1-[5-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)indol-1-yl]-3-phenylpropan-1-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三唑并吡啶类
• 英文名称: 1-[5-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)indol-1-yl]-3-phenylpropan-1-one
• 英文别名: 1-[5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)indol-1-yl]-3-phenylpropan-1-one
• 化学式: C₂₃H₁₉N₅O
• 分子量: 381.4
• InChiKey: WWWLCXZDJXYVPJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  78.2
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
  申请人：MENET Christel Jeanne Marie

  公开号：US20150150856A1

  公开（公告）日：2015-06-04

  [1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, 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.

  本文披露了一种具有以下公式表示的[1,2,4]三唑并[1,5-a]吡啶化合物。这些化合物可以制备成药物组合物，并可用于预防和治疗哺乳动物包括人类的各种疾病，包括但不限于涉及软骨降解、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情况，如克罗恩病、类风湿性关节炎、银屑病、过敏性空气道疾病（例如哮喘、鼻炎）、少年特发性关节炎、结肠炎、炎性肠病、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（例如涉及软骨细胞的合成刺激的疾病）、先天性软骨畸形、与IL6过度分泌相关的疾病和增殖性疾病。
• 1-METHYLPYRAZOLE MODULATORS OF SUBSTANCE P, CALCITONIN GENE-RELATED PEPTIDE, ADRENERGIC RECEPTOR, AND/OR 5-HT RECEPTOR
  申请人：Gant Thomas G.

  公开号：US20100291151A1

  公开（公告）日：2010-11-18

  The present invention relates to new 1-methylpyrazole modulators of substance P release, calcitonin gene-related peptide activity, adrenergic receptor activity, and/or 5-HT receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

  本发明涉及新的1-甲基吡唑调节物质P释放、降钙素基因相关肽活性、肾上腺素能受体活性和/或5-HT受体活性的调节剂，其制药组合物以及使用方法。
• Compounds useful for the treatment of degenerative and inflammatory diseases
  申请人：GALAPAGOS NV

  公开号：US10206907B2

  公开（公告）日：2019-02-19

  [1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, 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.

  所公开的[1,2,4]三唑并[1,5-a]吡啶化合物具有下式： 这些化合物可制备成药物组合物，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，包括非限制性实例，涉及软骨退化、骨和/或关节退化的疾病，例如骨关节炎；和/或涉及炎症或免疫反应的疾病，例如克罗恩病、类风湿性关节炎、银屑病、过敏性气道疾病（如哮喘、鼻炎、幼年特发性关节炎、荨麻疹等）。哮喘、鼻炎）、幼年特发性关节炎、结肠炎、肠道炎症性疾病、内毒素驱动的疾病状态（如搭桥手术后的并发症或导致慢性心力衰竭等的慢性内毒素状态）、涉及软骨代谢损伤的疾病（如涉及合成代谢疾病的疾病）、涉及骨质疏松症的疾病（如骨质疏松症）、涉及骨质疏松症的疾病（如骨质疏松症）、涉及骨质疏松症的疾病（如骨质疏松症）。先天性软骨畸形、与 IL6 分泌过多和移植排斥有关的疾病（如器官移植排斥）以及增殖性疾病。
• US9415037B2
  申请人：——

  公开号：US9415037B2

  公开（公告）日：2016-08-16