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公开(公告)号：US09181262B2
公开(公告)日：2015-11-10
申请号：US14507001
申请日：2014-10-06
发明人： Itzia Z. Arroyo , Davida Krueger , Ping Chen , Aaron J. Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
IPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513 , C07B2200/13 , Y02P20/55
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.
摘要翻译： （2R，3S，5R）-2-（2,5-二氟苯基）-5- [2-（甲基磺酰基）-2,6-二氢吡咯并[3,4-c]吡唑-5（4H） - 吡啶-3-基]四氢-2H-吡喃-3-胺是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖型（2型）糖尿病。 本发明还涉及含有这些新型形式的药物组合物，制备这些形式的方法及其药物组合物及其用于治疗2型糖尿病的用途。
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公开(公告)号：US20150099891A1
公开(公告)日：2015-04-09
申请号：US14507001
申请日：2014-10-06
发明人： Itzia Z. Arroyo , Davida Krueger , Ping Chen , Aaron J. Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513 , C07B2200/13 , Y02P20/55
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.
摘要翻译： （2R，3S，5R）-2-（2,5-二氟苯基）-5- [2-（甲基磺酰基）-2,6-二氢吡咯并[3,4-c]吡唑-5（4H） - 吡啶-3-基]四氢-2H-吡喃-3-胺是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖型（2型）糖尿病。 本发明还涉及含有这些新型形式的药物组合物，制备这些形式的方法及其药物组合物及其用于治疗2型糖尿病的用途。
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公开(公告)号：US20150197490A1
公开(公告)日：2015-07-16
申请号：US14669303
申请日：2015-03-26
IPC分类号： C07D209/18
CPC分类号： C07D209/18 , C07B2200/13
摘要： The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.
摘要翻译： 本发明涉及式A化合物的多晶型物质：该化合物可用作胰高血糖素受体拮抗剂并用作用于治疗2型糖尿病和相关病症的药物活性成分，例如高血糖症，肥胖症，血脂异常和 代谢综合征。 包括水合物，半水合物，水合物和类似的多晶型物质。
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公开(公告)号：US20140171480A1
公开(公告)日：2014-06-19
申请号：US14186829
申请日：2014-02-21
发明人： John Y. L. Chung , Yanfeng Zhang , Laura Artino , Aaron S. Cote , Donal Desmond , Jeremy Scott , Yekaterina Vaynshteyn
IPC分类号： C07D209/18
CPC分类号： C07D209/18 , C07B2200/13
摘要： The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.
摘要翻译： 本发明涉及式A化合物的多晶型物质：该化合物可用作胰高血糖素受体拮抗剂并用作用于治疗2型糖尿病和相关病症的药物活性成分，例如高血糖症，肥胖症，血脂异常和 代谢综合征。 包括水合物，半水合物，水合物和类似的多晶型物质。
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公开(公告)号：US09272999B2
公开(公告)日：2016-03-01
申请号：US14669303
申请日：2015-03-26
IPC分类号： C07D209/18
CPC分类号： C07D209/18 , C07B2200/13
摘要： The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.
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公开(公告)号：US09012488B2
公开(公告)日：2015-04-21
申请号：US14186829
申请日：2014-02-21
发明人： John Y. L. Chung , Yanfeng Zhang , Laura Artino , Aaron S. Cote , Donal Desmond , Jeremy Scott , Yekaterina Vaynshteyn
IPC分类号： A61K31/405 , C07D209/12 , C07D209/18
CPC分类号： C07D209/18 , C07B2200/13
摘要： The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.
摘要翻译： 本发明涉及式A化合物的多晶型物质：该化合物可用作胰高血糖素受体拮抗剂并用作用于治疗2型糖尿病和相关病症的药物活性成分，例如高血糖症，肥胖症，血脂异常和 代谢综合征。 包括水合物，半水合物，水合物和类似的多晶型物质。
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公开(公告)号：US10167298B2
公开(公告)日：2019-01-01
申请号：US15032663
申请日：2014-10-24
发明人： Michael McNevin , Yong Liu , Ian Mangion , Alfred Lee , Joyce Stellabott , Benjamin D. Sherry , Gary Martin , Kung-I Feng , Scott Schultz , Ryan Cohen , Yanfeng Zhang
IPC分类号： A61K31/5365 , C07D498/04 , A61P1/16 , A61K45/06
摘要： The present invention relates to novel Pseudopolymorphs of Compound A, compositions comprising at least one Pseudopolymorph of Compound A, and methods of using the Pseudopolymorphs of Compound A for preparing compositions useful for treating or preventing HCV infection in a patient, wherein Compound A has the structure.
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