发明名称 4-phenylamino-pyrimidine derivatives having protein kinase inhibitor activity
摘要 The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1 is halogen, vinylene-aryl, substituted aryl, heteroaryl or a benzo[1,3]dioxolil group,W is a group of formula —NH—SO2—R2 or heteroaryl group or NHR3 group where R3 is hydrogen or heteroaryl; and n is 1, 2, 3 or 4.;Furthermore, the present invention is directed to pharmaceutical composition containing at least one compound of general formula (I) and/or pharmaceutically acceptable salts or solvates thereof and for the use of them for the preparation of pharmaceutical compositions for the prophylaxis and/or the treatment of protein kinase related, especially CDK9-related diseases e.g. cell proliferative disease, infectious disease, pain, cardiovascular disease and inflammation.
申请公布号 US9040529(B2) 申请公布日期 2015.05.26
申请号 US201013517120 申请日期 2010.12.17
申请人 Vichem Chemie Kutató Kft. 发明人 Greff Zoltán;Varga Zoltán;Kéri György;Németh Gábor;Örfi László;Szántai Kis Csaba
分类号 A61K31/5377;C07D239/42;C07D401/04;C07D403/04;C07D403/14;C07D409/14 主分类号 A61K31/5377
代理机构 代理人 Voight Jason D.
主权项 1. A compound of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1 is halogen; vinylene-aryl;aryl, which is substituted with one or more substituent selected from the following group: alkoxy which is optionally substituted with one or more halogen or with aryl which is optionally substituted with one or more halogen, alkyl or alkoxy,halogen,alkyl which is optionally subsituted with one or more halogen or alkoxy,alkylaryloxy which is optionally substituted with alkoxy which is optionally substituted with one or more halogen,aminocarbonyl,amino, which is optionally substituted with one or two alkyl;alkylthio,alkylsulfinyl or alkylsulfonyl,aryloxy,hydroxyl; group of formula (a) wherein m is 1, 2 or 3 and R′ is hydrogen, halogen, alkyl or alkoxy; heteroaryl; W is a group of formula (b) wherein R2 stands for alkyl, alkoxy or aryl, which groups are optionally substituted with one or more halogen,heteroaryl,benzyl, which is optionally substituted with one or more halogen, alkyl or alkoxy,amino, which is optionally substituted with one or two alkyl;heteroaryl group, which is optionally substituted with a (CH2)k-heterocycloalkyl group, where k is 0, 1, 2 or 3;NH—R3, wherein R3 is hydrogen, alkyl, alkoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aminoalkyl, aminoaryl or aminoheteroaryl, or R3 is —CO-aryl, —CO—NH-aryl where the aryl is optionally substituted with one or more halogen; and n is 1, 2, 3 or 4.
地址 Budapest HU