发明名称 QUINOLYL AMINES AS KINASE INHIBITORS
摘要 Disclosed are compounds having the formula:;wherein R1, R2, R3, R4 and R5 are as defined herein, and methods of making and using the same.
申请公布号 US2016060249(A1) 申请公布日期 2016.03.03
申请号 US201514933201 申请日期 2015.11.05
申请人 GlaxoSmithKline Intellectual Property Development Limited 发明人 CASILLAS Linda N.;Charnley Adam Kenneth;Haile Pamela A.;Hughes Terry Vincent;Marquis, JR. Robert W.;Mehlmann John F.;Reilly Michael;Romano Joseph J.;Singhaus, JR. Robert R.
分类号 C07D401/12;C07D405/14 主分类号 C07D401/12
代理机构 代理人
主权项 1. A compound according to Formula (I): wherein: R1 is H, —SO2(C1-C4)alkyl, —CO(C1-C4)alkyl, or (C1-C4)alkyl; R2 is —SRa, —SORa, or —SO2Ra, wherein Ra is (C1-C6)alkyl, halo(C1-C6)alkyl, (C3-C7)cycloalkyl, 4-7 membered heterocycloalkyl, aryl, or heteroaryl, wherein: said (C1-C6)alkyl is optionally substituted by one or two groups each independently selected from cyano, hydroxyl, (C1-C6)alkoxy, (C1-C6)alkoxy(C2-C6)alkoxy, —CO2H, —CO2(C1-C4)alkyl, —SO2(C1-C4)alkyl, (C3-C7)cycloalkyl, phenyl, 5-6 membered heteroaryl, 9-10 membered heteroaryl, 4-7 membered heterocycloalkyl and (phenyl)(C1-C4 alkyl)amino-, wherein said (C3-C7)cycloalkyl, phenyl, (phenyl)(C1-C4 alkyl)amino-, 5-6 membered heteroaryl, 9-10 membered heteroaryl or 4-7 membered heterocycloalkyl is optionally substituted by 1-3 groups each independently selected from halogen, —CF3, hydroxyl, amino, ((C1-C4)alkyl)amino-, ((C1-C4)alkyl)((C1-C4)alkyl)amino-, (C1-C4)alkyl, phenyl(C1-C4)alkyl-, hydroxy(C1-C4)alkyl and (C1-C4)alkoxy, said (C3-C7)cycloalkyl or 4-7 membered heterocycloalkyl is optionally substituted by 1-3 groups each independently selected from halogen, —CF3, hydroxyl, amino, ((C1-C4)alkyl)amino-, ((C1-C4)alkyl)((C1-C4)alkyl)amino-, (C1-C4)alkyl, phenyl(C1-C4)alkyl-, hydroxy(C1-C4)alkyl-, oxo and (C1-C4)alkoxy, and said aryl or heteroaryl is optionally substituted by 1-3 groups each independently selected from halogen, —CF3, hydroxyl, amino, ((C1-C4)alkyl)amino-, ((C1-C4)alkyl)((C1-C4)alkyl)amino-, (C1-C4)alkyl, phenyl(C1-C4)alkyl-, hydroxy(C1-C4)alkyl- and (C1-C4)alkoxy; R3 is methyl, hydroxymethyl, trifluoromethyl, carboxy, or —CO2(C1-C4)alkyl; R4 is H, methyl, hydroxymethyl, trifluoromethyl, carboxy, or —CO2(C1-C4)alkyl; R5 is H or (C1-C3)alkyl; or a salt thereof, or hydrate thereof.
地址 Brentford GB