发明名称 ATX modulating agents
摘要 Compounds of formula (I) can modulate the activity of autotaxin (ATX).
申请公布号 US9555050(B2) 申请公布日期 2017.01.31
申请号 US201314417353 申请日期 2013.07.26
申请人 BIOGEN MA INC. 发明人 Guckian Kevin;Kumaravel Gnanasambandam;Ma Bin;Mi Sha;Shao Zhaohui;Sun Lihong;Taveras Arthur;Wang Deping;Xin Zhili;Zhang Lei
分类号 C07D215/20;A61K31/662;A61K45/06;C07D401/04;C07D401/06;C07C229/48;C07D265/30;C07D211/34;C07D211/62;C07D213/79;C07D223/06;C07C233/47;C07D205/04;C07D207/08;C07D207/16;C07C229/46;C07F9/38;A61K31/196;A61K31/397;A61K31/435;A61K31/445;A61K31/454;A61K31/47;A61K31/5375;A61K31/55;C07D213/80 主分类号 C07D215/20
代理机构 McCarter & English, LLP 代理人 McCarter & English, LLP ;Davis Steven G.;Zhang Xin
主权项 1. A compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein: X1, X2, and X3 are CH; or one of X1, X2, or X3 is N and the other two are CH; R1 is R2 is a C1-4haloalkyl or cyano; R3 is -L1-J-L2-R12; and R4 is hydrogen or a C1-6alkyl; or R3 and R4 together with the nitrogen to which they are attached are a 3- to 8-membered heterocyclyl which is substituted with -L2-R12, and is optionally substituted with a halo, hydroxyl, amino, or a C1-6alkyl; R5 is a halo, a C1-6alkyl or a C1-6haloalkyl; R6 and R7 are each independently hydrogen or C1-6alkyl; or R6 and R7 together with the carbon to which they are attached are —C(═O)—, a C3-8spirocycloalkyl, or a 3- to 8-membered spiroheterocyclalkyl; R8 and R9 are each independently hydrogen or a C1-6alkyl; or R8 and R9 taken together with the carbon to which they are attached are —C(═O)—; R10, for each occurrence, is halo; R11 is hydrogen, halo, or C1-4alkyl; R12 is —COOR13 or —P(O)(OR13)2; each R13, independently, is H, C1-4alkyl, aryl, or aryl-C1-4-alkyl; J is a C1-6alkylene, a C3-8cycloalkylene, a 3- to 8-membered divalent monocyclic heterocyclyl, a phenylene, or a 5- to 6-membered heteroarylene, wherein J is optionally substituted with one or two substituents independently selected from a halo and a C1-6alkyl; L1 and L2 are each independently, a C1-3alkylene or a direct bond; n is 1, 2 or 3; q is 1 or 2; and r is 0, 1, or 2.
地址 Cambridge MA US