5-[2-chloro-5-[(3,3-dimethyl-1-oxothiaziridin-2-yl)methyl]phenyl]-2-[4-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-[2-chloro-5-[(3,3-dimethyl-1-oxothiaziridin-2-yl)methyl]phenyl]-2-[4-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-one
• 化学式: C₁₉H₁₆ClF₃N₄O₂S
• 分子量: 456.9
• InChiKey: ZGGYPYITYIPXOU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  84
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS<br/>[FR] COMPOSÉS TRIAZOLONE UTILISÉS COMME INHIBITEURS DE LA MPGES-1
  申请人：GLENMARK PHARMACEUTICALS SA

  公开号：WO2013186692A1

  公开（公告）日：2013-12-19

  The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

  本公开涉及式(I)的化合物及其药用盐，作为mPGES-1抑制剂。这些化合物是微粒体前列腺素E合成酶-1（mPGES-1）酶的抑制剂，因此在治疗来自各种疾病或病况的疼痛和/或炎症方面具有用处，如哮喘、骨关节炎、类风湿关节炎、急性或慢性疼痛和神经退行性疾病。
• TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS
  申请人：Glenmark Pharmaceuticals S.A.

  公开号：US20150283117A1

  公开（公告）日：2015-10-08

  The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as raPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

  本公开涉及式（I）化合物及其药学上可接受的盐，作为raPGES-1抑制剂。这些化合物是微粒体前列腺素E合成酶-1（mPGES-1）酶的抑制剂，因此可用于治疗多种疾病或病况引起的疼痛和/或炎症，例如哮喘、骨关节炎、类风湿性关节炎、急性或慢性疼痛和神经退行性疾病。
• Triazolone compounds as mPGES-1 inhibitors
  申请人：Glenmark Pharmaceuticals S.A.

  公开号：US10821100B2

  公开（公告）日：2020-11-03

  The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

  本公开涉及作为 mPGES-1 抑制剂的式 (I) 化合物及其药学上可接受的盐。这些化合物是微粒体前列腺素 E 合酶-1（mPGES-1）酶的抑制剂，因此可用于治疗多种疾病或病症引起的疼痛和/或炎症，如哮喘、骨关节炎、类风湿性关节炎、急性或慢性疼痛和神经退行性疾病。
• TRIAZOLONE COMPOUNDS AS MPGES-1 INHIBITORS
  申请人：Glenmark Pharmaceuticals S.A.

  公开号：US20190282548A1

  公开（公告）日：2019-09-19

  The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
• US9439890B2
  申请人：——

  公开号：US9439890B2

  公开（公告）日：2016-09-13