, are preferred as the carbonyl component. The reaction temperatures are for the first reaction stage between -30 ° C and + 25 ° C, preferably -5 ° C and + 10 ° C, for the second reaction stage between + 15 ° C and the boiling temperature of the solvent used, preferably between + 20 ° C and + 70 ° C (See also: HA Staab and W. Rohr, "Syntheses with Heterocyclic Amides (Azolides)", Newer Methods of Preparative Organic Chemistry, Volume V, pp. 53-93, Verlag Chemie, Weinheim / Bergstr. 1967; P. Majer and RS Randad, J. Org. Chem. 59, 1937-1938 (1994); K. Takeda, Y. Akagi, A. Saiki, T. Sukahara and H. Ogura, Tetrahedron Letters 24 (42), 4569-4572 (1983)).
  • (b) For the preparation of compounds of general formula (I) in which X represents the methylene group and A, B, D, E, ----, R 1 and R 2 are as defined above, with the proviso that these groups contain no further free primary or secondary aliphatic amino function: Coupling of a carboxylic acid of the general formula
    Figure 00450001
    in which A, B, D, E, ---- and R 2 are defined as mentioned above, with a piperidine of the general formula
    Figure 00450002
    in which R 1 has the meanings mentioned above.

Die Kupplung wird bevorzugt unter Verwendung von aus der Peptidchemie bekannten Verfahren (siehe z. B. Houben-Weyl, Methoden der Organischen Chemie, Bd. 15/2) durchgeführt, wobei zum Beispiel Carbodiimide, wie z.B. Dicyclohexylcarbodiimid (DCC), Diisopropylcarbodiimid (DIC) oder Ethyl-(3-dimethylaminopropyl)-carbodiimid, O-(1H-Benzotriazol-1-yl)-N,N-N',N'-tetramethyluronium-hexafluorphosphat (HBTU) oder -tetrafluorborat (TBTU) oder 1H-Benzotriazol-1-yl-oxytris-(dimethylamino)-phosphoniumhexafluorphosphat (BOP) eingesetzt werden. Durch Zugabe von 1-Hydroxybenzotriazol (HOBt) oder von 3-Hydroxy-4-oxo-3,4-dihydro-1,2,3-benzotriazin (HOObt) kann die Reaktionsgeschwindigkeit gesteigert werden. Die Kupplungen werden normalerweise mit äquimolaren Anteilen der Kupplungskomponenten sowie des Kupplungsreagenz in Lösungsmitteln wie Dichlormethan, Tetrahydrofuran, Acetonitril, Dimethylformamid (DMF), Dimethylacetamid (DMA), N-Methylpyrrolidon (NMP) oder Gemischen aus diesen und bei Temperaturen zwischen –30°C und +30°C, bevorzugt –20°C und +25°C, durchgeführt. Sofern erforderlich, wird als zusätzliche Hilfsbase N-Ethyldiisopropylamin (DIEA) (Hünig-Base) bevorzugt.The Coupling is preferred using peptide chemistry known processes (see, for example, Houben-Weyl, Methoden der Organischen Chemie, Vol. 15/2), for example, carbodiimides, e.g. dicyclohexylcarbodiimide (DCC), diisopropylcarbodiimide (DIC) or ethyl (3-dimethylaminopropyl) carbodiimide, O- (1H-benzotriazol-1-yl) -N, N-N ', N'-tetramethyluronium hexafluorophosphate (HBTU) or tetrafluoroborate (TBTU) or 1H-benzotriazol-1-yl-oxytris- (dimethylamino) phosphonium hexafluorophosphate (BOP) are used. By addition of 1-hydroxybenzotriazole (HOBt) or 3-hydroxy-4-oxo-3,4-dihydro-1,2,3-benzotriazine (HOObt) the reaction rate can be increased. The couplings are usually equimolar Proportions of Coupling Components and Coupling Reagent in solvents such as dichloromethane, tetrahydrofuran, acetonitrile, dimethylformamide (DMF), dimethylacetamide (DMA), N-methylpyrrolidone (NMP) or mixtures from these and at temperatures between -30 ° C and + 30 ° C, preferably -20 ° C and + 25 ° C performed. Provided required, as an additional auxiliary base N-ethyldiisopropylamine (DIEA) (Hünig base) prefers.

Als weiteres Kupplungsverfahren zur Synthese von Verbindungen der allgemeinen Formel (I) wird das sogenannte "Anhydridverfahren" (siehe auch: M. Bodanszky, "Peptide Chemistry", Springer-Verlag 1988, S. 58-59; M. Bodanszky, "Principles of Peptide Synthesis", Springer-Verlag 1984, S. 21-27) eingesetzt. Bevorzugt wird das "gemischte Anhydridverfahren" in der Variante nach Vaughan (J.R. Vaughan Jr., J. Amer. Chem. Soc. 73, 3547 (1951)), bei der unter Verwendung von Chlorkohlensäureisobutylester in Gegenwart von Basen, wie 4-Methylmorpholin oder 4-Ethylmorpholin, das gemischte Anhydrid aus der zu kuppelnden Carbonsäure der allgemeinen Formel (VI) und dem Kohlensäure-monoisobutylester erhalten wird. Die Herstellung dieses gemischten Anhydrids und die Kupplung mit Aminen erfolgt im Eintopfverfahren, unter Verwendung der vorstehend genannten Lösungsmittel und bei Temperaturen zwischen –20 und +25°C, bevorzugt 0°C und +25°C.

  • (c) Zur Herstellung von Verbindungen der allgemeinen Formel (I), in der X die Methylengruppe bedeutet und A, B, D, E, ----, R1 und R2 wie eingangs erwähnt definiert sind, mit der Maßgabe, dass diese Gruppen kein freies primäres oder sekundäres Amin enthalten: Kupplung einer Verbindung der allgemeinen Formel
    Figure 00460001
    in der A, B, D, E, ----, und R2 wie eingangs erwähnt definiert sind, mit der Maßgabe, dass R2 kein primäres oder sekundäres Amin enthält, und Nu eine Austrittsgruppe, beispielsweise ein Halogenatom, wie das Chlor-, Brom- oder Iodatom, eine Alkylsulfonyloxygruppe mit 1 bis 10 Kohlenstoffatomen im Alkylteil, eine gegebenenfalls durch Chlor- oder Bromatome, durch Methyl- oder Nitrogruppen mono-, di- oder trisubstituierte Phenylsulfonyloxy- oder Naphthylsulfonyloxygruppe, wobei die Substituenten gleich oder verschieden sein können, eine 1H-Imidazol-1-yl-, eine gegebenenfalls durch eine oder zwei Methylgruppen im Kohlenstoffgerüst substituierte 1H-Pyrazol-1-yl-, eine 1H-1,2,4-Triazol-1-yl-, 1H-1,2,3-Triazol-1-yl-, 1H-1,2,3,4-Tetrazol-1-yl-, eine Vinyl-, Propargyl-, p-Nitrophenyl-, 2,4-Dinitrophenyl-, Trichlorphenyl-, Pentachlorphenyl-, Pentafluorphenyl-, Pyranyl- oder Pyridinyl-, eine Dimethylaminyloxy-, 2(1H)-Oxopyridin-1-yl-oxy-, 2,5-Dioxopyrrolidin-1-yloxy-, Phthalimidyloxy-, 1H-Benzo-triazol-1-yloxy- oder Azidgruppe bedeutet, mit einem Piperidin der allgemeinen Formel
    Figure 00470001
    in der R1 wie eingangs erwähnt definiert ist.
Another coupling method for the synthesis of compounds of the general formula (I) is the so-called "anhydride method" (see also: M. Bodanszky, "Peptide Chemistry", Springer-Verlag 1988, pages 58-59, M. Bodanszky, "Principles of Peptide Synthesis ", Springer-Verlag 1984, p 21-27). Preference is given to the "mixed anhydride process" in the variant according to Vaughan (JR Vaughan Jr., J. Amer Chem. Soc., 73, 3547 (1951)) using isobutyl chloroformate in the presence of bases, such as 4-methylmorpholine or 4-ethylmorpholine, the mixed anhydride is obtained from the carboxylic acid of the general formula (VI) to be coupled and the carbonic monoisobutyl ester. The preparation of this mixed anhydride and the coupling with amines is carried out in a one-pot process, using the abovementioned solvents and at temperatures between -20 and + 25 ° C, preferably 0 ° C and + 25 ° C.
  • (C) For the preparation of compounds of general formula (I), in which X represents the methylene group and A, B, D, E, ----, R 1 and R 2 are defined as mentioned above, with the proviso that these groups do not contain a free primary or secondary amine: Coupling of a compound of the general formula
    Figure 00460001
    in which A, B, D, E, ----, and R 2 are defined as mentioned above, with the proviso that R 2 is not a primary one or Nu is a leaving group, for example a halogen atom, such as the chlorine, bromine or iodine atom, an alkylsulfonyloxy group having 1 to 10 carbon atoms in the alkyl moiety, one optionally substituted by chlorine or bromine atoms, by methyl or nitro mono-, di- or trisubstituted phenylsulfonyloxy or naphthylsulfonyloxy group, where the substituents may be identical or different, a 1H-imidazol-1-yl, a 1H-pyrazol-1-yl, optionally substituted by one or two methyl groups in the carbon skeleton, a 1H- 1,2,4-triazol-1-yl, 1H-1,2,3-triazol-1-yl, 1H-1,2,3,4-tetrazol-1-yl, a vinyl, propargyl -, p-nitrophenyl, 2,4-dinitrophenyl, trichlorophenyl, pentachlorophenyl, pentafluorophenyl, pyranyl or pyridinyl, a Dimethylaminyloxy-, 2 (1H) -oxopyridin-1-yl-oxy-, 2.5 Dioxopyrrolidin-1-yloxy, phthalimidyloxy, 1H-benzo-triazol-1-yloxy or azide group, with a piperidine of the general formula
    Figure 00470001
    in which R 1 is defined as mentioned above.

Die Umsetzung wird unter Schotten-Baumann- oder Einhorn-Bedingungen durchgeführt, das heißt die Komponenten werden in Gegenwart von wenigstens einem Äquivalent einer Hilfsbase bei Temperaturen zwischen –50°C und +120°C, bevorzugt –10°C und +30°C, und gegebenenfalls in Gegenwart von Lösungsmitteln zur Reaktion gebracht. Als Hilfsbasen kommen bevorzugt Alkali- und Erdalkalihydroxide, beispielsweise Natriumhydroxid, Kaliumhydroxid oder Bariumhydroxid, Alkalicarbonate, z. B. Natriumcarbonat, Kaliumcarbonat oder Cäsiumcarbonat, Alkaliacetate, z.B. Natrium- oder Kaliumacetat, sowie tertiäre Amine, beispielsweise Pyridin, 2,4,6-Tri-methylpyridin, Chinolin, Triethylamin, N-Ethyl-diisopropylamin, N-Ethyl-dicyclohexylamin, 1,4-Di-azabicyclo[2,2,2]octan oder 1,8-Diazabicyclo[5,4,0]-undec-7-en, als Lösungsmittel beispielsweise Dichlormethan, Tetrahydrofuran, 1,4-Dioxan, Acetonitril, Dimethylformamid, Dimethylacetamid, N-Methylpyrrolidon oder Gemische davon in Betracht; werden als Hilfsbasen Alkali- oder Erdalkalihydroxide, Alkalicarbonate oder -acetate verwendet, kann dem Reaktionsgemisch auch Wasser als Cosolvens zugesetzt werden.

  • (d) Zur Herstellung von Verbindungen der allgemeinen Formel (I), in der alle Reste wie eingangs erwähnt definiert sind: Kupplung einer Carbonsäure der allgemeinen Formel
    Figure 00480001
    in der A, B, D, E, ----, R1 und X wie eingangs erwähnt definiert sind, mit einem Amin R2 mit der Maßgabe, dass keine weitere freie primäre oder sekundäre, aliphatische Aminofunktion enthalten ist.
The reaction is carried out under Schotten-Baumann or unicorn conditions, ie the components are reacted in the presence of at least one equivalent of an auxiliary base at temperatures between -50 ° C and + 120 ° C, preferably -10 ° C and + 30 ° C , and optionally reacted in the presence of solvents. Preferred auxiliary bases are alkali metal and alkaline earth metal hydroxides, for example sodium hydroxide, potassium hydroxide or barium hydroxide, alkali metal carbonates, eg. Example, sodium carbonate, potassium carbonate or cesium carbonate, alkali metal acetate, for example sodium or potassium acetate, and tertiary amines, for example pyridine, 2,4,6-tri-methylpyridine, quinoline, triethylamine, N-ethyl-diisopropylamine, N-ethyl-dicyclohexylamine, 1 , 4-Di-azabicyclo [2,2,2] octane or 1,8-diazabicyclo [5,4,0] undec-7-ene, as solvents, for example, dichloromethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, dimethylformamide Dimethylacetamide, N-methylpyrrolidone or mixtures thereof; If alkali metal or alkaline earth metal hydroxides, alkali metal carbonates or acetates are used as auxiliary bases, water may also be added to the reaction mixture as cosolvent.
  • (d) For the preparation of compounds of the general formula (I) in which all radicals are defined as mentioned above: coupling of a carboxylic acid of the general formula
    Figure 00480001
    in which A, B, D, E, ----, R 1 and X are as defined above, with an amine R 2 with the proviso that no further free primary or secondary, aliphatic amino function is included.

Die Kupplung wird bevorzugt unter Verwendung von aus der Peptidchemie bekannten Verfahren (siehe z. B. Houben-Weyl, Methoden der Organischen Chemie, Bd. 15/2) durchgeführt, wobei zum Beispiel Carbodiimide, wie z.B. Dicyclohexylcarbodiimid (DCC), Diisopropylcarbodiimid (DIC) oder Ethyl-(3-dimethylamino-propyl)carbodiimid, O-(1H-Benzotriazol-1-yl)-N,N-N',N'-tetramethyluronium-hexa-fluorphosphat (HBTU) oder -tetrafluorborat (TBTU) oder 1H-Benzotriazol-1-yl-oxytris-(dimethylamino)-phosphoniumhexafluorphosphat (BOP) eingesetzt werden. Durch Zugabe von 1-Hydroxybenzotriazol (HOBt) oder von 3-Hydroxy-4-oxo-3,4-dihydro-1,2,3-benzotriazin (HOObt) kann die Reaktionsgeschwindigkeit gesteigert werden. Die Kupplungen werden normalerweise mit äquimolaren Anteilen der Kupplungskomponenten sowie des Kupplungsreagenz in Lösungsmitteln wie Dichlormethan, Tetrahydrofuran, Acetonitril, Dimethylformamid (DMF), Dimethylacetamid (DMA), N-Methylpyrrolidon (NMP) oder Gemischen aus diesen und bei Temperaturen zwischen –30 und +30°C, bevorzugt –20 und +25°C, durchgeführt. Sofern erforderlich wird als zusätzliche Hilfsbase N-Ethyldiisopropylamin (DIEA) (Hünig-Base) bevorzugt.The Coupling is preferred using peptide chemistry known processes (see, for example, Houben-Weyl, Methoden der Organischen Chemie, Vol. 15/2), for example, carbodiimides, e.g. dicyclohexylcarbodiimide (DCC), diisopropylcarbodiimide (DIC) or ethyl (3-dimethylamino-propyl) carbodiimide, O- (1H-benzotriazol-1-yl) -N, N-N ', N'-tetramethyluronium hexa-fluorophosphate (HBTU) or tetrafluoroborate (TBTU) or 1H-benzotriazol-1-yl-oxytris- (dimethylamino) phosphonium hexafluorophosphate (BOP) are used. By addition of 1-hydroxybenzotriazole (HOBt) or 3-hydroxy-4-oxo-3,4-dihydro-1,2,3-benzotriazine (HOObt), the reaction rate can be increased. The couplings are usually equimolar Proportions of Coupling Components and Coupling Reagent in solvents such as dichloromethane, tetrahydrofuran, acetonitrile, dimethylformamide (DMF), dimethylacetamide (DMA), N-methylpyrrolidone (NMP) or mixtures from these and at temperatures between -30 and + 30 ° C, preferably -20 and + 25 ° C, performed. Provided is required as additional Auxiliary base N-ethyldiisopropylamine (DIEA) (Hünig base) is preferred.

Als weiteres Kupplungsverfahren zur Synthese von Verbindungen der allgemeinen Formel (I) wird das sogenannte "Anhydridverfahren" (siehe auch: M. Bodanszky, "Peptide Chemistry", Springer-Verlag 1988, S. 58-59; M. Bodanszky, "Principles of Peptide Synthesis", Springer-Verlag 1984, S. 21-27) eingesetzt. Bevorzugt wird das "gemischte Anhydridverfahren" in der Variante nach Vaughan (J.R. Vaughan Jr., J. Amer. Chem. Soc. 73, 3547 (1951)), bei der unter Verwendung von Chlorkohlensäureisobutylester in Gegenwart von Basen, wie 4-Methylmorpholin oder 4-Ethylmorpholin, das gemischte Anhydrid aus der zu kuppelnden Carbonsäure der allgemeinen Formel (VIII) und dem Kohlensäure-monoisobutylester erhalten wird. Die Herstellung dieses gemischten Anhydrids und die Kupplung mit den Aminen R2 erfolgt im Eintopfverfahren, unter Verwendung der vorstehend genannten Lösungsmittel und bei Temperaturen zwischen –20°C und +25°C, bevorzugt zwischen 0°C und +25°C.

  • (e) Zur Herstellung von Verbindungen der allgemeinen Formel (I), in der alle Reste wie eingangs erwähnt definiert sind: Kupplung einer Verbindung der allgemeinen Formel
    Figure 00490001
    in der A, B, D, E, ----, R1 und X wie eingangs erwähnt definiert sind und Nu eine Austrittsgruppe, beispielsweise ein Halogenatom, wie das Chlor-, Brom- oder Iodatom, eine Alkylsulfonyloxygruppe mit 1 bis 10 Kohlenstoffatomen im Alkylteil, eine gegebenenfalls durch Chlor- oder Bromatome, durch Methyl- oder Nitrogruppen mono-, di- oder trisubstituierte Phenylsulfonyloxy- oder Naphthylsulfonyloxygruppe, wobei die Substituenten gleich oder verschieden sein können, eine 1H-Imidazol-1-yl-, eine gegebenenfalls durch eine oder zwei Methylgruppen im Kohlenstoffgerüst substituierte 1H-Pyrazol-1-yl-, eine 1H-1,2,4-Triazol-1-yl-, 1H-1,2,3-Triazol-1-yl-, 1H-1,2,3,4-Tetrazol-1-yl-, eine Vinyl-, Propargyl-, p-Nitrophenyl-, 2,4-Dinitrophenyl-, Trichlorphenyl-, Pentachlorphenyl-, Pentafluorphenyl-, Pyranyl- oder Pyridinyl-, eine Dimethylaminyloxy-, 2(1H)-Oxopyridin-1-yl-oxy-, 2,5-Dioxopyrrolidin-1-yloxy-, Phthalimidyloxy-, 1H-Benzo-triazol-1-yloxy- oder Azidgruppe bedeutet, mit einem Amin R2, mit der Maßgabe, dass keine weitere freie primäre oder sekundäre aliphatische Aminofunktion enthalten ist.
Another coupling method for the synthesis of compounds of the general formula (I) is the so-called "anhydride method" (see also: M. Bodanszky, "Peptide Chemistry", Springer-Verlag 1988, pages 58-59, M. Bodanszky, "Principles of Peptide Synthesis ", Springer-Verlag 1984, p 21-27). Preference is given to the "mixed anhydride process" in the variant according to Vaughan (JR Vaughan Jr., J. Amer Chem. Soc., 73, 3547 (1951)) using isobutyl chloroformate in the presence of bases, such as 4-methylmorpholine or 4-ethylmorpholine, the mixed anhydride is obtained from the to-be-coupled carboxylic acid of the general formula (VIII) and the carbonic monoisobutyl ester. The preparation of this mixed anhydride and the coupling with the amines R 2 is carried out in a one-pot process, using the abovementioned solvents and at temperatures between -20 ° C and + 25 ° C, preferably between 0 ° C and + 25 ° C.
  • (E) For the preparation of compounds of the general formula (I) in which all radicals are defined as mentioned above: coupling of a compound of the general formula
    Figure 00490001
    in which A, B, D, E, ----, R 1 and X are defined as mentioned above and Nu is a leaving group, for example a halogen atom, such as the chlorine, bromine or iodine atom, an alkylsulfonyloxy group having 1 to 10 carbon atoms in the alkyl moiety, an optionally substituted by chlorine or bromine atoms, by methyl or nitro groups mono-, di- or trisubstituted Phenylsulfonyloxy- or Naphthylsulfonyloxygruppe, where the substituents may be identical or different, a 1H-imidazol-1-yl, optionally by 1H-pyrazol-1-yl substituted in the carbon skeleton by one or two methyl groups, 1H-1,2,4-triazol-1-yl, 1H-1,2,3-triazol-1-yl, 1H-1 , 2,3,4-tetrazol-1-yl, a vinyl, propargyl, p-nitrophenyl, 2,4-dinitrophenyl, trichlorophenyl, pentachlorophenyl, pentafluorophenyl, pyranyl or pyridinyl, a dimethylaminyloxy -, 2 (1H) -oxopyridin-1-yl-oxy, 2,5-dioxopyrrolidin-1-yloxy, phthalimidyloxy, 1H-benzo-triazol-1-yloxy or azide group, with an amine R 2 , Wed. t with the proviso that no further free primary or secondary aliphatic amino function is included.

Die Umsetzung wird unter Schotten-Baumann- oder Einhorn-Bedingungen durchgeführt, das heißt, die Komponenten werden in Gegenwart von wenigstens einem Äquivalent einer Hilfsbase bei Temperaturen zwischen –50°C und +120°C, bevorzugt –10°C und +30°C, und gegebenenfalls in Gegenwart von Lösungsmitteln zur Reaktion gebracht. Als Hilfsbasen kommen bevorzugt Alkali- und Erdalkalihydroxide, beispielsweise Natriumhydroxid, Kaliumhydroxid oder Bariumhydroxid, Alkalicarbonate, z.B. Natriumcarbonat, Kaliumcarbonat oder Cäsiumcarbonat, Alkaliacetate, z.B. Natrium- oder Kaliumacetat, sowie tertiäre Amine, beispielsweise Pyridin, 2,4,6-Trimethylpyridin, Chinolin, Triethylamin, N-Ethyldiisopropylamin, N-Ethyldicyclohexylamin, 1,4-Di-azabicyclo[2,2,2]octan oder 1,8-Diaza-bicyclo[5,4,0]undec-7-en, als Lösungsmittel beispielsweise Dichlormethan, Tetrahydrofuran, 1,4-Dioxan, Acetonitril, Dimethylformamid, Dimethylacetamid, N-Methylpyrrolidon oder Gemische davon in Betracht; werden als Hilfsbasen Alkali- oder Erdalkalihydroxide, Alkalicarbonate oder -acetate verwendet, kann dem Reaktionsgemisch auch Wasser als Cosolvens zugesetzt werden.The Implementation will be under bulkhead Baumann or unicorn conditions carried out, that is, the Components become in the presence of at least one equivalent an auxiliary base at temperatures between -50 ° C and + 120 ° C, preferably -10 ° C and + 30 ° C, and optionally in the presence of solvents reacted. As auxiliary bases are preferred alkali and Alkaline earth hydroxides, for example sodium hydroxide, potassium hydroxide or barium hydroxide, alkali carbonates, e.g. Sodium carbonate, potassium carbonate or cesium carbonate, Alkali acetates, e.g. Sodium or potassium acetate, as well as tertiary amines, for example, pyridine, 2,4,6-trimethylpyridine, quinoline, triethylamine, N-ethyldiisopropylamine, N-ethyldicyclohexylamine, 1,4-di-azabicyclo [2,2,2] octane or 1,8-diazabicyclo [5,4,0] undec-7-ene, as a solvent, for example Dichloromethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, dimethylformamide, Dimethylacetamide, N-methylpyrrolidone or mixtures thereof; are used as auxiliary bases alkali or alkaline earth metal hydroxides, alkali metal carbonates or Acetate used, the reaction mixture can also be water as cosolvent be added.

