cyclopropanecarboxylic acid {5-[4-(2-1H-indol-3-yl-acetyl)-piperazin-1-yl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide | 1206184-46-4

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: cyclopropanecarboxylic acid {5-[4-(2-1H-indol-3-yl-acetyl)-piperazin-1-yl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide
• 英文别名: N-[5-[4-[2-(1H-indol-3-yl)acetyl]piperazin-1-yl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide
• CAS: 1206184-46-4
• 化学式: C₂₄H₂₅N₇O₂
• 分子量: 443.508
• InChiKey: ZCFSTSQNNPKFGS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  33
• 可旋转键数：
  5
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  98.6
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES<br/>[FR] NOUVEAUX COMPOSÉS UTILES POUR LE TRAITEMENT DE MALADIES DÉGÉNÉRATIVES ET INFLAMMATOIRES
  申请人：GALAPAGOS NV

  公开号：WO2010010187A1

  公开（公告）日：2010-01-28

  [1,2,4]Triazolo[1,5-a]pyridine compounds are disclosed that have a Formula (I), represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

  揭示了具有以下式(I)的[1,2,4]三唑并[1,5-a]吡啶化合物：这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，例如涉及软骨降解、骨骼和/或关节降解的疾病，例如骨关节炎；以及涉及炎症或免疫反应的疾病，如克罗恩病、类风湿关节炎、牛皮癣、过敏性气道疾病（例如哮喘、鼻炎）、儿童特发性关节炎、结肠炎、炎症性肠病、内毒素驱动的疾病状态（例如旁路手术后的并发症或慢性内毒素状态导致的慢性心力衰竭等），涉及软骨周转障碍的疾病（例如涉及软骨细胞合成促进的疾病），先天性软骨畸形、与IL6过度分泌和移植排斥有关的疾病（例如器官移植排斥）和增生性疾病。