1-(Trifluoromethyl)indolizine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 1-(Trifluoromethyl)indolizine
• 英文别名: 1-(trifluoromethyl)indolizine
• 化学式: C₉H₆F₃N
• 分子量: 185.15
• InChiKey: DZLMLDFUWZHKNI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  4.4
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Bicyclic compounds, compositions and medicinal applications thereof
  申请人：Advinus Therapeutics Limited

  公开号：US10435402B2

  公开（公告）日：2019-10-08

  Substituted bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts and pharmaceutical compositions containing them are disclosed, as well as processes for preparing and using the compounds. These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of retinoic acid-related orphan receptor gamma (RORy). Representative conditions include inflammatory and/or autoimmune disorder, rheumatoid arthritis, psoriasis, psoriatic arthritis, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, COPD, cancer, cell proliferation, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, systemic lupus, crythematosus or other disorders.

  本发明公开了式(I)的取代双环化合物、它们的同素异形体、多晶型、立体异构体、原药、溶液剂、水合物、N-氧化物、共晶体、药学上可接受的盐和含有它们的药物组合物，以及制备和使用这些化合物的工艺。这些化合物可用于治疗、预防、预防、管理或辅助治疗与抑制视黄酸相关孤儿受体γ（RORy）有关的所有病症。具有代表性的病症包括炎症性和/或自身免疫性疾病、类风湿性关节炎、银屑病、银屑病关节炎、多发性硬化症、炎症性肠病、过敏性疾病、哮喘、慢性阻塞性肺病、癌症、细胞增殖、1 型糖尿病、重症肌无力、造血功能障碍、系统性红斑狼疮、隐性红斑狼疮或其他疾病。
• BICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
  申请人：Advinus Therapeutics Limited

  公开号：US20170362225A1

  公开（公告）日：2017-12-21

  The present disclosure relates to a class of substituted bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts and pharmaceutical compositions containing them. The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of retinoic acid-related orphan receptor gamma (RORγ) such as inflammatory and/or autoimmune disorder, rheumatoid arthritis, psoriasis, psoriatic arthritis, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, COPD, cancer, cell proliferation, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, systemic lupus, erythematosus or other disorders.