HK40003592B

HK40003592B - Tetrahydropyrimidodiazepine and tetrahydropyridodiazepine compounds for treating pain and pain related conditions

Info

Publication number: HK40003592B
Application number: HK19127014.9A
Authority: HK
Inventors: Félix CUEVAS-CORDOBÉS; Carmen ALMANSA-ROSALES
Original assignee: Esteve Pharmaceuticals, S.A.
Priority date: 2016-05-06
Filing date: 2017-05-05
Publication date: 2020-12-24

Claims

Verbindung der allgemeinen Formel (I): worin:
X CRx oder N ist;

Rx ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; oder ein Halogenatom ist;

Y CH₂ oder C=O ist;

m 0, 1 oder 2 ist;

R₁ ein Wasserstoffatom; oder ein linearer oder verzweigter C_1-6-Alkylrest ist;

R₂ ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; ein Halogenatom; Haloalkyl; -SR_2a; -NR_2aR_2b; oder -OR_2a ist;

R_2a und R_2b unabhängig voneinander ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-4-Alkylrest; ein C_3-6 Cycloalkylrest; -(CH₂)_r-Aryl, wobei die Arylgruppe ein 5- oder 6-gliedriger Ring ist und r 0, 1 oder 2 ist; ein -(CH₂)_s-Heteroaryl, wobei die Heteroarylgruppe ein 5- oder 6-gliedriger Ring mit mindestens einem Stickstoffatom als Heteroatom ist, das gegebenenfalls von mindestens einem Halogenatom ersetzt wird, und s 0, 1 oder 2 ist; oder -(CH₂)₂-O-CH₃ sind;

R₃ ein Wasserstoffatom; -CN; -OH; Halogen; verzweigter oder unverzweigter C_1-6-Alkylrest; -(CH₂)_p-O-R₄, wobei p 0, 1 oder 2 ist; -(CH₂)_q-NR₅R₆, wobei q 0, 1, 2 oder 3 ist; -C(CH₃)₂-CH₂-NR₅R₆; -C(=O)NR₅R₆; eine 5- oder 6-gliedrige Heteroarylgruppe mit mindestens einem Heteroatom, ausgewählt aus N, O oder S, die durch einen oder zwei R₇-Substituenten substituiert ist und die durch eine C_1-3-Alkylengruppe an den Phenylring gebunden sein kann; ein 5- oder 6-gliedriger Heterocycoalkylrest mit einem oder zwei Stickstoffen als Heteroatom, der unsubstituiert oder gegebenenfalls durch einen oder zwei R₈-Substituenten substituiert ist und der über eine C_1-3-Alkylengruppe an den Phenylring gebunden sein kann; oder -C(=O)OR₉ ist;

R₄ ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; ein tert-Butyldimethylsilylrest; ein Methylbenzolsulfonatrest; ein -CHR_4aR_4b; ein -CH₂-CHR_4aR_4b; oder ein 5- oder 6-gliedriger Heterocycloalkylrest mit mindestens einem N-Atom ist, der gegebenenfalls durch einen oder zwei R_4c-Reste substituiert ist;

R_4a ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; eine 5- oder 6-gliedrige Arylgruppe, die gegebenenfalls durch ein mindestens ein Halogenatom substituiert ist; oder eine 5- oder 6-gliedrige Heteroarylgruppe mit mindestens einem Heteroatom ist, ausgewählt aus N, O oder S und gegebenenfalls substituiert durch mindestens einen verzweigten oder unverzweigten C_1-6-Alkylrest;

R_4b ein -(CH₂)_j-NR_4b'R_4b ist, wobei j 0, 1, 2 oder 3 ist;

R_4b' und R_4b" unabhängig voneinander ein Wasserstoffatom; ein verzweigter oder unverzweigter C1-6-Alkylrest; ein C_1-6-Haloalkylrest; eine Benzylgruppe; eine Phenethylgruppe; eine tert-Butyloxycarbonylgruppe; oder eine (Trimethylsilyl)ethyloxycarbonylgruppe sind; oder

R_4b' und R_4b" zusammen mit dem brückenbildenden Stickstoff einen 5- oder 6-gliedrigen Heterocycloalkylrest bilden, der gegebenenfalls ein zusätzliches Heteroatom, ausgewählt aus N, O oder S, enthält;

R_4c ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; eine Phenylgruppe; eine Benzylgruppe; oder eine tert-Butyloxycarbonylgruppe ist;

R₅ und R₆ unabhängig voneinander ein Wasserstoffatom; einen verzweigten oder unverzweigten C_1-6-Alkylrest; eine tert-Butyloxycarbonylgruppe; eine Benzylgruppe; eine Phenethylgruppe darstellen; oder

R₅ und R₆ zusammen mit dem brückenbildenden Stickstoff einen 5- oder 6-gliedrigen Heterocycloalkylrest bilden, der ein- oder zweifach durch eine Phenylgruppe substituiert sein kann, die ihrerseits gegebenenfalls durch einen verzweigten oder unverzweigten C_1-6-Alkylrest, ein Halogenatom, -OH oder -CN; oder durch ein -NRR' substituiert ist; R und R' unabhängig voneinander ein Wasserstoffatom oder ein verzweigter oder unverzweigter C_1-6-Alkylrest sind; oder

R₅ und R₆ zusammen mit dem brückenbildenden Stickstoff einen 5- oder 6-gliedrigen Heterocycloalkylrest bilden, der an einen anderen 5- oder 6-gliedrigen Heterocycloalkylrest mit mindestens einem Heteroatom, ausgewählt aus N, O oder S, spirokondensiert werden kann, das wiederum durch einen oder mehrere Substituenten, ausgewählt aus einem verzweigten oder unverzweigten C_1-6-Alkylrest; ein Halogenatom, ein -OH, ein -CN oder ein =O substituiert sein kann;

R₇ ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; eine -C(=O)H-Gruppe; ein -(CH₂)_p-NR_7aR_7b, wobei p 0, 1, 2 oder 3 ist; oder ein -(CH)R_7cR_7d ist;

R_7a und R_7b unabhängig voneinander ein Wasserstoffatom; einen verzweigten oder unverzweigten C_1-6-Alkylrest; eine tert-Butyloxycarbonylgruppe; eine Benzylgruppe, die gegebenenfalls durch ein Halogen substituiert ist; eine Phenethylgruppe; ein -(CH₂)-Cyclopropyl; eine Hydroxyethoxyethylgruppe; ein -OH; eine -C(=O)H-Gruppe; eine Pyridinylmethylgruppe darstellen; oder

R_7a und R_7b zusammen mit dem brückenbildenden Stickstoff einen 5- oder 6-gliedrigen Heterocycloalkylrest bilden, der zusätzlich ein zweites N-Atom enthalten kann, wobei der Rest durch ein -NR_7a'R_7b' substituiert sein kann, wobei R_7a' und R_7b' ein Wasserstoffatom oder ein verzweigter oder unverzweigter C_1-6-Alkylrest ist; oder durch eine Phenylgruppe, die wiederum gegebenenfalls durch einen verzweigten oder unverzweigten C_1-6-Alkylrest, ein Halogenatom, ein -OH oder ein -CN substituiert ist; oder

