发明名称 Type II Raf kinase inhibitors
摘要 The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
申请公布号 US9180127(B2) 申请公布日期 2015.11.10
申请号 US201013519826 申请日期 2010.12.29
申请人 Dana-Farber Cancer Institute, Inc. 发明人 Gray Nathanael S.;Choi Hwan G.;Deng Xianming;Zhang Jianming
分类号 C07D471/02;C07D405/00;A61K31/44;A61K31/496;C07D487/04;C07D471/04 主分类号 C07D471/02
代理机构 Wolf, Greenfield & Sacks, P.C. 代理人 Wolf, Greenfield & Sacks, P.C.
主权项 1. A compound of formula I: or a pharmaceutically acceptable salt, ester, or prodrug thereof, wherein, ring D is aryl or heteroaryl; R is halo, or -A-B; A is NRAC(O), O, S(O)m, C(O), C(O)O, C(O)NRA, NRAC(O)NRA, or absent; B is alkyl, cycloalkyl, or aryl, each of which is optionally substituted; R1 is hydroxyl, alkyl, alkoxy, C(O)ORA, C(O)NRARB, or NRARB, each of which may be is optionally substituted, or halo; R′ is absent, or R and R′ together with the atoms to which each is attached, form a cycloalkyl, heterocycloalkyl, aryl, or heteroaryl ring, each of which is optionally substituted; Z is NRA, O, CR3R4 or S(O)m; R3 is H or alkyl; R4 is H, alkyl, or absent; ring E is 1H-pyrrolo[2,3-b]pyridine; RZ is NRAR2; R2 is H, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, C(O)RA, C(O)ORA, C(O)NRARB, C(NRB)RA, or C(NRB)ORA; R5 is H, halo, alkyl, alkoxy, or thioalkoxy; R6 is H, NRARB, or ORA; each RA is independently H, alkyl, alkenyl, cycloalkyl, heterocyclic, aryl or heteroaryl, each of which is optionally substituted; each RB is independently H, alkyl, alkenyl, cycloalkyl, heterocyclic, aryl or heteroaryl, each of which is optionally substituted; or, for each occurrence of NRARB, RA and RB are taken together with the nitrogen atom to which they are attached to form a 3-7 membered heterocycloalkyl ring; each m is independently 0, 1, or 2; and each n is independently 0 or 1.
地址 Boston MA US