首页> 外国专利> 3,3-Difluoropiperidine carbamate heterocyclic compounds as NR2 BNMDA receptor antagonists

3,3-Difluoropiperidine carbamate heterocyclic compounds as NR2 BNMDA receptor antagonists

机译:3,3-二氟哌啶氨基甲酸酯杂环化合物作为NR2 BNMDA受体拮抗剂

摘要

Chemical entities of formula (I), wherein R 1 and Z are defined herein, are disclosed as NR2B subtype selective receptor antagonists. Pharmaceutical compositions comprising a chemical entity of formula (I), and various diseases and disorders associated with NR2B antagonism, eg, diseases and disorders of the CNS such as depression, chemical entities of formula (I) Also disclosed are methods of treating by administering. The present invention provides, among other things, an NR2B receptor antagonist with improved pharmacokinetic performance, oral activity, cardiovascular safety and one or more points exemplified by in vitro and in vivo therapeutic safety index measures. Address the need.
机译:式(I)的化学实体,其中R 1 和Z在本文中定义,被公开为NR2B亚型选择性受体拮抗剂。包含式(I)的化学实体和与NR2B拮抗作用有关的各种疾病和病症(例如CNS的疾病和病症,例如抑郁症)的药物组合物,还公开了通过给药进行治疗的方法。本发明尤其提供了具有改善的药代动力学性能,口服活性,心血管安全性和一个或多个要点的NR2B受体拮抗剂,其通过体外和体内治疗安全性指数测量来举例说明。解决需求。

著录项

  • 公开/公告号JP2018522831A

    专利类型

  • 公开/公告日2018-08-16

    原文格式PDF

  • 申请/专利号JP20170562029

  • 发明设计人 シャピロ;ギデオン;

    申请日2016-05-31

  • 分类号C07D487/04;C07D471/04;C07D401/12;A61K31/4985;A61K31/4545;A61K31/519;A61K31/506;A61K31/497;A61P43;A61P25/24;A61P25/04;A61P25/16;A61P25/14;A61P25/28;A61P25;A61P25/08;A61P25/06;

  • 国家 JP

  • 入库时间 2022-08-21 13:12:09

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