R_7a und R_7b zusammen mit dem brückenbildenden Stickstoff einen 5- oder 6-gliedrigen Heterocycloalkylrest bilden, der an einen 5- oder 6-gliedrigen aromatischen Ring anelliert werden kann oder entweder an einen einzelnen 5- oder 6-gliedrigen Heterocycloalkylring mit mindestens einem Heteroatom, ausgewählt aus N, O oder S, spirokondensiert werden kann, das wiederum durch einen oder mehrere Substituenten, ausgewählt aus einem verzweigten oder unverzweigten C_1-6-Alkylrest, einem Halogenatom, einem -OH, einem - CN oder einem =O, substituiert sein kann; oder an ein bizyklisches Ringsystem spirokondensiert sein kann, das aus einem 5- oder 6-gliedrigen Heterocycloalkylring mit mindestens einem Heteroatom, ausgewählt aus N, O oder S, an einem 5- oder 6-gliedrigen aromatischen Ring gebildet ist;

R_7c und R_7d unabhängig voneinander ein Wasserstoffatom; einen verzweigten oder unverzweigten C_1-6-Alkylrest; oder C_1-6 -Alkoxyrest darstellen; und

R₈ ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; eine tert-Butyloxycarbonylgruppe; eine Phenylgruppe; eine Benzylgruppe; eine Phenethylgruppe; oder ein -NR_8a'R_8b ist, wobei R_8a' und R_8b' ein Wasserstoffatom oder ein verzweigter oder unverzweigter C_1-6-Alkylrest sind;

R₉ ein Wasserstoffatom; oder ein linearer oder verzweigter C_1-6-Alkylrest ist;

oder ein pharmazeutisch akzeptables Salz, Stereoisomer oder Solvat davon.
Verbindung nach Anspruch 1, wobei R₂ ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; ein Halogenatom; Haloalkyl; -SR_2a; -NR_2aR_2b; oder -OR_2a ist; wobei R_2a und R_2b unabhängig voneinander aus einem Wasserstoffatom; einem verzweigten oder unverzweigten C_1-4-Alkylrest; -(CH₂)₂-O- CH₃; oder einer Gruppe ausgewählt sind, die ausgewählt wird aus:
Verbindung nach Anspruch 1, wobei R₃ ein -(CH₂)_p-O-R₄ darstellt, wobei p 0, 1 oder 2 ist und wobei R₄:
• ein Wasserstoffatom;

• ein verzweigter oder unverzweigter C_1-6-Alkylrest;

• ein tert-Butyldimethylsilylrest;

• ein Methylbenzolsulfonatrest;

• ein-CHR_4aR_4b oder ein -CH₂-CHR_4aR_4b ist, wobei R_4a ein Wasserstoffatom ist; ein verzweigter oder unverzweigter C_1-6-Alkylrest; oder eine Gruppe, ausgewählt aus: und wobei R_4b ein -(CH₂)_j-NR_4b'R_4b" ist, wobei j 0, 1, 2 oder 3 ist und R_4b' und R_4b" unabhängig voneinander ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; ein C_1-6-Haloalkylrest; eine Benzylgruppe; eine Phenethylgruppe; eine tert-Butyloxycarbonylgruppe; eine (Trimethylsilyl)ethyl-oxycarbonylgruppe sind; oder R_4b' und R_4b" zusammen mit dem brückenbildenden Stickstoff eine Gruppe bilden, ausgewählt aus:

• einer Gruppe ausgewählt aus: wobei R_4c ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; eine Phenylgruppe; eine Benzylgruppe; oder eine tert-Butyloxycarbonylgruppe ist.
Verbindung nach Anspruch 1, wobei R₃ ein -(CH₂)_q-NR₅R₆; -C(CH₃)₂-CH₂-NR₅R₆; oder -C(=O)NR₅R₆ darstellt, wobei q 0, 1, 2 oder 3 ist und wobei R₅ und R₆ unabhängig voneinander:
• ein Wasserstoffatom;

• ein verzweigter oder unverzweigter C_1-6-Alkylrest;

• eine tert-Butyloxycarbonylgruppe;

• eine Gruppe ist, ausgewählt aus: oder wobei R₅ und R₆ zusammen mit dem brückenbildenden Stickstoff die folgenden Strukturen bilden: wobei R_a eine Phenylgruppe ist, die wiederum gegebenenfalls durch einen verzweigten oder unverzweigten C_1-6-Alkylrest, ein Halogenatom, ein -OH oder ein -CN; oder ein -NRR' substituiert ist, wobei R und R' unabhängig voneinander ein Wasserstoffatom oder einen verzweigten oder unverzweigten C_1-6-Alkylrest bilden; R_b ein verzweigter oder unverzweigter C_1-6-Alkylrest; ein Halogenatom; -OH; oder -CN ist; und ^R _c ein verzweigter oder unverzweigter C_1-6-Alkylrest; ein Halogenatom;-OH; -CN; oder =O ist.
Verbindung nach Anspruch 1, wobei R₃ eine Gruppe darstellt, ausgewählt aus: wobei R₇:
• ein Wasserstoffatom;

• ein verzweigter oder unverzweigter C_1-6-Alkylrest;

• eine -C(=O)H-Gruppe;

• eine -(CH₂)_p-NR_7aR_7b ist, wobei p 0, 1, 2 oder 3 oder ein -(CH)R_7cR_7d ist;
wobei R_7a und R_7b unabhängig voneinander ein Wasserstoffatom; einen verzweigten oder unverzweigten C_1-6-Alkylrest; eine tert-Butyloxycarbonylgruppe; eine Benzylgruppe, die gegebenenfalls durch ein Halogen substituiert ist; eine Phenethylgruppe; ein -(CH₂)-Cyclopropyl; eine Hydroxyethoxyethylgruppe; ein -OH; eine -C(=O)H-Gruppe; eine Pyridinylmethylgruppe darstellen; oder R_7a und R_7b zusammen mit dem brückenbildenden Stickstoff eine der folgenden Strukturen darstellen: wobei R" ein Wasserstoff oder eine -OH-Gruppe ist; und wobei R_7c und R_7d unabhängig voneinander ein Wasserstoffatom; einen verzweigten oder unverzweigten C_1-6-Alkylrest; oder C_1-6-Alkoxyrest darstellen.
Verbindung nach Anspruch 1, wobei R₃ eine Gruppe darstellt, ausgewählt aus: wobei R₈ ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; eine tert-Butyloxycarbonylgruppe; eine Benzylgruppe oder eine Phenethylgruppe ist.
Verbindung nach Anspruch 1, wobei R₃ ein -C(=O)OR₉ ist, wobei R₉ ein Wasserstoffatom oder ein linearer oder verzweigter C_1-6-Alkylrest ist.
Verbindung nach Anspruch 1, ausgewählt aus folgender Liste:
[1] tert-Butylmethyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)carbamat;

[2] tert-Butyl(R)-methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)carbamat;

[3] tert-Butyl(S)-methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)carbamat;

[4] tert-Butylmethyl(2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrim ido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)carbamat;

[5] tert-Butyl(2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)carbamat;

[6] tert-Butylmethyl(2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrim ido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)carbamat;