Die erfindungsgemäßen neuen Verbindungen der allgemeinen Formel (I) enthalten ein oder mehrere Chiralitätszentren. Sind beispielsweise zwei Chiralitätszentren vorhanden, dann können die Verbindungen in Form zweier diastereomerer Antipodenpaare auftreten. Die Erfindung umfasst die einzelnen Isomeren ebenso wie ihre Gemische.The new invention Compounds of general formula (I) contain one or more chiral centers. For example, if there are two chirality centers, then the Compounds in the form of two diastereomeric antipode pairs occur. The invention includes the individual isomers as well as their mixtures.

Die Trennung der jeweiligen Diastereomeren gelingt auf Grund ihrer unterschied lichen physikochemischen Eigenschaften, z.B. durch fraktionierte Kristallisation aus geeigneten Lösungsmitteln, durch Hochdruckflüssigkeits- oder Säulenchromatographie unter Verwendung chiraler oder bevorzugt achiraler stationärer Phasen.The separation of the respective diastereomers succeeds on the basis of their different physicochemical properties, for example by fractional crystallization from suitable solvents, by high pressure liquid or column chromatography using chiral or preferably achiral stationary Pha sen.

Die Trennung von unter die allgemeine Formel (I) fallenden Racematen gelingt beispielsweise durch HPLC an geeigneten chiralen stationären Phasen (z. B. Chiral AGP, Chiralpak AD). Racemate, die eine basische oder saure Funktion enthalten, lassen sich auch über die diastereomeren, optisch aktiven Salze trennen, die bei Umsetzung mit einer optisch aktiven Säure, beispielsweise (+)- oder (–)-Weinsäure, (+)- oder (–)-Diacetylweinsäure, (+)- oder (–)-Monomethyltartrat oder (+)- oder (–)-Camphersulfonsäure, bzw. einer optisch aktiven Base, beispielsweise mit (R)-(+)-1-Phenylethylamin, (S)-(–)-1-Phenylethylamin oder (S)-Brucin, entstehen.The Separation of racemates covered by the general formula (I) succeeds for example by HPLC on suitable chiral stationary phases (eg Chiral AGP, Chiralpak AD). Racemates, which is a basic or acidic function can also be visualized via the diastereomers active salts which, when reacted with an optically active Acid, for example, (+) - or (-) - tartaric acid, (+) - or (-) - diacetyltartaric acid, (+) - or (-) - monomethyl tartrate or (+) - or (-) - camphorsulfonic acid, or an optically active base, for example with (R) - (+) - 1-phenylethylamine, (S) - (-) - 1-phenylethylamine or (S) -Brucine, arise.

Nach einem üblichen Verfahren zur Isomerentrennung wird das Racemat einer Verbindung der allgemeinen Formel (I) mit einer der vorstehend angegebenen optisch aktiven Säuren bzw. Basen in äquimolarer Menge in einem Lösungsmittel umgesetzt und die erhaltenen kristallinen, diastereomeren, optisch aktiven Salze unter Ausnutzung ihrer verschiedenen Löslichkeit getrennt. Diese Umsetzung kann in jeder Art von Lösungsmitteln durchgeführt werden, solange sie einen ausreichenden Unterschied hinsichtlich der Löslichkeit der Salze aufweisen. Vorzugsweise werden Methanol, Ethanol oder deren Gemische, beispielsweise im Volumenverhältnis 50:50, verwendet. Sodann wird jedes der optisch aktiven Salze in Wasser gelöst, mit einer Base, wie Natriumcarbonat oder Kaliumcarbonat, oder mit einer geeigneten Säure, beispielsweise mit verdünnter Salzsäure oder wässeriger Methansulfonsäure, vorsichtig neutralisiert und dadurch die entsprechende freie Verbindung in der (+)- oder (–)-Form erhalten.To a usual one Isomer separation process becomes the racemate of a compound of the general formula (I) with one of the abovementioned optically active acids or bases in equimolar amount in a solvent reacted and the resulting crystalline diastereomers, optically active salts taking advantage of their different solubility separated. This implementation can be in any kind of solvents carried out be as long as they make a sufficient difference the solubility of the Have salts. Preferably, methanol, ethanol or their Mixtures, for example, in the volume ratio 50:50 used. thereupon each of the optically active salts is dissolved in water, with a base, such as sodium carbonate or potassium carbonate, or with a suitable acid, for example, with dilute hydrochloric acid or aqueous methane, carefully neutralized and thus the corresponding free compound in the (+) - or (-)-Shape receive.

Jeweils nur das (R)- oder (S)-Enantiomer bzw. ein Gemisch zweier optisch aktiver, unter die allgemeine Formel (I) fallender diastereomerer Verbindungen wird auch dadurch erhalten, dass man die oben beschriebenen Synthesen mit jeweils einer geeigneten (R)- bzw. (S)-konfigurierten Reaktionskomponente durchführt.Each only the (R) - or (S) -enantiomer or a mixture of two optical active, under the general formula (I) falling diastereomeric Compounds are also obtained by using the ones described above Syntheses each with a suitable (R) or (S) -configured Reaction component performs.

Die Ausgangsverbindungen der allgemeinen Formel (III) erhält man, soweit sie nicht literaturbekannt oder gar käuflich sind, entsprechend den in WO 98/11128 und DE 199 52 146 angegebenen Verfahren. Die Ausgangsverbindungen der allgemeinen Formel (IV) sind käuflich. Verbindungen der allgemeinen Formel (V) lassen sich nach dem Peptidchemiker geläufigen Methoden aus geschützten Phenylalaninen und Aminen der allgemeinen Formel R2 herstellen. Die Ausgangsverbindungen der allgemeinen Formel (Vi) erhält man beispielsweise durch Umsetzung von Aminen der allgemeinen Formel R2 mit 2-(Alkoxycarbonylmethyl)-3-aryl-propansäuren und anschließende hydrolytische Abspaltung der Alkylgruppe. Die erforderlichen 2-(Alkoxycarbonylmethyl)-3-aryl-propansäuren können in Analogie zu literaturbekannten Methoden (David A. Evans, Leester D. Wu, John J. M. Wiener, Jeffrey S. Johnson, David H. B. Ripin und Jason S. Tedrow, J. Org.Chem 64, 6411-6417 [1999]; Saul G. Cohen und Aleksander Milovanovic, J. Am. Chem. Soc. 90, 3495-3502 [1968]; Hiroyuki Kawano, Youichi Ishii, Takao Ikariya, Masahiko Saburi, Sadao Yoshikawa, Yasuzo Uchida und Hidenori Kumobayashi, Tetrahedron Letters 28, 1905-1908 [1987]) hergestellt werden. Carbonsäuren der allgemeinen Formel (VIII) können nach den in der WO 98/11128 angegebenen Verfahren aus allgemein zugänglichen Ausgangsmaterialien hergestellt werden.The starting compounds of general formula (III) are obtained, as far as they are not known from the literature or even commercially available, in accordance with the methods described in WO 98/11128 and US Pat DE 199 52 146 specified method. The starting compounds of the general formula (IV) are commercially available. Compounds of the general formula (V) can be prepared by methods familiar from the peptide chemist from protected phenylalanines and amines of the general formula R 2 . The starting compounds of the general formula (Vi) are obtained, for example, by reaction of amines of the general formula R 2 with 2- (alkoxycarbonylmethyl) -3-aryl-propanoic acids and subsequent hydrolytic cleavage of the alkyl group. The required 2- (alkoxycarbonylmethyl) -3-aryl-propanoic acids can be prepared in analogy to methods known from the literature (David A. Evans, Wester D., John JM Wiener, Jeffrey S. Johnson, David HB Ripin and Jason S. Tedrow, J. Org. Chem 64, 6411-6417 [1999]; Saul G. Cohen and Aleksander Milovanovic, J. Am. Chem. Soc. 90, 3495-3502 [1968]; Hiroyuki Kawano, Youichi Ishii, Takao Ikariya, Masahiko Saburi, Sadao Yoshikawa, Yasuzo Uchida and Hidenori Kumobayashi, Tetrahedron Letters 28, 1905-1908 [1987]). Carboxylic acids of the general formula (VIII) can be prepared from generally available starting materials by the processes specified in WO 98/11128.

Die erhaltenen Verbindungen der allgemeinen Formel (I) können, sofern sie geeignete basische Funktionen enthalten, insbesondere für pharmazeutische Anwendungen in ihre physiologisch verträglichen Salze mit anorganischen oder organischen Säuren übergeführt werden. Als Säuren kommen hierfür beispielsweise Salzsäure, Bromwasserstoffsäure, Phosphorsäure, Salpetersäure, Schwefelsäure, Methansulfonsäure, Ethansulfonsäure, Benzolsulfonsäure, p-Toluolsulfonsäure, Essigsäure, Fumarsäure, Bernsteinsäure, Milchsäure, Mandelsäure, Äpfelsäure, Zitronensäure, Weinsäure oder Maleinsäure in Betracht.The obtained compounds of general formula (I), if they contain suitable basic functions, in particular for pharmaceutical Applications in their physiologically acceptable salts with inorganic or organic acids are converted. As acids come for this for example, hydrochloric acid, hydrobromic, Phosphoric acid, Nitric acid, Sulfuric acid, Methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, acetic acid, fumaric acid, succinic acid, lactic acid, mandelic acid, malic acid, citric acid, tartaric acid or maleic into consideration.

Außerdem lassen sich die neuen Verbindungen der Formel (I), falls sie Carbonsäurefunktion enthalten, gewünschtenfalls in ihre Additionssalze mit anorganischen oder organischen Basen, insbesondere für die pharmazeutische Anwendung in ihre physiologisch verträglichen Additionssalze überführen. Als Basen kommen hierfür beispielsweise Natriumhydroxid, Kaliumhydroxid, Ammoniak, Cyclohexylamin, Dicyclohexylamin, Ethanolamin, Diethanolamin und Triethanolamin in Betracht.In addition, let the new compounds of the formula (I), if they carboxylic acid function included, if desired in their addition salts with inorganic or organic bases, especially for the pharmaceutical application in its physiologically acceptable Transfer addition salts. When Bases come for this for example, sodium hydroxide, potassium hydroxide, ammonia, cyclohexylamine, Dicyclohexylamine, ethanolamine, diethanolamine and triethanolamine into consideration.

Die vorliegende Erfindung betrifft Racemate, sofern die Verbindungen der allgemeinen Formel (I) nur ein Chiralitätselement besitzen. Die Anmeldung umfasst jedoch auch die einzelnen diastereomeren Antipodenpaare oder deren Gemische, die dann vorliegen, wenn mehr als ein Chiralitätselement in den Verbindungen der allgemeinen Formel (I) vorhanden ist, sowie die einzelnen optisch aktiven Enantiomeren, aus denen sich die erwähnten Racemate zusammensetzen.The The present invention relates to racemates, as far as the compounds of the general formula (I) have only one chiral element. The registration however, also encompasses the individual diastereomeric antipode pairs or their mixtures, which are present when more than one chiral element is present in the compounds of general formula (I), as well as the individual optically active enantiomers that make up the mentioned racemates put together.

Ebenfalls mit vom Gegenstand dieser Erfindung umfasst sind die erfindungsgemäßen Verbindungen, einschließlich deren Salze, in denen ein oder mehrere Wasserstoffatome durch Deuterium ausgetauscht sind.Also included in the subject matter of this invention are the compounds according to the invention, including their salts, in which one or more hydrogen atoms are replaced by deuterium.

Die neuen Verbindungen der allgemeinen Formel (I) und deren physiologisch verträgliche Salze weisen wertvolle pharmakologische Eigenschaften auf, die auf ihre selektiven CGRP-antagonistischen Eigenschaften zurückgehen. Ein weiterer Gegenstand der Erfindung sind diese Verbindungen enthaltende Arzneimittel, deren Verwendung und deren Herstellung.The new compounds of general formula (I) and their physiological compatible Salts have valuable pharmacological properties their selective CGRP antagonistic properties decline. Another object of the invention are those compounds containing Medicines, their use and their manufacture.

Die voranstehend genannten neuen Verbindungen und deren physiologisch verträgliche Salze besitzen CGRP-antagonistische Eigenschaften und zeigen gute Affinitäten in CGRP-Rezeptorbindungsstudien. Die Verbindungen weisen in den nachstehend beschriebenen pharmakologischen Testsystemen CGRP-antagonistische Eigenschaften auf.The above-mentioned new compounds and their physiological compatible Salts have CGRP antagonistic properties and show good affinities in CGRP receptor binding studies. The compounds have in the CGRP antagonistic pharmacological test systems described below Properties on.

Zum Nachweis der Affinität der voranstehend genannten Verbindungen zu humanen CGRP-Rezeptoren und ihrer antagonistischen Eigenschaften wurden die folgenden Versuche durchgeführt:To the Proof of affinity the above compounds to human CGRP receptors and their antagonistic properties were the following experiments carried out:

A. Bindungsstudien mit (den humanen CGRP-Rezeptor exprimierenden) SK-N-MC-ZellenA. Binding studies with (the human CGRP receptor expressing) SK-N-MC cells

SK-N-MC-Zellen werden in "Dulbecco's modified Eagle Medium" kultiviert. Das Medium konfluenter Kulturen wird entfernt. Die Zellen werden zweimal mit PBS- Puffer (Gibco 041-04190 M) gewaschen, durch Zugabe von PBS-Puffer, versetzt mit 0.02% EDTA, abgelöst und durch Zentrifugation isoliert. Nach Resuspension in 20 ml "Balanced Salts Solution" [BSS (in mM): NaCl 120, KCl 5.4, NaHCO3 16.2, MgSO4 0.8, NaHPO4 1.0, CaCl2 1.8, D-Glucose 5.5, HEPES 30, pH 7.40] werden die Zellen zweimal bei 100 × g zentrifugiert und in BSS resuspendiert. Nach Bestimmung der Zellzahl werden die Zellen mit Hilfe eines Ultra-Turrax homogenisiert und für 10 Minuten bei 3000 × g zentrifugiert. Der Überstand wird verworfen und das Pellet in Tris-Puffer (10 mM Tris, 50 mM NaCl, 5 mM MgCl2, 1 mM EDTA, pH 7.40), angereichert mit 1 % Rinderserum-Albumin und 0.1 % Bacitracin, rezentrifugiert und resuspendiert (1 ml/1000000 Zellen). Das Homogenat wird bei –80°C eingefroren. Die Membranpräparationen sind bei diesen Bedingungen für mehr als 6 Wochen stabil.SK-N-MC cells are cultured in "Dulbecco's modified Eagle Medium". The medium of confluent cultures is removed. The cells are washed twice with PBS buffer (Gibco 041-04190 M), removed by addition of PBS buffer, mixed with 0.02% EDTA, and isolated by centrifugation. After resuspension in 20 ml of Balanced Salts Solution [BSS (in mM): NaCl 120, KCl 5.4, NaHCO 3 16.2, MgSO 4 0.8, NaHPO 4 1.0, CaCl 2 1.8, D-glucose 5.5, HEPES 30, pH 7.40] The cells are centrifuged twice at 100 x g and resuspended in BSS. After determining the number of cells, the cells are homogenized using an Ultra-Turrax and centrifuged for 10 minutes at 3000 × g. The supernatant is discarded and the pellet recentrifuged and resuspended in Tris buffer (10 mM Tris, 50 mM NaCl, 5 mM MgCl 2 , 1 mM EDTA, pH 7.40) supplemented with 1% bovine serum albumin and 0.1% bacitracin (1 ml / 1000000 cells). The homogenate is frozen at -80 ° C. The membrane preparations are stable under these conditions for more than 6 weeks.

Nach Auftauen wird das Homogenat 1:10 mit Assay-Puffer (50 mM Tris, 150 mM NaCl, 5 mM MgCl2, 1 mM EDTA, pH 7.40) verdünnt und 30 Sekunden lang mit einem Ultra-Turrax homogenisiert. 230 μl des Homogenats werden für 180 Minuten bei Raumtemperatur mit 50 pM 125I-Iodotyrosyl-Calcitonin-Gene-Related Peptide (Amersham) und ansteigenden Konzentrationen der Testsubstanzen in einem Gesamtvolumen von 250 μl inkubiert. Die Inkubation wird durch rasche Filtration durch mit Polyethylenimin (0.1 %) behandelte GF/B-Glasfaserfilter mittels eines Zellharvesters beendet. Die an Protein gebundene Radioaktivität wird mit Hilfe eines Gammacounters bestimmt. Als nichtspezifische Bindung wird die gebundene Radioaktivität nach Gegenwart von 1 μM humanem CGRP-alpha während der Inkubation definiert.After thawing, the homogenate is diluted 1:10 with assay buffer (50 mM Tris, 150 mM NaCl, 5 mM MgCl 2 , 1 mM EDTA, pH 7.40) and homogenized for 30 seconds with an Ultra-Turrax. 230 μl of the homogenate are incubated for 180 minutes at room temperature with 50 pM 125 I-iodotyrosyl-calcitonin gene-related peptides (Amersham) and increasing concentrations of the test substances in a total volume of 250 μl. Incubation is terminated by rapid filtration through polyethyleneimine (0.1%) treated GF / B glass fiber filters using a cell harvester. The protein bound radioactivity is determined using a gamma counter. Non-specific binding is defined as the bound radioactivity after the presence of 1 μM human CGRP-alpha during the incubation.

Die Analyse der Konzentrations-Bindungskurven erfolgt mit Hilfe einer computergestützten nichtlinearen Kurvenanpassung.The Analysis of the concentration-binding curves is carried out with the help of a computerized nonlinear curve fitting.

Die eingangs erwähnten Verbindungen zeigen in dem beschriebenen Test IC50-Werte ≤ 10000 nM.The compounds mentioned in the introduction exhibit IC 50 values ≦ 10000 nM in the test described.

B. CGRP-Antagonismus in SK-N-MC-ZellenB. CGRP antagonism in SK-N-MC cells

SK-N-MC-Zellen (1 Mio. Zellen) werden zweimal mit 250 μl Inkubationspuffer (Hanks' HEPES, 1 mM 3-Isobutyl-1-methylxanthin, 1% BSA, pH 7.4) gewaschen und bei 37°C für 15 Minuten vorinkubiert. Nach Zugabe von CGRP (10 μl) als Agonist in steigenden Konzentrationen (10–11 bis 10–6 M) bzw. zusätzlich von Substanz in 3 bis 4 verschiedenen Konzentrationen wird nochmals 15 Minuten inkubiert.SK-N-MC cells (1 million cells) are washed twice with 250 μl of incubation buffer (Hanks' HEPES, 1 mM 3-isobutyl-1-methylxanthine, 1% BSA, pH 7.4) and at 37 ° C for 15 minutes pre-incubated. After addition of CGRP (10 μl) as agonist in increasing concentrations (10 -11 to 10 -6 M) or additionally of substance in 3 to 4 different concentrations is incubated again for 15 minutes.

Intrazelluläres cAMP wird anschließend durch Zugabe von 20 μl 1 M HCl und Zentrifugation (2000 × g, 4°C für 15 Minuten) extrahiert. Die Überstände werden in flüssigem Stickstoff eingefroren und bei –20°C gelagert.Intracellular cAMP will follow by adding 20 μl 1M HCl and centrifugation (2000 xg, 4 ° C for 15 minutes). The supernatants are in liquid Nitrogen frozen and stored at -20 ° C.

Die cAMP-Gehalte der Proben werden mittels Radioimmunassay (Fa. Amersham) bestimmt und die pA2-Werte antagonistisch wirkender Substanzen graphisch ermittelt.The cAMP contents of the samples are determined by means of radioimmunoassay (Amersham) and the pA 2 values of antagonistic substances are determined graphically.

Die erfindungsgemäßen Verbindungen zeigen in dem beschriebenen in vitro-Testmodell CGRP-antagonistische Eigenschaften in einem Dosisbereich zwischen 10–12 bis 10–5 M.In the described in vitro test model, the compounds according to the invention exhibit CGRP-antagonistic properties in a dose range between 10 -12 to 10 -5 M.

Aufgrund ihrer pharmakologischen Eigenschaften eignen sich die erfindungsgemäßen Verbindungen und deren Salze mit physiologisch verträglichen Säuren somit zur akuten und prophylaktischen Behandlung von Kopfschmerzen, insbesondere Migräne- bzw. Cluster-Kopfschmerz. Weiterhin beeinflussen die erfindungsgemäßen Verbindungen auch die folgenden Erkrankungen positiv: Nicht-insulinabhängigen Diabetes mellitus ("NIDDM"), cardiovaskuläre Erkrankungen, Morphintoleranz, Clostritiumtoxin-bedingte Durchfallerkrankungen, Erkrankungen der Haut, insbesondere thermische und strahlenbedingte Hautschäden inklusive Sonnenbrand, entzündliche Erkrankungen, z.B. entzündliche Gelenkerkrankungen (Arthritis), neurogene Entzündungen der oralen Mucosa, entzündliche Lungenerkrankungen, allergische Rhinitis, Asthma, Erkrankungen, die mit einer überschießenden Gefäßerweiterung und dadurch bedingter verringerter Gewebedurchblutung einhergehen, z.B. Schock und Sepsis. Darüber hinaus zeigen die erfindungsgemäßen Verbindungen eine lindernde Wirkung auf Schmerzzustände im allgemeinen.Due to their pharmacological properties, the compounds of the invention are suitable and their salts with physiologically tolerated acids thus for the acute and prophylactic treatment of headache, especially migraine or cluster headache. Furthermore, the compounds according to the invention also have a positive influence on the following diseases: non-insulin-dependent diabetes mellitus ("NIDDM"), cardiovascular diseases, morphine tolerance, diarrheal diseases caused by Clostritium toxins, diseases of the skin, in particular thermal and radiation-related skin damage including sunburn, inflammatory diseases, eg inflammatory joint diseases (Arthritis), neurogenic inflammation of the oral mucosa, inflammatory lung disease, allergic rhinitis, asthma, diseases associated with excessive vasodilation and consequent reduced tissue perfusion, eg, shock and sepsis. In addition, the compounds according to the invention have a soothing effect on pain conditions in general.

Die Symptomatik menopausaler, durch Gefäßerweiterung und erhöhten Blutfluss verursachter Hitzewallungen östrogendefizienter Frauen sowie hormonbehandelter Prostatakarzinompatienten wird durch die CGRP-Antagonisten der vorliegenden Anwendung präventiv und akut-therapeutisch günstig beeinflusst, wobei sich dieser Therapieansatz vor der Hormonsubstitution durch Nebenwirkungsarmut auszeichnet.The Symptoms of menopausal, due to vasodilation and increased blood flow caused hot flashes estrogendefizienter Women as well as hormone-treated prostate cancer patients will by the CGRP antagonists of the present application are preventive and acutely beneficial influenced, this therapy approach before the hormone substitution characterized by low side effects.

Die zur Erzielung einer entsprechenden Wirkung erforderliche Dosierung beträgt zweckmäßigerweise bei intravenöser oder subkutaner Gabe 0.0001 bis 3 mg/kg Körpergewicht, vorzugsweise 0.01 bis 1 mg/kg Körpergewicht, und bei oraler, nasaler oder inhalativer Gabe 0.01 bis 10 mg/kg Körpergewicht, vorzugsweise 0.1 bis 10 mg/kg Körpergewicht, jeweils 1 bis 3 × täglich.The To achieve a corresponding effect required dosage is expediently at intravenous or subcutaneous administration 0.0001 to 3 mg / kg body weight, preferably 0.01 to 1 mg / kg body weight, and by oral, nasal or inhalation administration 0.01 to 10 mg / kg Body weight, preferably 0.1 to 10 mg / kg of body weight, 1 to 3 times a day.

