1-amino-4,4-dimethyl-1,2,3,4-tetrahydro-naphthalen-2-ol

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 1-amino-4,4-dimethyl-1,2,3,4-tetrahydro-naphthalen-2-ol
• 英文别名: 1-Amino-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-2-ol；1-amino-4,4-dimethyl-2,3-dihydro-1H-naphthalen-2-ol
• 化学式: C₁₂H₁₇NO
• 分子量: 191.273
• InChiKey: ARLFGNRPKQKZHI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-溴嘧啶 、 1-amino-4,4-dimethyl-1,2,3,4-tetrahydro-naphthalen-2-ol 在 copper(l) iodide potassium phosphate 、 N,N-二乙基水杨酰胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 21.0h， 以58%的产率得到4,4-Dimethyl-1-pyrimidin-5-ylamino-1,2,3,4-tetrahydronaphthalen-2-ol
  参考文献：
  名称：

  Tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents

  摘要：

  本发明涉及公式(I)的多取代四氢萘衍生物，其制备过程及其作为抗炎药物的用途。

  公开号：

  US20070015761A1
• 作为产物：
  描述：

  2-hydroxy-4,4-dimethyl-3,4-dihydro-2H-naphthalen-1-one oxime 在 palladium 10% on activated carbon 盐酸 、 氢气 作用下， 以 甲醇 、 水 为溶剂， 反应 6.0h， 以90%的产率得到1-amino-4,4-dimethyl-1,2,3,4-tetrahydro-naphthalen-2-ol
  参考文献：
  名称：

  Tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents

  摘要：

  本发明涉及公式(I)的多取代四氢萘衍生物，其制备过程及其作为抗炎药物的用途。

  公开号：

  US20070015761A1

文献信息

• [EN] BICYCLIC UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF PAIN<br/>[FR] COMPOSÉS DE THIO-URÉE, GUANIDINE, CYNOGUANIDINE ET D'URÉE BICYCLIQUES UTILES POUR LE TRAITEMENT DE LA DOULEUR
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2014078454A1

  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 and pelvic pain syndrome.

  公式I的化合物：或立体异构体、互变异构体、或药用可接受的盐、溶剂化物或前药，其中环A、环C和X如本文定义，是TrkA激酶的抑制剂，可用于治疗可以用TrkA激酶抑制剂治疗的疾病，如疼痛、癌症、炎症/炎症性疾病、神经退行性疾病、某些传染病、舍格伦综合症、子宫内膜异位症、糖尿病周围神经病、前列腺炎和盆腔疼痛综合症。
• NOVEL TETRAHYDRONAPHTHYL UREA DERIVATIVE
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：US20190023657A1

  公开（公告）日：2019-01-24

  The present invention aims to provide a compound having a TrkA inhibitory action, a pharmaceutically acceptable salt thereof, or a solvate thereof, a pharmaceutical composition containing the same as an active ingredient, and a preventive and/or therapeutic agent for medicinal use, in particular for a disease in which TrkA in involved (pain, cancers, inflammation/inflammatory diseases, allergic diseases, skin diseases, neurodegenerative diseases, infectious diseases, Sjogren's syndrome, endometriosis, renal diseases, osteoporosis, and the like). Specifically, the present invention provides a compound or an optical isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or the like, the compound represented by formula (I):

  本发明旨在提供一种具有TrkA抑制作用的化合物，其药学上可接受的盐或其溶剂合物，以及含有其作为活性成分的药物组合物，特别用于TrkA参与的疾病（疼痛、癌症、炎症/炎症性疾病、过敏疾病、皮肤疾病、神经退行性疾病、传染病、干燥综合征、子宫内膜异位症、肾脏疾病、骨质疏松症等）的预防和/或治疗剂。具体地，本发明提供一种化合物或其光学异构体，其药学上可接受的盐、其溶剂合物或类似物，该化合物由式（I）表示：
• CRYSTALS OF TETRAHYDRONAPHTHYL UREA DERIVATIVE
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：US20200308136A1

  公开（公告）日：2020-10-01

  Provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea which are useful as bulk pharmaceutical crystals. Also provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea having excellent TrkA inhibitory effect, medicines and medicinal composition containing these crystals, and a method for producing these crystals.

  提供的是1-((1R,2R)-2-羟基-4,4-二甲基-1,2,3,4-四氢萘-1-基)-3-(5-甲基-6-(2-甲基嘧啶-5-基)-2-苯基吡啶-3-基)脲的I型、III型、V型和VI型晶体，可用作大批量制药晶体。还提供了具有优异TrkA抑制作用的1-((1R,2R)-2-羟基-4,4-二甲基-1,2,3,4-四氢萘-1-基)-3-(5-甲基-6-(2-甲基嘧啶-5-基)-2-苯基吡啶-3-基)脲的I型、III型、V型和VI型晶体，以及含有这些晶体的药物和药物组合物，以及制备这些晶体的方法。
• NOVEL TETRAHYDRONAPHTHYL UREA DERIVATIVES
  申请人：Mochida Pharmaceutical Co., Ltd.

  公开号：EP3617195A1

  公开（公告）日：2020-03-04

  The present invention aims to provide a compound having a TrkA inhibitory action, a pharmaceutically acceptable salt thereof, or a solvate thereof, a pharmaceutical composition containing the same as an active ingredient, and a preventive and/or therapeutic agent for medicinal use, in particular for a disease in which TrkA in involved (pain, cancers, inflammation/inflammatory diseases, allergic diseases, skin diseases, neurodegenerative diseases, infectious diseases, Sjogren's syndrome, endometriosis, renal diseases, osteoporosis, and the like). Specifically, the present invention provides a compound or an optical isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or the like, the compound represented by formula (I):

  本发明的目的是提供一种具有TrkA抑制作用的化合物、其药学上可接受的盐或其溶液剂、含有其作为活性成分的药物组合物，以及用于医疗用途的预防和/或治疗剂，特别是用于TrkA参与的疾病（疼痛、癌症、炎症/炎症性疾病、过敏性疾病、皮肤病、神经退行性疾病、传染性疾病、Sjogren综合征、子宫内膜异位症、肾脏疾病、骨质疏松症等）。具体而言，本发明提供了一种由式（I）表示的化合物或其光学异构体、其药学上可接受的盐、其溶液或类似物：
• Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
  申请人：Array BioPharma Inc.

  公开号：US10351575B2

  公开（公告）日：2019-07-16

  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 and pelvic pain syndrome.

  式 I 的化合物或其立体异构体、同系物或药学上可接受的盐、溶液剂或原药，其中环 A、环 C 和 X 如本文所定义，是 TrkA 激酶的抑制剂，可用于治疗可使用 TrkA 激酶抑制剂治疗的疾病，如疼痛、癌症、炎症/炎症性疾病、神经退行性疾病、某些传染性疾病、Sjogren 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。