[7] tert-Butylmethyl(3-methyl-2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)butyl)carbamat;

[8] tert-Butylmethyl(2-(4-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)carbamat;

[9] tert-Butylmethyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamat;

[10] tert-Butyl (R)-methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamat;

[11] tert-Butyl (S)-methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamat;

[12] tert-Butylmethyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)carbamat;

[13] tert-Butyl (R)-methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4] diazepin-6-yl)phenoxy) -3-(thiophen-2-yl)propyl)-carbamat;

[14] tert-Butyl (S)-methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)-carbamat;

[15] tert-Butylmethyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrim ido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)carbamat;

[16] tert-Butyl (R)-methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)-carbamat;

[17] tert-Butyl (S)-methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)-carbamat;

[18] tert-Butylmethyl(2-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-1-phenylethyl)carbamat;

[19] 2-(Trimethylsilyl)ethylmethylmethyl(2-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-2-phenylethyl)carbamat;

[20] tert-Butylmethyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrim ido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)carbamat;

[21] tert-Butylbenzyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrim ido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)carbamat;

[22] tert-Butylmethyl(2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrim ido[4,5-e][1,4]diazepin-6-yl)phenoxy)ethyl)carbamat;

[23] tert-Butylmethyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)propyl)carbamat;

[24] tert-Butylmethyl(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenethyl)carbamat;

[25] tert-Butylmethyl(2-methyl-2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)propyl)carbamat;

[26] tert-Butylmethyl(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)carbamat;

[27] tert-Butyl 3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)pyrrolidin-1-carboxylat;

[28] tert-Butyl 4-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-4-phenylpiperidin-1-carboxylat;

[29] 9-Methyl-6-(3-(5-methyl-1,3)4-oxadiazol-2-yl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[30] 9-Ethyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[31] 9-Methyl-6-(3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[32] 6-(3-Methoxyphenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[33] 3-(9-Methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzonitril;

[34] 6-(3-((tert-Butyldimethylsilyl)oxy)phenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[35] 6-(3-Bromphenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[36] 6-(3-(2-Hydroxyethyl)phenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[37] 6-(4-Methoxyphenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[38] 6-(4-((tert-Butyldimethylsilyl)oxy)phenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[39] tert-Butylmethyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamat;

[40] tert-Butyl ((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamat;

[41] tert-Butylbenzyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamat;

[42] 6-(3-(4-(Diethoxymethyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[43] tert-Butylmethyl(2-(1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)ethyl)-carbamat;

[44] tert-Butylmethyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)-1H-1,2,3-triazol-4-yl)methyl)carbamat;

[45] tert-Butylmethyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-pyrazol-4-yl)methyl)carbamat;

[46] tert-Butylmethyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-imidazol-4-yl)methyl)carbamat;

[47] tert-Butylmethyl((5-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1,3,4-oxadiazol-2-yl)methyl)carbamat;

[48] tert-Butylmethyl(3-(2-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrim ido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)carbamat;

[49] tert-Butylmethyl(4-methyl-3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)pentyl)carbamat;

[50] tert-Butylmethyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)butyl)carbamat;

[51] 2-(Trimethylsilyl)ethylmethyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)-propyl)carbamat;

[52] tert-Butylmethyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(pyridin-2-yl)propyl)carbamat;

[53] tert-Butylmethyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(pyridin-3-yl)propyl)carbamat;

[54] 8-(Ethylamino)-1-methyl-4-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[55] 4-(3-(4-Ethyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)-8-(ethylamino)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[56] tert-Butyl (3-(3-(8-(ethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-phenylpropyl)-(methyl)carbamat;

[57] tert-Butyl (3-((3-(8-(ethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[58] 2-(Trimethylsilyl)ethyl (3-(3-(8-(ethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)-(methyl)carbamat;

[59] 2-(Trimethylsilyl)ethyl (3-(3-(8-(dimethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[60] 2-(Trimethylsilyl)ethyl (3-((3-(8-(ethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)-(methyl)carbamat;

[61] tert-Butyl (2-fluorethyl)(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)-carbamat;

[62] tert-Butylmethyl(2-(3-((9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)phenoxy)-2-phenylethyl)carbamat;

[63] tert-Butylmethyl(2-(4-((9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)phenoxy)-2-phenylethyl)carbamat;

[64] tert-Butylmethyl(4-((9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)benzyl)carbamat;

[65] tert-Butyl (R)-(3-((3-(2-(ethylamino)-9-methyl-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[66] N-Ethyl-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-2-amin;

[67] N-Ethyl-6-(3-methoxybenzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido-[4,5-e][1,4]diazepin-2-amin;

[68] N-Ethyl-6-(4-methoxybenzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido-[4,5-e][1,4]diazepin-2-amin;

[69] tert-Butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)(methyl)carbamat;

[70] tert-Butyl (R)-(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)(methyl)carbamat;

[71] tert-Butyl (S)-(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)(methyl)carbamat;

[72] tert-Butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)(methyl)carbamat;

[73] tert-Butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)carbamat;

[74] tert-Butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)(methyl)carbamat;

[75] tert-Butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-methylbutyl)(methyl)carbamat;

[76] tert-Butyl (2-(4-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)(methyl)carbamat;

[77] tert-Butyl (3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[78] tert-Butyl (R)-(3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[79] tert-Butyl (S)-(3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,75859-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[80] tert-Butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[81] tert-Butyl (R)-(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)-carbamat;

[82] tert-Butyl (S)-(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)-carbamat;

[83] tert-Butyl (3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)-carbamat;

[84] tert-Butyl (R)-(3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[85] tert-Butyl (S)-(3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[86] tert-Butyl (2-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-1-phenylethyl)(methyl)carbamat;

[87] 2-(Trimethylsilyl)ethyl(2-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-2-phenylethyl)(methyl)carbamat;

[88] tert-Butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)(methyl)carbamat;

[89] tert-Butylbenzyl(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)carbamat;

[90] tert-Butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)ethyl)(methyl)carbamat;

[91] tert-Butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)propyl)(methyl)carbamat;

[92] tert-Butyl (3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenethyl)(methyl)carbamat;

[93] tert-Butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-2-methylpropyl)(methyl)carbamat;

[94] tert-Butyl (3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)(methyl)carbamat;

[95] tert-Butyl 3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)pyrrolidin-1-carboxylat;

[96] tert-Butyl 4-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-4-phenylpiperidin-1-carboxylat;

[97] 2-(Ethylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[98] 2-(Isobutylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,5,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[99] 2-((2-Methoxyethyl)amino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[100] 9-Methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-2-(methylamino)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[101] 2-Amino-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4)5-e][1,4]di2-(benzylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on azepin-5-on;

[102] 2-(Benzylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[103] 2-(Cyclohexylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[104] 2-(Benzyl(methyl)amino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[105] 9-Methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-2-(phenethylamino)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[106] 9-Methyl-2-(methyl(pyridin-2-ylmethyl)amino)-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[107] 9-Ethyl-2-(ethylamino)-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[108] 2-(Ethylamino)-9-methyl-6-(3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[109] 2-(Ethylamino)-6-(3-methoxyphenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[110] 3-(2-(Ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzonitril;

