6-tert-butyl-1H-1,8-naphthyridin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 6-tert-butyl-1H-1,8-naphthyridin-2-one
• 化学式: C₁₂H₁₄N₂O
• 分子量: 202.25
• InChiKey: YQTFQTMCJXQHEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• QUINOLONE COMPOUND
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：US20140179675A1

  公开（公告）日：2014-06-26

  The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R 1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R 2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R 3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile -associated diarrhea.

  本发明提供了一种由式(I)表示的化合物 其中X是氢原子或氟原子；R是氢原子或烷基；R 1 是(1)环丙基，可选地取代1至3个卤素原子，或(2)苯基，可选地取代1至3个卤素原子；R 2 是烷基，烷氧基，卤代烷氧基，卤素原子，氰基等；R 3 是7-氧代-7,8-二氢-1,8-萘啉基，3-吡啶基等，或其盐。本发明的化合物对 艰难梭菌 具有优异的抗菌活性，并可用于预防或治疗肠道感染，如 艰难梭菌 相关性腹泻。
• [EN] NOVEL INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE GAMMA<br/>[FR] NOUVEAUX INHIBITEURS DE LA PHOSPHATIDYLINOSITOL 3-KINASE GAMMA
  申请人：ASTRAZENECA AB

  公开号：WO2017153527A1

  公开（公告）日：2017-09-14

  There are disclosed certain novel compounds (including pharmaceutically acceptable salts thereof), that inhibit phosphatidylinositol 3-kinase gamma (ΡΒΚγ) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

  已披露某些新颖化合物（包括其药用盐），这些化合物抑制磷脂酰肌醇3-激酶γ（PI3Kγ）的活性，用于治疗和/或预防临床疾病，包括呼吸道疾病，如哮喘和慢性阻塞性肺病（COPD），以及它们在治疗中的用途，包含它们的药物组合物和制备这些化合物的过程。
• Inhibitors of phosphatidylinositol 3-kinase gamma
  申请人：AstraZeneca AB

  公开号：US10858355B2

  公开（公告）日：2020-12-08

  There are disclosed certain novel compounds (including pharmaceutically acceptable salts thereof), that inhibit phosphatidylinositol 3-kinase gamma (PI3Kδ) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

  本文公开了某些新型化合物（包括其药学上可接受的盐）、 抑制磷脂酰肌醇 3- 激酶γ（PI3Kδ）活性的化合物，它们在治疗和/或预防包括呼吸系统疾病（如哮喘和慢性阻塞性肺病（COPD））在内的临床疾病中的用途，它们在治疗中的使用，含有它们的药物组合物，以及制备此类化合物的工艺。
• NOVEL INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE GAMMA
  申请人：AstraZeneca AB

  公开号：US20200299289A1

  公开（公告）日：2020-09-24

  There are disclosed certain novel compounds (including pharmaceutically acceptable salts thereof), that inhibit phosphatidylinositol 3-kinase gamma (P13Kδ) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
• INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE GAMMA
  申请人：AstraZeneca AB

  公开号：US20210047312A1

  公开（公告）日：2021-02-18

  There are disclosed certain novel compounds (including pharmaceutically acceptable salts thereof), that inhibit phosphatidylinositol 3-kinase gamma (PI3Kδ) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.