(3R)-1-(2-methoxyethyl)-3-phenylpyrrolidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: (3R)-1-(2-methoxyethyl)-3-phenylpyrrolidine
• 化学式: C₁₃H₁₉NO
• 分子量: 205.3
• InChiKey: KRDQWOHOOYIHKV-ZDUSSCGKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• Inhibitors of TrkA kinase
  申请人：GVK BIOSCIENCES PRIVATE LIMITED

  公开号：US10336723B2

  公开（公告）日：2019-07-02

  The present invention is directed to the compounds of Formula I which are inhibitors of tropomyosin-related kinase A (TrkA): Formula (I) or stereoisomers, tautomers or a pharmaceutically acceptable salts, metabolites, isotopes, solvates or prodrugs thereof, wherein, Ra, Rb, Rc, Rd, R1, R2, L and Het-Ar are as defined herein. These compounds can be used for the preventive and/or therapeutic treatment of diseases or disorders associated with abnormal activities of nerve growth factor (NGF) receptor TrkA such as Pain, inflammation or an inflammatory diseases, Cancer, atherosclerosis, restenosis, thrombosis, Neurodegenerative diseases, Erectile Dysfunction (ED), Skin disorders, Autoimmune disease like Multiple sclerosis, Sjögren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, Infectious diseases, diseases related to an imbalance of the regulation of bone remodeling, endometriosis, pelvic pain syndrome and diseases resulting from abnormal tissue remodelling and fibrotic disorders; or a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination.

  本发明涉及式 I 的化合物，它们是肌球蛋白相关激酶 A（TrkA）的抑制剂：式(I)或其立体异构体、同分异构体或药学上可接受的盐、代谢物、同位素、溶媒或原药，其中，Ra、Rb、Rc、Rd、R1、R2、L 和 Het-Ar 如本文所定义。这些化合物可用于预防和/或治疗与神经生长因子（NGF）受体 TrkA 的异常活动有关的疾病或紊乱，如疼痛、炎症或炎症性疾病、癌症、动脉粥样硬化、血管再狭窄、血栓形成、神经退行性疾病、勃起功能障碍（ED）、皮肤病、自身免疫性疾病（如多发性硬化症、斯约格伦综合征）、子宫内膜异位症、糖尿病周围神经病变、前列腺炎、传染病、与骨重塑调节失衡有关的疾病、子宫内膜异位症、盆腔疼痛综合征以及由异常组织重塑和纤维化紊乱引起的疾病；或与髓鞘脱落或脱髓鞘有关的疾病、失调、损伤或功能障碍。
• 1-((3S,4R)-4-(3-FLUOROPHENYL)-1-(2-METHOXYETHYL)PYRROLIDIN-3-YL)-3-(4-METHYL-3-(2-METHYLPYRIMIDIN-5-YL)-1-PHENYL-1H-PYRAZOL-5-YL)UREA AS A TRKA KINASE INHIBITOR
  申请人：Array Biopharma, Inc.

  公开号：EP3154959B1

  公开（公告）日：2019-07-10
• N-PYRROLIDINYL, N'-PYRAZOLYL- UREA COMPOUNDS AS TRKA KINASE INHIBITORS
  申请人：Array Biopharma, Inc.

  公开号：EP3409670B1

  公开（公告）日：2020-09-09
• PYRROLIDINYL UREA, PYRROLIDINYL THIOUREA AND PYRROLIDINYL GUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
  申请人：Array BioPharma Inc.

  公开号：US20170217936A1

  公开（公告）日：2017-08-03

  Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R 1 , R 2 , R a , R b , R c , R d , X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(═X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
• US9562055B2
  申请人：——

  公开号：US9562055B2

  公开（公告）日：2017-02-07