Sofern die Behandlung mit CGRP-Antagonisten oder/und CGRP-Release-Hemmern in Ergänzung zu einer üblichen Hormonsubstitution erfolgt, empfiehlt sich eine Verringerung der vorstehend angegebenen Dosierungen, wobei die Dosierung dann 1/5 der vorstehend angegebenen Untergrenzen bis zu 1/1 der vorstehend angegebenen Obergrenzen betragen kann.Provided treatment with CGRP antagonists and / or CGRP release inhibitors in addition to a usual Hormone substitution takes place, it is recommended to reduce the above dosages, the dosage then 1/5 the lower limits specified above up to 1/1 of the above may be upper limits.

Die erfindungsgemäß hergestellten Verbindungen können entweder alleine oder gegebenenfalls in Kombination mit anderen Wirksubstanzen zur Behandlung von Migräne intravenös, subkutan, intramuskulär, intrarektal, intranasal, durch Inhalation, transdermal oder oral erfolgen, wobei zur Inhalation insbesondere Aerosolformulierungen geeignet sind. Die Kombinationen können entweder simultan oder sequentiell verabreicht werden.The produced according to the invention Connections can either alone or optionally in combination with others Active substances for the treatment of migraine intravenously, subcutaneously, intramuscularly, intrarectally, intranasally, by inhalation, transdermally or orally, wherein For inhalation in particular aerosol formulations are suitable. The combinations can be administered either simultaneously or sequentially.

Als Kombinationspartner denkbare Wirkstoffklassen sind z.B. Antiemetica, Prokinetica, Neuroleptica, Antidepressiva, Neurokinin-Antagonisten, Anticonvulsiva, Histamin-H1-Rezeptorantagonisten, Antimuscarinika, β-Blocker, α-Agonisten und α-Antagonisten, Ergotalkaloiden, schwachen Analgetica, nichtsteroidalen Antiphlogistica, Corticosteroiden, Calcium-Antagonisten, 5-HT1B/1D-Agonisten oder andere Antimigränemitteln, die zusammen mit einem oder mehreren inerten üblichen Trägerstoffen und/oder Verdünnungsmitteln, z.B. mit Maisstärke, Milchzucker, Rohrzucker, mikrokristalliner Zellulose, Magnesiumstearat, Polyvinylpyrrolidon, Zitronensäure, Weinsäure, Wasser, Wasser/Ethanol, Wasser/Glycerin, Wasser/-Sorbit, Wasser/Polyethylenglykol, Propylenglykol, Cetylstearylalkohol, Carboxymethylcellulose oder fetthaltigen Substanzen wie Hartfett oder deren geeigneten Gemischen, in übliche galenische Zubereitungen wie Tabletten, Dragees, Kapseln, Pulver, Suspensionen, Lösungen, Dosieraerosole oder Zäpfchen eingearbeitet werden können.Possible combinations of agents are, for example, antiemetics, prokinetics, neuroleptics, antidepressants, neurokinin antagonists, anticonvulsants, histamine H1 receptor antagonists, antimuscarinics, β-blockers, α-agonists and α-antagonists, ergot alkaloids, weak analgesics, non-steroidal anti-inflammatory drugs, corticosteroids, Calcium antagonists, 5-HT 1B / 1D agonists or other antimigraine agents, which together with one or more inert customary carriers and / or diluents, for example with corn starch, lactose, cane sugar, microcrystalline cellulose, magnesium stearate, polyvinylpyrrolidone, citric acid, tartaric acid, water , Water / ethanol, water / glycerin, water / sorbitol, water / polyethylene glycol, propylene glycol, cetylstearyl alcohol, carboxymethylcellulose or fatty substances such as hard fat or their suitable mixtures, in conventional pharmaceutical preparations such as tablets, dragees, capsules, powders, suspensions, solutions, Metered aerosols or z suppositories can be incorporated.

Für die oben erwähnten Kombinationen kommen somit als weitere Wirksubstanzen beispielsweise die nicht-steroidalen Antiphlogistika Acclofenac, Acemetacin, Acetylsalicylsäure, Azathioprin, Diclofenac, Diflunisal, Fenbufen, Fenoprofen, Flurbiprofen, Ibuprofen, Indometacin, Ketoprofen, Leflunomid, Lornoxicam, Mefenaminsäure, Naproxen, Phenylbutazon, Piroxicam, Sulfasalazin, Zomepirac oder deren pharmazeutisch verträgliche Salze sowie Meloxicam und andere selektive COX2-Inhibitoren, wie beispielsweise Rofecoxib und Celecoxib, in Betracht.For the above mentioned Combinations come thus as further active substances for example the non-steroidal anti-inflammatory drugs Acclofenac, Acemetacin, Acetylsalicylic acid, Azathioprine, Diclofenac, diflunisal, fenbufen, fenoprofen, flurbiprofen, ibuprofen, Indomethacin, ketoprofen, leflunomide, lornoxicam, mefenamic acid, naproxen, Phenylbutazone, piroxicam, sulfasalazine, zomepirac or their pharmaceutically compatible Salts as well as meloxicam and other selective COX2 inhibitors, such as For example, rofecoxib and celecoxib, into consideration.

Weiterhin können Ergotamin, Dihydroergotamin, Metoclopramid, Domperidon, Diphenhydramin, Cyclizin, Promethazin, Chlorpromazin, Vigabatrin, Timolol, Isomethepten, Pizotifen, Botox, Gabapentin, Topiramat, Riboflavin, Montelukast, Lisinopril, Prochlorperazin, Dexamethason, Flunarizin, Dextropropoxyphen, Meperidin, Metoprolol, Propranolol, Nadolol, Atenolol, Clonidin, Indoramin, Carbamazepin, Phenytoin, Valproat, Amitryptilin, Lidocain oder Diltiazem und andere 5-HT1B/1D-Agonisten wie z.B. Almotriptan, Avitriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Sumatriptan und Zolmitriptan verwendet werden.Furthermore, ergotamine, dihydroergotamine, metoclopramide, domperidone, diphenhydramine, cyclizine, promethazine, chlorpromazine, vigabatrin, timolol, isomethepten, pizotifen, botox, gabapentin, topiramate, riboflavin, montelukast, lisinopril, prochlorperazine, dexamethasone, flunarizine, dextropropoxyphene, meperidine, metoprolol, Propranolol, nadolol, atenolol, clonidine, indoramine, carbamazepine, phenytoin, valproate, amitryptiline, lidocaine or diltiazem and other 5-HT 1B / 1D agonists such as almotriptan, avitriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan and zolmitriptan ,

Die Dosis für diese Wirksubstanzen beträgt hierbei zweckmäßigerweise 1/5 der üblicherweise empfohlenen niedrigsten Dosierung bis zu 1/1 der normalerweise empfohlenen Dosierung, also beispielsweise 20 bis 100 mg Sumatriptan.The Dose for these active substances is this expediently 1/5 of the usual recommended lowest dosage up to 1/1 of the normally recommended Dosage, so for example 20 to 100 mg Sumatriptan.

Ein weiterer Gegenstand der Erfindung ist die Verwendung der erfindungsgemäßen Verbindungen als wertvolle Hilfsmittel zur Erzeugung und Reinigung (Affinitätschromatographie) von Antikörpern sowie, nach geeigneter radioaktiver Markierung, beispielsweise durch Tritiierung geeigneter Vorstufen, beispielsweise durch katalytische Hydrierung mit Trithium oder Ersatz von Halogenatomen durch Tritium, in RIA- und ELISA-Assays und als diagnostische bzw. analytische Hilfsmittel in der Neurotransmitter-Forschung.One Another object of the invention is the use of the compounds of the invention as valuable tools for the production and purification (affinity chromatography) of antibodies and, after suitable radioactive labeling, for example by Tritiation of suitable precursors, for example by catalytic Hydrogenation with trithium or replacement of halogen atoms with tritium, in RIA and ELISA assays and as diagnostic or analytical Aids in neurotransmitter research.

Experimenteller Teilexperimental part

Für hergestellten Verbindungen liegen in der Regel IR-, UV-, 1H-NMR und/oder Massenspekten vor. Wenn nicht anders angegeben, wurden Rf-Werte unter Verwendung von DC-Fertigplatten Kieselgel 60 F254 (E. Merck, Darmstadt, Artikel-Nr. 1.05714) ohne Kammersättigung bestimmt. Die unter der Bezeichnung Alox ermittelten Rf-Werte wurden unter Verwendung von DC-Fertigplatten Aluminiumoxid 60 F254 (E. Merck, Darmstadt, Artikel-Nr. 1.05713) ohne Kammersättigung bestimmt. Die bei den Fliessmitteln angegebenen Verhältnisse beziehen sich auf Volumeneinheiten der jeweiligen Lösungsmittel. Zu chromatographischen Reinigungen wurde Kieselgel der Firma Millipore (MATREXTM, 35-70my) verwendet. Die angegebenen HPLC-Daten werden unter nachstehend angeführten Parametern gemessen:
Analytische Säule: Zorbax-Säule (Agilent Technologies), SB (Stable Bond) – C18; 3.5 μm; 4.6 × 75 mm; Säulentemperatur: 30°C; Fluss: 0.8 mL/min; Injektionsvolumen: 5 μL; Detektion bei 254 nm

Figure 00580001
For prepared compounds are usually present IR, UV, 1 H-NMR and / or mass spectra. Unless otherwise stated, R f values were determined using GCF Finished Tops Kieselgel 60 F 254 (E. Merck, Darmstadt, Article No. 1.05714) with no chamber saturation. The Rf values determined under the name Alox were determined using TLC plates alumina 60 F 254 (E. Merck, Darmstadt, Article No. 1.05713) without chamber saturation. The ratios indicated for the flow agents relate to volume units of the respective solvents. For chromatographic purifications silica gel from Millipore (MATREX ™ , 35-70my) was used. The indicated HPLC data are measured under the following parameters:
Analytical column: Zorbax column (Agilent Technologies), SB (stable bond) - C18; 3.5 μm; 4.6 × 75 mm; Column temperature: 30 ° C; Flow: 0.8 mL / min; Injection volume: 5 μL; Detection at 254 nm
Figure 00580001

Bei präparativen HPLC-Reinigungen werden in der Regel die gleichen Gradienten verwendet, die bei der Erhebung der analytischen HPLC-Daten benutzt wurden.at preparative HPLC purifications usually use the same gradients used in the collection of analytical HPLC data.

Die Sammlung der Produkte erfolgt massengesteuert, die Produkt enthaltenden Fraktionen werden vereinigt und gefriergetrocknet.The Collection of products is mass-controlled, containing the product Fractions are combined and freeze-dried.

Falls nähere Angaben zur Konfiguration fehlen, bleibt offen, ob es sich um reine Enantiomere handelt oder ob partielle oder gar völlige Racemisierung eingetreten ist.If details Information about the configuration is missing, remains open, whether it is pure Enantiomers or whether partial or even complete racemization occurred is.

In den Versuchsbeschreibungen werden die folgenden Abkürzungen verwendet:

abs.
absolutiert
Boc
tert.-Butoxycarbonyl
CDI
N,N'-Carbonyldiimidazol
CDT
1,1'-Carbonyldi-(1,2,4-triazol)
DMF
N,N-Dimethylformamid
EtOAc
Essigsäureethylester
EtOH
Ethanol
ges.
gesättigt
halbkonz.
halbkonzentriert
HCl
Salzsäure
HOAc
Essigsäure
HOBt
1-Hydroxybenzotriazol-hydrat
i.vac.
in vacuo (im Vakuum)
KOH
Kaliumhydroxid
konz.
konzentriert
MeOH
Methanol
MTBE
Methyl-tert.-butylether
NaCl
Natriumchlorid
NaOH
Natriumhydroxid
org.
organisch
RT
Raumtemperatur
TBTU:
2-(1H-Benzotriazol-1-yl)-1,1,3,3-tetramethyluronium-Tetrafluorborat
TFA
Trifluoressigsäure
THF
Tetrahydrofuran
wässr.
wässrig
The test descriptions use the following abbreviations:
Section.
made absolute
Boc
tert-butoxycarbonyl
CDI
N, N'-carbonyldiimidazole
CDT
1,1'-Carbonyldi- (1,2,4-triazole)
DMF
N, N-dimethylformamide
EtOAc
ethyl acetate
EtOH
ethanol
ges.
saturated
half-concentrated.
semi focused
HCl
hydrochloric acid
HOAc
acetic acid
HOBt
1-hydroxybenzotriazole hydrate
dried i.
in vacuo (in vacuum)
KOH
potassium hydroxide
conc.
concentrated
MeOH
methanol
MTBE
Methyl tert-butyl ether
NaCl
sodium chloride
NaOH
sodium hydroxide
org.
organic
RT
room temperature
TBTU:
2- (1H-benzotriazol-1-yl) -1,1,3,3-tetramethyluronium tetrafluoroborate
TFA
trifluoroacetic
THF
tetrahydrofuran
aq.
aqueous

A) Herstellung von ZwischenproduktenA) Preparation of intermediates

Zwischenprodukt 1:Intermediate 1:

1H-Indazol-5-carbaldehyd

Figure 00600001
1H-indazole-5-carbaldehyde
Figure 00600001

Zu einer Lösung von 11.64 g (59.08 mmol) 5-Brom-1H-indazol in 150 mL THF wurde unter Argon portionsweise innerhalb von 10 Minuten 2.60 g (65.00 mmol) Natriumhydrid (60% in Mineralöl) zugegeben und das Gemisch 15 Minuten bei RT gerührt. Das Reaktionsgemisch wurde auf –70 °C gekühlt und innerhalb von 30 Minuten 100.00 mL (130.00 mmol) sec-Butyllithium (1.3 M in Cyclohexan) zugetropft, wobei die Temperatur unter –60 °C gehalten wurde. Das Gemisch wurde weitere 2 h bei –70 °C gerührt und anschließend eine Lösung von 20.00 mL (0.260 mol) DMF in 20 mL THF zugetropft, wobei die Temperatur unter –50 °C gehalten wurde. Das Reaktionsgemisch wurde langsam auf RT erwärmt und 16 h gerührt. Anschließend wurde das Gemisch auf 0 °C gekühlt und langsam 180 mL 2N wässriger HCl zugetropft, weitere 15 Minuten gerührt und mit ges. wässriger Natriumbicarbonat-Lösung ein pH von 9-10 eingestellt. Die wässrige Phase wurde erschöpfend mit EtOAc extrahiert, die vereinigten org. Phasen über Magnesiumsulfat getrocknet und i. vac. eingeengt. Säulenchromatographie (Kieselgel, Petrolether/EtOAc 1:1 v/v), Verreiben mit Hexan und Trocknen i. vac. bei 50 °C lieferte das Produkt.
Ausbeute: 4.40 g (51 % der Theorie)
Rf = 0.37 (Kieselgel, Petrolether/EtOAc 1/1 v/v)
ESI-MS: (M+H)+ = 147To a solution of 11.64 g (59.08 mmol) of 5-bromo-1H-indazole in 150 ml of THF was added under argon in portions within 10 minutes 2.60 g (65.00 mmol) of sodium hydride (60% in mineral oil) and the mixture for 15 minutes at RT touched. The reaction mixture was cooled to -70 ° C and added dropwise within 30 minutes 100.00 mL (130.00 mmol) sec-butyllithium (1.3 M in cyclohexane), keeping the temperature below -60 ° C. The mixture was stirred for a further 2 h at -70 ° C and then added dropwise a solution of 20.00 mL (0.260 mol) of DMF in 20 mL THF, the temperature was kept below -50 ° C. The reaction mixture was slowly warmed to RT and stirred for 16 h. The mixture was then cooled to 0 ° C and slowly added dropwise 180 mL of 2N aqueous HCl, stirred for a further 15 minutes and washed with sat. aqueous sodium bicarbonate solution has a pH of 9-10. The aqueous phase was exhaustively extracted with EtOAc, the combined org. Phases dried over magnesium sulfate and i. vac. concentrated. Column chromatography (silica gel, petroleum ether / EtOAc 1: 1 v / v), trituration with hexane and drying i. vac. at 50 ° C provided the product.
Yield: 4.40 g (51% of theory)
R f = 0.37 (silica gel, petroleum ether / EtOAc 1/1 v / v)
ESI-MS: (M + H) + = 147

Zwischenprodukt 2:Intermediate 2:

2-[1-(1H-Indazol-5-yl)-methyliden]-bernsteinsäure-methylester

Figure 00610001
2- [1- (1H-indazol-5-yl) -methylidene] -succinic acid methylester
Figure 00610001

Zu einer Lösung von 2.00 g (13.68 mmol) 1H-Indazol-5-carbaldehyd und 2.80 mL (20.97 mmol) Bernsteinsäure-dimethylester in 100 mL tert-Butanol wurde 3.40 g (29.69 mmol) Kalium-tert-butylat zugegeben und das Gemisch 2 h bei 60 °C gerührt. Das Reaktionsgemisch wurde auf RT gekühlt, mit 200 mL Wasser verdünnt und die wässrige Phase zweimal mit EtOAc gewaschen. Die wässrige Phase wurde mit halbkonz. wässriger HCl auf pH 3-4 angesäuert und erschöpfend mit EtOAc extrahiert. Die vereinigten org. Phasen wurde über Magnesiumsulfat getrocknet, über Aktivkohle filtriert und i. vac. eingeengt. Das Rohprodukt wurde mit Diisopropylether und wenig Isopropanol verrieben, abfiltriert und der Rückstand mit Diisopropylether gewaschen (3.60 g, 1. Stereoisomer). Die Mutterlauge wurde i. vac. eingeengt und der Rückstand mittels Säulenchromatographie (Kieselgel, EtOAc / HOAc 10/0.1 v/v) gereinigt und i. vac. getrocknet (3.60 g, 2. Stereoisomer).
Ausbeute: 7.20 g (2 Stereoisomeren, 74 % der Theorie)
Rf = 0.49 (Kieselgel, EtOAc/HOAc 100/1 v/v)
ESI-MS: (M+H)+ = 261To a solution of 2.00 g (13.68 mmol) of 1H-indazole-5-carbaldehyde and 2.80 mL (20.97 mmol) succinic acid dimethyl ester in 100 mL tert-butanol was added 3.40 g (29.69 mmol) of potassium tert-butoxide and the mixture 2 h stirred at 60 ° C. The reaction mixture was cooled to RT, diluted with 200 mL of water and the aqueous phase washed twice with EtOAc. The aqueous phase was washed with half-conc. Aqueous HCl acidified to pH 3-4 and exhaustively extracted with EtOAc. The united org. Phases were dried over magnesium sulfate, filtered through charcoal and i. vac. concentrated. The crude product was triturated with diisopropyl ether and a little isopropanol, filtered off and the residue was washed with diisopropyl ether (3.60 g, 1st stereoisomer). The mother liquor was i. vac. concentrated and the residue by column chromatography (Silica gel, EtOAc / HOAc 10 / 0.1 v / v) and i. vac. dried (3.60 g, 2nd stereoisomer).
Yield: 7.20 g (2 stereoisomers, 74% of theory)
R f = 0.49 (silica gel, EtOAc / HOAc 100/1 v / v)
ESI-MS: (M + H) + = 261

Zwischenprodukt 3:Intermediate 3:

2-(1H-Indazol-5-ylmethyl)-bernsteinsäure-methylester

Figure 00610002
2- (1 H-indazol-5-ylmethyl) -succinic acid methylester
Figure 00610002

Eine Suspension von 1.30 g (5.00 mmol) 2-[1-(1H-Indazol-5-yl)-methyliden]-bernsteinsäure-methylester und 0.60 g Pd/C (10%) in 40 mL MeOH/EtOAc (1:1) wurde 3 h bei 50 °C und 3 bar Wasserstoffdruck hydriert. Der Katalysator wurde abfiltriert und das Filtrat i. vac. eingeengt.
Ausbeute: 1.30 g (99 % der Theorie)
Rf = 0.64 (Kieselgel, EtOAc/HOAc 100/1 v/v)
ESI-MS: (M+H)+ = 263A suspension of 1.30 g (5.00 mmol) of methyl 2- [1- (1H-indazol-5-yl) methylidene] -succinate and 0.60 g of Pd / C (10%) in 40 mL MeOH / EtOAc (1: 1 ) Was hydrogenated at 50 ° C and 3 bar hydrogen pressure for 3 h. The catalyst was filtered off and the filtrate i. vac. concentrated.
Yield: 1.30 g (99% of theory)
R f = 0.64 (silica gel, EtOAc / HOAc 100/1 v / v)
ESI-MS: (M + H) + = 263

Zwischenprodukt 4:Intermediate 4:

2-(1H-Indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-buttersäure-methylester

Figure 00620001
2- (1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 yl] butyric acid methylester
Figure 00620001

Zu einer Lösung von 1.50 g (5.72 mmol) 2-(1H-Indazol-5-ylmethyl)-bernsteinsäuremethylester und 1.30 mL (7.25 mmol) Hünigsbase in 50 mL THF wurde 2.30 g (6.88 mmol) TBTU zugegeben und das Gemisch 30 Minuten bei RT gerührt. 1.50 g (6.11 mmol) 3-Piperidin-4-yl-1,3,4,5-tetrahydro-1,3-benzodiazepin-2-on wurde zugegeben und weitere 5 h bei RT gerührt. Das Reaktionsgemisch wurde mit 50 mL EtOAc verdünnt, die org. Phase zweimal mit 15% wässriger Kaliumcarbonat-Lösung gewaschen, über Magnesiumsulfat getrocknet und i. vac. eingeengt. Der Rückstand wurde mittels Säulenchromatographie (Kieselgel, Dichlormethan/MeOH/ges. wässriger Ammoniak 50/45/5 v/v/v) gereinigt und das Rohprodukt mit Diisopropylether verrieben.
Ausbeute: 1.60 g (57 % der Theorie)
Rf = 0.51 (Kieselgel, Dichlormethan/MeOH/ges. wässriger Ammoniak 50/45/5 v/v/v)
ESI-MS: (M+H)+ = 492To a solution of 1.50 g (5.72 mmol) 2- (1H-indazol-5-ylmethyl) -succinic acid methyl ester and 1.30 mL (7.25 mmol) Hünigsbase in 50 mL THF was added 2.30 g (6.88 mmol) TBTU and the mixture at 30 minutes RT stirred. 1.50 g (6.11 mmol) of 3-piperidin-4-yl-1,3,4,5-tetrahydro-1,3-benzodiazepin-2-one was added and the mixture was stirred at RT for a further 5 h. The reaction mixture was diluted with 50 mL EtOAc, the org. Washed twice with 15% aqueous potassium carbonate solution, dried over magnesium sulfate and i. vac. concentrated. The residue was purified by column chromatography (silica gel, dichloromethane / MeOH / saturated aqueous ammonia 50/45/5 v / v / v) and the crude product triturated with diisopropyl ether.
Yield: 1.60 g (57% of theory)
R f = 0.51 (silica gel, dichloromethane / MeOH / saturated aqueous ammonia 50/45/5 v / v / v)
ESI-MS: (M + H) + = 492

Zwischenprodukt 5:Intermediate 5:

2-(1H-Indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-buttersäure

Figure 00630001
2- (1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 yl] butyric acid
Figure 00630001