[111] 6-(3-((tert-Butyldimethylsilyl)oxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[112] 2-(Ethylamino)-6-(3-(2-hydroxyethyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[113] 2-(Ethylamino)-6-(3-(2-hydroxyethyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[114] 2-(Ethylamino)-6-(4-methoxyphenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[115] 6-(4-((tert-Butyldimethylsilyl)oxy)phenyl)-2-(ethylamino) -9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[116] tert-Butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)(methyl)carbamat;

[117] tert-Butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamat;

[118] tert-Butylbenzyl((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamat;

[119] 6-(3-(4-(Diethoxymethyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[120] tert-Butyl (2-(1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)ethyl)(methyl)-carbamat;

[121] tert-Butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)-1H-1,2,3-triazol-4-yl)methyl)(methyl)carbamat;

[122] tert-Butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-pyrazol-4-yl)methyl)(methyl)carbamat;

[123] tert-Butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-imidazol-4-yl)methyl)(methyl)-carbamat;

[124] tert-Butyl ((5-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1,3,4-oxadiazol-2-yl)methyl)(methyl)carbamat;

[125] tert-Butyl (3-(2-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)(methyl)carbamat;

[126] tert-Butyl (3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-4-methylpentyl)(methyl)carbamat;

[127] tert-Butyl (3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)butyl)(methyl)carbamat;

[128] tert-Butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(pyridin-2-yl)propyl)(methyl)carbamat;

[129] tert-Butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(pyridin-3-yl)propyl)(methyl)carbamat;

[130] tert-Butyl (R)-(3-((3-(2-amino-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[131] tert-Butyl (R)-(3-((3-(2-(dimethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[132] tert-Butyl(R)-Methyl(3-((3-(9-methyl-2-(methylamino)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamat;

[133] 2-(Trimethylsilyl)ethyl (3-(3-(2-(dimethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[134] tert-Butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(2-fluorethyl)carbamat;

[135] tert-Butyl (2-(3-((2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)phenoxy)-2-phenylethyl)(methyl)carbamat;

[136] tert-Butyl (2-(4-((2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)phenoxy)-2-phenylethyl)(methyl)carbamat;

[137] tert-Butyl (4-((2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)benzyl)(methyl)carbamat;

[138] tert-Butyl (R)-(3-((3-(2-methoxy-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[139] tert-Butyl (3-((3-(2-methoxy-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)-carbamat;

[140] tert-Butyl (R)-(3-((3-(2-hydroxy-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[141] tert-Butyl (3-((3-(2-hydroxy-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[142] tert-Butyl (R)-(3-((3-(2)9-dimethyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4)5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[143] tert-Butyl (3-((3-(2)9-Dimethyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4)5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[144] 2-(Trimethylsilyl)ethyl (3-(3-(2)9-dimethyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)-carbamat;

[145] tert-Butyl (R)-methyl(3-((3-(9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamat;

[146] tert-Butylmethyl(3-((3-(9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido-[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)carbamat;

[147] 2-(Trimethylsilyl)ethylmethyl(3-(3-(9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)carbamat;

[148] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[149] (R)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[150] (S)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[151] 9-Methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[152] (R)-9-Methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[153] (S)-9-Methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[154] 2-(Ethylamino)-9-methyl-6-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[155] 9-Methyl-6-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[156] 6-(3-(2-Amino-1-phenylethoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[157] 2-(Ethylamino)-9-methyl-6-(3-((1-(methylamino)propan-2-yl)oxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[158] 2-(Ethylamino)-9-methyl-6-(3-((3-methyl-1-(methylamino)butan-2-yl)-oxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[159] 2-(Ethylamino)-9-methyl-6-(4-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[160] 2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[161] (R)-2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[162] (S)-2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)-methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[163] 9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[164] (R)-9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[165] (S)-9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[166] 2-(Ethylamino)-9-methyl-6-(3-((2-(methylamino)-2-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[167] 9-Methyl-6-(3-((2-(methylamino)-2-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[168] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[169] 6-(3-(3-(Benzylamino)propoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[170] 2-(Ethylamino)-9-methyl-6-(3-(2-(methylamino)ethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[171] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)propyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[172] 2-(Ethylamino)-9-methyl-6-(3-(2-(methylamino)ethyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[173] 2-(Ethylamino)-9-methyl-6-(3-(2-methyl-1-(methylamino)propan-2-yl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[174] 2-(Ethylamino)-9-methyl-6-(3-((methylamino)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[175] 2-(Ethylamino)-9-methyl-6-(3-(pyrrolidin-3-yloxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[176] 2-(Ethylamino)-9-methyl-6-(3-(((4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-6,7,8,9- tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[177] 2-(Ethylamino)-6-(3-hydroxyphenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[178] 2-(Ethylamino)-6-(4-hydroxyphenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[179] 9-Methyl-2-(methylthio)-6-(3-(((4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[180] 2-(Ethylamino)-9-methyl-6-(3-(4-((methylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[181] 6-(3-(4-(Aminomethyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[182] 6-(3-(4-((Benzylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[183] 2-(Ethylamino)-9-methyl-6-(3-(4-(2-(methylamino)ethyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[184] 2-(Ethylamino)-9-methyl-6-(3-((4-((methylamino)methyl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[185] 2-(Ethylamino)-9-methyl-6-(3-(4-((methylamino)methyl)-1H-pyrazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[186] 2-(Ethylamino)-9-methyl-6-(3-(4-((methylamino)methyl)-1H-imidazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[187] 2-(Ethylamino)-9-methyl-6-(3-(5-((methylamino)methyl)-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[188] 2-(Ethylamino)-9-methyl-6-(2-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[189] 2-(Ethylamino)-9-methyl-6-(3-(((4-methyl-1-(methylamino)pentan-3-yl)-oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[190] 9-Methyl-6-(3-(((4-methyl-1-(thylamino)pentan-3-yl)oxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[191] 2-(Ethylamino)-9-methyl-6-(3-(((4-(methylamino)butan-2-yl)oxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[192] 9-Methyl-6-(3-(((4-(methylamino)butan-2-yl)oxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[193] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(pyridin-2-yl)propoxy)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[194] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(pyridin-3-yl)propoxy)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[195] (R)-2-Amino-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[196] (R)-2-(Dimethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[197] (R)-9-Methyl-2-(methylamino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[198] 8-(Ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[199] 8-(Ethylamino)-1-methyl-4-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[200] 2-(Ethylamino)-9-methyl-6-(3-(2-(methylamino)-1-phenylethoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[201] 2-(Ethylamino)-9-methyl-6-(4-(2-(methylamino)-1-phenylethoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[202] 2-(Ethylamino)-9-methyl-6-(4-((methylamino)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[203] (R)-N-Ethyl-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-2-amin;

