3-[1-(indole-6-carbonyl)-piperidin-4-yl]-benzylamine | 375847-12-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 3-[1-(indole-6-carbonyl)-piperidin-4-yl]-benzylamine
• 英文别名: [4-[3-(aminomethyl)phenyl]piperidin-1-yl]-(1H-indol-6-yl)methanone
• CAS: 375847-12-4
• 化学式: C₂₁H₂₃N₃O
• 分子量: 333.433
• InChiKey: OCBLHVOVZOVDBU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  62.1
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• Chemical compounds
  申请人：——

  公开号：US20030187020A1

  公开（公告）日：2003-10-02

  Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration of an inhibitor of tryptase, e.g., asthma and inflammatory diseases, to name only a few.

  本文提供了具有胰蛋白酶抑制活性的新颖和有用化合物，包括含有这些化合物的药物组合物，以及治疗患有可以通过给予胰蛋白酶抑制剂（例如哮喘和炎症性疾病等）而得到改善的疾病、疾病或紊乱的方法。
• [EN] DISUBSTITUTED [4-(5-AMINOMETHYL-PHENYL)-PIPERIDIN-1-YL]-1H-INDOL-3-YL]-METHANONES<br/>[FR] [4-(5-AMINOMÉTHYL-PHÉNYL)-PIPÉRIDIN-1-YL]-1H-INDOL-3-YL]-MÉTHANONES DISUBSTITUÉES
  申请人：SANOFI AVENTIS

  公开号：WO2011022449A1

  公开（公告）日：2011-02-24

  The present invention extends to the compound of formula I: or a prodrug, pharmaceutically acceptable salt, or solvate of said compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed to the use of a compound of formula I as an inhibitor of tryptase, comprising introducing the compound into a composition comprising tryptase. In addition, the present invention is directed to the use of a compound of formula I for treating a patient suffering from, or subject to, a physiological condition in need of amelioration of an inhibitor of tryptase comprising administering to the patient a therapeutically effective amount of the compound of Claim 1. The present invention is directed also to the preparation of a compound of formula I.

  本发明涉及到式I的化合物：或者该化合物的前药、药用可接受的盐或溶剂。此外，本发明涉及一种包括式I化合物的药物组合物，以及药用可接受的载体的药学有效量。此外，本发明涉及将式I化合物用作色氨酸蛋白酶抑制剂的用途，包括将该化合物引入含有色氨酸蛋白酶的组合物中。此外，本发明还涉及将式I化合物用于治疗患有或患有需要改善色氨酸蛋白酶抑制剂的生理状况的患者的用途，包括向患者施用权利要求1中的化合物的治疗有效量。本发明还涉及制备式I化合物。
• [EN] ARYLMETHYLAMINE DERIVATIVES FOR USE AS TRYPTASE INHIBITORS<br/>[FR] DERIVES D'ARYLMETHYLAMINE UTILISES COMME INHIBITEURS DE LA TRYPTASE
  申请人：AVENTIS PHARM PROD INC

  公开号：WO2001090101A1

  公开（公告）日：2001-11-29

  Provided herein are compounds of formula (I) wherein R1-4, n and Ar are as defined in claim 1, and their pharmaceutical compositions. These compounds are tryptase inhibitors and may be used in the treatment of e.g. asthma and inflammatory diseases.

  本发明提供了式(I)的化合物，其中R1-4、n和Ar如权利要求1所定义，以及它们的药物组成物。这些化合物是胰蛋白酶抑制剂，可用于治疗哮喘和炎症性疾病等疾病。
• ARYLMETHYLAMINE DERIVATIVES FOR USE AS TRYPTASE INHIBITORS
  申请人：Aventis Pharmaceuticals Inc.

  公开号：EP1296972B1

  公开（公告）日：2009-12-23
• [4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-[7-FLUORO-1-(2-METHOXY-ETHYL)-4TRIFLUOROMETHOXY-1H-INDOL-3-YL]METHANONE AS AN INHIBITOR OF MAST CELL TRYPTASE
  申请人：SANOFI

  公开号：EP2367812B1

  公开（公告）日：2015-09-16