(R)-1-benzyl-7-chloro-3-(4-hydroxy-phenyl)-3-methyl-5-piperazin-1-yl-1H-quinoline-2,4-dione | 929116-83-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: (R)-1-benzyl-7-chloro-3-(4-hydroxy-phenyl)-3-methyl-5-piperazin-1-yl-1H-quinoline-2,4-dione
• 英文别名: 9KE3M69Zbl；(3R)-1-benzyl-7-chloro-3-(4-hydroxyphenyl)-3-methyl-5-piperazin-1-ylquinoline-2,4-dione
• CAS: 929116-83-6
• 化学式: C₂₇H₂₆ClN₃O₃
• 分子量: 475.975
• InChiKey: QFOBHYKKXFZEPW-HHHXNRCGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  34
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  72.9
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• N-Substituted-1H-Quinoline-2,4-Diones, Preparation Method Thereof, And Pharmaceutical Composition Containing The Same
  申请人：Seong Churlmin

  公开号：US20080275058A1

  公开（公告）日：2008-11-06

  The present invention relates to compounds of N-substituted -1H-quinoline-2,4-diones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of N-substituted-1H-quinoline-2,4-diones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by methamphetamine and don't show rotatod deficit in mice. Thereof the compounds according to the present invention may be valuably used for treatment if a 5HT6 receptor relating disorder

  本发明涉及N-取代-1H-喹啉-2,4-二酮化合物，其作为5HT6受体拮抗剂，其制备方法以及含有该化合物的制剂，用于治疗中枢神经系统疾病。根据本发明的N-取代-1H-喹啉-2,4-二酮化合物具有优异的5HT6受体结合亲和力和对5HT6受体的优异选择性。此外，这些化合物能够逆转甲基苯丙胺引起的PPI破坏，并且在小鼠中不表现出旋转缺陷。因此，根据本发明的化合物可以有价值地用于治疗与5HT6受体相关的疾病。
• N-SUBSTITUTED-1H-QUINOLINE-2, 4-DIONES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
  申请人：KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

  公开号：EP1954689A1

  公开（公告）日：2008-08-13
• EP1954689A4
  申请人：——

  公开号：EP1954689A4

  公开（公告）日：2009-09-02
• [EN] N-SUBSTITUTED-1H-QUINOLINE-2, 4-DIONES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME<br/>[FR] 1H-QUINOLINE-2,4-DIONES A SUBSTITUTION N, PROCEDE DE PREPARATION DE CES COMPOSES ET COMPOSITION PHARMACEUTIQUE RENFERMANT CEUX-CI
  申请人：KOREA RESERACH INST OF CHEMICA

  公开号：WO2007032572A1

  公开（公告）日：2007-03-22

  [EN] The present invention relates to compounds of N-substituted-1H-quinoline-2,4-diones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of N-substituted-1H-quinoline-2,4-diones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by methamphetamine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders.
  [FR] L'invention concerne des composés de 1H-quinoline-2,4-diones à substitution N agissant comme un antagoniste du récepteur 5HT6, un procédé de préparation de ceux-ci, une composition pharmaceutique contenant ces composés et destinée à traiter les troubles du système nerveux central. Les composés de 1H-quinoline-2,4-diones à substitution N possèdent une excellente affinité de liaison pour le récepteur 5HT6, et une excellente sélectivité à l'égard du récepteur 5HT6 par rapport aux autres récepteurs. De plus, ces composés ont pour effet d'inverser l'interruption de l'inhibition du réflexe de sursaut (PPI) par la méthamphétamine, et n'engendrent pas d'insuffisance au test rotarod chez les souris. Lesdits composés peuvent être avantageusement utilisés dans le traitement de troubles liés au récepteur 5HT6.