[204] (R)-2-Methoxy-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[205] (R)-2-Hydroxy-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[206] (R)-2,9-Dimethyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[207] (R)-9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[208] 9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[209] (R)-9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)-phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[210] (S)-9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)-phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[211] 2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[212] (R)-2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)-propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[213] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[214] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[215] (R)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[216] (S)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[217] 9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[218] (R)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[219] (S)-9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[220] 2-(Ethylamino)-6-(3-(3-((2-fluorethyl)amino)-1-(thiophen-2-yl)propoxy)-phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[221] 2-Methoxy-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)-methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[222] 2-Hydroxy-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)-methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[223] 2,9-Dimethyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[224] 9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[225] 2-(Ethylamino)-9-methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[226] 9-Methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[227] 8-(Ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[228] 8-(Ethylamino)-1-methyl-4-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[229] 8-(Dimethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[230] 2-(Dimethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[231] 2,9-Dimethyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[232] 9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[233] tert-Butyl 4-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-356-dihydropyridin-1(2H)-carboxylat;

[234] tert-Butyl 4-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)piperidin-1-carboxylat;

[235] 2-(Ethylamino)-9-methyl-6-(3-(piperidin-4-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[236] (R)-6-(3-((3-(Dimethylamino)-1-phenylpropoxy)methyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[237] (S)-6-(3-((3-(Dimethylamino)-1-phenylpropoxy)methyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[238] 6-(3-(3-(Dimethylamino)-1-phenylpropoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[239] 6-(3-(2-(Dimethylamino)-1-phenylethoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[240] 6-(3-(3-(Benzyl(methyl)amino)propyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[241] 6-(3-(3-(Dimethylamino)propyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[242] 6-(3-(4-((Dimethylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[243] 6-(3-(4-((Benzyl(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[244] 2-(Ethylamino)-9-methyl-6-(3-(4-((methyl(phenethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[245] 6-(3-(4-((Bis(Cyclopropylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)-phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[246] 6-(3-(4-(((Cyclopropylmethyl)(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[247] 6-(3-(4-(2-(Benzyl(methyl)amino)ethyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[248] 6-(3-(4-(2-(Dimethylamino)ethyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[249] 2-(Ethylamino)-9-methyl-6-(3-(4-(2-(methyl(phenethyl)amino)ethyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[250] 6-(3-((4-((Benzyl(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)methyl)-phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[251] 6-(3-(4-((Benzyl(methyl)amino)methyl)-1H-pyrazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[252] 2-(Ethylamino)-9-methyl-6-(3-(4-((methyl(phenethyl)amino)methyl)-1H-pyrazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[253] 6-(3-(4-((Benzyl(methyl)amino)methyl)-1H-imidazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[254] 2-(Ethylamino)-9-methyl-6-(3-(4-((methyl(phenethyl)amino)methyl)-1H-imidazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[255] 6-(3-(5-((Benzyl(methyl)amino)methyl)-1)3,4-oxadiazol-2-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[256] 6-(3-(3-(Benzyl(methyl)amino)propoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[257] 6-(3-(3-(Dimethylamino)propoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[258] 2-(Ethylamino)-9-methyl-6-(3-(3-(methyl(phenethyl)amino)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[259] 6-(3-(1-Benzylpiperidin-4-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[260] 2-(Ethylamino)-9-methyl-6-(3-(1-methylpiperidin-4-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[261] 2-(Ethylamino)-9-methyl-6-(3-(1-phenethylpiperidin-4-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[262] 6-(3-((1-(Benzyl(methyl)amino)propan-2-yl)oxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[263] 2-(Ethylamino)-9-methyl-6-(3-((1-(methyl(phenethyl)amino)propan-2-yl)-oxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[264] 6-(3-(2-(Benzyl(methyl)amino)ethoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[265] 2-(Ethylamino)-9-methyl-6-(3-(2-(methyl(phenethyl)amino)ethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[266] 6-(3-((1-Benzylpyrrolidin-3-yl)oxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[267] 6-(3-((1-(Benzyl(methyl)amino)-3-methylbutan-2-yl)oxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[268] 2-(Ethylamino)-9-methyl-6-(3-((3-methyl-1-(methyl(phenethyl)amino)butan-2-yl)oxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[269] 6-(3-(2-(Benzyl(methyl)amino)ethyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[270] 2-(Ethylamino)-9-methyl-6-(3-(2-(methyl(phenethyl)amino)ethyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[271] 9-Methyl-6-(3-(((1-methyl-4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[272] 2-(Ethylamino)-9-methyl-6-(3-(((1-methyl-4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[273] 2-(Ethylamino)-6-(3-(4-(((2-(2-hydroxyethoxy)ethyl)(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[274] 3-(2-(Ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4)5-e][1,4]diazepin-6-yl)phenethyl 4-methylbenzolsulfonat;

[275] 2-(Ethylamino)-6-(3-(2-(4-(3-hydroxyphenyl)piperidin-1-yl)ethyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[276] (R)-9-(3-(2-(Ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenethyl)-4-isopropyl-2-methyl-1-oxa-4,9-diazaspiro[5,5]undecan-3-on;

[277] 1-(3-(2-(Ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido-[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-carbaldehyd;

[278] 2-(Ethylamino)-9-methyl-6-(3-(4-((4-phenylpiperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[279] 2-(Ethylamino)-6-(3-(4-((4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[280] 2-(Ethylamino)-9-methyl-6-(3-(4-((4-phenylpiperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[281] 2-(Ethylamino)-9-methyl-6-(3-(4-(piperidin-1-ylmethyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[282] 6-(3-(4-((3)4-Dihydroisochinolin-2(1H)-yl)methyl)-1H-1)2,3-triazol-1-yl)-phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[283] 6-(3-(4-((3,4-Dihydro-2H-spiro[Isochinolin-1,4'-piperidin]-1'-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[284] (R)-9-((1-(3-(2-(Ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)-4-isopropyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-on;

[285] 6-(3-(4-(((Cyclopropylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[286] 2-(Ethylamino)-6-(3-(4-((ethylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[287] 2-(Ethylamino)-6-(3-(4-(((4-fluorbenzyl)(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[288] 2-(Ethylamino)-9-methyl-6-(3-(4-((methyl(pyridin-2-ylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[289] 2-(Ethylamino)-9-methyl-6-(3-(4-((methyl(pyridin-3-ylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[290] 2-(Ethylamino)-6-(3-(4-(((2-(2-hydroxyethoxy)ethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[291] 6-(3-(4-((4-(Dimethylamino)-4-phenylpiperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[292] 6-(3-((4-(Dimethylamino)-4-phenylpiperidin-1-yl)methyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[293] 6-(3-(4-((4-(Dimethylamino)-4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[294] 6-(3-(4-((4-(Dimethylamino)-4-phenylpiperidin-1-yl)methyl)-1H-pyrazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[295] 6-(3-(4-((4-(Dimethylamino)-4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1H-pyrazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[296] 6-(3-(4-((4-(Dimethylamino)-4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1H-imidazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[297] 2-(Trimethylsilyl)ethyl (3-(3-(8-chlor-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)-carbamat;

[298] 2-(Trimethylsilyl)ethyl (S)-(3-(3-(8-chlor-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[299] 2-(Trimethylsilyl)ethyl (S)-(3-(4-((8-chlor-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)methyl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[300] tert-Butyl (3-((3-(8-chlor-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[301] 2-(Trimethylsilyl)ethyl (S)-(3-(4-((1,8-dimethyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)methyl)phenoxy)-3-(thiophen-2-yl)propyl)-(methyl)carbamat;

[302] 2-(Trimethylsilyl)ethyl (3(3(1,8-dimethyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3 e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamat;

