1-Methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡唑类
• 英文名称: 1-Methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carboxylic acid
• 英文别名: 1-methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carboxylic acid
• 化学式: C₇H₉N₃O₄S
• 分子量: 231.23
• InChiKey: AUXDRGZNZXJREM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  101
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• NOVEL CRYSTALLINE FORMS OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR
  申请人：Arroyo Itzia

  公开号：US20140080884A1

  公开（公告）日：2014-03-20

  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.

  (2R,3S,5R)-2-(2,5-二氟苯基)-5-[2-(甲磺酰基)-2,6-二氢吡咯并[3,4-c]吡唑-5(4H)-基]四氢-2H-吡喃-3-胺的新晶体形态是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖性（2型）糖尿病。该发明还涉及含有这些新形态的制药组合物、制备这些形态及其制药组合物的过程，以及用于治疗2型糖尿病的用途。
• NOVEL CRYSTALLINE FORMS OF A DIPEPTIDYL PEPTIDASE-IV INHIBITORS
  申请人：Merck Sharp & Dohme Corp

  公开号：US20150099891A1

  公开（公告）日：2015-04-09

  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.

  “(2R,3S,5R)-2-(2,5-二氟苯基)-5-[2-(甲磺酰基)-2,6-二氢吡咯并[3,4-c]吡唑-5(4H)-基]四氢-2H-吡喃-3-胺的新型晶体形态是强效的二肽基肽酶-IV抑制剂，可用于治疗非胰岛素依赖性（2型）糖尿病。本发明还涉及含有这些新型形态的制药组合物，制备这些形态及其制药组合物的工艺以及它们用于治疗2型糖尿病的用途。”
• US8895603B2
  申请人：——

  公开号：US8895603B2

  公开（公告）日：2014-11-25
• US9181262B2
  申请人：——

  公开号：US9181262B2

  公开（公告）日：2015-11-10