[1-(2,5-Difluorophenyl)-1-oxopent-4-yn-2-yl]carbamic acid

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: [1-(2,5-Difluorophenyl)-1-oxopent-4-yn-2-yl]carbamic acid
• 英文别名: [1-(2,5-difluorophenyl)-1-oxopent-4-yn-2-yl]carbamic acid
• 化学式: C₁₂H₉F₂NO₃
• 分子量: 253.2
• InChiKey: DSCFEUSVCPXFNP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  66.4
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES OF OMARIGLIPTIN<br/>[FR] PROCÉDÉ DE PRÉPARATION D'INTERMÉDIAIRES CLÉ D'OMARIGLIPTINE
  申请人：ITALIANA SINT SPA

  公开号：WO2015139859A1

  公开（公告）日：2015-09-24

  Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of the active pharmaceutical ingredient named Omarigliptin.

  本发明的对象是一种改进的工艺，用于制备合成活性药物成分奥马利格普汀的关键中间体。
• 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。”
• AMINO PYRANOID RING DERIVATIVE AND COMPOSITION AND USE THEREOF
  申请人：Sichuan Haisco Pharmaceutical Co., Ltd.

  公开号：EP3159344A1

  公开（公告）日：2017-04-26

  The present invention relates to an amino pyran ring derivative and a composition and use thereof, and in particular, to an amino pyran ring derivative represented by general formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof, a pharmaceutical composition comprising the derivative, and their medical use in the manufacture of a di-peptidyl peptidase IV (DPP-IV) inhibitor, in formula (I) the substituents are defined the same as those in the specification.

  本发明涉及一种氨基吡喃环衍生物及其组合物和用途，特别是通式（I）代表的氨基吡喃环衍生物或其立体异构体、其药学上可接受的盐或原药、包含该衍生物的药物组合物，以及它们在制造二肽基肽酶 IV（DPP-IV）抑制剂中的医疗用途、 在式 (I) 中，取代基的定义与说明书中的相同。
• SUBSTITUTED AMINO SIX-MEMBERED SATURATED HETEROCYCLIC FAT USED AS LONG-ACTING DPP-IV INHIBITOR
  申请人：Centaurus BioPharma Co., Ltd.

  公开号：EP3257857A1

  公开（公告）日：2017-12-20

  The present application relates to a substituted amino six-membered saturated heteroalicycle represented by formula I as a long-acting DPP-IV inhibitor, a method for preparing the same, a pharmaceutical composition comprising the same, and a use of the same in treating and/or preventing diseases and disorders benefitting from DPP-IV inhibition.

  本申请涉及由式 I 代表的作为长效 DPP-IV 抑制剂的取代氨基六元饱和杂环、制备方法、包含其的药物组合物，以及其在治疗和/或预防受益于 DPP-IV 抑制的疾病和失调中的用途。