[303] tert-Butyl (3-((3-(1,8-dimethyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamat;

[304] (S)-8-Amino-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[305] (S)-8-Amino-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[306] 1,8-Dimethyl-4-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[307] 1,8-Dimethyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[308] (S)-1,8-Dimethyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[309] Methyl 3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzoat;

[310] 2-(Ethylamino)-6-(3-(2-hydroxyethyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[311] 6-(3-Bromphenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[312] 6-(3-(4-(Dimethylamino)-4-phenylpiperidin-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[313] 3-(2-(Ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzoesäure;

[314] 6-(3-(4-(Dimethylamino)-4-phenylpiperidin-1-carbonyl)-phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]-diazepin-5-on;

[315] 9-Methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[316] 9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[317] 1-Methyl-4-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-1,2,3,4-Tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[318] 9-Methyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[319] 9-Methyl-6-(2-(2-(methylamino)-1-phenylethoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[320] 9-Methyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[321] 9-Methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[322] 9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(trifluormethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[323] 1-Methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[324] (R)-8-(Ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[325] (S)-8-(Ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[326] (S)-1-Methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[327] (R)-1-Methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[328] 9-Methyl-6-(4-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[329] 9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(trifluormethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[330] 9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(trifluormethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[331] (S)-8-Methoxy-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[332] (S)-2-Amino-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[333] 2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[334] 2-(Ethylamino)-9-methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[335] 2-(Benzylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[336] 9-Methyl-2-(methyl(pyridin-2-ylmethyl)amino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[337] 2-(Ethylamino)-9-methyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[338] 2-(Ethylamino)-9-methyl-6-(2-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[339] 2-(Ethylamino)-9-methyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[340] 2-(Ethylamino)-9-methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[341] (R)-9-Methyl-2-(methyl(pyridin-2-ylmethyl)amino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[342] (R)-9-Methyl-2-(methyl(pyridin-3-ylmethyl)amino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[343] (R)-9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-((pyridin-2-ylmethyl)amino)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[344] (R)-2-(((5-Fluorpyridin-2-yl)methyl)(methyl)amino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[345] 2-(Ethylamino)-6-(3-((3-((2-fluorethyl)amino)-1-(thiophen-2-yl)propoxy)-methyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[346] (S)-2-Amino-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)-methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[347] (R)-2-Amino-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[348] 2-(Ethylamino)-9-methyl-6-(4-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[349] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-3-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[350] (S)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-3-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on

[351] (R)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-3-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[352] (S)-2-Amino-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[353] 2,9-Dimethyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[354] 2-Ethyl-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[355] 2,9-Dimethyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[356] (R)-2-Ethyl-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[357] (R)-2,9-Dimethyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[358] (S)-2,9-Dimethyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[359] (S)-2,9-Dimethyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[360] (R)-2,9-Dimethyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[361] 9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[362] 9-Methyl-6-(2-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[363] (R)-9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[364] (S)-9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[365] 9-Methyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[366] 9-Methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[367] 9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[368] 9-Methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[369] 9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[370] 9-Methyl-6-(2-(3-(methylamino)-1-phenylpropoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[371] 9-Methyl-6-(2-(2-(methylamino)-1-phenylethoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[372] 9-Methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[373] 9-Methyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[374] 9-Methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[375] (S)-2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[376] 6-(4-(1-(2-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[377] (S)-1-Methyl-4-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[378] 9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[379] (S)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[380] (R)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[381] 1-Methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[382] (S)-1-Methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[383] (S)-8-(Ethylamino)-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[43e][1,4]diazepin-5-on;

[384] (S)-8-(Dimethylamino)-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[43e][1,4]diazepin-5-on;

[385] (S)-8-Methoxy-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[386] (S)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(trifluormethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[387] 2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-3-yl)propoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[388] 2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(3-methylthiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[389] (S)-1-Ethyl-8-methoxy-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[390] 2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiazol-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[391] (S)-1-Ethyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[392] 2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(5-methylthiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[393] (S)-2-Methoxy-9-methyl-6-(3-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[394] (S)-6-(3-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[395] (S)-9-Ethyl-2-methoxy-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[396] 2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(4-methylthiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[397] (S)-2-Methoxy-9-methyl-6-(2-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[398] (S)-9-Ethyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[399] (S)-9-Fluor-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[400] (S)-9-Chlor-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[401] (S)-6-(2-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[402] (S)-2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[403] (S)-6-(4-Fluor-2-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[404] 2-(Ethylamino)-9-methyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[405] 2-(Ethylamino)-9-methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[406] 2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[407] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[408] 2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[409] 2-(Ethylamino)-9-methyl-6-(2-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[410] 2-(Ethylamino)-9-methyl-6-(2-(2-(methylamino)-1-phenylethoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[411] 2-(Ethylamino)-9-methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[412] 2-(Ethylamino)-9-methyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[413] 2-(Ethylamino)-9-methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[414] (S)-2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[415] (R)-2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[416] 2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[417] (S)-2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[418] (R)-2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[419] (S)-2-(Dimethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[420] (S)-2-Amino-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[421] 2,9-Dimethyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[422] 2,9-Dimethyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[423] 2,9-Dimethyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[424] 2,9-Dimethyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[425] 2,9-Dimethyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[426] 2-Ethyl-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[427] (R)-2,9-Dimethyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[428] (S)-2,9-Dimethyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[429] 9-Methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[430] 9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[431] 9-Methyl-6-(2-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[432] 9-Methyl-6-(2-(2-(methylamino)-1-phenylethoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[433] (S)-9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[434] (R)-9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[435] 9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[436] (S)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[437] (R)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[438] 6-(3-(2-(4-(Dimethylamino)-4-phenylpiperidin-1-yl)ethyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[439] 2-(Ethylamino)-9-methyl-6-(3-(2-(piperidin-1-yl)ethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[440] 2-(Ethylamino)-9-methyl-6-(3-(2-morpholinoethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[441] 6-(3-(5-((4-(Dimethylamino)-4-phenylpiperidin-1-yl)methyl)-1,3,4-oxadiazol-2-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[442] 6-(3-(5-((4-(Dimethylamino)-4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1)3,4-oxadiazol-2-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[443] 6-(4-(1-(2-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[444] 4-(4-(1-(2-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[445] 4-(4-(1-(2-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[446] 6-(4-(1-(3-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-2-Methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[447] 6-(4-(1-(3-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[448] 4-(4-(1-(3-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[449] 4-(4-(1-(3-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[450] 6-(4-(1-(4-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[451] 6-(4-(1-(4-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[452] 4-(4-(1-(4-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[453] 4-(4-(1-(4-Fluorphenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[454] 6-(4-(1-(2-Chlorphenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[455] 6-(4-(1-(2-Chlorphenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[456] 4-(4-(1-(2-Chlorphenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[457] 6-(4-(1-(3-Chlorphenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[458] 6-(4-(1-(3-Chlorphenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[459] 4-(4-(1-(3-Chlorphenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[460] 6-(4-(1-(4-Chlorphenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[461] 6-(4-(1-(4-Chlorphenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[462] 4-(4-(1-(4-Chlorphenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[463] (S)-8-Methoxy-1-methyl-4-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[464] 1-Methyl-4-(4-(3-(methylamino)-1-(5-methylthiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[465] 9-Methyl-6-(4-(3-(methylamino)-1-(5-methylthiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[466] 8-Methoxy-1-methyl-4-(4-(3-(methylamino)-1-(5-methylthiophen-2-yl)-propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[43e][1,4]diazepin-5-on;

