发明名称 PYRAZOLO[1,5-A]PYRIDINE DERIVATIVES AND METHODS OF THEIR USE
摘要 The invention is directed to pyrazolo[1,5-a]pyridine derivatives and their use as AXL and c-MET kinase inhibitors.
申请公布号 US2016318929(A1) 申请公布日期 2016.11.03
申请号 US201415108400 申请日期 2014.12.18
申请人 CEPHALON, INC. 发明人 Hudkins Robert L;Zulli Allison L.
分类号 C07D471/04 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound of Formula I: wherein R1 is H; halo; —C1-6alkyl; —C1-6alkoxy; optionally substituted pyridyl; optionally substituted pyrimidinyl; optionally substituted pyrazinyl; optionally substituted pyrazolyl; optionally substituted imidazolyl; optionally substituted isoxazolyl; optionally substituted oxazolyl; optionally substituted thiazolyl; optionally substituted isothiazolyl; optionally substituted morpholinyl; optionally substituted piperazinyl, optionally substituted piperidinyl; optionally substituted tetrahydropyranyl; optionally substituted pyrrolidinyl; tetrahydrothiopyranyl 1,1-dioxide; thiomorpholinyl 1,1-dioxide; pyrrolidinyl-one; piperidinyl-one; optionally substituted —NH-aryl; optionally substituted —NH-pyridyl; optionally substituted —NH-pyrimidinyl; —C(O)NHC1-6alkyl; —C(O)N(C1-6alkyl)2; —NHS(O)2C1-6alkyl; —N(C1-6alkyl)S(O)2C1-6alkyl; —NHC(O)C1-6alkyl; —NC1-6alkylC(O)C1-6alkyl; —NHC(O)OC1-6alkyl; —NC1-6alkylC(O)OC1-6alkyl; —NHC(O)NHC1-6alkyl; —NC1-6alkylC(O)N(C1-6alkyl)2; optionally substituted —NHC(O)-piperazinyl; or optionally substituted —NC1-6alkylC(O)-piperazinyl; each R2 is independently H, halo, —C1-6alkyl, —C1-6alkoxy, —OH, —O-alkaryl, or trihaloalkyl; R3 is H or halo; A is CR2 or N; B is CR2 or N; Q is —S(O)2aryl optionally substituted with halo or C1-6alkyl; pyridyl optionally substituted with halo or —C(O)NHphenyl; pyrimidinyl; pyrazinyl; —C(O)—NHC(O)-alkaryl optionally substituted with halo or C1-6alkyl; —C(S)—NHC(O)-alkaryl optionally substituted with halo or C1-6alkyl; —C(O)-alkaryl optionally substituted with halo or C1-6 alkyl; —C(O)NH-aryl optionally substituted with halo, C1-6alkyl or C1-6alkoxy; —C(O)—O-aryl optionally substituted with halo, C1-6alkyl or C1-6alkoxy; orwherein X is CR6, wherein R6 is H or C1-6alkyl; or N; R4 is H; C1-6alkoxy; halo; —OC1-6alkylene-O—C1-6alkyl; —NHC1-6alkyl; or —N(C1-6alkyl)2; R5 is aryl optionally substituted with halo or C1-6alkyl; or alkaryl optionally substituted with halo or C1-6alkyl;orwherein Y is C or N; R7 is H or C1-6alkyl; R8 is H; C1-6alkylene-O—C1-6alkyl; C1-6alkyl; C1-6alkylene-O—C1-6alkaryl; or C1-6alkylene-OH; R9 is H, C1-6alkyl; or halo;orwherein R10 is H; halo; or C1-6alkyl;orwherein R11 is H or C1-6alkyl; R12 is H; C1-6alkyl; or aryl optionally substituted with halo; R13 is H; C1-6alkyl; or trihaloC1-6alkyl;orwherein R14 is H; C1-6alkyl; or halo;or a pharmaceutically acceptable salt thereof.
地址 Frazer PA US