1-((3S,4R)-4-(3,5-difluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(8-methyl-2-phenylimidazo[1,2-a]pyrazin-3-yl)urea | 1610362-43-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-((3S,4R)-4-(3,5-difluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(8-methyl-2-phenylimidazo[1,2-a]pyrazin-3-yl)urea
• 英文别名: 1-[(3S,4R)-4-(3,5-difluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl]-3-(8-methyl-2-phenylimidazo[1,2-a]pyrazin-3-yl)urea
• CAS: 1610362-43-0
• 化学式: C₂₇H₂₈F₂N₆O₂
• 分子量: 506.555
• InChiKey: NCHOLHHTVNUOJU-XZOQPEGZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  37
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  83.8
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• [EN] PYRROLIDINYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS<br/>[FR] COMPOSÉS DE N-PYRROLIDINYLE URÉE, THIO-URÉE,GUANIDINE ET CYANOGUANIDINE EN TANT QU'INHIBITEURS DE LA KINASE TRKA
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2014078372A1

  公开（公告）日：2014-05-22

  Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring 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/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

  化合物的公式I：或其立体异构体、互变异构体、药用可接受的盐、溶剂合物或前药，其中R1、R2、Ra、Rb、Rc、Rd、X、环B和环C的定义如本文所述，并且环B基团和NH-C(=X)-NH基团处于反式构型，是TrkA激酶的抑制剂，对可以用TrkA激酶抑制剂治疗的疾病具有用处，如疼痛、癌症、炎症/炎症性疾病、神经退行性疾病、某些传染病、干燥综合征、子宫内膜异位症、糖尿病周围神经病变、前列腺炎和盆腔疼痛综合征。
• PYRROLIDINYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
  申请人：ARRAY BIOPHARMA INC.

  公开号：US20160297758A1

  公开（公告）日：2016-10-13

  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, Ring B, and Ring C are as defined herein, and wherein Ring 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/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
• US9790178B2
  申请人：——

  公开号：US9790178B2

  公开（公告）日：2017-10-17