[467] 8-Methoxy-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-3-yl)propoxy)-benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[468] 1-Methyl-4-(4-(3-(methylamino)-1-(thiophen-3-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[469] 9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-3-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[470] (S)-4-(3-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[471] (S)-4-(3-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[472] (S)-6-(3-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[473] (S)-6-(2-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[474] (S)-4-(2-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[475] (S)-4-(2-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[476] (S)-8-Methoxy-1-methyl-4-(2-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[43e][1,4]diazepin-5-on;

[477] (S)-1-Methyl-4-(2-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[478] (S)-9-Methyl-6-(2-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[479] (S)-6-(3-Chlor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[480] (S)-6-(3-Chlor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[481] (S)-4-(3-Chlor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[482] (S)-6-(2-Chlor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[483] (S)-6-(2-Chlor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[484] (S)-4-(2-Chlor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[485] (S)-2-Ethoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[486] (S)-8-Methoxy-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[487] (S)-1-Isopropyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on; und

[488] (S)-9-Isopropyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on.
Verbindung nach Anspruch 1 mit einer der folgenden Formeln (Ia), (Ib), (Ic), (Id), (Ie), (If) oder (Ig):
worin X, Y, R₁ , R₂ , m und p wie in Anspruch 1 definiert sind;

R₄ eine Gruppe -CHR_4aR4_b oder eine Gruppe -CH₂-CHR_4aR_4b darstellt, wobei R_4a eine Gruppe ist, ausgewählt aus: und R_4b eine Gruppe -(CH₂)_j-NR_4b'R_4b" darstellt, wobei j 0, 1, 2 oder 3 ist und R_4b' und R_4b" unabhängig voneinander ein Wasserstoffatom; ein verzweigter oder unverzweigter C_1-6-Alkylrest; eine Benzylgruppe; oder eine Phenethylgruppe sind;

R₅ und R₆ unabhängig voneinander ein Wasserstoffatom oder ein verzweigter oder unverzweigter C_1-6-Alkylrest sind;

R₇ eine Gruppe -(CH₂)_p-NR_7aR_7b ist, wobei p 0, 1, 2 oder 3 ist und wobei R_7a und R_7b unabhängig voneinander ein Wasserstoffatom; einen verzweigten oder unverzweigten C_1-6-Alkylrest; eine Benzylgruppe, die gegebenenfalls durch ein Halogen substituiert ist; eine Phenethylgruppe; ein -(CH₂)-Cyclopropyl; eine Pyridinylmethylgruppe darstellen; oder

R_7a und R_7b zusammen mit dem brückenbildenden Stickstoff eine der folgenden Strukturen bilden:

R₈ eine Phenethylgruppe ist; und

R_a eine Phenylgruppe ist, die gegebenenfalls mit -OH-Gruppe substituiert ist.
Verbindung nach Anspruch 8, die aus der folgenden Gruppe ausgewählt ist:
[148] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[149] (R)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[150] (S)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)-phenyl)-6, 7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[151] 9-Methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[152] (R)-9-Methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[153] (S)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[154] 2-(Ethylamino)-9-methyl-6-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[156] 6-(3-(2-Amino-1-phenylethoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[159] 2-(Ethylamino)-9-methyl-6-(4-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[160] 2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[161] (R)-2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)-methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[162] (S)-2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)-methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[163] 9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[164] (R)-9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[165] (S)-9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[166] 2-(Ethylamino)-9-methyl-6-(3-((2-(methylamino)-2-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[167] 9-Methyl-6-(3-((2-(methylamino)-2-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[169] 6-(3-(3-(Benzylamino)propoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[173] 2-(Ethylamino)-9-methyl-6-(3-(2-methyl-1-(methylamino)propan-2-yl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[176] 2-(Ethylamino)-9-methyl-6-(3-(((4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[179] 9-Methyl-2-(methylthio)-6-(3-(((4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[182] 6-(3-(4-((Benzylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[183] 2-(Ethylamino)-9-methyl-6-(3-(4-(2-(methylamino)ethyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[193] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(pyridin-2-yl)propoxy)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[194] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(pyridin-3-yl)propoxy)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[195] (R)-2-Amino-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[196] (R)-2-(Dimethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[197] (R)-9-Methyl-2-(methylamino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[198] 8-(Ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[199] 8-(Ethylamino)-1-methyl-4-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[201] 2-(Ethylamino)-9-methyl-6-(4-(2-(methylamino)-1-phenylethoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[203] (R)-N-Ethyl-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-2-amin;

[204] (R)-2-Methoxy-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[205] (R)-2-Hydroxy-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[206] (R)-2,9-Dimethyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[207] (R)-9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[208] 9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[209] (R)-9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)-phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[210] (S)-9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)-phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[211] 2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[212] (R)-2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)-propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[213] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[214] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[215] (R)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[216] (S)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[217] 9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[218] (R)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[219] (S)-9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[220] 2-(Ethylamino)-6-(3-(3-((2-fluorethyl)amino)-1-(thiophen-2-yl)propoxy)-phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[221] 2-Methoxy-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)-methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[222] 2-Hydroxy-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)-methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[223] 2,9-Dimethyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[224] 9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[225] 2-(Ethylamino)-9-methyl-6-(3-((2-(methylamino)-1-phenylethoxy) methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[226] 9-Methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[227] 8-(Ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[229] 8-(Dimethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[230] 2-(Dimethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[231] 2,9-Dimethyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[232] 9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[236] (R)-6-(3-((3-(Dimethylamino)-1-phenylpropoxy)methyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[237] (S)-6-(3-((3-(Dimethylamino)-1-phenylpropoxy)methyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[238] 6-(3-(3-(Dimethylamino)-1-phenylpropoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[239] 6-(3-(2-(Dimethylamino)-1-phenylethoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[240] 6-(3-(3-(Benzyl(methyl)amino)propyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[241] 6-(3-(3-(Dimethylamino)propyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[242] 6-(3-(4-((Dimethylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[243] 6-(3-(4-((Benzyl(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[244] 2-(Ethylamino)-9-methyl-6-(3-(4-((methyl(phenethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[246] 6-(3-(4-(((Cyclopropylmethyl)(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[251] 6-(3-(4-((Benzyl(methyl)amino)methyl)-1H-pyrazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[252] 2-(Ethylamino)-9-methyl-6-(3-(4-((methyl(phenethyl)amino)methyl)-1H-pyrazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[253] 6-(3-(4-((Benzyl(methyl)amino)methyl)-1H-imidazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[254] 2-(Ethylamino)-9-methyl-6-(3-(4-((methyl(phenethyl)amino)methyl)-1H-imidazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[256] 6-(3-(3-(Benzyl(methyl)amino)propoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[261] 2-(Ethylamino)-9-methyl-6-(3-(1-phenethylpiperidin-4-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrim ido[4,5-e][1,4]diazepin-5-on;

