发明名称 AMINOHETEROARYL BENZAMIDES AS KINASE INHIBITORS
摘要 The present invention provides a compound of Formula (I) or a salt thereof;;;and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
申请公布号 US2015126490(A1) 申请公布日期 2015.05.07
申请号 US201414527328 申请日期 2014.10.29
申请人 BAGDANOFF Jeffrey T.;DING Yu;HAN Wooseok;HUANG Zilin;JIANG Qun;JIN Jeff Xianming;KOU Xiang;LEE Patrick;LINDVALL Mika;MIN Zhongcheng;PAN Yue;PECCHI Sabina;PFISTER Keith Bruce;POON Daniel;RAUNIYAR Vivek;WANG Xiaojing Michael;ZHANG Qiong;ZHOU Jianguang;ZHU Shejin 发明人 BAGDANOFF Jeffrey T.;DING Yu;HAN Wooseok;HUANG Zilin;JIANG Qun;JIN Jeff Xianming;KOU Xiang;LEE Patrick;LINDVALL Mika;MIN Zhongcheng;PAN Yue;PECCHI Sabina;PFISTER Keith Bruce;POON Daniel;RAUNIYAR Vivek;WANG Xiaojing Michael;ZHANG Qiong;ZHOU Jianguang;ZHU Shejin
分类号 C07D498/04;A61K31/497;A61K45/06;C07D401/04;A61K31/4545;C07D405/14;A61K31/506;C07D409/04;A61K31/4436;A61K31/5383;C07D241/20;A61K31/4965;A61K31/4439;C07D413/14;A61K31/5377;A61K31/553;C07D405/04 主分类号 C07D498/04
代理机构 代理人
主权项 1. A compound of formula (I):or a pharmaceutically acceptable salt thereof, wherein: R1 is an optionally substituted group selected from C3-8 cycloalkyl, 5-8 membered heterocyclyl containing 1-2 heteroatoms selected from N, O and S as ring members, phenyl, —SO2-phenyl, —C(O)-phenyl, —C(R8)2-phenyl, and 5-6 membered heteroaryl ring, wherein said heterocyclyl and heteroaryl contain 1-2 heteroatoms selected from N, O and S as ring members, and wherein the optional substituents for R1 are 1-3 groups independently selected from D, halo, hydroxy, amino, —N(R8)2, CN, C1-4 alkyl, C1-4 alkoxy, —S(C1-4 alkyl), C1-4 haloalkyl, C1-4 haloalkoxy, C3-6 cycloalkyl, 3-6 membered heterocyclyl containing 1-2 heteroatoms selected from N, O and S, oxo (except on aromatic rings), CN, COOR8, CON(R8)2, —NR8—C(O)R8, —NR8—C(O)OR8—SO2R8, —NR8SO2R8, and SO2N(R8)2, where each R8 is independently H or C1-4 alkyl; L is a bond, or L is selected from C1-4 alkylene, C2-4 alkenylene, C1-4 alkynylene, C3-6 cycloalkyl or a 4-7 membered heterocycloyl containing 1-2 heteroatoms selected from N, O and S as ring members, wherein L is optionally substituted with 1-3 groups independently selected from R11, D, OH, NH2, —NHR11, —NHC(═O)R11, —NHC(═O)—OR11, —NHC(═O)—NH2, —NHC(═O)—NHR11, —N(R11)2, CN, halo, N3, CON(R7)2, and COOR7; where each R11 is independently C1-4 alkyl, which may be substituted with up to three groups independently selected from D, halo, OH, NH2,—NHMe, —NMe2, —OP(O)(OH)2 and O—C1-4 alkyl; X and Y are independently selected from H, D, halo, CN, amino, hydroxy, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, and C1-4 haloalkoxy; R2 is H, C1-4 alkyl, or aryl-C1-2-alkyl-, wherein the aryl and C1-4 alkyl are optionally substituted with halo, CN, C1-4 alkyl, C1-4 haloalkyl, C3-6 cycloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, or C1-4 alkylsulfonyl; or R2 can cyclize with X to form a 5-7 membered heterocyclic ring containing 1-2 heteroatoms selected from N, O and S fused to the phenyl ring to which X is attached,or R2 can cyclize with L to form a 5-7 membered heterocyclic ring containing 1-2 heteroatoms selected from N, O and S, wherein the optional heterocyclic ring formed by R2 cyclizing with X, or by R2 cyclizing with L, can be optionally substituted with one or two groups independently selected from CN, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, oxo, CN, COOR7, CON(R7)2, and —SO2R7; each R7 is independently H or C1-4 alkyl; Z is N or CR4; R4 is H, D, halo, C1-4 alkyl, C1-4 haloalkyl, or C1-4 alkoxy; R5 is selected from —C(O)—R5a and R5a; wherein R5a is an optionally substituted C3-8 cycloalkyl, C3-8 cycloalkenyl, saturated or unsaturated 3-8 membered heterocyclic ring containing 1-2 heteroatoms selected from N, O and S, phenyl, or 5-6 membered heteroaryl ring containing 1-3 heteroatoms selected from N, O and S, wherein the optional substituents for R5 are 1-4 groups independently selected from D, halo, hydroxy, amino, CN, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 hydroxyalkyl, C1-4 haloalkoxy, C3-6 cycloalkyl, 3-6 membered heterocyclyl containing 1-2 heteroatoms selected from N, O and S, oxo (except on aromatic rings), CN, —COOR9, —C(O)R9, CON(R9)2, —NR9C(O)R9, —NR9CO2R9, —SO2R9, —NR9SO2R9, and —SO2N(R9)2, where each R9 is independently H or C1-4 alkyl optionally substituted with 1-3 groups independently selected from D, halo, OH, NH2, NHMe and NMe2; and two substituents on the same or adjacent carbon atoms of R5 can optionally be taken together to form a 5-6 membered ring that can be saturated or aromatic and contains 1-2 heteroatoms selected from N, O and S and can optionally be substituted with 1-2 groups independently selected from D, Me, halo, OH, oxo, O(C1-4 alkyl), NH2, C1-4 alkylamino, alkyl)amino; and R6 is H, D, halo, C1-4 alkyl, or C1-4 haloalkyl.
地址 North Reading MA US