Zu einer Lösung von 1.60 g (3.27 mmol) 2-(1H-Indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-buttersäure-methylester in 20 mL THF wurde eine Lösung von 0.20 g (8.18 mmol) Lithiumhydroxid in 10 mL Wasser zugegeben und das Gemisch 16 h bei RT gerührt. Das Reaktionsgemisch wurde mit 15 mL 1 N wässriger HCl angesäuert und die wässrige Phase mit EtOAc erschöpfend extrahiert. Die vereinigten org. Phasen wurden über Magnesiumsulfat getrocknet und i. vac. eingeengt. Das Rohprodukt wurde mit Diisopropylether verrieben und i. vac. getrocknet.
Ausbeute: 1.20 g (77 % der Theorie)
Rf = 0.05 (Kieselgel, Dichlormethan/Cyclohexan/MeOH/ges. wässriger Ammoniak 70/15/15/2 v/v/v/v)
ESI-MS: (M+H)+ = 476To a solution of 1.60 g (3.27 mmol) 2- (1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- Benzodiazepin-3-yl) -piperidin-1-yl] -butyric acid methyl ester in 20 mL THF was added a solution of 0.20 g (8.18 mmol) of lithium hydroxide in 10 mL water and the mixture was stirred at RT for 16 h. The reaction mixture was acidified with 15 mL of 1 N aqueous HCl and the aqueous phase extracted exhaustively with EtOAc. The united org. Phases were dried over magnesium sulfate and i. vac. concentrated. The crude product was triturated with diisopropyl ether and i. vac. dried.
Yield: 1.20 g (77% of theory)
R f = 0.05 (silica gel, dichloromethane / cyclohexane / MeOH / saturated aqueous ammonia 70/15/15/2 v / v / v / v)
ESI-MS: (M + H) + = 476

Zwischenprodukt 6:Intermediate 6:

7-Methyl-1H-indazol-5-carbaldehyd

Figure 00630002
7-methyl-1H-indazol-5-carbaldehyde
Figure 00630002

Das Zwischenprodukt wurde analog Zwischenprodukt 1 ausgehend von 5-Brom-7-methyl-1H-indazol erhalten.
Ausbeute: 7.10 g (69 % der Theorie)
Rf = 0.05 (Kieselgel, Petrolether/EtOAc 2/1 v/v)
ESI-MS: (M)+ = 160The intermediate was obtained analogously to Intermediate 1 starting from 5-bromo-7-methyl-1H-indazole.
Yield: 7.10 g (69% of theory)
R f = 0.05 (silica gel, petroleum ether / EtOAc 2/1 v / v)
ESI-MS: (M) + = 160

Zwischenprodukt 7:Intermediate 7:

2-[1-(7-Methyl-1H-indazol-5-yl)-meth-(E)-yliden]-bernsteinsäure-methylester

Figure 00640001
2- [1- (7-methyl-1H-indazol-5-yl) -meth- (E) -ylidene] -succinic acid methylester
Figure 00640001

Eine Suspension von 5.90 g (36.84 mmol) 7-Methyl-1H-indazol-5-carbaldehyd und 28.88 g (73.60 mmol) 2-(Triphenyl-λ5-phosphanyliden)-bernsteinsäure-methylester in 120 mL THF wurde 5 Tage bei 40 °C gerührt. 50 mL DMSO und weitere 14.0 g 2-(Triphenyl-λ5-phosphanyliden)-bernsteinsäure-methylester wurden zugegeben und das Gemisch 7 h bei 95 °C gerührt. Das Reaktionsgemisch wurde auf 1 L Wasser gegossen, die wässrige Phase mit 500 mL EtOAc gewaschen und die org. Phase je zweimal mit Wasser und 15%-iger wässriger Kaliumcarbonat-Lösung extrahiert. Die vereinigten Wasserphasen wurden mit konz. wässriger HCl auf pH 1 angesäuert und die wässrigen Phasen mit EtOAc erschöpfend extrahiert. Die vereinigten org. Phasen wurden mit Wasser gewaschen, über Magnesiumsulfat getrocknet und i. vac. eingeengt. Der Rückstand wurde mittels Säulenchromatographie (Kieselgel, Gradient innerhalb von 60 Minuten, Dichlormethan/MeOH/ges. wässriger Ammoniak 100/0/0 → 0/93/7 v/v/v) gereinigt.
Ausbeute: 2.40 g (24 % der Theorie)
Rf = 0.40 (Kieselgel, Dichlormethan/MeOH/ges. wässriger Ammoniak 85/15/1.5 v/v/v)
ESI-MS: (M+H)+ = 275A suspension of 5.90 g (36.84 mmol) of 7-methyl-1H-indazole-5-carbaldehyde and 28.88 g (73.60 mmol) of methyl 2- (triphenyl-λ 5 -phosphanylidene) -succinate in 120 mL of THF was kept at 40 for 5 days ° C stirred. 50 mL of DMSO and another 14.0 g of 2- (triphenyl-λ 5 -phosphanylidene) -succinic acid methyl ester were added and the mixture was stirred at 95 ° C for 7 h. The reaction mixture was poured onto 1 L of water, the aqueous phase was washed with 500 mL EtOAc and the org. Phase extracted twice each with water and 15% aqueous potassium carbonate solution. The combined aqueous phases were treated with conc. acidified to pH 1 aqueous HCl and the aqueous phases extracted exhaustively with EtOAc. The united org. phases were washed with water, dried over magnesium sulfate and i. vac. concentrated. The residue was purified by column chromatography (silica gel, gradient over 60 minutes, dichloromethane / MeOH / saturated aqueous ammonia 100/0/0 → 0/93/7 v / v / v).
Yield: 2.40 g (24% of theory)
R f = 0.40 (silica gel, dichloromethane / MeOH / saturated aqueous ammonia 85/15 / 1.5 v / v / v)
ESI-MS: (M + H) + = 275

Zwischenprodukt 8:Intermediate 8:

2-(7-Methyl-1H-indazol-5-ylmethyl)-bernsteinsäure-methylester

Figure 00650001
2- (7-methyl-1H-indazol-5-ylmethyl) -succinic acid methylester
Figure 00650001

Das Zwischenprodukt wurde analog zu Zwischenprodukt 3 ausgehend von 2-[1-(7-Methyl-1H-indazol-5-yl)-meth-(E)-yliden]-bernsteinsäure-methylester erhalten.
Ausbeute: 1.10 g (45 % der Theorie)
HPLC-MS: 5.6 Minuten (Agilent Zorbax Stable Bond SB C18, 5 μm, 75 × 4.6 mm, Gradient in 9 Minuten, Wasser/Acetonitril/Ameisensäure 10/90/0.1 → 90/10/0.1 v/v/v)
ESI-MS: (M+H)+ = 277The intermediate was obtained analogously to intermediate 3 starting from methyl 2- [1- (7-methyl-1H-indazol-5-yl) -meth- (E) -ylidene] -succinate.
Yield: 1.10 g (45% of theory)
HPLC-MS: 5.6 minutes (Agilent Zorbax Stable Bond SB C18, 5 μm, 75 × 4.6 mm, gradient in 9 minutes, water / acetonitrile / formic acid 10/90 / 0.1 → 90/10 / 0.1 v / v / v)
ESI-MS: (M + H) + = 277

Zwischenprodukt 9:Intermediate 9:

2-(7-Methyl-1H-indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-buttersäure-methylester

Figure 00650002
2- (7-methyl-1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) piperidin-1-yl] -butyric acid methylester
Figure 00650002

Das Zwischenprodukt wurde analog zu Zwischenprodukt 4 ausgehend von 2-(7-Methyl-1H-indazol-5-ylmethyl)-bernsteinsäure-methylester und 3-Piperidin-4-yl-1,3,4,5-tetrahydro-1,3-benzodiazepin-2-on erhalten. Das Rohprodukt wurde ohne weitere Reinigung in den nachfolgenden Reaktionsschritt eingesetzt.
Ausbeute: 0.90 g (90 % der Theorie)
Rf = 0.35 (Kieselgel, EtOAc/MeOH 9/1 v/v)
HPLC-MS: 6.9 Minuten (Agilent Zorbax Stable Bond SB C18, 5 μm, 75 × 4.6 mm, Gradient in 9 Minuten, Wasser/Acetonitril/Ameisensäure 10/90/0.1 → 90/10/0.1 v/v/v)
ESI-MS: (M+H)+ = 504The intermediate was analogously to intermediate 4 starting from methyl 2- (7-methyl-1H-indazol-5-ylmethyl) -succinate and 3-piperidin-4-yl-1,3,4,5-tetrahydro-1,3 -benzodiazepin-2-one obtained. The crude product was used without further purification in the subsequent reaction step.
Yield: 0.90 g (90% of theory)
R f = 0.35 (silica gel, EtOAc / MeOH 9/1 v / v)
HPLC-MS: 6.9 minutes (Agilent Zorbax Stable Bond SB C18, 5 μm, 75 × 4.6 mm, gradient in 9 minutes, water / acetonitrile / formic acid 10/90 / 0.1 → 90/10 / 0.1 v / v / v)
ESI-MS: (M + H) + = 504

Zwischenprodukt 10:Intermediate 10:

2-(7-Methyl-1H-indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-buttersäure

Figure 00660001
2- (7-methyl-1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) piperidin-1-yl] butyric acid
Figure 00660001

Das Zwischenprodukt wurde analog zu Zwischenprodukt 5 ausgehend von 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-buttersäure-methylester erhalten. Das Rohprodukt wurde ohne weitere Reinigung in den nachfolgenden Reaktionsschritt eingesetzt.
Ausbeute: 0.80 g (82 % der Theorie)
HPLC-MS: 6.2 Minuten (Agilent Zorbax Stable Bond SB C18, 5 μm, 75 × 4.6 mm, Gradient in 9 Minuten, Wasser/Acetonitril/Ameisensäure 10/90/0.1 → 90/10/0.1 v/v/v)
ESI-MS: (M+H)+ = 490The intermediate was analogously to intermediate 5 starting from 2- (7-methyl-1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1 Methyl 3-benzodiazepin-3-yl) piperidin-1-yl] butyrate. The crude product was used without further purification in the subsequent reaction step.
Yield: 0.80 g (82% of theory)
HPLC-MS: 6.2 minutes (Agilent Zorbax Stable Bond SB C18, 5 μm, 75 × 4.6 mm, gradient in 9 minutes, water / acetonitrile / formic acid 10/90 / 0.1 → 90/10 / 0.1 v / v / v)
ESI-MS: (M + H) + = 490

B) Herstellung von EndverbindungenB) Preparation of end compounds

Herstellung von Beispiel (5):Production of example (5):

(S)-2-(1H-Indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion

Figure 00670001
(S) -2- (1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione
Figure 00670001

Zu einer Lösung von 600.0 mg (1.262 mmol) 2-(1H-Indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-buttersäure in 30 mL THF wurde bei RT 450.0 mg (1.345 mmol) TBTU und 0. 270 mL (1.532 mmol) Hünigsbase zugegeben und das Gemisch 30 Minuten gerührt. 250.0 mg (1.373 mmol) 1-Methyl-4-piperidin-4-yl-piperazin wurde zugegeben und das Gemisch weiter 16 h bei RT gerührt. Das Reaktionsgemisch wurde mit 50 mL EtOAc verdünnt und die org. Phase zweimal mit 15%-iger wässriger Kaliumcarbonat-Lösung gewaschen. Die org. Phase wurde über Magnesiumsulfat getrocknet und i. vac. eingeengt. Das Rohprodukt wurde mittels Säulenchromatographie (Kieselgel, Gradient Dichlormethan/MeOH/ges. wässriger Ammoniak 100/0/0 → 80/18/2) gereinigt. Der Rückstand wurde mit Diisopropylether verrieben und i. vac. bei 50 °C getrocknet.
Ausbeute: 520 mg (64% der Theorie)
Rf = 0.37 (Kieselgel, Dichlormethan/Cyclohexan/MeOH/konz. wässriger Ammoniak 70/15/15/2 v/v/v/v)
ESI-MS: (M+H)+ = 641To a solution of 600.0 mg (1.262 mmol) 2- (1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -butyric acid in 30 mL THF at RT 450.0 mg (1.345 mmol) TBTU and 0. 270 mL (1.532 mmol) Hünigsbase was added and the mixture was stirred for 30 minutes. 250.0 mg (1.373 mmol) of 1-methyl-4-piperidin-4-yl-piperazine was added and the mixture was stirred at RT for a further 16 h. The reaction mixture was diluted with 50 mL EtOAc and the org. Phase washed twice with 15% aqueous potassium carbonate solution. The org. Phase was dried over magnesium sulfate and i. vac. concentrated. The crude product was purified by column chromatography (silica gel, gradient dichloromethane / MeOH / saturated aqueous ammonia 100/0/0 → 80/18/2). The residue was triturated with diisopropyl ether and i. vac. dried at 50 ° C.
Yield: 520 mg (64% of theory)
R f = 0.37 (silica gel, dichloromethane / cyclohexane / MeOH / concentrated aqueous ammonia 70/15/15/2 v / v / v / v)
ESI-MS: (M + H) + = 641

Herstellung von Beispiel 39:Production of example 39:

2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion

Figure 00670002
2- (7-methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione
Figure 00670002

Das Produkte wurde analog zu Beispiel 1 aus 2-(7-Methyl-1H-indazol-5-ylmethyl)-4- oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-buttersäure (Zwischenprodukt 10) und 1-Methyl-4-piperidin-4-yl-piperazin erhalten. Das Rohprodukt wurde mittels HPLC-MS (Agilent Zorbax Stable Bond SB C18, 5 μm, 75 × 4.6 mm, Wasser/Acetonitril/Ameisensäure 10/90/0.1 → 90/10/0.1 v/v/v) gereinigt.
Ausbeute: 360 mg (34% der Theorie)
Rf = 0.35 (Kieselgel, Dichlormethan/MeOH/konz. wässriger Ammoniak 85/15/1.5 v/v/v)
ESI-MS: (M+H)+ = 655The product was prepared analogously to Example 1 from 2- (7-methyl-1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) -piperidin-1-yl] -butyric acid (interm. 10) and 1-methyl-4-piperidin-4-yl-piperazine. The crude product was purified by HPLC-MS (Agilent Zorbax Stable Bond SB C18, 5 μm, 75 x 4.6 mm, water / acetonitrile / formic acid 10/90 / 0.1 → 90/10 / 0.1 v / v / v).
Yield: 360 mg (34% of theory)
R f = 0.35 (silica gel, dichloromethane / MeOH / concentrated aqueous ammonia 85/15 / 1.5 v / v / v)
ESI-MS: (M + H) + = 655

Analog können folgende Beispiele hergestellt werden:

