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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在此定义为NR2B亚型选择性受体拮抗剂。包含式(I)的化学实体的药物组合物,以及与NR2B拮抗作用相关的各种疾病和疾病,例如CN的疾病和式(I)的化学实体,也公开了通过施用治疗方法。除其他内容中,本发明提供了NR2B受体拮抗剂,其具有改善的药代动力学性能,口服活性,心血管安全性和体外和体内治疗安全指标措施所例举的一个或多个点。满足需求。

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