发明名称 Substituted bicyclic amines for the treatment of diabetes
摘要 Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
申请公布号 US8759539(B2) 申请公布日期 2014.06.24
申请号 US200913125088 申请日期 2009.11.11
申请人 Merck Sharp & Dohme Corp. 发明人 He Jiafang;Bawiec John;Liu Weiguo;Liang Gui-Bai;Yang Lihu
分类号 C07D401/12;C07D401/14;C07D403/12;C07D403/14;C07D209/52;C07D413/12;C07D417/12;A61K31/403;A61K31/4184;A61K31/4192;A61K31/427;A61K31/4709;A61K31/4725;A61K31/423 主分类号 C07D401/12
代理机构 代理人 Fair Janet E.;Cocuzzo Anna L.
主权项 1. A compound of structural formula I:or a pharmaceutically acceptable salt thereof; wherein Ar is an aryl or heteroaryl, wherein the aryl or heteroaryl are optionally substituted with one or more substituents independently selected from the group consisting of: —OC1-10 alkyl,—OC3-6 cycloalkyl,—O-heteroaryl,—O-aryl,aryl,aryl substituted with one to three halogen,aryl substituted with one to three C1-10 alkyl,heteroaryl,heteroaryl substituted with one to three halogen,heteroaryl substituted with one to three C1-10 alkyl,halogen,—CO2H,—C1-10 alkoxycarbonyl,—CN,—CF3,NH2pyrrolidone,cycloheteroalkyl,C1-10 alkyl,C3-6 cycloalkyl, andC3-6 cycloalkyl substituted with one to three C1-10 alkyl; X is O, NH or OCH2; R1 is SO2H, CONHC1-10 alkyl, —C1-10 alkoxycarbonyl, aroyl, heteroaroyl, aryl, heteroaryl, cycloalkyl or cycloheteroalkyl wherein the CONHC1-10 alkyl, —C1-10 alkoxycarbonyl, aroyl, heteroaroyl, aryl, heteroaryl, cycloalkyl or cycloheteroalkyl are optionally substituted with one or more substituents independently selected from the group consisting of: —OH,—OC1-10 alkyl,—OC3-6 cycloalkyl,—O heteroaryl,—O aryl,aryl substituted with one to three halogen,aryl,aryl substituted with one to three C1-10 alkyl,heteroaryl,halogen,SO2C1-10 alkyl,SO2-aryl,SO2-aryl-C1-10 alkyl,—C(O)H,—C(O)C1-10 alkyl,—C(O)C3-6 cycloalkyl,—C(O) cycloalkyl,—C(O) heteroaryl,—C(O) aryl,—OC(O)H,—OC(O)C1-10 alkyl,—OC(O)C3-6 cycloalkyl,—OC(O) cycloalkyl,—OC(O) heteroaryl,—OC(O) aryl,—NH2,CONH—C1-10 alkyl-aryl,—CONH2,—CO2H,—C1-10 alkoxycarbonyl,—CO2C1-10 alkylaryl,—CN,—CF3,—OCF3,—OCHF2,cycloheteroalkyl,pyrrolidone,C1-10 alkyl-OH,C1-10 alkyl, andC3-6 cycloalkyl.
地址 Rahway NJ US