8-(Trifluoromethyl)imidazo[1,2-a]pyrazine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡嗪类
• 英文名称: 8-(Trifluoromethyl)imidazo[1,2-a]pyrazine
• 英文别名: 8-(trifluoromethyl)imidazo[1,2-a]pyrazine
• 化学式: C₇H₄F₃N₃
• 分子量: 187.12
• InChiKey: CCORZFFPRUFFRC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  30.2
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• [EN] HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS<br/>[FR] COMPOSÉS HÉTÉROAROMATIQUES ET LEUR UTILISATION COMME LIGANDS DE LA DOPAMINE D1
  申请人：PFIZER

  公开号：WO2014072881A1

  公开（公告）日：2014-05-15

  The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced β- arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.

  本发明部分提供了化合物I的公式：及其药学上可接受的盐和N-氧化物；制备的过程和中间体；以及其组合物和用途。本发明进一步提供了具有减少D1R耐受性的D1激动剂，相对于多巴胺具有减少β-阿雷斯汀招募活性的D1激动剂，当结合到D1R时与D1R的Ser188显著相互作用但与Ser202的相互作用不显著的D1激动剂，当结合到D1R时与D1R的Asp103相互作用较弱并且与Ser198相互作用较弱的D1激动剂，以及它们的用途。
• [EN] PESTICIDALLY ACTIVE BI- OR TRICYCLIC HETEROCYCLES WITH SULFUR CONTAINING SUBSTITUENTS<br/>[FR] HÉTÉROCYCLES BI- OU TRICYCLIQUES À ACTION PESTICIDE AVEC SUBSTITUANTS SOUFRÉS
  申请人：SYNGENTA PARTICIPATIONS AG

  公开号：WO2015000715A1

  公开（公告）日：2015-01-08

  Pesticidally active bi-or tricyclic heterocycles with sulphur-containing substituents, stereoisomers and tautomeric forms thereof that can be used as insecticides and can be prepared in a manner known per se.

  具有含硫取代基的杀虫活性的双环或三环杂环化合物，其立体异构体和互变异构体形式可用作杀虫剂，并可按照已知方法制备。
• PESTICIDALLY ACTIVE BI- OR TRICYCLIC HETEROCYCLES WITH SULFUR CONTAINING SUBSTITUENTS
  申请人：SYNGENTA PARTICIPATIONS AG

  公开号：US20160255837A1

  公开（公告）日：2016-09-08

  Pesticidally active bi- or tricyclic heterocycles with sulphur-containing substituents, stereoisomers and tautomeric forms thereof that can be used as insecticides and can be prepared in a manner known per se.

  具有含硫取代基的双环或三环杂环的杀虫活性化合物，其立体异构体和互变异构体可以用作杀虫剂，并可以采用已知的方法制备。
• Pesticidally active bi- or tricyclic heterocycles with sulfur containing substituents
  申请人：Syngenta Participations AG

  公开号：US10939682B2

  公开（公告）日：2021-03-09

  Pesticidally active bi- or tricyclic heterocycles with sulphur-containing substituents, stereoisomers and tautomeric forms thereof that can be used as insecticides and can be prepared in a manner known per se.

  具有杀虫活性的含硫取代基的双环或三环杂环化合物及其立体异构体和同分异构体，可用作杀虫剂，并能以本身已知的方式制备。
• HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS
  申请人：Pfizer Inc.

  公开号：EP2917219A1

  公开（公告）日：2015-09-16