Figure 00680001
1-1,4'-Bipiperidinyl-1'-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00680002
2-(1H-Indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00680003
1-4,4'-Bipiperidinyl-1-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00680004
1-(4-Dimethylamino-piperidin-1-yl)-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00690001
2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00690002
2-(1H-Indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00690003
2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00690004
2-(1H-Indazol-5-ylmethyl)-1-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00690005
2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00700001
2-(1H-Indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00700002
2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-butan-1,4-dion,
Figure 00700003
1-[4-(4-fluor-phenyl)-piperazin-1-yl]-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00700004
1-[4-(4-fluor-phenyl)-piperidin-1-yl]-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00700005
2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-pyridin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00710001
(1'-{2-(1H-Indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butyryl}-4,4'-bipiperidinyl-1-yl)-essigsäure-methylester,
Figure 00710002
2-(1H-Indazol-5-ylmethyl)-1-(1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00710003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00710004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 00710005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00720001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(4-dimethylamino-piperidin-1-yl)-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00720002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 00720003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 00720004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 00720005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 00730001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 00730002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 00730003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-2-oxo-ethyl}-amid,
Figure 00730004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-ethyl]-amid,
Figure 00740001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperazin-1-yl]-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00740002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperidin-1-yl]-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00740003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-pyridin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 00740004
[1'-(3-(1H-Indazol-5-yl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionyl)-4,4'-bipiperidinyl-1-yl]-essigsäure-methylester,
Figure 00740005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-(1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 00750001
1-1,4'-Bipiperidinyl-1'-yl-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00750002
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-1H-indazol-5-ylmethyl)-4-(4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00750003
1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00750004
1-(4-Dimethylamino-piperidin-1-yl)-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00750005
2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00760001
2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00760002
2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00760003
2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00760004
2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00760005
2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00770001
2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-butan-1,4-dion,
Figure 00770002
1-[4-(4-fluor-phenyl)-piperazin-1-yl]-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00770003
1-[4-(4-fluor-phenyl)-piperidin-1-yl]-2-(7-methyl-1H-indazol-5-ylmethyl)-4-(4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00770004
2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-pyridin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00780001
(1'-{2-(7-Methyl-1H-indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butyryl}-4,4'-bipiperidinyl-1-yl)-essigsäure-methylester,
Figure 00780002
1-(1'-Methanesulfonyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00780003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00780004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00780005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00790001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(4-dimethylamino-piperidin-1-yl)-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00790002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 00790003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 00790004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 00800001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 00800002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 00800003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 00800004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-2-oxo-ethyl}-amid,
Figure 00800005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-ethyl]-amid,
Figure 00810001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperazin-1-yl]-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00810002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperidin-1-yl]-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00810003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-pyridin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 00810004
[1'-(3-(7-Methyl-1H-indazol-5-yl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionyl)-4,4'-bipiperidinyl-1-yl]-essigsäure-methylester,
Figure 00820001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00820002
2-(1H-Indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00820003
1-4,4'-Bipiperidinyl-1-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00820004
2-(1H-Indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00820005
2-(1H-Indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00830001
2-(1H-Indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00830002
2-(1H-Indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00830003
1-1,4'-Bipiperidinyl-1'-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00830004
1-(4-Dimethylamino-piperidin-1-yl)-2-(1H-indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00830005
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 00840001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00840002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 00840003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 00840004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 00840005
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 00850001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00850002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [2-(4-dimethylamino-piperidin-1-yl)-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00850003
2-(7-Ethyl-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00850004
1-4,4'-Bipiperidinyl-1-yl-2-(7-ethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00850005
2-(7-Ethyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00860001
2-(7-Ethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00860002
2-(7-Ethyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00860003
2-(7-Ethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00860004
2-(7-Chlor-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00860005
1-4,4'-Bipiperidinyl-1-yl-2-(7-chlor-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00870001
2-(7-Chlor-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00870002
2-(7-Chlor-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00870003
2-(7-chlor-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00870004
2-(7-Chlor-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00870005
2-(7-Brom-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00880001
1-4,4'-Bipiperidinyl-1-yl-2-(7-brom-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00880002
2-(7-Brom-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00880003
2-(7-Brom-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00880004
2-(7-Brom-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00890001
2-(7-Brom-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00890002
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
Figure 00890003
1-4,4'-Bipiperidinyl-1-yl-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
Figure 00890004
2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00890005
4-[4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
Figure 00900001
1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
Figure 00900002
4-[4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion,
Figure 00900003
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(1-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00900004
1-4,4'-Bipiperidinyl-1-yl-2-(1-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00900005
2-(1-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00910001
2-(1-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00910002
2-(1-Methyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00910003
2-(1-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00910004
2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00920001
1-4,4'-Bipiperidinyl-1-yl-2-(1,7-dimethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00920002
2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00920003
2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00920004
2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00920005
2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00930001
2-(1H-Benzotriazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00930002
2-(1H-Benzotriazol-5-ylmethyl)-1-4,4'-bipiperidinyl-1-yl-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00930003
2-(1H-Benzotriazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00930004
2-(1H-Benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00930005
2-(1H-Benzotriazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00940001
2-(1H-Benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00940002
2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00940003
1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-1H-benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00940004
2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00940005
2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00950001
2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00950002
2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00950003
2-(1H-Indol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00950004
1-4,4'-Bipiperidinyl-1-yl-2-(1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00950005
2-(1H-Indol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00960001
2-(1H-Indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00960002
2-(1H-Indol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00960003
2-(1H-Indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00960004
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00960005
1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00970001
2-(7-Methyl-1H-indol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00970002
2-(7-Methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 00970003
2-(7-Methyl-1H-indol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 00970004
2-(7-Methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 00980001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-ethyl-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 00980002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-ethyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00980003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-ethyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 00980004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-ethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 00980005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-ethyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 00990001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-ethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 00990002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-chlor-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 00990003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-chlor-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 00990004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-chlor-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 00990005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-chlor-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01000001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-chlor-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01000002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-chlor-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01000003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-brom-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 01000004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-brom-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01000005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-brom-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01010001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-brom-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01010002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-brom-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01010003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-brom-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01010004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
Figure 01020001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
Figure 01020002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
Figure 01020003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
Figure 01020004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
Figure 01020005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid,
Figure 01030001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(1-methyl-H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01030002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01030003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1-methyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01030004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01040001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1-methyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01040002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01040003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 01040004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01040005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01050001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01050002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01050003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01050004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 01060001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-4,4'-bipiperidinyl-1-yl-2-oxo-ethyl]-amid,
Figure 01060002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-benzotriazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01060003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01060004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-benzotriazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01060005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01070001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 01070002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01070003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01070004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01070005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01080001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01080002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 01080003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1H-indol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01080004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01090001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01090002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01090003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01090004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01090005
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01100001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01100002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01100003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01100004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01100005
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01110001
1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01110002
1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01110003
2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01110004
1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01120001
2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01120002
1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01120003
1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01120004
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01130001
1-4,4'-Bipiperidinyl-1-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01130002
2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01130003
2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01130004
2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01140001
2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01140002
1-1,4'-Bipiperidinyl-1'-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01140003
1-(4-Dimethylamino-piperidin-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01140004
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01150001
1-4,4'-Bipiperidinyl-1-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01150002
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01150003
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01150004
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01160001
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01160002
1-1,4'-Bipiperidinyl-1'-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01160003
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(4-dimethylamino-piperidin-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01160004
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01170001
1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-(4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01170002
1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01170003
2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01170004
1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01180001
2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01180002
1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01180003
1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01180004
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01190001
1-4,4'-Bipiperidinyl-1-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01190002
2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01190003
2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01190004
2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01200001
2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01200002
1-1,4'-Bipiperidinyl-1'-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01200003
1-(4-Dimethylamino-piperidin-1-yl)-2-(4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01200004
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01210001
1-4,4'-Bipiperidinyl-1-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01210002
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methylpiperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01210003
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01210004
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methylpiperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01220001
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01220002
1-1,4'-Bipiperidinyl-1'-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01220003
2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(4-dimethylaminopiperidin-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01220004
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01230001
1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01230002
1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01230003
2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01230004
1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01240001
2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01240002
1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01240003
1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01240004
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01250001
1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01250002
2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01250003
2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01250004
2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01260001
2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01260002
1-1,4'-Bipiperidinyl-1'-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01260003
1-(4-Dimethylamino-piperidin-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01260004
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01270001
1-4,4'-Bipiperidinyl-1-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01270002
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01270003
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01270004
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methylpiperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01280001
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01280002
1-1,4'-Bipiperidinyl-1'-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01280003
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(4-dimethylamino-piperidin-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01280004
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01290001
1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01290002
1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01290003
2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01290004
1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01300001
2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01300002
1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01300003
1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01300004
1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01310001
1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01310002
2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01310003
2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-ylpiperidin-1-yl)-butan-1,4-dion,
Figure 01310004
2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methylpiperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01320001
2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion,
Figure 01320002
1-1,4'-Bipiperidinyl-1'-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01320003
1-(4-Dimethylamino-piperidin-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01320004
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01330001
1-4,4'-Bipiperidinyl-1-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01330002
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01330003
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01330004
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01340001
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-ylpiperazin-1-yl)-butan-1,4-dion,
Figure 01340002
1-1,4'-Bipiperidinyl-1'-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01340003
2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(4-dimethylamino-piperidin-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01340004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01350001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01350002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01350003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01350004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01360001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01360002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01360003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01360004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01370001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-4,4'-bipiperidinyl-1-yl-1-(4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01370002
2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion,
Figure 01370003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01370004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-{1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01380001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01380002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-1,4'-bipiperidinyl-1'-yl-1-(4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01380003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-(4-dimethylamino-piperidin-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01380004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 01390001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-4,4'-bipiperidinyl-1-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01390002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01390003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01390004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01400001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01400002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-1,4'-bipiperidinyl-1'-yl-1-(4-chlor-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01400003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-dimethylamino-piperidin-1-yl)-2-oxo-ethyl]-amid,
Figure 01400004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01410001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01410002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01410003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperazin-1-ylpiperidin-1-yl)-ethyl]-amid,
Figure 01410004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01420001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01420002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01420003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid,
Figure 01420004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01430001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01430002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(4-methylpiperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01430003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01430004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01440001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01440002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01440003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01440004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 01450001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01450002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01450003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01450004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methylpiperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01460001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01460002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01460003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-dimethylamino-piperidin-1-yl)-2-oxo-ethyl]-amid,
Figure 01460004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01470001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01470002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01470003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01470004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01480001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01480002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01480003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01480004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01490001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01490002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01490003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01490004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01500001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01500002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-1,4'-bipiperidinyl-1'-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01500003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-(4-dimethylamino-piperidin-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01500004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 01510001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-4,4'-bipiperidinyl-1-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01510002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01510003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01510004
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01520001
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01520002
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[2-1,4'-bipiperidinyl-1'-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01520003
4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure-[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-dimethylamino-piperidin-1-yl)-2-oxo-ethyl]-amid,
Figure 01520004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01530001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01530002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01530003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperazin-1-ylpiperidin-1-yl)-ethyl]-amid,
Figure 01530004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01540001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperidin-4-ylpiperazin-1-yl)-ethyl]-amid,
Figure 01540002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01540003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid,
Figure 01540004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01550001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01550002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methylpiperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01550003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01550004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methylpiperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01560001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01560002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01560003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01560004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid,
Figure 01570001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01570002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methylpiperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid,
Figure 01570003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid,
Figure 01570004
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methylpiperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid,
Figure 01580001
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid,
Figure 01580002
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid,
Figure 01580003
4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-dimethylamino-piperidin-1-yl)-2-oxo-ethyl]-amid,
Figure 01580004
2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidin-1-yl]-1-(4-pyrrolidin-1-yl-piperidin-1-yl)-butan-1,4-dion,
Figure 01580005
4-(2-Oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carbonsäure-[1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-pyrrolidin-1-yl-piperidin-1-yl)-ethyl]-amid. The following examples can be prepared analogously:
Figure 00680001
1-1,4'-Bipiperidinyl-1'-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00680002
2- (1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00680003
1-4,4'-bipiperidinyl-1-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine -3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00680004
1- (4-dimethylamino-piperidin-1-yl) -2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00690001
2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00690002
2- (1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00690003
2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00690004
2- (1H-indazol-5-yl-methyl) -1- [4- (4-methyl-perhydro-1,4-diazepin-1-yl) piperidin-1-yl] -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00690005
2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00700001
2- (1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00700002
2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -butan-1,4-dione,
Figure 00700003
1- [4- (4-fluoro-phenyl) -piperazin-1-yl] -2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00700004
1- [4- (4-fluoro-phenyl) -piperidin-1-yl] -2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00700005
2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-pyridin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00710001
(1 '- {2- (1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) piperidin-1-yl] -butyryl} -4,4'-bipiperidinyl-1-yl) -acetic acid methylester,
Figure 00710002
2- (1H-indazol-5-ylmethyl) -1- (1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00710003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1 (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00710004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2- (1 'methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 00710005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00720001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00720002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4 - (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 00720003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo] 2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 00720004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4 - (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 00720005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo] 2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 00730001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4 - (4-methyl-perhydro-1,4-diazepin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 00730002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo] 2- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 00730003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4 - (1-methyl-piperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -2-oxo-ethyl} -amide,
Figure 00730004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo] 2- (4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -ethyl] -amide,
Figure 00740001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -piperazine-1 -yl] -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00740002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -piperidine-1 -yl] -1- (1H-indazol-5ylmethyl) -2-oxo-ethyl] -amide,
Figure 00740003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo] 2- (4-pyridin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 00740004
[1 '- (3- (1H-indazol-5-yl) -2 - {[4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine -1-carbonyl] -amino} -propionyl) -4,4'-bipiperidinyl-1-yl] -acetic acid methylester,
Figure 00740005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2- (1 '-methanesulfonyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 00750001
1-1,4'-Bipiperidinyl-1'-yl-2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro- 1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00750002
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-1H-indazol-5-ylmethyl) -4- (4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00750003
1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00750004
1- (4-dimethylamino-piperidin-1-yl) -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro- 1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00750005
2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00760001
2- (7-methyl-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00760002
2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00760003
2- (7-methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-perhydro-1,4-diazepin-1-yl) piperidin-1-yl] -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00760004
2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00760005
2- (7-methyl-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00770001
2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -butan-1,4-dione,
Figure 00770002
1- [4- (4-fluoro-phenyl) -piperazin-1-yl] -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00770003
1- [4- (4-fluoro-phenyl) -piperidin-1-yl] -2- (7-methyl-1H-indazol-5-ylmethyl) -4- (4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00770004
2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-pyridin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00780001
(1 '- {2- (7-methyl-1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine -3-yl) -piperidin-1-yl] -butyryl} -4,4'-bipiperidinyl-1-yl) -acetic acid methylester,
Figure 00780002
1- (1'-Methanesulfonyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00780003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1 (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00780004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1 -yl) -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00780005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00790001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00790002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazol-5-ylmethyl) - 2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 00790003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 00790004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazol-5-ylmethyl) - 2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 00800001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 00800002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazol-5-ylmethyl) - 2- [4- (4-methyl-perhydro-1,4-diazepin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 00800003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 00800004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazol-5-ylmethyl) - 2- [4- (1-methyl-piperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -2-oxo-ethyl} -amide,
Figure 00800005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -ethyl] -amide,
Figure 00810001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -piperazine-1 -yl] -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00810002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -piperidine-1 -yl] -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00810003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-pyridin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 00810004
[1 '- (3- (7-Methyl-1H-indazol-5-yl) -2 - {[4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3- yl) -piperidine-1-carbonyl] -amino} -propionyl) -4,4'-bipiperidinyl-1-yl] -acetic acid methylester,
Figure 00820001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methanesulfonyl-4,4'-bipiperidinyl-1 -yl) -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00820002
2- (1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (5-oxo-3-phenyl-4,5- dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 00820003
1-4,4'-bipiperidinyl-1-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4 triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 00820004
2- (1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (5-oxo-3-phenyl- 4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 00820005
2- (1H-indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl ] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00830001
2- (1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (5-oxo-3-phenyl- 4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 00830002
2- (1H-indazol-5-yl-methyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl ] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00830003
1-1,4'-Bipiperidinyl-1'-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2, 4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 00830004
1- (4-dimethylamino-piperidin-1-yl) -2- (1H-indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2, 4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 00830005
4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 00840001
4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 - (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00840002
4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 00840003
4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2- oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 00840004
4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 00840005
4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2- oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 00850001
4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl] 1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00850002
4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -] 1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00850003
2- (7-ethyl-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00850004
1-4,4'-bipiperidinyl-1-yl-2- (7-ethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00850005
2- (7-ethyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00860001
2- (7-ethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00860002
2- (7-ethyl-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00860003
2- (7-ethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00860004
2- (7-chloro-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00860005
1-4,4'-bipiperidinyl-1-yl-2- (7-chloro-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00870001
2- (7-chloro-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00870002
2- (7-chloro-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00870003
2- (7-chloro-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00870004
2- (7-chloro-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00870005
2- (7-bromo-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00880001
1-4,4'-bipiperidinyl-1-yl-2- (7-bromo-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00880002
2- (7-bromo-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00880003
2- (7-bromo-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00880004
2- (7-bromo-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00890001
2- (7-bromo-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00890002
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) piperidin-1-yl] -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
Figure 00890003
1-4,4'-bipiperidinyl-1-yl-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
Figure 00890004
2- (7-methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00890005
4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidine -1-yl) -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
Figure 00900001
1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) -piperidin-1-yl] -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
Figure 00900002
4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazine -1-yl) -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione,
Figure 00900003
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (1-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00900004
1-4,4'-bipiperidinyl-1-yl-2- (1-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00900005
2- (1-methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00910001
2- (1-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00910002
2- (1-methyl-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00910003
2- (1-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00910004
2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00920001
1-4,4'-bipiperidinyl-1-yl-2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepine-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00920002
2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00920003
2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine -1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00920004
2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00920005
2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine -1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00930001
2- (1H-benzotriazole-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00930002
2- (1H-benzotriazol-5-ylmethyl) -1-4,4'-bipiperidinyl-1-yl-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine -3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00930003
2- (1H-benzotriazole-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00930004
2- (1H-benzotriazole-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00930005
2- (1H-benzotriazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00940001
2- (1H-benzotriazole-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00940002
2- (7-methyl-1H-benzotriazole-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00940003
1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-1H-benzotriazole-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00940004
2- (7-methyl-1H-benzotriazole-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00940005
2- (7-methyl-1H-benzotriazole-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00950001
2- (7-methyl-1H-benzotriazole-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00950002
2- (7-methyl-1H-benzotriazole-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00950003
2- (1H-Indol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00950004
1-4,4'-bipiperidinyl-1-yl-2- (1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine -3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00950005
2- (1H-Indol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00960001
2- (1H-Indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00960002
2- (1H-Indol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00960003
2- (1H-Indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00960004
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00960005
1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1 , 3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00970001
2- (7-methyl-1H-indol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00970002
2- (7-methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 00970003
2- (7-methyl-1H-indol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 00970004
2- (7-methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 00980001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-ethyl-1H-indazol-5-ylmethyl) -] 2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 00980002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 7-ethyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00980003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-ethyl-1H-indazol-5-ylmethyl) - 2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 00980004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-ethyl-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 00980005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-ethyl-1H-indazol-5-ylmethyl) - 2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 00990001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-ethyl-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 00990002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-1H-indazol-5-ylmethyl) -] 2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 00990003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 7-chloro-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 00990004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-1H-indazol-5-ylmethyl) - 2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 00990005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01000001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-1H-indazol-5-ylmethyl) - 2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01000002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01000003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-bromo-1H-indazol-5-ylmethyl) - 2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 01000004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 7-bromo-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01000005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-bromo-1H-indazol-5-ylmethyl) - 2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01010001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-bromo-1H-indazol-5-ylmethyl) - 2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01010002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-bromo-1H-indazol-5-ylmethyl) - 2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01010003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-bromo-1H-indazol-5-ylmethyl) - 2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01010004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1 -yl) -2-oxo-1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
Figure 01020001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2-oxo -1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
Figure 01020002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -2-oxo-1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
Figure 01020003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-2- (4-piperazin-1-yl-piperidine -1-yl) -1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
Figure 01020004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2-oxo-1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
Figure 01020005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-2- (4-piperidin-4-yl-piperazine -1-yl) -1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide,
Figure 01030001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1 -yl) -1- (1-methyl-H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01030002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 1-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01030003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1-methyl-1H-indazol-5-ylmethyl) - 2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01030004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1-methyl-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01040001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1-methyl-1H-indazol-5-ylmethyl) - 2- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01040002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1-methyl-1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01040003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1,7-dimethyl-1H-indazol-5-ylmethyl ) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 01040004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 1,7-dimethyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01040005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1,7-dimethyl-1H-indazol-5-ylmethyl ) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01050001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1,7-dimethyl-1H-indazol-5-ylmethyl ) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01050002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1,7-dimethyl-1H-indazol-5-ylmethyl ) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01050003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1,7-dimethyl-1H-indazol-5-ylmethyl ) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01050004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-ylmethyl) -2- (1 'methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 01060001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-ylmethyl) -2-4, 4'-bipiperidinyl-1-yl-2-oxo-ethyl] -amide,
Figure 01060002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-benzotriazol-5-ylmethyl) -2- [4 - (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01060003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-ylmethyl) -2-oxo] 2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01060004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-benzotriazol-5-ylmethyl) -2- [4 - (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01060005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-ylmethyl) -2-oxo] 2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01070001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-benzotriazol-5-ylmethyl) -] 2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 01070002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 7-methyl-1H-benzotriazole-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01070003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-benzotriazol-5-ylmethyl) - 2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01070004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-benzotriazol-5-ylmethyl) -] 2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01070005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-benzotriazol-5-ylmethyl) - 2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01080001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-benzotriazol-5-ylmethyl) -] 2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01080002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indol-5-ylmethyl) -2- (1 'methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 01080003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 1H-indol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01080004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indol-5-ylmethyl) -2- [4 - (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01090001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indol-5-ylmethyl) -2-oxo 2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01090002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indol-5-ylmethyl) -2- [4 - (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01090003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indol-5-ylmethyl) -2-oxo 2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01090004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1 -yl) -1- (7-methyl-1H-indol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01090005
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 ( 7-methyl-1H-indol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01100001
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indol-5-ylmethyl) - 2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01100002
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indol-5-ylmethyl) -] 2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01100003
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indol-5-ylmethyl) - 2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01100004
4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indol-5-ylmethyl) -] 2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01100005
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01110001
1-4,4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01110002
1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- ( 2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01110003
2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01110004
1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- ( 2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01120001
2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01120002
1-1,4'-Bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4, 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01120003
1- (4-dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4, 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01120004
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- ( 2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01130001
1-4,4'-bipiperidinyl-1-yl-2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2 , 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01130002
2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01130003
2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) piperidine-1yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01130004
2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01140001
2- (4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01140002
1-1,4'-Bipiperidinyl-1'-yl-2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01140003
1- (4-dimethylamino-piperidin-1-yl) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01140004
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- ( 2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01150001
1-4,4'-bipiperidinyl-1-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2 , 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01150002
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01150003
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01150004
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01160001
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01160002
1-1,4'-Bipiperidinyl-1'-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01160003
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (4-dimethylamino-piperidin-1-yl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01160004
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo- 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01170001
1-4,4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- (4- (5-oxo-3-phenyl-4,5 dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01170002
1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- ( 5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01170003
2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1- yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01170004
1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- ( 5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01180001
2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1- yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01180002
1-1,4'-Bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4, 5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01180003
1- (4-dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4, 5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01180004
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- ( 5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01190001
1-4,4'-bipiperidinyl-1-yl-2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl -4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01190002
-2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01190003
2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4- triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01190004
2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01200001
2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4- triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazine-1-yl) -butan-1,4-dione,
Figure 01200002
1-1,4'-Bipiperidinyl-1'-yl-2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-yl-methyl) -4- [4- (5-oxo- 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01200003
1- (4-dimethylamino-piperidin-1-yl) -2- (4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl- 4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01200004
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- ( 5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01210001
1-4,4'-bipiperidinyl-1-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl -4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01210002
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -4- [4 - (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01210003
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4- triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01210004
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -4- [4 - (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01220001
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4- triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01220002
1-1,4'-Bipiperidinyl-1'-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3- phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01220003
2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (4-dimethylaminopiperidine-1-yl) -4- [4- (5-oxo-3-phenyl- 4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01220004
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1yl] -butan-1,4-dione,
Figure 01230001
1-4,4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01230002
1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01230003
2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3- yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01230004
1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01240001
2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3- yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01240002
1-1,4'-Bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01240003
1- (4-dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01240004
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01250001
1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01250002
2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] - 4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01250003
2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01250004
2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] - 4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01260001
2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01260002
1-1,4'-Bipiperidinyl-1'-yl-2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01260003
1- (4-dimethylamino-piperidin-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01260004
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01270001
1-4,4'-bipiperidinyl-1-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01270002
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] - 4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01270003
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butane-1,4-dione,
Figure 01270004
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01280001
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01280002
1-1,4'-Bipiperidinyl-1'-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01280003
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (4-dimethylamino-piperidin-1-yl) -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01280004
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5- oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01290001
1-4,4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4 , 5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01290002
1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4 - (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione;
Figure 01290003
2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazole 1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01290004
1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4 - (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01300001
2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazole 1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01300002
1-1,4'-Bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl- 4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01300003
1- (4-dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl- 4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01300004
1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4 - (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01310001
1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01310002
2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] - 4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01310003
2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2, 4-triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01310004
2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01320001
2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2, 4-triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01320002
1-1,4'-Bipiperidinyl-1'-yl-2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo- 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01320003
1- (4-dimethylamino-piperidin-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo- 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01320004
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4 - (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01330001
1-4,4'-bipiperidinyl-1-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01330002
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] - 4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01330003
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2, 4-triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01330004
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] - 4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01340001
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2, 4-triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butan-1,4-dione,
Figure 01340002
1-1,4'-Bipiperidinyl-1'-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo- 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01340003
2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (4-dimethylamino-piperidin-1-yl) -4- [4- (5-oxo- 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione,
Figure 01340004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl- 1-yl) -2-oxo-1- (2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01350001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2- oxo-1- (2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01350002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazin-1-yl ) piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01350003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01350004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidin-4-yl ) piperazin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01360001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3- -dihydro-benzoxazol-ylmethyl 6) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01360002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-2 oxo-1- (2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01360003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -2 oxo-1- (2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01360004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl- 1-yl) -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01370001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01370002
2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione,
Figure 01370003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01370004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (4-methyl-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01380001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01380002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1 - (4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01380003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1 - (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01380004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 01390001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01390002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01390003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01390004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01400001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01400002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1 - (4-chloro-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01400003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -2- (4-dimethylamino-piperidin-1-yl) -2-oxo-ethyl] -amide,
Figure 01400004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl -1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01410001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2 oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01410002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazin-1- yl) piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01410003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01410004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidin-4- yl) piperazin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01420001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01420002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl 2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01420003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) - 2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide,
Figure 01420004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl -1-yl) -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01430001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 - (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01430002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4-methyl-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01430003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo-2,3 dihydro-benzoxazol-6--ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01430004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4-methyl-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01440001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01440002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl 1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01440003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) - 1- (4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01440004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 01450001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 - (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01450002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01450003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01450004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01460001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01460002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl 1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01460003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -2- (4-dimethylamino-piperidin-1-yl) -2-oxo-ethyl] -amide,
Figure 01460004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl- 1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01470001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2- oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01470002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazin-1-yl ) piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01470003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01470004
4- (2-oxo 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidin-4-yl ) piperazin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01480001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01480002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-2 oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01480003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -2 oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01480004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl- 1-yl) -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01490001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01490002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01490003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01490004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01500001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01500002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1 - (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01500003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1 - (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01500004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 01510001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01510002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01510003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01510004
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01520001
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01520002
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1 - (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01520003
4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-dimethylamino-piperidin-1-yl) -2-oxo-ethyl] -amide,
Figure 01520004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl -1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01530001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2 oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01530002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazin-1- yl) piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01530003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperazin-1-ylpiperidin-1-yl) -ethyl] -amide,
Figure 01530004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidin-4- yl) piperazin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01540001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01540002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl 2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01540003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) - 2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide,
Figure 01540004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl -1-yl) -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01550001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 - (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01550002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01550003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01550004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01560001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01560002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl 1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01560003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) - 1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01560004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide,
Figure 01570001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1 - (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01570002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide,
Figure 01570003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide,
Figure 01570004
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide,
Figure 01580001
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2,3 dihydro-1H-benzimidazol-5ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide,
Figure 01580002
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl 1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide,
Figure 01580003
4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2,3 dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-dimethylamino-piperidin-1-yl) -2-oxo-ethyl] -amide,
Figure 01580004
2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-benzo [d] [1,3] diazepin-3-yl) -piperidine 1-yl] -1- (4-pyrrolidin-1-yl-piperidin-1-yl) -butan-1,4-dione,
Figure 01580005
4- (2-oxo-1,2,4,5-tetrahydro-benzo [d] [1,3] diazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl ) -2-oxo-2- (4-pyrrolidin-1-yl-piperidin-1-yl) -ethyl] -amide.

Die nachfolgenden Beispiele beschreiben die Herstellung pharmazeutischer Anwendungsformen, die als Wirkstoff eine beliebige Verbindung der allgemeinen Formel (I) enthalten:The The following examples describe the preparation of pharmaceutical Forms of use, as the active ingredient any compound of general formula (I) include:

Beispiel I:Example I:

Kapseln zur Pulverinhalation mit 1 mg WirkstoffCapsules for powder inhalation with 1 mg of active ingredient

Zusammensetzung:Composition:

1 Kapsel zur Pulverinhalation enthält: Wirkstoff 1.0 mg Milchzucker 20.0 mg Hartgelatinekapseln 50.0 mg 71.0 mg 1 capsule for powder inhalation contains: active substance 1.0 mg lactose 20.0 mg Hard gelatin capsules 50.0 mg 71.0 mg

Herstellungsverfahren:Production method:

Der Wirkstoff wird auf die für Inhalativa erforderliche Korngröße gemahlen. Der gemahlene Wirkstoff wird mit dem Milchzucker homogen gemischt. Die Mischung wird in Hartgelatinekapseln abgefüllt.Of the Active ingredient will be on the for Inhalativa required grain size ground. The ground active substance is mixed homogeneously with the milk sugar. The mixture is filled into hard gelatin capsules.

Beispiel II:Example II:

Inhalationslösung für Respimat® mit 1 mg WirkstoffInhalation solution for Respimat ® with 1 mg active substance

Zusammensetzung:Composition:

1 Hub enthält: Wirkstoff 1.0 mg Benzalkoniumchlorid 0.002 mg Dinatriumedetat 0.0075 mg Wasser gereinigt ad 15.0 μl 1 hub contains: active substance 1.0 mg benzalkonium chloride 0.002 mg disodium edetate 0.0075 mg Water cleaned ad 15.0 μl

Herstellungsverfahren:Production method:

Der Wirkstoff und Benzalkoniumchlorid werden in Wasser gelöst und in Respimat®-Kartuschen abgefüllt.The active ingredient and benzalkonium chloride are dissolved in water and filled into Respimat ® cartridges.

Beispiel III:Example III:

Inhalationslösung für Vernebler mit 1 mg WirkstoffInhalation solution for nebulizers with 1 mg of active ingredient

Zusammensetzung:Composition:

1 Fläschchen enthält: Wirkstoff 0.1 g Natriumchlorid 0.18 g Benzalkoniumchlorid 0.002 g Wasser gereinigt ad 20.0 ml 1 vial contains: active substance 0.1 g sodium chloride 0.18 g benzalkonium chloride 0.002 g Water cleaned ad 20.0 ml

Herstellungsverfahren:Production method:

Wirkstoff, Natriumchlorid und Benzalkoniumchlorid werden in Wasser gelöst.agent Sodium chloride and benzalkonium chloride are dissolved in water.

Beispiel IV:Example IV:

Treibgas-Dosieraerosol mit 1 mg WirkstoffLPG metered with 1 mg of active ingredient

Zusammensetzung:Composition:

1 Hub enthält: Wirkstoff 1.0 mg Lecithin 0.1 Treibgas ad 50.0 μl 1 hub contains: active substance 1.0 mg lecithin 0.1 Propellant ad 50.0 μl

Herstellungsverfahren:Production method:

Der mikronisierte Wirkstoff wird in dem Gemisch aus Lecithin und Treibgas homogen suspendiert. Die Suspension wird in einen Druckbehälter mit Dosierventil abgefüllt.Of the Micronized drug is in the mixture of lecithin and propellant homogeneously suspended. The suspension is in a pressure vessel with Dispensed filling valve.

Beispiel V:Example V:

Nasalspray mit 1 mg WirkstoffNasal spray with 1 mg of active ingredient

Zusammensetzung: Wirkstoff 1.0 mg Natriumchlorid 0.9 mg Benzalkoniumchlorid 0.025 mg Dinatriumedetat 0.05 mg Wasser gereinigt ad 0.1 ml Composition: active substance 1.0 mg sodium chloride 0.9 mg benzalkonium chloride 0.025 mg disodium edetate 0.05 mg Water cleaned ad 0.1 ml

Herstellunasverfahren:Herstellunasverfahren:

Der Wirkstoff und die Hilfsstoffe werden in Wasser gelöst und in ein entsprechendes Behältnis abgefüllt.Of the Active ingredient and the excipients are dissolved in water and in a corresponding container bottled.

