[1,3]dioxolo[4,5-g]quinolin-7-amine | 87199-85-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: [1,3]dioxolo[4,5-g]quinolin-7-amine
• CAS: 87199-85-7
• 化学式: C₁₀H₈N₂O₂
• 分子量: 188.186
• InChiKey: OQCRTKXIEZKECJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  57.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  [1,3]dioxolo[4,5-g]quinolin-7-amine 、 对甲苯磺酰氯 在 吡啶 、 4-二甲氨基吡啶 作用下， 以81%的产率得到N-([1,3]dioxolo[4,5-g]quinolin-7-yl)-4-methylbenzenesulfonamide
  参考文献：
  名称：

  对映选择性转移氢化，是合成3-氨基四氢喹啉的关键步骤†

  摘要：

  已经成功实现对映选择性转移氢化，以提供3-氨基四氢喹啉。反应在温和条件下在汉兹二氢吡啶和催化量的手性磷酸的存在下进行。

  DOI：

  10.1039/c6nj02249a
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 盐酸 、 sodium sulfide 、 乙醇 作用下， 生成 [1,3]dioxolo[4,5-g]quinolin-7-amine
  参考文献：
  名称：

  229. 3-氨基喹啉的某些衍生物

  摘要：

  DOI：

  10.1039/jr9450000867

文献信息

• [EN] INHIBITORS OF TRKA KINASE<br/>[FR] INHIBITEURS DE TRKA KINASE
  申请人：GVK BIOSCIENCES PRIVATE LTD

  公开号：WO2016116900A1

  公开（公告）日：2016-07-28

  The present invention is directed to the compounds of Formula I which are inhibitors of tropomyosin-related kinase A (TrkA): Formula (I) or steroisomers, 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，该化合物是Tropomyosin-related kinase A（TrkA）的抑制剂：式（I）或其立体异构体、互变异构体或药学上可接受的盐、代谢物、同位素、溶剂合物或前药，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的异常活动相关的疾病或障碍，如疼痛、炎症或炎症性疾病、癌症、动脉粥样硬化、再狭窄、血栓形成、神经退行性疾病、勃起功能障碍（ED）、皮肤疾病、多发性硬化、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、传染病、与骨重塑调节失衡相关的疾病、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疾病引起的疾病；或与失髓鞘形成或脱髓鞘相关的疾病、障碍、损伤或功能障碍。
• Pyrazole Compounds Useful In The Treatment Of Inflammation
  申请人：Nilsson Peter

  公开号：US20070225318A1

  公开（公告）日：2007-09-27

  There is provided compounds of formula (I), wherein R 1 , R 2 , R a and R b have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.

  提供了公式(I)的化合物，其中R1、R2、Ra和Rb的含义在说明中给出，并且其药学上可接受的盐，在抑制脂氧化酶（例如15-脂氧化酶）活性所需或所期望的疾病的治疗中非常有用，特别是在治疗炎症方面。
• 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。
• INHIBITORS OF TRKA KINASE
  申请人：GVK Biosciences Private Limited

  公开号：EP3247692A1

  公开（公告）日：2017-11-29