发明名称 Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
摘要 The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.;
申请公布号 US9051329(B2) 申请公布日期 2015.06.09
申请号 US201214125116 申请日期 2012.07.02
申请人 Merck Sharp & Dohme Corp. 发明人 Wu Wen-Lian
分类号 A61K31/505;C07D491/00;C07D487/14;A61K31/519;A61K31/529 主分类号 A61K31/505
代理机构 代理人 Fair Janet E.;Fitch Catherine D.
主权项 1. A compound of structural formula I: or a pharmaceutically acceptable salts thereof; wherein R1 is selected from the group consisting of C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C10cycloalkyl, benzyl, heterocycle and C1-C6alkylheterocycle; wherein the C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C10cycloalkyl, benzyl, heterocycle and C1-C6alkylheterocycle are unsubstituted or substituted with 1-3 substituents each independently selected from R5;R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-C6 alkyl wherein the C1-C6 alkyl is unsubstituted or substituted with one or more substituents selected from R5; andR5 is selected from the group consisting of hydrogen, halogen, C1-C6alkyl, halogen-substitutedC1-C6alkyl, —OH, C1-C6alkylOH, halogen-substitutedC1-C6alkylOH, —OC1-C6alkyl, —Ohalogen-substitutedC1-C6alkyl, —COOH, —COOC1-C6alkyl, —C1-C6alkylCOOC1-C6alkyl, —C1-C6alkylCOOH, —OC1-C6alkylCOOH, —CN, C1-C6alkylCN, NH2, NHC1-C6alkyl, N(C1-C6alkyl)2, —NHCOOC1-C6alkyl, C1-C6alkylCONH2, —CONH2, —CONHC1-C6alkyl, —NHCOC1-C6alkyl, —CON(C1-C6alkyl)2, —NHSO2C1-C6alkyl, SO2aryl, —SO2C1-C6alkyl, C1-C6alkyl SO2C1-C6alkyl, aryl, —NHCOaryl, and —NHCOheterocycle.
地址 Rahway NJ US