7-甲基-1H-吲唑-4-胺 | 221681-73-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 中文名称: 7-甲基-1H-吲唑-4-胺
• 中文别名: (9ci)-7-甲基-1H-吲唑-4-胺
• 英文名称: 7-methyl-1H-indazol-4-amine
• CAS: 221681-73-8
• 化学式: C₈H₉N₃
• mdl: MFCD18808778
• 分子量: 147.18
• InChiKey: HIYNOMAXHVDMHV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.125
• 拓扑面积：
  54.7
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  7-甲基-1H-吲唑-4-胺 在 硫酸 作用下， 生成 4-羟基-7-甲基-吲唑
  参考文献：
  名称：

  吲唑衍生物：各种氨基吲哚和羟基吲唑及其衍生磺酸的合成

  摘要：

  DOI：

  10.1039/jr9550002412
• 作为产物：
  描述：

  7-甲基-4-硝基-1H-吲唑 在 镍 作用下， 生成 7-甲基-1H-吲唑-4-胺
  参考文献：
  名称：

  吲唑衍生物：各种氨基吲哚和羟基吲唑及其衍生磺酸的合成

  摘要：

  DOI：

  10.1039/jr9550002412

文献信息

• Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
  申请人：——

  公开号：US20040157849A1

  公开（公告）日：2004-08-12

  Compounds of formula (I) 1 are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.

  式（I）的化合物是新颖的VR1拮抗剂，可用于治疗疼痛、炎症性热性过敏、尿失禁和膀胱过度活动。
• [EN] BENZOTHIADIAZINE COMPOUNDS<br/>[FR] COMPOSÉS BENZOTHIADIAZINE
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2017098421A1

  公开（公告）日：2017-06-15

  The invention is directed to substituted benzothiadiazine derivatives. Specifically, the invention is directed to compounds according to Formula (I):wherein R, R1, R2, R3, R4 and R5 are as defined herein. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, autoimmune diseases, infections, atherosclerosis, and ischemia-reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

  本发明涉及取代苯并噻二嗪衍生物。具体而言，本发明涉及式(I)化合物：其中R、R1、R2、R3、R4和R5定义如下。本发明的化合物是CD73的抑制剂，可用于治疗癌症、前癌综合症和与CD73抑制相关的疾病，如艾滋病、自身免疫病、感染、动脉粥样硬化和缺血-再灌注损伤。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明更进一步的涉及使用本发明化合物或包含本发明化合物的药物组合物抑制CD73活性和治疗相关疾病的方法。
• N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: Indazoles as phenol isosteres with improved pharmacokinetics
  作者：Paul Bamborough、Richard M. Angell、Inder Bhamra、David Brown、James Bull、John A. Christopher、Anthony W.J. Cooper、Lynsey H. Fazal、Ilaria Giordano、Lucy Hind、Vipulkumar K. Patel、Lisa E. Ranshaw、Martin J. Sims、Philip A. Skone、Kathryn J. Smith、Emma Vickerstaff、Melanie Washington

  DOI：10.1016/j.bmcl.2007.04.029

  日期：2007.8

  2,4-Dianilino pyrimidines are well-known inhibitors of tyrosine kinases including lymphocyte specific kinase (Lek). Structure-activity relationships at the 4-position are discussed and rationalised. Examples bearing a 2-methyl-5-hydroxyaniline substituent at the 4-position were especially potent but showed poor oral pharmacokinetics. Replacement of this substituent by 4-amino(5methyl-IH-indazole) yielded compounds with comparable enzyme potency and improved pharmacokinetic properties. (c) 2007 Elsevier Ltd. All rights reserved.
• Compositions de teinture des fibres kératiniques contenat des dérivés d'indazoles amines et procédé de teinture
  申请人：L'OREAL

  公开号：EP0904769B1

  公开（公告）日：2002-09-25
• FUSED AZABICYCLIC COMPOUNDS THAT INHIBIT VANILLOID RECEPTOR SUBTYPE 1 (VR1) RECEPTOR
  申请人：ABBOTT LABORATORIES

  公开号：EP1660455B1

  公开（公告）日：2008-10-15