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AR054047A1 - Derivados de fenilquinazolina - Google Patents

Derivados de fenilquinazolina

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Publication number
AR054047A1
AR054047A1 ARP060102035A ARP060102035A AR054047A1 AR 054047 A1 AR054047 A1 AR 054047A1 AR P060102035 A ARP060102035 A AR P060102035A AR P060102035 A ARP060102035 A AR P060102035A AR 054047 A1 AR054047 A1 AR 054047A1
Authority
AR
Argentina
Prior art keywords
hal
atoms
nhcoa
mono
so2naa
Prior art date
Application number
ARP060102035A
Other languages
English (en)
Inventor
Hans-Michael Eggenweiler
Michael Wolf
Hans-Peter Buchstaller
Original Assignee
Merck Patent Gmbh
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Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR054047A1 publication Critical patent/AR054047A1/es

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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • C—CHEMISTRY; METALLURGY
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    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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Abstract

Nuevos derivados de fenilquinazolinas de la formula (1) en donde R1 es Hal, OH; OA, SH, SA, H o A, R2 y R3 son en cada caso, de modo independiente entre sí, -O-(X)s-Q,-S-(X)s-Q, -NHCO- (X) s -Q, -CONH- (X)s -Q, -CONA-(X)s-Q, NH(CO)NH-(X)s-Q, - NH(CO)O-(X)s-Q, -NHSO2-(X)s-Q, -SO2NH-(X)s-Q, -SO2NA-(X)s-Q, NHCOA, Hal, Het o H, en donde, en el caso de que R2 = H, entonces R3 es distinto H, o en caso de que R3 = H, entonces R2 es distinto de H, R4, R5 son en cada caso, de modo independiente entre sí, H, Hal, CN, NO2, A, OH, OA, SH, SA, (CH2)nCOOH, (CH2)nCOOA, O(CH2)0CONH2, CONHA, CONNA', NH2, NHA, NAA', NHCOOA, NHCO(CH2)nNH2, NHCONHA, SOA, SO2A; SO2NH2, SO2NHA, SO2NAA' u O(CH2)0Het1, dos radicales adyacentes, seleccionados del grupo R1, R2, R3, también son juntos metilendioxi o etilendioxi, A, A' son en cada caso, de modo independiente entre sí alquilo no ramificado o ramificado con 1-10 átomos de C, en donde 1-5 átomos de H pueden estar reemplazados por F, Cl y/o Br, Alk o alquilo cíclico con 3-7 átomos de C, A y A' también son juntos una cadena alquileno con 2, 3, 4, 5 o 6 átomos de C, en donde uno o dos grupos CH2, pueden estar reemplazados por O, S, SO, SO2; NH, NA y/o N-COOA, Alk es alquenilo con 2-6 átomos de C, X es alquileno C1-10 o alquenileno C2-C10 no ramificado o ramificado no sustituido o mono-, di-, tri - tetrasustituido con A, OA, OH, SH, SA, Hal, NO2, CN, Ar, O ar, COOH, COOA, CHO, C(=O)A, C(=O)Ar, SO2A, CONH2, SO2NH2, CONHA, XONNA', SO2NHA, SO2NAA?,NH2, NHA, NAA'OCONH2, OCONHA, OCONAA', NHCOA, NHCOOA, NACOOA, NHSO2OA, NASO2OA, NHCONH2, NACONH2, NHCONH2, NHCONHA, NACONHA; NHCONAA', NACONAA', y/u =O, en donde también uno, dos o tres grupos C pueden estar reemplazados por O, S, SO, SO2, NCO, NACO, CONH, CONA, SO2NH, SO2NA, NHSO2, NASO2 y/o por grupos NH, Q es H, Carb, Ar o Het, Carb es cicloalquilo con 3-7 átomos de C o cicloalquenilo con 3-7 átomos de C no sustituido o mono-, di, tri-, tetra- o pentasustituido con