Beispiel VI:Example VI:

Injektionslösung mit 5 mg Wirksubstanz pro 5 mlSolution for injection with 5 mg of active substance per 5 ml

Zusammensetzung: Wirksubstanz 5 mg Glucose 250 mg Human-Serum-Albumin 10 mg Glykofurol 250 mg Wasser für Injektionszwecke ad 5 ml Composition: active substance 5 mg glucose 250 mg Human serum albumin 10 mg glycofurol 250 mg Water for injections ad 5 ml

Herstellung:production:

Glykofurol und Glucose in Wasser für Injektionszwecke auflösen (Wfl); Human-Serum-Albumin zugeben; Wirkstoff unter Erwärmen auflösen; mit Wfl auf Ansatzvolumen auffüllen; unter Stickstoff-Begasung in Ampullen abfüllen.glycofurol and glucose in water for Dissolve injections (Wfl); Human serum albumin release; Active ingredient with heating dissolve; fill with Wfl to batch volume; Fill into ampoules under nitrogen fumigation.

Beispiel VII:Example VII:

Injektionslösung mit 100 mg Wirksubstanz pro 20 mlSolution for injection with 100 mg of active substance per 20 ml

Zusammensetzung: Wirksubstanz 100 mg Monokaliumdihydrogenphosphat = KH2PO4 12 mg Dinatriumhydrogen phosphat = Na2HPO4·2H2O 2 mg Natriumchlorid 180 mg Human-Serum-Albumin 50 mg Polysorbat 80 20 mg Wasser für Injektionszwecke ad 20 ml Composition: active substance 100 mg Monopotassium dihydrogenphosphate = KH 2 PO 4 12 mg Disodium hydrogen phosphate = Na 2 HPO 4 .2H 2 O 2 mg sodium chloride 180 mg Human serum albumin 50 mg Polysorbate 80 20 mg Water for injections ad 20 ml

Herstellung:production:

Polysorbat 80, Natriumchlorid, Monokaliumdihydrogenphosphat und Dinatriumhydrogenphosphat in Wasser für Injektionszwecke (Wfl) auflösen; Human-Serum-Albumin zugeben; Wirkstoff unter Erwärmen auflösen; mit Wfl auf Ansatzvolumen auffüllen; in Ampullen abfüllen.polysorbate 80, sodium chloride, monopotassium dihydrogen phosphate and disodium hydrogen phosphate in water for Injection (Wfl) dissolve; Add human serum albumin; Dissolve active ingredient with heating; with Wfl on batch volume fill up; fill in ampoules.

Beispiel VIII:Example VIII:

Lyophilisat mit 10 mg WirksubstanzLyophilisate with 10 mg active substance

Zusammensetzung: Wirksubstanz 10 mg Mannit 300 mg Human-Serum-Albumin 20 mg Composition: active substance 10 mg mannitol 300 mg Human serum albumin 20 mg

Herstellung:production:

Mannit in Wasser für Injektionszwecke (Wfl) auflösen; Human-Serum-Albumin zugeben; Wirkstoff unter Erwärmen auflösen; mit Wfl auf Ansatzvolumen auffüllen; in Vials abfüllen; gefriertrocknen.mannitol in water for Injection (Wfl) dissolve; Add human serum albumin; Dissolve active ingredient with heating; with Wfl on batch volume fill up; to fill in vials; freeze-dry.

Lösungsmittel für Lyophilisat: Polysorbat 80 = Tween 80 20 mg Mannit 200 mg Wasser für Injektionszwecke ad 10 ml Solvent for lyophilisate: Polysorbate 80 = Tween 80 20 mg mannitol 200 mg Water for injections ad 10 ml

Herstellung:production:

Polysorbat 80 und Mannit in Wasser für Injektionszwecke (Wfl) auflösen; in Ampullen abfüllen.polysorbate 80 and mannitol in water for Injection (Wfl) dissolve; fill in ampoules.

Beispiel IX:Example IX:

Tabletten mit 20 mg WirksubstanzTablets containing 20 mg of active substance

Zusammensetzung: Wirksubstanz 20 mg Lactose 120 mg Maisstärke 40 mg Magnesiumstearat 2 mg Povidon K 25 18 mg Composition: active substance 20 mg lactose 120 mg corn starch 40 mg magnesium stearate 2 mg Povidone K 25 18 mg

Herstellung:production:

Wirksubstanz, Lactose und Maisstärke homogen mischen; mit einer wässerigen Lösung von Povidon granulieren; mit Magnesiumstearat mischen; auf einer Tablettenpresse abpressen; Tablettengewicht 200 mg.Active substance, Lactose and corn starch mix homogeneously; with a watery solution granulate of povidone; mix with magnesium stearate; on a Press off tablet press; Tablet weight 200 mg.

Beispiel X:Example X:

Kapseln mit 20 mg WirksubstanzCapsules with 20 mg active substance

Zusammensetzung: Wirksubstanz 20 mg Composition: active substance 20 mg

Maisstärkecorn starch 80 mg80 mg Kieselsäure. hochdispersSilica. highly dispersed 5 mg5 mg Magnesiumstearatmagnesium stearate 2.5 mg2.5 mg

Herstellung:production:

Wirksubstanz, Maisstärke und Kieselsäure homogen mischen; mit Magnesiumstearat mischen; Mischung auf einer Kapselfüllmaschine in Hartgelatine-Kapseln Grösse 3 abfüllen.Active substance, corn starch and silica mix homogeneously; mix with magnesium stearate; Mix on one capsule in hard gelatin capsules size 3 fill.

Beispiel XI:Example XI:

Zäpfchen mit 50 mg WirksubstanzSuppository with 50 mg active substance

Zusammensetzung: Wirksubstanz 50 mg Hartfett (Adeps solidus) q.s. ad 1700 mg Composition: active substance 50 mg Hard fat (Adeps solidus) qs ad 1700 mg

Herstellung:production:

Hartfett bei ca. 38°C aufschmelzen; gemahlene Wirksubstanz im geschmolzenen Hartfett homogen dispergieren; nach Abkühlen auf ca. 35°C in vorgekühlte Formen ausgiessen.hard fat at about 38 ° C melt; homogeneously disperse the ground active substance in the molten hard fat; after cooling to about 35 ° C in pre-cooled Pour out molds.

Beispiel XII:Example XII:

Injektionslösung mit 10 mg Wirksubstanz pro 1 mlSolution for injection with 10 mg of active substance per 1 ml

Zusammensetzung: Wirksubstanz 10 mg Mannitol 50 mg Human-Serum-Albumin 10 mg Wasser für Injektionszwecke ad 1 ml Composition: active substance 10 mg mannitol 50 mg Human serum albumin 10 mg Water for injections ad 1 ml

Herstellung:production:

Mannitol in Wasser für Injektionszwecke auflösen (Wfl); Human-Serum-Albumin zugeben; Wirkstoff unter Erwärmen auflösen; mit Wfl auf Ansatzvolumen auffüllen; unter Stickstoff-Begasung in Ampullen abfüllen.mannitol in water for Dissolve injections (Wfl); Add human serum albumin; Dissolve active ingredient with heating; With Fill Wfl to batch volume; Fill into ampoules under nitrogen fumigation.

Claims (10)

