发明名称 Amino-quinolines as kinase inhibitors
摘要 Disclosed are compounds having the formula:;wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
申请公布号 US9604963(B2) 申请公布日期 2017.03.28
申请号 US201214002147 申请日期 2012.03.02
申请人 GlaxoSmithKline Intellectual Property Development Limited 发明人 Bury Michael Jonathan;Casillas Linda N.;Charnley Adam Kenneth;Haile Pamela A.;Marquis, Jr. Robert W.;Mehlmann John F.;Romano Joseph J.;Singhaus, Jr. Robert R.;Wang Gren Z.
分类号 C07D405/12;C07D401/12;A61K31/4709;C07D405/14;C07D417/12;C07D215/44;C07D417/14;C07D471/04 主分类号 C07D405/12
代理机构 代理人 Lutomski Kathryn A.;Gimmi Edward R.;Majarian William R.
主权项 1. A compound according to Formula (I): wherein: R1is H, —SO2(C1-C4alkyl), —CO(C1-C4alkyl), or (C1-C4alkyl); R2 is —SORa or —SO2Ra, wherein Ra is an optionally substituted (C1-C6)alkyl, (C3-C7)cycloalkyl, 4-7membered heterocycloalkyl, aryl, or heteroaryl group, wherein: said (C1-C6)alkyl is optionally substituted by one or two groups each independently selected from the group consisting of cyano, hydroxyl, (C1—C6)alkoxy, (C1-C6)alkoxy(C2-C6)alkoxy, —CO2H, —CO2(C1-C4)alkyl, —SO2(C1-C4 alkyl), —CONH2, —CONH(C1-C4 alkyl), —CON(C1-C4 alkyl)(C1-C4 alkyl), —SO2NH2, —SO2NH(C1-C4 alkyl), —SO2N(C1-C4 alkyl)(C1-C4 alkyl), amino, (C1-C4 alkyl)amino-, (C1-C4 alkyl)(C1-C4 alkyl)amino-, C3-C7cycloalkyl, phenyl, 5-6membered heteroaryl, 9-10membered heteroaryl, 4-7membered heterocycloalkyl and (phenyl)(C1-C4 alkyl)amino-, wherein said C3-C7cycloalkyl, phenyl, (phenyl)(C1-C4 alkyl)amino-, 5-6membered heteroaryl, 9-10membered heteroaryl or 4-7membered heterocycloalkyl is optionally substituted by 1-3groups each independently selected from the group consisting of halogen, —CF3, (C1-C4)alkyl, hydroxy(C1-C4)alkyl and (C1-C4)alkoxy, said (C3-C7)cycloalkyl or 4-7membered heterocycloalkyl is optionally substituted by 1-3groups each independently selected from the group consisting of halogen, —CF3, hydroxyl, 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 the group consisting of halogen, —CF3, hydroxyl, amino, (C1-C4)alkyl, phenyl(C1-C4)alkyl-, hydroxy(C1-C4)alkyl- and (C1-C4)alkoxy, and wherein said heteroaryl is a 5-6 membered heteroaryl or a 9-10 membered heteroaryl, and any of said 4-7 membered heterocycloalkyl contains one heteroatom selected from the group consisting of N, O and S, any of said 5-6 membered heteroaryl contains one heteroatom selected from the group consisting of N, O and S and optionally further containing one or two nitrogen atoms, and any of said 9-10 membered heteroaryl contains one heteroatom selected from the group consisting of N, O and S and optionally further containing 1, 2 or 3 nitrogen atoms; R3 is halogen, hydroxy, (C1-C4)alkoxy-, halo(C1-C4)alkyl-, halo(C1-C4)alkoxy-, (C1-C4)alkoxy(C1-C6)alkyl-, halo(C1-C4)alkoxy(C1-C6)alkyl-, (C1-C4)alkoxy(C2-C6)alkoxy-, halo(C1-C4)alkoxy(C2-C6)alkoxy-, hydroxy(C1-C4)alkyl-, hydroxy(C2-C6)alkoxy-, cyano(C1-C4)alkyl-, cyano(C2-C6)alkoxy-, or (C3-C6)cycloalkoxy-, wherein the halo(C1-C4)alkyl-, halo(C1-C4)alkoxy-, halo(C1-C4)alkoxy(C1-C6)alkyl-, or halo(C1-C4)alkoxy(C2-C6)alkoxy- contains 2 or 3 halo atoms and wherein the (C3-C6)cycloalkyl moiety of the (C3-C6)cycloalkoxy- group, is optionally substituted by a group selected from the group consisting of cyano, halo, hydroxyl, (C1-C6)alkoxy and (C1-C4)alkoxy(C2-C6)alkoxy; Z is pyrazolyl, having the formula:  wherein: R12 is methyl or trifluoromethyl; R13 is H, methyl, or trifluoromethyl; R14 is H or (C1-C3)alkyl; or R12 and R13, taken together with the atoms to which they are attached, form a 6membered carbocyclic ring or heterocyclic ring substituted by R15 and R16, wherein the heterocyclic ring contains 1 nitrogen atom; wherein R15 and R16 are each independently selected from the group consisting of H, halogen, cyano, (C1-C4)alkyl, halo(C1-C4)alkyl, (C1-C4)alkoxy, phenoxy, phenyl(C1-C4)alkoxy, hydroxyl, hydroxy(C1-C4)alkyl-, and aminocarbonyl, wherein the phenyl moiety of said phenoxy or phenyl(C1-C4)alkoxy is optionally substituted by 1-3 substituents each independently selected from the group consisting of halogen, —CF3, (C1-C4)alkyl and (C1-C4)alkoxy; or a salt thereof.
地址 Brentford, Middlesex GB
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