A, OA, OH, SH, SA, Hal, NO2; CN, (CH2)nAr', (CH2)nCOOH, (CH2)nCOOA, CHO, COA, SO2A, CONH2, SO2NH2, CONHA, CONAA', SO2NHA, SO2NAA', NH2, NHA, NAA', OCONH2, OCONHA, OCONAA', NHCOA, NHCOOA, NACOOA, NHSO2OA, NASO2OA, NHCONH, NACONH2, NHCONHA, NACONHA, NHCONAA' y/o NACONAA', Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con A, OA, OH, SH, SA, Hal, NO2, CN (CH2)nAr', (CH2)nCOOA, CHO, COA, SO2A, CONH2, SO2NH2, CONHA, CONAA', SO2NHA, SO2NAA', NH2, NHA, NAA', OCoN2; OCONHA, OCONAA', NHCOA, NHCOA, NHCOOA, NACOOA, NHSO2OA, NASO2OA, NHCONH2, NACONH2, NHCONHA; NACONHA, NHCONAA', NACONAA', y/o tetraazol, Ar' es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con A, OA, OH, SH, SA, Hal, NO2, CH, (CH2)n fenilo, (CH2)nCOOH, (CH2)nCOOA, CHO, COA, SO2A, CONH2, SO2NH2, CONHA, CONAA', SO2NHA, SO2NAA', NH2, NHA, NAA', OCONH2, OCONHA, OCONAA', NHCOA, NACOOA, NHSO2OA, NASO2OA, NHCONH2, NACONH2, NHCONHA, NACONHA, NHCONAA' y/o NACONAA', Het es un heterociclo mono-, o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar mono-, di o trisustituido con A, OA, OH, SH,SA, Hal, NO2, CN, (CH2)nAr', (CH2)nCOOH, (CH2)nCOOA, CHO, COA, SO2A, CONH2, SO2nH2, CONHA, CONNA', SO2NHA, SO2NAA', NH2, NHA, NAA', OCONH2, OCONHA, OCONAA, NHCOA, NHCOOA, NACOOA, NHSO2OA, NASO2OA, NHCONH2, NACONH2, NHCONHA, NACONHA, NHCONAA', NACONAA', SO2A, =S, =NH, =NA y/u =O (oxígeno del carbonilo),,Het1 un heterociclo monocíclico saturado, insaturado o aromático con 1 a 2 átomos de N y/u O, que puede estar mono- o disustituido con A, OA, OH, Hal y/u =O (oxígeno el carbonilo), Hal es F Cl, Br, o I, n es 0, 1, 2, 3, o 4, o es 1, 2, o 3, s es 0, 1 o 2, así como sus derivados, sales, ,solvatos, tautomeros y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de HSP90 y pueden ser utilizados para preparar un medicamento para el tratamiento de enfermedades en las que la inhibicion, la regulacion y/o la modulacion de la HSP90 desempana un papel importante
ARP060102035A 2005-05-19 2006-05-19 Derivados de fenilquinazolina AR054047A1 (es)

Applications Claiming Priority (1)

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DE102005022977A DE102005022977A1 (de) 2005-05-19 2005-05-19 Phenylchinazolinderivate

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AR054047A1 true AR054047A1 (es) 2007-05-30

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US (1) US7947696B2 (es)
EP (1) EP1881965A1 (es)
JP (1) JP5075117B2 (es)
KR (1) KR20080016651A (es)
CN (1) CN101180278B (es)
AR (1) AR054047A1 (es)
AU (1) AU2006246744B2 (es)
BR (1) BRPI0610134A2 (es)
CA (1) CA2608766A1 (es)
DE (1) DE102005022977A1 (es)
MX (1) MX2007014264A (es)
RU (1) RU2421449C2 (es)
WO (1) WO2006122631A1 (es)
ZA (1) ZA200710966B (es)

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CA2608766A1 (en) 2006-11-23
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WO2006122631A1 (de) 2006-11-23
AU2006246744B2 (en) 2011-11-03
DE102005022977A1 (de) 2006-12-07
CN101180278B (zh) 2011-05-04
JP2008540587A (ja) 2008-11-20
RU2421449C2 (ru) 2011-06-20
ZA200710966B (en) 2008-12-31
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RU2007146388A (ru) 2009-06-27
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