5-(4-(4-cyanobut-1-ynyl)phenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-morpholino-1H-pyrazole-3-carboxamide | 1245626-15-6

• 英文名称: 5-(4-(4-cyanobut-1-ynyl)phenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-morpholino-1H-pyrazole-3-carboxamide
• 英文别名: 5-[4-(4-cyanobut-1-ynyl)phenyl]-1-(2,4-dichlorophenyl)-4-ethyl-N-morpholin-4-ylpyrazole-3-carboxamide
• CAS: 1245626-15-6
• 化学式: C₂₇H₂₅Cl₂N₅O₂
• 分子量: 522.434
• InChiKey: JFCYGCIPHMDEDF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  83.2
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] NOVEL HETERO PYRROLE ANALOGS ACTING ON CANNAPINOID RECEPTORS<br/>[FR] NOUVEAUX ANALOGUES HÉTÉROPYRROLES AGISSANT SUR LES RÉCEPTEURS CANNABINOÏDES
  申请人：UNIV CONNECTICUT

  公开号：WO2010104488A1

  公开（公告）日：2010-09-16

  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.

  本文披露了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。本文披露了作为CB1和/或CB 1受体拮抗剂的杂环吡咯类似物，具有对CB 1或CB2受体的选择性，作为中性拮抗剂，首选作用于外周神经系统中的CB 1受体，和/或作为一氧化氮供体的作用。还披露了使用披露的类似物的药物制剂和通过给予治疗有效量的披露的类似物以提供生理效应的方法。
• 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