CGRP-Antagonisten der allgemeinen Formel
Figure 01660001
in der A ein Stickstoff- oder Sauerstoffatom oder eine CH-Gruppe, B ein Stickstoffatom, eine CH- oder eine Carbonyl-Gruppe, D ein Wasserstoffatom oder eine Methylgruppe, E ein Wasserstoff-, Fluor-, Chlor- oder Bromatom, eine Methyl-, Ethyl- oder Trifluormethylgruppe, X eine Methylen- oder NH-Gruppe, ---- eine Einfachbindung, wenn A ein Sauerstoffatom darstellt, oder eine Doppelbindung, wenn A ein Stickstoffatom oder eine CH-Gruppe darstellt, R1 einen Rest der Formel
Figure 01670001
und R2 einen Rest der Formel
Figure 01670002
bedeuten, deren Tautomere, deren Diastereomere, deren Enantiomere, deren Hydrate, deren Gemische und deren Salze sowie die Hydrate der Salze.CGRP antagonists of the general formula
Figure 01660001
A is a nitrogen or oxygen atom or a CH group, B is a nitrogen atom, a CH or a carbonyl group, D is a hydrogen atom or a methyl group, E is a hydrogen, fluorine, chlorine or bromine atom, a methyl, , Ethyl or trifluoromethyl group, X is a methylene or NH group, ---- is a single bond when A is an oxygen atom, or a double bond when A is a nitrogen atom or a CH group, R 1 is a radical of the formula
Figure 01670001
and R 2 is a radical of the formula
Figure 01670002
their tautomers, their diastereomers, their enantiomers, their hydrates, their mixtures and their salts and the hydrates of the salts. Verbindungen der allgemeinen Formel I gemäß Anspruch 1, in der die Kombination von A, B, D, E und ---- eine Gruppe der Formel
Figure 01680001
R1 einen Rest der Formel
Figure 01680002
und R2 einen Rest der Formel
Figure 01690001
bedeuten, deren Tautomere, deren Diastereomere, deren Enantiomere, deren Hydrate, deren Gemische und deren Salze sowie die Hydrate der Salze.Compounds of the general formula I according to claim 1, in which the combination of A, B, D, E and ---- is a group of the formula
Figure 01680001
R 1 is a radical of the formula
Figure 01680002
and R 2 is a radical of the formula
Figure 01690001
their tautomers, their diastereomers, their enantiomers, their hydrates, their mixtures and their salts and the hydrates of the salts. Folgende Verbindungen der allgemeinen Formel (I) gemäß Anspruch 1: (1) 1-1,4'-Bipiperidinyl-1'-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (2) 2-(1H-Indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (3) 1-4,4'-Bipiperidinyl-1-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (4) 1-(4-Dimethylamino-piperidin-1-yl)-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (5) (S)-2-(1H-Indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (6) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (7) 2-(1H-Indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (8) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (9) 2-(1H-Indazol-5-ylmethyl)-1-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (10) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-butan-1,4-dion, (11) 2-(1H-Indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (12) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-butan-1,4-dion, (13) 1-[4-(4-fluor-phenyl)-piperazin-1-yl]-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (14) 1-[4-(4-fluor-phenyl)-piperidin-1-yl]-2-(1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (15) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-pyridin-4-yl-piperazin-1-yl)-butan-1,4-dion, (16) (1'-{2-(1H-Indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butyryl}-4,4'-bipiperidinyl-1-yl)-essigsäure-methylester, (17) 2-(1H-Indazol-5-ylmethyl)-1-(1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (18) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (19) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (20) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (21) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(4-dimethylamino-piperidin-1-yl)-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (22) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (23) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (24) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (25) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (26) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (27) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-ethyl]-amid, (28) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-2-oxo-ethyl}-amid, (29) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-ethyl]-amid, (30) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperazin-1-yl]-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (31) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperidin-1-yl]-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (32) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-pyridin-4-yl-piperazin-1-yl)-ethyl]-amid, (33) [1'-(3-(1H-Indazol-5-yl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionyl)-4,4'-bipiperidinyl-1-yl]-essigsäure-methylester, (34) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure (1-(1H-indazol-5-ylmethyl)-2-(1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (35) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (36) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (37) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (38) 1-(4-Dimethylamino-piperidin-1-yl)-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (39) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (40) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (41) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (42) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (43) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (44) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-butan-1,4-dion, (45) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (46) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-butan-1,4-dion, (47) 1-[4-(4-fluor-phenyl)-piperazin-1-yl]-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (48) 1-[4-(4-fluor-phenyl)-piperidin-1-yl]-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (49) 2-(7-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-pyridin-4-yl-piperazin-1-yl)-butan-1,4-dion, (50) (1'-{2-(7-Methyl-1H-indazol-5-ylmethyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butyryl}-4,4'-bipiperidinyl-1-yl)-essigsäure-methylester, (51) 1-(1'-Methanesulfonyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (52) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (53) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (54) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (55) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(4-dimethylamino-piperidin-1-yl)-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (56) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (57) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)- ethyl]-amid, (58) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (59) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (60) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-perhydro-1,4-diazepin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (61) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl)-ethyl]-amid, (62) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-perhydro-1,4-diazepin-1-yl]-2-oxo-ethyl}-amid, (63) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl)-ethyl]-amid, (64) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperazin-1-yl]-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (65) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-fluor-phenyl)-piperidin-1-yl]-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (66) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-pyridin-4-yl-piperazin-1-yl)-ethyl]-amid, (67) [1'-(3-(7-Methyl-1H-indazol-5-yl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionyl)-4,4'-bipiperidinyl- 1-yl]-essigsäure-methylester, (68) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (69) 2-(1H-Indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (70) 1-4,4'-Bipiperidinyl-1-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (71) 2-(1H-Indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (72) 2-(1H-Indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (73) 2-(1H-Indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (74) 2-(1H-Indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (75) 1-1,4'-Bipiperidinyl-1'-yl-2-(1H-indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (76) 1-(4-Dimethylamino-piperidin-1-yl)-2-(1H-indazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (77) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (78) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (79) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (80) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (81) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure {1-(1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (82) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (83) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (84) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [2-(4-dimethylamino-piperidin-1-yl)-1-(1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (85) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl)-butan-1,4-dion, (86) 1-4,4'-Bipiperidinyl-1-yl-2-(7-ethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (87) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (88) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (89) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (90) 2-(7-Ethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (91) 2-(7-Chlor-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (92) 1-4,4'-Bipiperidinyl-1-yl-2-(7-chlor-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (93) 2-(7-Chlor-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (94) 2-(7-Chlor-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (95) 2-(7-chlor-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (96) 2-(7-Chlor-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (97) 2-(7-Brom-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (98) 1-4,4'-Bipiperidinyl-1-yl-2-(7-brom-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (99) 2-(7-Brom-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (100) 2-(7-Brom-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (101) 2-(7-Brom-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (102) 2-(7-Brom-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (103) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)- butan-1,4-dion, (104) 1-4,4'-Bipiperidinyl-1-yl-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion, (105) 2-(7-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (106) 4-[4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion, (107) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion, (108) 4-[4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-2-(7-trifluormethyl-1H-indazol-5-ylmethyl)-butan-1,4-dion, (109) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(1-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (110) 1-4,4'-Bipiperidinyl-1-yl-2-(1-methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (111) 2-(1-Methyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (112) 2-(1-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (113) 2-(1-Methyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (114) 2-(1-Methyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan- 1,4-dion, (115) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (116) 1-4,4'-Bipiperidinyl-1-yl-2-(1,7-dimethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (117) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (118) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (119) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (120) 2-(1,7-Dimethyl-1H-indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (121) 2-(1H-Benzotriazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (122) 2-(1H-Benzotriazol-5-ylmethyl)-1-4,4'-bipiperidinyl-1-yl-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (123) 2-(1H-Benzotriazol-5-ylmethyl)-1-(4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (124) 2-(1H-Benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (125) 2-(1H-Benzotriazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4- dion, (126) 2-(1H-Benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (127) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (128) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-1H-benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (129) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (130) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (131) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (132) 2-(7-Methyl-1H-benzotriazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (133) 2-(1H-Indol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (134) 1-4,4'-Bipiperidinyl-1-yl-2-(1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (135) 2-(1H-Indol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (136) 2-(1H-Indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (137) 2-(1H-Indol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (138) 2-(1H-Indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (139) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (140) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (141) 2-(7-Methyl-1H-indol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (142) 2-(7-Methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (143) 2-(7-Methyl-1H-indol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (144) 2-(7-Methyl-1H-indol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (145) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-ethyl-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxoethyl]-amid, (146) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-ethyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (147) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-ethyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (148) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-ethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (149) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-ethyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (150) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-ethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (151) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-chlor-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxoethyl]-amid, (152) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-chlor-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (153) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-chlor-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (154) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-chlor-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (155) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-chlor-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (156) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-chlor-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (157) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-brom-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxoethyl]-amid, (158) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-brom-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (159) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-brom-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1- yl]-2-oxo-ethyl}-amid, (160) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-brom-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (161) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-brom-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (162) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-brom-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (163) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid, (164) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid, (165) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid, (166) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid, (167) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid, (168) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-1-(7-trifluormethyl-1H-indazol-5-ylmethyl)-ethyl]-amid, (169) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo ethyl]-amid, (170) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (171) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1-methyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (172) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (173) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1-methyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (174) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1-methyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (175) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (176) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-oxo-ethyl]-amid, (177) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (178) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (179) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (180) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1,7-dimethyl-1H-indazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (181) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxoethyl]-amid, (182) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-4,4'-bipiperidinyl-1-yl-2-oxo-ethyl]-amid, (183) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-benzotriazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (184) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (185) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-benzotriazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (186) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (187) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (188) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-oxo-ethyl]-amid, (189) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (190) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (191) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (192) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-benzotriazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (193) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (194) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(1H-indol-5-ylmethyl)-2-oxo-ethyl]-amid, (195) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (196) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (197) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(1H-indol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (198) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(1H-indol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (199) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-ethyl]-amid, (200) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-ethyl]-amid, (201) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (202) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (203) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(7-methyl-1H-indol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (204) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [1-(7-methyl-1H-indol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (205) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (206) 1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (207) 1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (208) 2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (209) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (210) 2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (211) 1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (212) 1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]- butan-1,4-dion, (213) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (214) 1-4,4'-Bipiperidinyl-1-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (215) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (216) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (217) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazi n-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (218) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (219) 1-1,4'-Bipiperidinyl-1'-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (220) 1-(4-Dimethylamino-piperidin-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (221) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (222) 1-4,4'-Bipiperidinyl-1-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan- 1,4-dion, (223) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (224) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (225) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (226) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (227) 1-1,4'-Bipiperidinyl-1'-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (228) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(4-dimethylaminopiperidin-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (229) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (230) 1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (231) 1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (232) 2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (233) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (234) 2-(2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (235) 1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (236) 1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (237) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (238) 1-4,4'-Bipiperidinyl-1-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (239) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (240) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (241) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (242) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (243) 1-1,4'-Bipiperidinyl-1'-yl-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-yl methyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (244) 1-(4-Dimethylamino-piperidin-1-yl)-2-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (245) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (246) 1-4,4'-Bipiperidinyl-1-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (247) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (248) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (249) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (250) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (251) 1-1,4'-Bipiperidinyl-1'-yl-2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (252) 2-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-(4-dimethylaminopiperidin-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (253) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol- 5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (254) 1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (255) 1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (256) 2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (257) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (258) 2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (259) 1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (260) 1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (261) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-(4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (262) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (263) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl- piperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (264) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-ylpiperidin-1-yl)-butan-1,4-dion, (265) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (266) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-ylpiperazin-1-yl)-butan-1,4-dion, (267) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (268) 1-(4-Dimethylamino-piperidin-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (269) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(1'-methyl-4,4'-bipiperidinyl-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (270) 1-4,4'-Bipiperidinyl-1-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (271) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methylpiperazin-1-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (272) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (273) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methyl- piperidin-4-yl)-piperazin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (274) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (275) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (276) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(4-dimethylamino-piperidin-1-yl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (277) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (278) 1-4,4'-Bipiperidinyl-1-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (279) 1-[4-(4-Methyl-piperazin-1-yl)-piperidin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (280) 2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-yl-piperidin-1-yl)-butan-1,4-dion, (281) 1-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-yl]-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (282) 2-(2-Oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-yl-piperazin-1-yl)-butan-1,4-dion, (283) 1-1,4'-Bipiperidinyl-1'-yl-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)- 4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (284) 1-(4-Dimethylamino-piperidin-1-yl)-2-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (285) 1-(1'-Methyl-4,4'-bipiperidinyl-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (286) 1-4,4'-Bipiperidinyl-1-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (287) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (288) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-ylpiperidin-1-yl)-butan-1,4-dion, (289) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (290) 2-(7-Methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-ylpiperazin-1-yl)-butan-1,4-dion, (291) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (292) 1-(4-Dimethylamino-piperidin-1-yl)-2-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (293) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(1'-methyl-4,4'- bipiperidinyl-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (294) 1-4,4'-Bipiperidinyl-1-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (295) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (296) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperazin-1-ylpiperidin-1-yl)-butan-1,4-dion, (297) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-[4-(1-methylpiperidin-4-yl)-piperazin-1-yl]-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (298) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-1-(4-piperidin-4-ylpiperazin-1-yl)-butan-1,4-dion, (299) 1-1,4'-Bipiperidinyl-1'-yl-2-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (300) 2-(7-Chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-1-(4-dimethylamino-piperidin-1-yl)-4-[4-(5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-yl]-butan-1,4-dion, (301) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid, (302) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid, (303) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-ethyl]-amid, (304) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (305) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-ethyl]-amid, (306) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (307) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid, (308) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid, (309) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (310) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (311) 2-(4-Methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-ylj-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dion, (312) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (313) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure {1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (314) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (315) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (316) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (317) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (318) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (319) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (320) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (321) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (322) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (323) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (324) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-dimethylaminopiperidin-1-yl)-2-oxo-ethyl]-amid, (325) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid, (326) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid, (327) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid, (328) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (329) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl)-ethyl]-amid, (330) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (331) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid, (332) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-ethyl]-amid, (333) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (334) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (335) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (336) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (337) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (338) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (339) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (340) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (341) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (342) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (343) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure {1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (344) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (345) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (346) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (347) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-ethyl]-amid, (348) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(4-chlor-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-(4-dimethylamino-piperidin-1-yl)-2-oxo-ethyl]-amid, (349) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (350) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (351) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (352) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperazin-1-ylpiperidin-1-yl)-ethyl]-amid, (353) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (354) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (355) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (356) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (357) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (358) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (359) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (360) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (361) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (362) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (363) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure [2-1,4'-bipiperidinyl-1'-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (364) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (365) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (366) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (367) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (368) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (369) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (370) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (371) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (372) 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-dimethylamino-piperidin-1-yl)-2-oxo-ethyl]-amid, (373) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure [2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (374) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (375) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (376) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperazin-1-ylpiperidin-1-yl)-ethyl]-amid, (377) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (378) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (379) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (380) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-2-oxo-1-(2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-ethyl]-amid, (381) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (382) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (383) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure {1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (384) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (385) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (386) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (387) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (388) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-(4-dimethylamino-piperidin-1-yl)-1-(7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (389) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amid, (390) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-4,4'-bipiperidinyl-1-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (391) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure{1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amid, (392) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperazin-1-yl-piperidin-1-yl)-ethyl]-amid, (393) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure {1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-[4-(1-methylpiperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amid, (394) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-2-(4-piperidin-4-yl-piperazin-1-yl)-ethyl]-amid, (395) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[2-1,4'-bipiperidinyl-1'-yl-1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-oxo-ethyl]-amid, (396) 4-(5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl)-piperidin-1-carbonsäure[1-(7-chlor-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl)-2-(4-dimethylamino-piperidin-1-yl)-2-oxo-ethyl]-amid, (397) 2-(1H-Indazol-5-ylmethyl)-4-[4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidin-1-yl]-1-(4-pyrrolidin-1-yl-piperidin-1-yl)-butan-1,4-dion, (398) 4-(2-Oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carbonsäure-[1-(1H-indazol-5-ylmethyl)-2-oxo-2-(4-pyrrolidin-1-yl-piperidin-1-yl)-ethyl]-amid, deren Tautomere, deren Diastereomere, deren Enantiomere, deren Hydrate, deren Gemische und deren Salze sowie die Hydrate der Salze.The following compounds of general formula (I) according to claim 1: (1) 1-1,4'-bipiperidinyl-1'-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo -1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (2) 2- (1H-indazol-5-ylmethyl ) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3- yl) -piperidin-1-yl] -butane-1,4-dione, (3) 1-4,4'-bipiperidinyl-1-yl-2- (1H-indazol-5-ylmethyl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (4) 1- (4- dimethylamino-piperidin-1-yl) -2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) -piperidin-1-yl] -butane-1,4-dione, (5) (S) -2- (1H-indazol-5-ylmethyl) -1- [4- (4-methylpiperazine-1-) yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan 1,4-dione, (6) 2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butane-1,4-dione, (7) 2- (1H-indaz ol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (8) 2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - 1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (9) 2- (1H-indazol-5-ylmethyl) -1- [4- (4-methyl -perhydro-1,4-diazepin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) -piperidin-1-yl] -butane-1,4-dione, (10) 2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) butane-1,4- dione, (11) 2- (1H-Indazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -4- [ 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (12) 2- (1H -indazole-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4 -piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -butane-1,4-dione, (13) 1- [4- (4-fluoro-phenyl) -piperazin-1-yl] -2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (14) 1- [4- (4-fluoro-phenyl) -piperidin-1-yl] -2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (15) 2- (1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-pyridin-4-yl-piperazin-1-yl) butane-1,4- dione, (16) (1 '- {2- (1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -butyryl} -4,4'-bipiperidinyl-1-yl) -acetic acid methyl ester, (17) 2- (1H-indazol-5-ylmethyl) -1- (1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine 1-yl] -butane-1,4-dione, (18) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (19) 4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl] 1-yl) -2-oxo-ethyl] -amide, (20) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodi azepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (21) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (22) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide , (23) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -] 2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (24) 4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] - 2-oxo-ethyl} -amide, (25) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H -indazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (26) 4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepi n-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4- (4-methyl-perhydro-1,4-diazepin-1-yl) -piperidine] 1-yl] -2-oxo-ethyl} -amide, (27) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo-2- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -ethyl] -amide, (28) 4 - (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -2-oxo-ethyl} -amide, (29) 4- (2-oxo-1,2,4, 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-perhydro- 1,4-diazepin-1-yl) -ethyl] -amide, (30) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -carboxylic acid [2- [4- (4-fluoro-phenyl) -piperazin-1-yl] -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (31) 4- ( 2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -piperidin-1-yl] -1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl l] -amide, (32) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazole-5 -ylmethyl) -2-oxo-2- (4-pyridin-4-yl-piperazin-1-yl) -ethyl] -amide, (33) [1 '- (3- (1H-indazol-5-yl) -2 - {[4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine 1-carbonyl] -amino} -propionyl) -4,4'-bipiperidinyl-1-yl] -acetic acid methyl ester, (34) 4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid (1- (1H-indazol-5-ylmethyl) -2- (1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl) -2-oxo -ethyl] -amide, (35) 1-1,4'-bipiperidinyl-1'-yl-2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (36) 1- (1'-methyl-4,4 ' -bipiperidinyl-1-yl) -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) piperidin-1-yl] -butane-1,4-dione, (37) 1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-1H-indazol-5-ylmethyl ) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (38 ) 1- (4-Dimethylamino-piperidin-1-yl) -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (39) 2- (7-methyl-1H- indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (40) 2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl ) -butane-1,4-dione, (41) 2- (7-methyl-1H-indazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -piperazine-1] yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, 42) 2- (7-Methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine 1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (43) 2- (7-methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-perhydro-1,4-diazepin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (44) 2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-perhydro-1,4-diazepin-1-yl piperidin-1-yl) -b uterine-1,4-dione, (45) 2- (7-methyl-1H-indazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -perhydro-1,4- diazepin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4 dione, (46) 2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3-dione] yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -butane-1,4-dione, (47) 1- [4- (4-fluoro-phenyl) -piperazin-1-yl] -2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (48) 1- [4- (4-fluoro-phenyl) -piperidin-1-yl] - 2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -butane-1,4-dione, (49) 2- (7-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-pyridin-4-yl-piperazin-1-yl) -butane-1,4-dione, (50) (1 '- {2- (7-methyl-1H-indazol-5-ylmethyl) -4-oxo-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3 -yl) piperidin-1-yl] butyryl} -4, 4'-bipiperidinyl-1-yl) -acetic acid methyl ester, (51) 1- (1'-methanesulfonyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-1H-indazole-5-yl) ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, ( 52) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl] 1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (53) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -1- (7-methyl-1H-indazol-5-ylmethyl) -2- oxo-ethyl] -amide, (54) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4 '] -bipiperidi nyl-1-yl-1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (55) 4- (2-oxo-1,2,4,5-tetrahydro 1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (7-methyl-1H-indazol-5-ylmethyl) -2- oxo-ethyl] -amide, (56) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl -1H-indazol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (57) 4- (2 -Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo] 2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (58) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazol-5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) -piperazin-1-yl] - 2-oxo-ethyl} -amide, (59) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7 -methyl-1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (60) 4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazol-5-ylmethyl) -2- [4- (4-methyl-perhydro-1,4-diazepin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (61) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine 1-carboxylic acid [1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-2- (4-perhydro-1,4-diazepin-1-yl-piperidin-1-yl) -ethyl] -amide, (62) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indazole -5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) -perhydro-1,4-diazepin-1-yl] -2-oxo-ethyl} -amide, (63) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazol-5-ylmethyl) -2- oxo-2- (4-piperidin-4-yl-perhydro-1,4-diazepin-1-yl) -ethyl] -amide, (64) 4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-fluoro-phenyl) -piperazin-1-yl] -1- (7-methyl-1H-indazole-5 -ylmethyl) -2-oxo-ethyl] -amide, (65) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [ 2- [4- (4-fluoro-phenyl) -piperidi n-1-yl] -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (66) 4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-2- (4-pyridin-4-yl] piperazin-1-yl) -ethyl] -amide, (67) [1 '- (3- (7-methyl-1H-indazol-5-yl) -2 - {[4- (2-oxo-1,2 , 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carbonyl] -amino} -propionyl) -4,4'-bipiperidinyl-1-yl] -acetic acid methyl ester, (68) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methanesulfonyl-4,4'-bipiperidinyl-1 -yl) -1- (7-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (69) 2- (1H-indazol-5-ylmethyl) -1- (1'- methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1 -yl] -butane-1,4-dione, (70) 1-4,4'-bipiperidinyl-1-yl-2- (1H-indazol-5-ylmethyl) -4- [4- (5-oxo) 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butane-1,4-dione, (71) 2- (1H-indazole-5- ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (5-oxo-3-phenyl-4, 5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butane-1,4-dione, (72) 2- (1H-indazol-5-ylmethyl) -4- [ 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin- 1-yl) -butane-1,4-dione, (73) 2- (1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl ] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione, (74) 2- (1H-Indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine 1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (75) 1-1,4'-bipiperidinyl-1'-yl-2 (1H-indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] - Butan-1,4-dione, (76) 1- (4-Dimethylamino-piperidin-1-yl) -2- (1H-indazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl -4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (77) 4- (5-oxo-3-phenyl-4 , 5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl -1-yl) -2-oxo-ethyl] -amide, (78) 4- (5-oxo 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (1H-indazole) 5-ylmethyl) -2-oxo-ethyl] -amide, (79) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1 -carboxylic acid {1- (1H-indazol-5-ylmethyl) -2- [4- (4-m ethyl-piperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (80) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4 -triazol-1-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (81) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (1H-indazole-5 -ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2-oxo-ethyl} -amide, (82) 4- (5-oxo-3-phenyl 4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperidine-4 -yl-piperazin-1-yl) -ethyl] -amide, (83) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine 1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (84) 4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (1H-indazole-5 -ylmethyl) -2-oxo-ethyl] -amide, (85) 2- (7-ethyl-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl ) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl) -butane-1,4-dione, (86) 1,4,4'-bipiperidinyl-1-yl-2- (7-ethyl-1H-indazol-5-ylmethyl) -4- [ 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (87) 2- (7 ethyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (88) 2- (7-ethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl piperidin-1-yl) -butane-1,4-dione, (89) 2- (7-ethyl-1H-indazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1, 4-dione, (90) 2- (7-ethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (91) 2- (7-chloro-1H-indazole -5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl ] -butane-1,4-dione, (92) 1-4,4'-bipiperidinyl-1-yl-2- (7-chloro-1H-indazol-5-ylmethyl) -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (93) 2- (7-chloro-1H- indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (94) 2- (7-chloro-1H-indazol-5-ylmethyl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl ) -butane-1,4-dione, (95) 2- (7-chloro-1H-indazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -piperazine-1] yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, 96) 2- (7-chloro-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine 1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (97) 2- (7-bromo-1H-indazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) piperidin-1-yl] -butan-1,4-dio n, (98) 1-4,4'-bipiperidinyl-1-yl-2- (7-bromo-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4, 5-tetrahydro-1,3-benzodiazepin-3-yl) piperidin-1-yl] -butane-1,4-dione, (99) 2- (7-bromo-1H-indazol-5-ylmethyl) -1 - [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3 -yl) -piperidin-1-yl] -butane-1,4-dione, (100) 2- (7-bromo-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) butane-1,4- dion, (101) 2- (7-bromo-1H-indazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (102) 2- (7-bromo-1H-indazole) 5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidine 4-yl-piperazin-1-yl) -butane-1,4-dione, (103) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1, 4-dione, (104) 1-4,4'-bipiperidinyl-1-yl-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione, (105) 2- (7-methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) -piperidin-1-yl] -butane-1,4-dione, (106) 4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -but an-1,4-dione, (107) 1- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepin-3-yl) piperidin-1-yl] -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione, (108) 4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazine -1-yl) -2- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -butane-1,4-dione, (109) 1- (1'-methyl-4,4'-bipiperidinyl-1-one yl) -2- (1-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidin-1-yl] -butane-1,4-dione, (110) 1-4,4'-bipiperidinyl-1-yl-2- (1-methyl-1H-indazol-5-ylmethyl) -4- [ 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (III) 2- (1 methyl-1H-indazol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (112) 2- (1-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl piper idin-1-yl) -butane-1,4-dione, (113) 2- (1-methyl-1H-indazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1, 4-dione, (114) 2- (1-methyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (115) 2- (1,7-dimethyl-1H -indazole-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) piperidin-1-yl] -butane-1,4-dione, (116) 1-4,4'-bipiperidinyl-1-yl-2- (1,7-dimethyl-1H -indazole-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1, 4-dione, (117) 2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4 [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (118) 2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piper azin-1-yl-piperidin-1-yl) -butane-1,4-dione, (119) 2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -1- [4- (1- methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -butane-1,4-dione, (120) 2- (1,7-dimethyl-1H-indazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (121) 2- (1H-benzotriazole-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (122) 2- (1H-benzotriazol-5-ylmethyl) -1-4,4'- bipiperidinyl-1-yl-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4- dione, (123) 2- (1H-Benzotriazol-5-ylmethyl) -1- (4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2-oxo -1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (124) 2- (1H-benzotriazol-5-ylmethyl ) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl -piperidin-1-yl) -butane-1,4-dione, (125) 2- (1H-Benzotriazol-5-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -piperazine 1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione , (126) 2- (1H-Benzotriazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (127) 2- (7-methyl-1H-benzotriaz ol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (128) 1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-1H-benzotriazole) 5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione , (129) 2- (7-Methyl-1H-benzotriazol-5-ylmethyl) -1- [4- (4-methyl-1-piperazin-1-yl) -piperidin-1-yl] -4- 2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (130) 2- (7-methyl- 1H-benzotriazole-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- ( 4-piperazin-1-yl-piperidin-1-yl) -butane-1,4-dione, (131) 2- (7-methyl-1H-benzotriazol-5-ylmethyl) -1- [4- (1- methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -butane-1,4-dione, (132) 2- (7-methyl-1H-benzotriazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (13 3) 2- (1H-indol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1,2,4, 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (134) 1-4,4'-bipiperidinyl-1-yl-2- (1H indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1, 4-dione, (135) 2- (1H-indol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -4- [4- (2 -oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (136) 2- (1H-indole-5 ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1 1-yl) -butane-1,4-dione, piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4 -dione, (138) 2- (1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine 1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (139) 1- (1'-methyl-4,4'-bipiperidinyl) 1-yl) -2- (7-methyl-1H-indol-5-YLM ethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, ( 140) 1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (141) 2- (7-methyl-1H-indol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo- 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (142) 2- (7-methyl-1H-indole- 5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin- 1-yl-piperidin-1-yl) -butane-1,4-dione, (143) 2- (7-methyl-1H-indol-5-ylmethyl) -1- [4- (1-methylpiperidine). 