发明名称 Crystalline forms of a dipeptidyl peptidase-IV inhibitor
摘要 Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
申请公布号 US8895603(B2) 申请公布日期 2014.11.25
申请号 US201214118998 申请日期 2012.06.25
申请人 Merck Sharp & Dohme Corp.;Merck Sharp & Dohme Ltd. 发明人 Arroyo Itzia;Krueger Davida;Chen Ping;Moment Aaron;Biftu Tesfaye;Sheen Faye;Zhang Yanfeng
分类号 A61K31/4162;C07D231/00;C07D487/04;A61K31/4439;A61K31/4985;A61K31/513 主分类号 A61K31/4162
代理机构 代理人 Fair Janet E.;Cocuzzo Anna L.
主权项 1. Crystalline (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine of Compound I:characterized by having at least four peaks in its powder X-ray diffraction pattern selected from the group consisting of 10.3±0.1 2θ, 12.7±0.1 2θ, 14.6±0.1 2θ, 16.1±0.1 2θ, 17.8±0.1 2θ, 19.2±0.1 2θ, 22.2±0.1 2θ, 24.1±0.1 2θ and 26.9±0.1 2θ.
地址 Rahway NJ US