发明名称 Treating diabetes with dipeptidyl peptidase-IV inhibitors
摘要 The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N 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 US9156848(B2) 申请公布日期 2015.10.13
申请号 US201314415759 申请日期 2013.07.18
申请人 Merck Sharp & Dohme Corp. 发明人 Biftu Tesfaye;Khan Tanweer A.
分类号 A61K31/4162;C07D231/00;C07D487/04 主分类号 A61K31/4162
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 R1, R9, R10 and R11 are selected from the group consisting of halogen and hydrogen; X is selected from the group consisting of —NR4— and —CHR4—; Y is selected from the group consisting of —N— and —CHR2—; Z is selected from the group consisting of —N— and —CH—; R2 is selected from the group consisting of hydrogen or taken with R8 forms (CH2)n; R3 is selected from the group consisting of hydrogen, SO2NH2, SO2NH(C1-6alkyl), SO2N(C1-6alkyl)2, SO2NHC3-6cycloalkyl, SOC1-6alkylNP, SO2NHP, SO2C1-6alkyl and SO2C3-6cycloalkyl, wherein Q is a amine protecting group; R4 is hydrogen or C1-6alkyl or taken together with R6 forms a six-membered ring; R5 is hydrogen or C1-6alkyl or taken together with R7 forms —(CH2)n-; R6 is hydrogen or C1-6alkyl or taken together with R4 forms a six-membered ring; R7 is hydrogen or C1-6alkyl or taken together with R5 forms —(CH2)n-; R8 is hydrogen or C1-6alkyl or taken together with R2 forms —(CH2)n-, wherein when Y and X are CH2 and R3 is SO2C1-6alkyl or SO2C3-6cycloalkyl then R5, R6, R7 and R8 cannot be simultaneously hydrogen; and n is 1 or 2.
地址 Rahway NJ US