5-(4-(4-azidobut-1-ynyl)phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide | 1245626-04-3

• 英文名称: 5-(4-(4-azidobut-1-ynyl)phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide
• 英文别名: 5-[4-(4-azidobut-1-ynyl)phenyl]-1-(2,4-dichlorophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide
• CAS: 1245626-04-3
• 化学式: C₂₆H₂₅Cl₂N₇O
• 分子量: 522.437
• InChiKey: UEDPQUKNBDOVEV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.4
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  64.5
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• NOVEL HETEROPYRROLE ANALOGS ACTING ON CANNABINOID RECEPTORS
  申请人：Makriyannis Alexandros

  公开号：US20120046280A1

  公开（公告）日：2012-02-23

  Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.

  本发明涉及一种生物活性的杂环吡咯类似物，如咪唑、噻唑、噁唑和吡唑，能够与CB1和/或CB2大麻素受体相互作用。其中一些方面揭示了作为CB1和/或CB1受体拮抗剂的杂环吡咯类似物，具有选择性作用于CB1或CB2受体，作为中性拮抗剂，优先作用于位于周围神经系统中的CB1受体，和/或作为一氧化氮供体。还揭示了采用所述类似物的制药制剂和治疗有效量的方法，以提供生理效应。
• US8853205B2
  申请人：——

  公开号：US8853205B2

  公开（公告）日：2014-10-07