N,4-dimethyl-5-[(1-methylazetidin-3-yl)methoxy]-2-phenylpyrazol-3-amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: N,4-dimethyl-5-[(1-methylazetidin-3-yl)methoxy]-2-phenylpyrazol-3-amine
• 化学式: C₁₆H₂₂N₄O
• 分子量: 286.37
• InChiKey: SVWCJMNRYZMHCE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  42.3
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] N-(MONOCYCLIC ARYL),N'-PYRAZOLYL-UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS<br/>[FR] COMPOSÉS DE N-ARYLE MONOCYCLIQUES, N'-PYRAZOLYL-URÉE, THIOURÉE, GUANIDINE ET CYANOGUANIDINE UTILES COMME INHIBITEURS DE TRKA KINASE
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2014078325A1

  公开（公告）日：2014-05-22

  Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, 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 or pelvic pain syndrome.

  化合物的公式(I)或其立体异构体、互变异构体、或其药学上可接受的盐、溶剂合物或前药，其中环A、环C和X如本文所定义，是TrkA激酶的抑制剂，并且在治疗可以用TrkA激酶抑制剂治疗的疾病中具有用处，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、前列腺炎或盆腔疼痛综合征。
• HETEROCYCLIC DERIVATIVE HAVING TrkA-INHIBITING ACTIVITY
  申请人：Shionogi & Co., Ltd.

  公开号：EP3330256A1

  公开（公告）日：2018-06-06

  The present invention provides a compound having a TrkA inhibitory activity or a pharmaceutically acceptable salt thereof. The present invention relates to a compound represented by Formula (I): wherein -L- is -C(=X)-, or the like, -Z- is -NR5-, or the like, -ZA- is -NR5A-, or the like, B is substituted or unsubstituted aromatic carbocyclyl, or the like, Y is a single bond, or the like, the ring C is a substituted or unsubstituted aromatic heterocycle, or the like, R2 is a hydrogen atom, or the like, and the group represented by is a group represented by Formula: or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.

  本发明提供了一种具有 TrkA 抑制活性的化合物或其药学上可接受的盐。 本发明涉及一种由式（I）表示的化合物： 其中-L-是-C(＝X)-，或类似物，-Z-是-NR5-，或类似物，-ZA-是-NR5A-，或类似物，B是取代或未取代的芳香族碳环，或类似物，Y是单键，或类似物，环C是取代或未取代的芳香族杂环，或类似物，R2是氢原子，或类似物，以及由以下式子代表的基团 是由式 或其药学上可接受的盐，以及由其组成的药物组合物。