发明名称 BENZO-FUSED HETEROCYCLIC DERIVATIVES USEFUL AS AGONISTS OF GPR120
摘要 The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
申请公布号 US2014275172(A1) 申请公布日期 2014.09.18
申请号 US201414200093 申请日期 2014.03.07
申请人 Janssen Pharmaceutica NV 发明人 Sui Zhihua;Subasinghe Nalin
分类号 C07D493/04;C07D307/80;C07D333/56;C07D307/81;C07D405/12;C07D277/64 主分类号 C07D493/04
代理机构 代理人
主权项 1. A compound of formula (I) whereinis selected from the group consisting of, R1 is selected from the group consisting of cyano, C1-6alkyl, -(hydroxy substituted C1-4alkyl), chloro substituted C1-4alkyl, fluoro substituted C1-4alkyl, C2-4alkenyl, chloro substituted C2-4alkenyl, fluoro substituted C2-4alkenyl, C2-4alkynyl, —(C1-4alkyl)-O—(C1-4alkyl), —(C1-4alkyl)-SO—(C1-4alkyl), —(C1-4alkyl)-SO2—(C1-4alkyl), —(C1-4alkyl)-NRARB, —(C1-4alkyl)-NRA—C(O)—(C1-4alkyl), —(C1-4alkyl)-NRA—SO2—(C1-4alkyl), —C(O)OH, —C(O)O—(C1-4alkyl), —C(O)—(C1-4alkyl), —C(O)—NRARB, C3-8cycloalkyl, —(C1-4alkyl)-(C3-8cycloalkyl), aryl and —(C1-2alkyl)-(aryl); wherein RA and RB are each independently selected from the group consisting of hydrogen and C1-4alkyl; R2 is selected from the group consisting of hydrogen, halogen and C1-4alkyl; R3 is selected from the group consisting of hydrogen, chloro and fluoro; R4 and R5 are each independently selected from the group consisting of hydrogen, halogen, cyano, C1-4alkyl, chloro substituted C1-4alkyl, fluoro substituted C1-4alkyl, C2-4alkenyl, chloro substituted C2-4alkenyl, fluoro substituted C2-4alkenyl, C2-4alkynyl, chloro substituted C2-4alkynyl, fluoro substituted C2-4alkynyl, C1-4alkoxy, fluoro substituted C1-4alkoxy, —O—(C1-4alkyl)-O—(C1-4alkyl), —(C1-4alkyl)-O—(C1-4alkyl), —(C1-4alkyl)-SO2—(C1-4alkyl), —(C2-4alkenyl)-SO2—(C1-4alkyl), —C(O)—NRCRD, —O-(aryl) and —O—(C1-2alkyl)-aryl; wherein RC and RD are each independently selected from the group consisting of hydrogen and C1-4alkyl; provided that at least one of R4 or R5 is selected from the group consisting of hydrogen, chloro and fluoro; alternatively, whereinR4 and R5 may be taken together with the carbon atoms to which they are bound to form a ring structure selected from the group consisting of W is selected from the group consisting of C(R9); wherein R9 is selected from the group consisting of hydrogen, fluoro and bromo; alternatively, whereinW may be N; R6 and R7 are each independently selected from the group consisting of hydrogen, halogen, cyano, C1-6alkyl, chloro substituted C1-4alkyl, fluoro substituted C1-4alkyl, bromo substituted C1-4alkyl, C1-4alkoxy and fluoro substituted C1-4alkoxy; alternatively, whereinand W is C(R9), R6 and R7 may be taken together with the carbon atoms to which they are bound to form R8 is selected from the group consisting of hydrogen, halogen, cyano, C1-6alkyl, chloro substituted C1-4alkyl, fluoro substituted C1-4alkyl, bromo substituted C1-4alkyl, C1-4alkoxy, fluoro substituted C1-4alkoxy and —(C1-4alkyl)-C(O)OH; R0 is selected from the group consisting of —CH2OH and —C(O)OH; or a pharmaceutically acceptable salt thereof.
地址 Beerse BE