4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] - butane-1,4-dione, (144) 2- (7-methyl-1H-indol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3 -benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (145) 4- (2-oxo 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-ethyl-1H-indazol-5-ylmethyl) -2- (1'- methyl-4,4'-bipiperidinyl-1-yl) -2-oxoethyl] -amide, (146) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (7-ethyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (147) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-ethyl-1H-indazole-5- ylmethyl) -2- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -2-oxo-ethyl} -amide, (148) 4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-ethyl-1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperazine- 1-yl-piperidin-1-yl) -ethyl] -amide, (149) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -carboxylic acid {1- (7-ethyl-1H-indazol-5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} - amide, (150) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-ethyl-1H-indazole) 5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (151) 4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-1H-indazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl] 1-yl) -2-oxoethyl] -amide, (152) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2 -4,4'-bipiperidinyl-1-yl-1 (7-chloro-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (153) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) piperidine-1-carboxylic acid {1- (7-chloro-1H-indazol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (154) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- ( 7-chloro-1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (155) 4- (2-oxo) 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-1H-indazol-5-ylmethyl) -2- [4- (1 -methyl-piperidin-4-yl) -piperazin-1-yl] -2-oxo-ethyl} -amide, (156) 4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) ethyl] -amide, (157) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-bromo- 1H-indazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxoethyl] -amide, (158) 4- (2-oxo-1,2, 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -Pip eridine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (7-bromo-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (159) 4- ( 2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-bromo-1H-indazol-5-ylmethyl) -2- [ 4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (160) 4- (2-oxo-1,2,4,5-tetrahydro-) 1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-bromo-1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidine] 1-yl) -ethyl] -amide, (161) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- ( 7-bromo-1H-indazol-5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide, (162) 4 - (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-bromo-1H-indazol-5-ylmethyl) -2 -oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (163) 4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-1- (7-trifluoromethyl-1H-indazole-5- ylmethyl) ethyl] amide, (164 ) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2] oxo-1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide, (165) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) -piperidine-1-carboxylic acid [2- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-1- (7-trifluoromethyl-1H-indazole-5 -ylmethyl) -ethyl] -amide, (166) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-2-hydroxybenzoyl] 2- (4-piperazin-1-yl-piperidin-1-yl) -1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide, (167) 4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (1-methylpiperidin-4-yl) -piperazin-1-yl] - 2-oxo-1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) -ethyl] -amide, (168) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) piperidine-1-carboxylic acid [2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -1- (7-trifluoromethyl-1H-indazol-5-ylmethyl) - ethyl] -amide, (169) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperi dinyl-1-yl) -1- (1-methyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (170) 4- (2-oxo-1,2,4,5-tetrahydro 1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (1-methyl-1H-indazol-5-ylmethyl) -2-oxo ethyl] -amide, (171) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1-methyl) 1H-indazol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (172) 4- (2- Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1-methyl-1H-indazol-5-ylmethyl) -2-oxo-2 (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (173) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 yl) -piperidine-1-carboxylic acid {1- (1-methyl-1H-indazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2 -oxo-ethyl} -amide, (174) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1 methyl-1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (175) 4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) piperidine-1-carboxylic acid [1- (1,7-dimethyl-1H-indazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2 -oxo-ethyl] -amide, (176) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4.4 '-bipiperidinyl-1-yl-1- (1,7-dimethyl-1H-indazol-5-ylmethyl) -2-oxo-ethyl] -amide, (177) 4- (2-oxo-1,2,4 , 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1,7-dimethyl-1H-indazol-5-ylmethyl) -2- [4- (4-methyl- piperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (178) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) -piperidine-1-carboxylic acid [1- (1,7-dimethyl-1H-indazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -] ethyl] -amide, (179) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (1,7-dimethyl -1H-indazol-5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide, (180) 4- (2 -Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1,7-dimethyl-1H-indazol-5-ylmethyl) -2- oxo-2- (4-piperidin-4-yl -piperazin-1-yl) -ethyl] -amide, (181) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [ 1- (1H-Benzotriazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide, (182) 4- (2-Oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-ylmethyl) -2,4,4'-bipiperidinyl-1-yl 2-oxo-ethyl] -amide, (183) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- ( 1H-benzotriazol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (184) 4- (2- Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-ylmethyl) -2-oxo-2- (4- piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (185) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine 1-carboxylic acid {1- (1H-benzotriazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2-oxo-ethyl} -amide, (186) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-benzotriazol-5-yl methyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (187) 4- (2-oxo-1,2,4,5-tetrahydro- 1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-benzotriazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-one] yl) -2-oxo-ethyl] -amide, (188) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2 4,4'-bipiperidinyl-1-yl-1- (7-methyl-1H-benzotriazol-5-ylmethyl) -2-oxo-ethyl] -amide, (189) 4- (2-oxo-1,2 , 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-benzotriazol-5-ylmethyl) -2- [4- (4-methyl- piperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (190) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-benzotriazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (191) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-benzotriazole -5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide, (192) 4- (2-oxo-1 , 2,4,5-tetra hydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-benzotriazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl] piperazin-1-yl) -ethyl] -amide, (193) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1 - (1H-indol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide, (194) 4- (2-oxo) 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (1H-indol-5-ylmethyl ) -2-oxo-ethyl] -amide, (195) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1 (1H-indol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (196) 4- (2 -Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indol-5-ylmethyl) -2-oxo-2- (4 -piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (197) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) - piperidine-1-carboxylic acid {1- (1H-indol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2-oxo-ethyl} -amide , (198) 4- (2-oxo-1,2,4 , 5-Tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazine 1-yl) -ethyl] -amide, (199) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperi dinyl-1-yl) -1- (7-methyl-1H-indol-5-ylmethyl) -2-oxo-ethyl] -amide, (200) 4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (7-methyl-1H-indol-5-ylmethyl) -2- oxo-ethyl] -amide, (201) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl -1H-indol-5-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (202) 4- (2 -Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-1H-indol-5-ylmethyl) -2-oxo] 2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (203) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) -piperidine-1-carboxylic acid {1- (7-methyl-1H-indol-5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) -piperazin-1-yl] - 2-oxo-ethyl} -amide, (204) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7 -methyl-1H-indol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (205) 1- (1'-methyl- 4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1, 4-dione, (206) 1-4, 4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo) 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (207) 1- [4- (4-methylpiperazine -1-yl) piperidin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5 -tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (208) 2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl ) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl -piperidin-1-yl) -butane-1,4-dione, (209) 1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2- (2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (210) 2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (211) 1 1,4 '-Bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (212) 1- (4-dimethylamino-piperidin-1-yl) -2- (2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane -1,4-dione, (213) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazole-6 ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione, (214) 1-4,4'-bipiperidinyl-1-yl-2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo) 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (215) 2- (4-methyl-2-oxo) 2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2 , 4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (216) 2- (4-methyl-2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1- yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butane-1,4-dione, (217) 2- (4-methyl-2-oxo-2,3-dihydro-benzoxazole -6-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) piperazi-n-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (218) 2- (4-methyl-2-oxo-2,3-dihydro-benzoxazole-6 ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4 -yl-piperazin-1-yl) -butane-1,4-dione, (219) 1-1,4'-bipiperidinyl-1'-yl-2- (4-methyl-2-oxo-2,3- dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1 , 4-dione, (220) 1- (4-dimethylamino-piperidin-1-yl) -2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (221) 2- (4- chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1 , 2,4,5-t etrahydro-1,3-benzodiazepin-3-yl) piperidin-1-yl] -butane-1,4-dione, (222) 1-4,4'-bipiperidinyl-1-yl-2- (4-chloro -2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine -1-yl] -butane-1,4-dione, (223) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (4-methyl piperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1- yl] -butane-1,4-dione, (224) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) butane-1,4- dione, (225) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- [4- (1-methylpiperidin-4-yl) -piperazine-1] yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, 226) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (227) 1-1,4'- Bip iperidinyl-1'-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro -1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (228) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazole-6 -ylmethyl) -1- (4-dimethylaminopiperidine-1-yl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -yl] -butane-1,4-dione, (229) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-benzoxazole) 6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4 -dione, (230) 1-4,4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (231) 1- [4- (4-methyl- piperazin-1-yl) piperidin-1-yl] -2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4, 5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (232) 2- (2-oxo-2,3-dihydro-benzoxazole) 6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1- (4- piperazin-1-yl-piperidin- 1-yl) -butane-1,4-dione, (233) 1- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2- (2-oxo-2,3 dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] - Butan-1,4-dione, (234) 2- (2-Oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro -1,2,4-triazol-1-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (235) 1-1,4'-bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4, 5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butane-1,4-dione, (236) 1- (4-dimethylamino-piperidin-1-yl) -2 - (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl ) -piperidin-1-yl] -butane-1,4-dione, (237) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (4-methyl-2-oxo -2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1 -yl] -butane-1,4-dione, (238) 1-4,4'-bipiperidinyl-1-yl-2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl ) -4- [4- (5-oxo-3-phenyl-4,5-d ihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (239) 2- (4-methyl-2-oxo-2,3-dihydro- benzoxazol-6-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro -1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (240) 2- (4-methyl-2-oxo-2,3-dihydro-benzoxazole -6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1- (4 -piperazin-1-yl-piperidin-1-yl) -butane-1,4-dione, (241) 2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1 - [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (5-ox o-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (242) 2- (4-methyl- 2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) - piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (243) 1-1,4'-bipiperidinyl-1'-yl 2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4 -triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (244) 1- (4-dimethylamino-piperidin-1-yl) -2- (4-methyl-2-oxo -2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1 -yl] -butane-1,4-dione, (245) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (1'-methyl-4,4 '-bipiperidinyl-1-yl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan -1,4-dione, (246) 1-4,4'-bipiperidinyl-1-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [ 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (247) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazo l-6-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro -1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (248) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazole -6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1- (4 -piperazin-1-yl-piperidin-1-yl) -butane-1,4-dione, (249) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1 - [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazole -1-yl) -piperidin-1-yl] -butane-1,4-dione, (250) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazine 1-yl) -butane-1,4-dione, (251) 1-1,4'-bipiperidinyl-1'-yl-2- (4-chloro-2-oxo-2,3-dihydro-benzoxazole) 6-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4 dione, (252) 2- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -1- (4-dimethylaminopiperidin-1-yl) -4- [4- (5- oxo-3-phenyl-4,5-dihydro-1,2,4-Triaz ol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (253) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (2- oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine 1-yl] -butane-1,4-dione, (254) 1-4,4'-bipiperidinyl-1-yl-2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (255) 1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (256) 2- (2- oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine 1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) -butane-1,4-dione, (257) 1- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro- 1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (258) 2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl- piperazin-1-yl) -butane-1,4-dione, (259) 1-1,4'-bipiperidinyl-1'-yl-2- (2-oxo-2,3-dihydro-1H-benzimidazole-5 ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione, (260) 1- (4-Dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1 , 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (261) 1- (1'-methyl-4,4 ' -bipiperidinyl-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- (4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (262) 1-4,4'-bipiperidinyl-1-yl 2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (263) 2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) -piperidin-1-yl] -butane-1,4-dione, (264) 2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) - 4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1 -yl) -butane-1,4-dione, (265) 2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methyl piperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1- yl] -butane-1,4-dione, (266) 2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo) 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-y 1) -butane-1,4-dione, (267) 1-1,4'-bipiperidinyl-1'-yl-2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazole-5 ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butan-1,4-dione, (268) 1- (4-Dimethylamino-piperidin-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2 -oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (269) 2- (7-chloro-2 oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (270) 1-4,4'-bipiperidinyl-1-yl 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3- benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (271) 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3 -yl) -piperidin-1-yl] -butane-1,4-dione, (272) 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylme thyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperazin-1- yl-piperidin-1-yl) -butane-1,4-dione, (273) 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4 - (1-methylpiperidin-4-yl) piperazin-1-yl] -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (274) 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (275) 1-1,4'-bipiperidinyl-1'-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl ) -4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (276 ) 2- (7-Chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (4-dimethylamino-piperidin-1-yl) -4- [4- (2-oxo -1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidin-1-yl] -butane-1,4-dione, (277) 1- (1'-methyl-4, 4'-bipiperidinyl-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5- dihydro 1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (278) 1-4,4'-bipiperidinyl-1-yl-2 (2-yl) oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) - piperidin-1-yl] -butane-1,4-dione, (279) 1- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2- (2-oxo-2 , 3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1 -yl] -butane-1,4-dione, (280) 2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl -4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperazin-1-yl-piperidin-1-yl) butane-1,4 -dione, (281) 1- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl ) -4- [4- (5-oxo-3- phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (282) 2- (2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (283) 1-1,4'-bipiperidinyl-1'-yl-2- (2-oxo -2,3-dihydro-1H-benzimidazol-5-ylmethyl) - 4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine -1-yl] -butane-1,4-dione, (284) 1- (4-dimethylamino-piperidin-1-yl) -2- (2-oxo-2,3-dihydro-1H-benzimidazole-5- ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan-1,4-dione , (285) 1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) - 4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (286 ) 1-4,4'-bipiperidinyl-1-yl-2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo) 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (287) 2- (7-methyl-2-) oxo-2,3-dihydro-1H-benzimida zol-5-ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro -1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (288) 2- (7-methyl-2-oxo-2,3-dihydro-1H -benzimidazole-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1 (4-piperazin-1-yl-piperidin-1-yl) -butan-1,4-dione, (289) 2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4 -triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (290) 2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl ) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperidin-4 -ylpiperazin-1-yl) -butane-1,4-dione, (291) 1-1,4'-bipiperidinyl-1'-yl-2- (7-methyl-2-oxo-2,3-dihydro- 1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -butan -1,4-dione, (292) 1- (4-dimethylamino-piperidin-1-yl) -2- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) - 4- [4- (5-oxo-3 -phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (293) 2- (7-chloro-2-oxo -2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (1'-methyl-4,4'-bipiperidinyl-1-yl) -4- [4- (5-oxo-3-phenyl- 4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (294) 1-4, 4'-bipiperidinyl-1-yl 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2, 4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (295) 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazole-5- ylmethyl) -1- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2 , 4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (296) 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazole-5 ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) piperidin-1-yl] -1- (4-piperazin 1-yl-piperidin-1-yl) -butane-1,4-dione, (297) 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- [ 4- (1-methylpiperidin-4-yl) piperazin-1-yl] -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl ) piperidin-1-yl] -butan-1,4-d ion, (298) 2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro 1,2,4-triazol-1-yl) -piperidin-1-yl] -1- (4-piperidin-4-yl-piperazin-1-yl) -butane-1,4-dione, (299) 1- 1,4'-bipiperidinyl-1'-yl-2- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -4- [4- (5-oxo-3- phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (300) 2- (7-chloro-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -1- (4-dimethylamino-piperidin-1-yl) -4- [4- (5-oxo-3-phenyl-4,5-dihydro-1 , 2,4-triazol-1-yl) -piperidin-1-yl] -butane-1,4-dione, (301) 4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepine-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1- yl) -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide, (302) 4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol 6-ylmethyl) -ethyl] -amide, (303) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-methylpiperazin-1-yl) piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) ethyl] -amide, 304) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3 -dihydro-benzoxazol-6-ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (305) 4- (2-oxo-1,2,4,5 tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydrobenzoxazol-6-ylmethyl) -ethyl] -amide, (306) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) - ethyl] -amide, (307) 4- (2-O xo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-2-oxo-1- ( 2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide, (308) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] - amide, (309) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4 '-bipiperidinyl-1-yl) -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide, (310) 4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (4-methyl-2 -oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide, (311) 2- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl ) -1- [4- (4-methyl-piperazin-1-yl) -piperidine-1-YLJ-4- [4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine 3-yl) piperidin-1-yl] -butane-1,4-dione, (312) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl ) -piperidine-1-carboxylic acid [1- (4-met hyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (313) 4 - (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (4-methyl-2-oxo-2,3-dihydroxy) benzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2-oxo-ethyl} -amide, (314) 4- (2-oxo-ethyl) -amide 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (315) 4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6- ylmethyl) -2-oxo-ethyl] -amide, (316) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2 - (4-dimethylamino-piperidin-1-yl) -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide, (317) 4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3-dihydro- benzoxazol-6-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide, (318) 4- (2-oxo-1,2,4,5-tetrahydro- 1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6 -ylmethyl) -2-oxo-ethyl] -amide, (319) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid { 1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2- oxo-ethyl} -amide, (320) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro -2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (321) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo-2,3-dihydro-be nzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2-oxo-ethyl} -amide, (322) 4- (2-oxo-ethyl) -amide 1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) 2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (323) 4- (2-oxo-1,2,4,5-tetrahydro-1, 3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (4-chloro-2-oxo-2,3-dihydro-benzoxazole-6- ylmethyl) -2-oxo-ethyl] -amide, (324) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1 - (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2- (4-dimethylaminopiperidin-1-yl) -2-oxo-ethyl] -amide, (325) 4- ( 5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1- yl) -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide, (326) 4- (5-oxo-3-phenyl-4,5- dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2-oxo-1- (2-oxo-2,3-dihydro benzoxazol-6-ylmethyl) -ethyl] -amide, ( 327) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazine- 1-yl) -piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide, (328) 4- (5-oxo -3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6 -ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide, (329) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2 , 4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-1- (2-oxo -2,3-dihydrobenzoxazol-6-ylmethyl) -ethyl] -amide, (330) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) - piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (331) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl 1'-yl-2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide, (332) 4- (5-oxo-3-phenyl-4 , 5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dim ethylamino-piperidin-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -ethyl] -amide, (333) 4- (5-oxo-3-yl) phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -1- ( 4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide, (334) 4- (5-oxo-3-phenyl-4,5-dihydro- 1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol -6-ylmethyl) -2-oxo-ethyl] -amide, (335) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine 1-carboxylic acid {1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl ] -2-oxo-ethyl} -amide, (336) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [ 1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) -ethyl] -amide , (337) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4-methyl-2-oxo -2,3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methyl-p iperidin-4-yl) -piperazin-1-yl] -2-oxo-ethyl} -amide, (338) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazole -1-yl) -piperidine-1-carboxylic acid [1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl -piperazin-1-yl) -ethyl] -amide, (339) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1 carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide, 340) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl ) -1- (4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide, (341) 4- (5-oxo-3-phenyl-4 , 5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3-dihydro-benzo xazol-6-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide, (342) 4- (5-oxo-3-phenyl- 4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (4-chloro-2-oxo-2 , 3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide, (343) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazole-1 -yl) -piperidine-1-carboxylic acid {1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (4-methylpiperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (344) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) - piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl ) -ethyl] -amide, (345) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (4 -chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide, (346) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2 oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-p iperazin-1-yl) -ethyl] -amide, (347) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (4-chloro-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl) -2-oxo-ethyl] -amide, (348 ) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (4-chloro-2-oxo-2, 3-dihydro-benzoxazol-6-ylmethyl) -2- (4-dimethylamino-piperidin-1-yl) -2-oxo-ethyl] -amide, (349) 4- (2-oxo-1,2,4, 5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-1- (2- oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide, (350) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) ethyl] amide, (351) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl- piperazin-1-yl) -piperidin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide, (352) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benz odiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperazin-1-ylpiperidin- 1-yl) -ethyl] -amide, (353) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- [ 4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) ethyl] - amide, (354) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (355) 4- (2-oxo-1, 2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-2-oxo-1- (2-oxo- 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide, (356) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) ethyl] - amide, (357) 4- (2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4 '-bipip eridinyl-1-yl) -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (358) 4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (7-methyl-2 -oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (359) 4- (2-oxo-1,2,4,5-tetrahydro-1,3 benzodiazepine-3-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methyl- piperazin-1-yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (360) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepine-3 -yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl -piperidin-1-yl) -ethyl] -amide, (361) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid { 1- (7-methyl-2-oxo-2,3-dihydro- 1H-benzimidazol-5-ylmethyl) -2- [4- (1-methylpiperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} -amide, (362) 4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazole 5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (363) 4- (2-oxo-1,2,4,5- tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (7-methyl-2-oxo-2,3-dihydro- 1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (364) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine -1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl ] -amide, (365) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2- oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide, (366) 4 - (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (7 chloro-2-oxo-2,3- dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (367) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methyl-piperazin-1-yl) - piperidin-1-yl] -2-oxo-ethyl} -amide, (368) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -carboxylic acid [1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) ethyl] -amide, (369) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid {1- (7-chloro) 2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-ethyl} - amide, (370) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo) 2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (371) 4- (2- oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (7-chloro- 2-oxo-2,3-dihydro-1H-b enzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (372) 4- (2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl) -piperidine-1 -carboxylic acid [1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-dimethylamino-piperidin-1-yl) -2-oxo-ethyl] - amide, (373) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4 , 4'-bipiperidinyl-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide, (374) 4- (5- oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide, (375) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4 triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] -2-oxo-1- (2-oxo-2 , 3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide, (376) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl ) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-piperazin-1-yl-piperidin-1-yl) - ethyl] -amide, (377) 4- (5-oxo-3-phe nyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] -2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -ethyl] -amide, (378) 4- (5-oxo-3-phenyl-4,5- dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- ( 4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (379) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazole-1 yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-2-oxo-1- (2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) ethyl ] -amide, (380) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino) -carboxylic acid]. piperidin-1-yl) -2-oxo-1- (2-oxo-2,3-dihydro-1 H -benzimidazol-5-ylmethyl) -ethyl] -amide, (381) 4- (5-oxo-3- phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (1'-methyl-4,4'-bipiperidinyl-1-yl) - 1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (382) 4- (5-oxo-3-phenyl-4 , 5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-yl-1- (7-methyl-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (383) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazole 1-yl) piperidine-1-carboxylic acid {1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (4-methyl-piperazine-1 -yl) -piperidin-1-yl] -2-oxo-ethyl} -amide, (384) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazole-1 yl) -piperidine-1-carboxylic acid [1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl piperidin-1-yl) -ethyl] -amide, (385) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) piperazin-1-yl] 2-oxo-ethyl} -amide, (386) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1 - (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmet hyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (387) 4- (5-oxo-3-phenyl-4,5-dihydro- 1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (7-methyl-2-oxo-2,3-dihydro- 1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (388) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2- (4-dimethylamino-piperidin-1-yl) -1- (7-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo ethyl] -amide, (389) 4- (5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7 chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (1'-methyl-4,4'-bipiperidinyl-1-yl) -2-oxo-ethyl] -amide, (390) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-4,4'-bipiperidinyl-1-one yl-1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (391) 4- (5-oxo-3-phenyl -4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl ) -2- [4- (4-methyl-piperazin-1-yl) piperidin-1-yl] 2-oxo-ethyl} -amide, (392) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1 - (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperazin-1-yl-piperidin-1-yl) ethyl] - amide, (393) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid {1- (7-chloro-2-) oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- [4- (1-methyl-piperidin-4-yl) -piperazin-1-yl] -2-oxo-ethyl} -amide, (394 ) 4- (5-Oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2, 3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-2- (4-piperidin-4-yl-piperazin-1-yl) -ethyl] -amide, (395) 4- (5-oxo) 3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl) -piperidine-1-carboxylic acid [2-1,4'-bipiperidinyl-1'-yl-1- (7-chloro- 2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2-oxo-ethyl] -amide, (396) 4- (5-oxo-3-phenyl-4,5-dihydro-1, 2,4-triazol-1-yl) -piperidine-1-carboxylic acid [1- (7-chloro-2-oxo-2,3-dihydro-1H-benzimidazol-5-ylmethyl) -2- (4-dimethylamino- piperidin-1-yl) -2-oxo-ethyl] -amide, (397) 2- (1H-In dazol-5-ylmethyl) -4- [4- (2-oxo-1,2,4,5-tetrahydro-benzo [d] [1,3] diazepin-3-yl) -piperidin-1-yl] - 1- (4-pyrrolidin-1-yl-piperidin-1-yl) -butane-1,4-dione, (398) 4- (2-oxo-1,2,4,5-tetrahydro-benzo [d] [1,3] diazepin-3-yl) -piperidine-1-carboxylic acid [1- (1H-indazol-5-ylmethyl) -2-oxo-2- (4-pyrrolidin-1-yl-piperidin-1- yl) -ethyl] -amide, their tautomers, their diastereomers, their enantiomers, their hydrates, their mixtures and their salts, and the hydrates of the salts. Physiologisch verträgliche Salze der Verbindungen nach einem der Ansprüche 1 bis 3 mit anorganischen oder organischen Säuren oder Basen.Physiologically acceptable salts of the compounds according to one of the claims 1 to 3 with inorganic or organic acids or bases. Arzneimittel, enthaltend eine Verbindung nach mindestens einem der Ansprüche 1 bis 3 oder ein physiologisch verträgliches Salz gemäß Anspruch 4 neben gegebenenfalls einem oder mehreren inerten Trägerstoffen und/oder Verdünnungsmitteln.A pharmaceutical composition containing a compound according to any one of claims 1 to 3 or a physiologically acceptable salt according to claim 4, optionally together with one or more inert excipients fen and / or diluents. Verwendung einer Verbindung nach mindestens einem der Ansprüche 1 bis 4 zur Herstellung eines Arzneimittels zur akuten und prophylaktischen Behandlung von Kopfschmerzen, insbesondere Migräne- bzw. Cluster-Kopfschmerz.Use of a compound after at least one the claims 1 to 4 for the preparation of a medicament for acute and prophylactic Treatment of headache, especially migraine or cluster headache. Verwendung einer Verbindung nach mindestens einem der Ansprüche 1 bis 4 zur Herstellung eines Arzneimittels zur Bekämpfung von nicht-insulinabhängigem Diabetes-mellitus (NIDDM).Use of a compound after at least one the claims 1 to 4 for the manufacture of a medicament for controlling non-insulin dependent Diabetes mellitus (NIDDM). Verwendung einer Verbindung nach mindestens einem der Ansprüche 1 bis 4 zur Herstellung eines Arzneimittels zur Behandlung von cardiovaskulären Erkrankungen, von Morphintoleranz, von Chlostritiumtoxin-bedingten Durchfallerkrankungen, von Erkrankungen der Haut, insbesondere von thermischen und strahlungsbedingten Schäden inklusive Sonnenbrand, von entzündlichen Erkrankungen wie insbesondere entzündlicher Gelenkerkrankungen wie Arthritis, von neurogenen Entzündungen der oralen Mucosa, von entzündlichen Lungenerkrankungen, von allergischer Rhinitis, von Asthma, von Erkrankungen, die mit einer überschießenden Gefäßerweiterung und dadurch bedingter verringerter Gefäßdurchblutung, wie insbesondere Schock oder Sepsis, einhergeht, zur Linderung von Schmerzzuständen im allgemeinen oder zu präventiven oder akut therapeutischen Beeinflussung der durch Gefäßerweiterung und erhöhten Blutfluss verursachten Symptomatik von Hitzewallungen menopausaler, östrogendefizienter Frauen sowie hormonbehandelter Prostatakarzinompatienten.Use of a compound after at least one the claims 1 to 4 for the manufacture of a medicament for the treatment of cardiovascular diseases, of morphine tolerance, of chlostritium-toxin-related diarrheal diseases, of diseases of the skin, in particular of thermal and radiation-related damage including sunburn, from inflammatory Diseases such as in particular inflammatory joint diseases like arthritis, from neurogenic inflammation of the oral mucosa, of inflammatory Lung diseases, allergic rhinitis, asthma, diseases, those with an overshooting vascular dilation and consequent reduced vascular blood flow, in particular Shock or sepsis, associated with relief of pain in the general or preventive or acute therapeutic influence by vascular dilation and increased Blood flow caused symptoms of hot flushes menopausal, estrogen-deficient Women and hormone-treated prostate cancer patients. Verfahren zur Herstellung eines Arzneimittels gemäß Anspruch 5, dadurch gekennzeichnet, dass auf nichtchemischem Weg eine Verbindung nach mindestens einem der Ansprüche 1 bis 4 in einen oder mehrere inerte Trägerstoffe und/oder Verdünnungsmittel eingearbeitet wird.Process for the preparation of a medicament according to claim 5, characterized in that non-chemical way a compound according to at least one of the claims 1 to 4 in one or more inert carriers and / or diluents is incorporated. Verfahren zur Herstellung der Verbindungen der allgemeinen Formel (I) nach mindestens einem der Ansprüche 1 bis 3, dadurch gekennzeichnet, dass (a) zur Herstellung von Verbindungen der allgemeinen Formel (I), in der X die NH-Gruppe bedeutet und A, B, D, E, ----, R1 und R2 wie in Anspruch 1 definiert sind, ein Piperidin der allgemeinen Formel
Figure 02090001
in der R1 wie in Anspruch 1 definiert ist, mit einem Kohlensäurederivat der allgemeinen Formel
Figure 02090002
in der G eine nucleofuge Gruppe bedeutet, und mit einem primären Amin der allgemeinen Formel
Figure 02090003
in der A, B, D, E, ---- und R2 wie in Anspruch 1 definiert ist, mit der Maßgabe, dass diese Gruppen keine weitere freie primäre oder sekundäre aliphatische Aminofunktion enthalten, umgesetzt wird oder (b) zur Herstellung von Verbindungen der allgemeinen Formel (I), in der X die Methylengruppe bedeutet und A, B, D, E, ----, R1 und R2 wie in Anspruch 1 definiert sind, mit der Maßgabe, dass diese Gruppen keine weitere freie primäre oder sekundäre aliphatische Aminofunktion enthalten, eine Carbonsäure der allgemeinen Formel
Figure 02100001
in der A, B, D, E, ---- und R2 wie in Anspruch 1 definiert sind, mit einem Piperidin der allgemeinen Formel
Figure 02100002
in der R1 die in Anspruch 1 erwähnten Bedeutungen besitzt, gekuppelt wird oder (c) zur Herstellung von Verbindungen der allgemeinen Formel (I), in der X die Methylengruppe bedeutet und A, B, D, E, ----, R1 und R2 wie in Anspruch 1 definiert sind, mit der Maßgabe, dass diese Gruppen kein freies primäres oder sekundäres Amin enthalten, eine Verbindung der allgemeinen Formel
Figure 02100003
in der A, B, D, E, ---- und R2 wie in Anspruch 1 definiert sind, mit der Maßgabe, dass R2 kein primäres oder sekundäres Amin enthält, und Nu eine Austrittsgruppe bedeutet, mit einem Piperidin der allgemeinen Formel
Figure 02110001
in der R1 wie in Anspruch 1 definiert ist, gekuppelt wird oder (d) zur Herstellung von Verbindungen der allgemeinen Formel (I), in der alle Reste wie in Anspruch 1 definiert sind, eine Carbonsäure der allgemeinen Formel
Figure 02110002
in der A, B, D, E, ----, R1 und X wie in Anspruch 1 definiert sind, mit einem Amin R2 mit der Maßgabe, dass keine weitere freie primäre oder sekundäre aliphatische Aminofunktion enthalten ist, gekuppelt wird oder (e) zur Herstellung von Verbindungen der allgemeinen Formel (I), in der alle Reste wie in Anspruch 1 definiert ist, mit der Maßgabe, dass kein freies primäres oder sekundäres Amin enthalten ist, eine Verbindung der allgemeinen Formel
Figure 02120001
in der A, B, D, E, ----, R1 und X wie in Anspruch 1 definiert sind und Nu eine Austrittsgruppe bedeutet, mit einem Amin R2, mit der Maßgabe, dass keine weitere freie primäre oder sekundäre aliphatische Aminofunktion enthalten ist, gekuppelt wird und erforderlichenfalls ein bei den vorstehend beschriebenen Umsetzungen verwendeter Schutzrest wieder abgespalten wird und/oder gegebenenfalls verwendete Präcurserfunktionen in einer so erhaltenen Verbindung abgewandelt werden und/oder gegebenenfalls eine so erhaltene Verbindung der allgemeinen Formel (I) in ihre Stereoisomere aufgetrennt wird und/oder eine so erhaltene Verbindung der allgemeinen Formel (I) in ihre Salze, insbesondere für die pharmazeutische Anwendung in ihre physiologisch verträglichen Salze übergeführt wird.Process for the preparation of the compounds of the general formula (I) according to at least one of Claims 1 to 3, characterized in that (a) for the preparation of compounds of the general formula (I) in which X denotes the NH group and A, B , D, E, ----, R 1 and R 2 are as defined in claim 1, a piperidine of the general formula
Figure 02090001
in which R 1 is as defined in claim 1, with a carbonic acid derivative of the general formula
Figure 02090002
in which G represents a nucleofugic group, and with a primary amine of the general formula
Figure 02090003
in which A, B, D, E, - and R 2 are as defined in claim 1, with the proviso that these groups contain no further free primary or secondary aliphatic amino function, or (b) for the preparation of Compounds of general formula (I) in which X represents the methylene group and A, B, D, E, ----, R 1 and R 2 are as defined in claim 1, with the proviso that these groups are not further free contain primary or secondary aliphatic amino function, a carboxylic acid of the general formula
Figure 02100001
in which A, B, D, E, ---- and R 2 are as defined in claim 1, with a piperidine of the general formula
Figure 02100002
in which R 1 has the meanings mentioned in claim 1, or (c) for preparing compounds of the general formula (I) in which X represents the methylene group and A, B, D, E, ----, R 1 and R 2 are as defined in claim 1, with the proviso that these groups do not contain a free primary or secondary amine, a compound of the general formula
Figure 02100003
in which A, B, D, E, - and R 2 are as defined in claim 1, with the proviso that R 2 does not contain a primary or secondary amine, and Nu represents a leaving group, with a piperidine of the general formula
Figure 02110001
in which R 1 is as defined in claim 1, or (d) for the preparation of compounds of general formula (I) in which all radicals are as defined in claim 1, a carboxylic acid of the general formula
Figure 02110002
in which A, B, D, E, ----, R 1 and X are as defined in claim 1, coupled with an amine R 2 with the proviso that no further free primary or secondary aliphatic amino function is included, or (e) for the preparation of compounds of the general formula (I) in which all radicals are as defined in claim 1, with the proviso that no free primary or secondary amine is present, a compound of the general formula
Figure 02120001
in which A, B, D, E, ----, R 1 and X are as defined in claim 1 and Nu is a leaving group, with an amine R 2 , with the proviso that no further free primary or secondary aliphatic amino function and, if necessary, a protective moiety used in the reactions described above is cleaved off again and / or optionally used precursor functions are modified in a compound thus obtained and / or optionally a compound of the general formula (I) thus obtained is resolved into its stereoisomers and / or a compound of the general formula (I) thus obtained is converted into its salts, in particular for the pharmaceutical application, into its physiologically tolerated salts.
DE200410028751 2004-03-03 2004-06-15 New 4-heterocyclyl-1-acyl-piperidine derivatives, useful e.g. for treating headache, diabetes and cardiovascular disease, are antagonists of calcitonin-gene related peptide Withdrawn DE102004028751A1 (en)

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