(3R,4R)-N-[1-(4-fluorophenyl)-5-[3-(2,2,2-trifluoroethoxy)phenyl]pyrazol-3-yl]-4-methyl-5-oxopyrrolidine-3-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: (3R,4R)-N-[1-(4-fluorophenyl)-5-[3-(2,2,2-trifluoroethoxy)phenyl]pyrazol-3-yl]-4-methyl-5-oxopyrrolidine-3-carboxamide
• 化学式: C₂₃H₂₀F₄N₄O₃
• 分子量: 476.4
• InChiKey: MJTAQCAEBIPHPQ-ACJLOTCBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  34
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  85.2
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• PYRAZOLE COMPOUNDS SUBSTITUTED WITH HETEROARYL AND PHARMACEUTICAL USE THEREOF
  申请人：Japan Tobacco Inc.

  公开号：US20190330193A1

  公开（公告）日：2019-10-31

  Pyrazole compounds substituted with heteroaryl or pharmaceutically acceptable salts thereof that have an SGLT1 inhibitory activity and are useful for a drug, pharmaceutical compositions comprising the same, and pharmaceutical use thereof are disclosed. Specifically, a compound of Formula [X]: wherein R 1 is hydrogen or halogen, R 2 is C 1-6 alkyl or halo-C 1-6 alkyl, Ring Het is substituted pyridyl or optionally substituted pyrazinyl, pyrimidinyl, or pyridazinyl, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof is provided.

  揭示了具有SGLT1抑制活性的以杂环芳基取代的吡唑化合物或其药学可接受的盐，用作药物，包括它们的药物组合物，以及其药用。具体地，提供了以下式[X]的化合物：其中R1为氢或卤素，R2为C1-6烷基或卤代C1-6烷基，环Het为取代的吡啶基或可选择取代的吡嗪基、嘧啶基或吡啉基，或其药学可接受的盐，包括它的药物组合物和药用。
• PYRAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF
  申请人：JAPAN TOBACCO INC.

  公开号：US20150183763A1

  公开（公告）日：2015-07-02

  The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.

  本发明提供了一种具有SGLT1抑制活性的吡唑化合物，或其药学上可接受的盐，其一般式[Ib]如下，以及包含其的药物组合物和其药用：其中每个符号如描述中所定义。
• CHRONIC KIDNEY DISEASE TREATMENT OR PREVENTION METHOD
  申请人：Japan Tobacco Inc.

  公开号：EP4026562A1

  公开（公告）日：2022-07-13

  One aim of the present invention is to treat or prevent chronic kidney disease. Provided is a treatment or prophylactic pharmaceutical composition for chronic kidney disease, that contains an SGLT1-inhibiting compound or a pharmaceutically acceptable salt thereof.

  本发明的一个目的是治疗或预防慢性肾脏疾病。提供了一种用于慢性肾脏疾病的治疗或预防性药物组合物，其含有一种SGLT1抑制化合物或其药学上可接受的盐。
• Pyrazole compounds substituted with heteroaryl and pharmaceutical use thereof
  申请人：Japan Tobacco Inc.

  公开号：US10988462B2

  公开（公告）日：2021-04-27

  Pyrazole compounds substituted with heteroaryl or pharmaceutically acceptable salts thereof that have an SGLT1 inhibitory activity and are useful for a drug, pharmaceutical compositions comprising the same, and pharmaceutical use thereof are disclosed. Specifically, a compound of Formula [X]: wherein R1 is hydrogen or halogen, R2 is C1-6 alkyl or halo-C1-6 alkyl, Ring Het is substituted pyridyl or optionally substituted pyrazinyl, pyrimidinyl, or pyridazinyl, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof is provided.

  本发明公开了具有 SGLT1 抑制活性并可用于药物的杂芳基取代的吡唑化合物或其药学上可接受的盐，以及包含这些化合物的药物组合物及其药物用途。具体地说，一种式[X]的化合物： 其中 R1 是氢或卤素，R2 是 C1-6 烷基或卤代-C1-6 烷基，环 Het 是取代的吡啶基或任选取代的吡嗪基、嘧啶基或哒嗪基，或其药学上可接受的盐、由其组成的药物组合物及其药物用途。
• US8846746B2
  申请人：——

  公开号：US8846746B2

  公开（公告）日：2014-09-30