[264] 6-(3-(2-(Benzyl(methyl)amino)ethoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[265] 2-(Ethylamino)-9-methyl-6-(3-(2-(methyl(phenethyl)amino)ethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[271] 9-Methyl-6-(3-(((1-methyl-4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[272] 2-(Ethylamino)-9-methyl-6-(3-(((1-methyl-4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[275] 2-(Ethylamino)-6-(3-(2-(4-(3-hydroxyphenyl)piperidin-1-yl)ethyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[278] 2-(Ethylamino)-9-methyl-6-(3-(4-((4-phenylpiperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[279] 2-(Ethylamino)-6-(3-(4-((4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[281] 2-(Ethylamino)-9-methyl-6-(3-(4-(piperidin-1-ylmethyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[285] 6-(3-(4-(((Cyclopropylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[287] 2-(Ethylamino)-6-(3-(4-(((4-fluorbenzyl)(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[288] 2-(Ethylamino)-9-methyl-6-(3-(4-((methyl(pyridin-2-ylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6575&9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[289] 2-(Ethylamino)-9-methyl-6-(3-(4-((Methyl(pyridin-3-ylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6575&9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[304] (S)-8-Amino-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[305] (S)-8-Am ino-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[307] 1,8-Dimethyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[308] (S)-1,8-Dimethyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[315] 9-Methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[316] 9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[321] 9-Methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[322] 9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(trifluormethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[323] 1-Methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[325] (S)-8-(Ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[326] (S)-1-Methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[327] (R)-1-Methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[328] 9-Methyl-6-(4-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[329] 9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(trifluormethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[330] 9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(trifluormethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[331] (S)-8-Methoxy-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[333] 2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9 tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[334] 2-(Ethylamino)-9-methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[335] 2-(Benzylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[336] 9-Methyl-2-(methyl(pyridin-2-ylmethyl)amino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[340] 2-(Ethylamino)-9-methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[341] (R)-9-Methyl-2-(methyl(pyridin-2-ylmethyl)amino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[342] (R)-9-Methyl-2-(methyl(pyridin-3-ylmethyl)amino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[343] (R)-9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-((pyridin-2-ylmethyl)amino)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[344] (R)-2-(((5-Fluorpyridin-2-yl)methyl)(methyl)amino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on

[347] (R)-2-Amino-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[348] 2-(Ethylamino)-9-methyl-6-(4-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[349] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-3-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[350] (R)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-3-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[351] (S)-2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-3-yl)-propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[352] (S)-2-Amino-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[353] 2,9-Dimethyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[354] 2-Ethyl-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[355] 2,9-Dimethyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[356] (R)-2-Ethyl-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)-phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[357] (R)-2,9-Dimethyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[358] (S)-2,9-Dimethyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[360] (R)-2,9-Dimethyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[364] (S)-9-Methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[366] 9-Methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[367] 9-Methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[368] 9-Methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[369] 9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[372] 9-Methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[374] 9-Methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[375] (S)-2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[378] 9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[379] (S)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[380] (R)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[381] 1-Methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[382] (S)-1-Methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[383] (S)-8-(Ethylamino)-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[43e][1,4]diazepin-5-on;

[384] (S)-8-(Dimethylamino)-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[43e][1,4]diazepin-5-on;

[385] (S)-8-Methoxy-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[386] (S)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(trifluormethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[387] 2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-3-yl)propoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[388] 2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(3-methylthiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[389] (S)-1-Ethyl-8-methoxy-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[391] (S)-1-Ethyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[392] 2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(5-methylthiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[394] (S)-6-(3-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[395] S)-9-Ethyl-2-methoxy-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[396] 2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(4-methylthiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[397] (S)-2-Methoxy-9-methyl-6-(2-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[398] (S)-9-Ethyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[399] (S)-9-Fluor-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[400] (S)-9-Chlor-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-on;

[401] (S)-6-(2-Fluor-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[402] (S)-2-Methoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[405] 2-(Ethylamino)-9-methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[406] 2-(Ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[408] 2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[411] 2-(Ethylamino)-9-methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[413] 2-(Ethylamino)-9-methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[414] (S)-2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[415] (R)-2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[416] 2 -(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[417] (S)-2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[418] (R)-2-(Ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)-propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[419] (S)-2-(Dimethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[420] (S)-2-Amino-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)-benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[422] 2,9-Dimethyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[423] 2,9-Dimethyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[425] 2,9-Dimethyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrim ido[4,5-e][1,4]diazepin-5-on;

[426] 2-Ethyl-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[427] (R)-2,9-Dimethyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[428] (S)-2,9-Dimethyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[430] 9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[433] (S)-9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrim ido[4,5-e][1,4]diazepin-5-on;

[434] (R)-9-Methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrim ido[4,5-e][1,4]diazepin-5-on;

[435] 9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[436] (S)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on;

[437] (R)-9-Methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on und

[442] 6-(3-(5-((4-(Dimethylamino)-4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1,3,4-oxadiazol-2-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-on.
Verfahren zur Herstellung einer Verbindung der allgemeinen Formel (I') umfassend die Reaktion zwischen einer Verbindung der Formel (VII) oder Formel (IV): und einer Verbindung der Formel (VIII): wobei R₁ , R₂ , R₃, X und Y wie in Anspruch 1 definiert sind, m 0 ist und Z eine geeignete Abgangsgruppe ist.
Verfahren zur Herstellung einer Verbindung der allgemeinen Formel (I"): umfassend die Reaktion zwischen einer Verbindung der Formel (IV): und einer Verbindung der Formel (VIII): wobei R₁ , R₂ , R₃ und X wie in Anspruch 1 definiert sind, m 1 oder 2 darstellt und Z eine geeignete Abgangsgruppe darstellt.
Verfahren zur Herstellung einer Verbindung der allgemeinen Formel (I"'): umfassend die Reaktion zwischen einer Verbindung der Formel (VII): und entweder:
a) einer Verbindung der Formel (IX): oder

b) einer Verbindung der Formel (VIII): wobei R₁ , R₂ , R₃ und X wie in Anspruch 1 definiert sind, m 1 oder 2 ist und Z eine geeignete Abgangsgruppe ist.
Verbindung nach einem der Ansprüche 1 bis 10 zur Verwendung als Medikament.
Verbindung nach einem der Ansprüche 1 bis 10 zur Verwendung bei der Behandlung und/oder Prophylaxe von Schmerzen, einschließlich neuropathischer Schmerzen, entzündlicher Schmerzen und chronischer Schmerzen oder anderer Schmerzzustände, die Allodynie und/oder Hyperalgesie, Depression, Angst und Aufmerksamkeitsdefizit-/Hyperaktivitätsstörung (ADHS) betreffen.
Pharmazeutische Zusammensetzung, umfassend eine Verbindung (I) nach einem der Ansprüche 1 bis 10 oder ein pharmazeutisch annehmbares Salz, Stereoisomer oder Solvat davon und mindestens einen pharmazeutisch akzeptablen Träger, Additiv, Adjuvans oder Trägersubstanz.