(10S)-5-chloro-8-oxa-6-thia-1-azatricyclo[8.3.0.03,7]trideca-3(7),4-dien-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 英文名称: (10S)-5-chloro-8-oxa-6-thia-1-azatricyclo[8.3.0.03,7]trideca-3(7),4-dien-2-one
• 化学式: C₁₀H₁₀ClNO₂S
• 分子量: 243.71
• InChiKey: OYAFEMPNWYIIIF-LURJTMIESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  57.8
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• (PYRIDO/THIENO)-[f]-OXAZEPINE-5-ONE DERIVATIVES
  申请人：Grove Simon James Anthony

  公开号：US20080262221A1

  公开（公告）日：2008-10-23

  The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R 1 , R 2 and R 3 are independently H or (C 1-4 )alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C 1-4 )alkyl, (C 1-4 )alkyloxy, (C 1-4 )alkyloxy(C 1-4 )alkyl, CF 3 , halogen, nitro, cyano, NR 4 R 5 , NR 4 COR 6 , and CONR 4 R 5 ; R 4 and R 5 are independently H or (C 1-4- )alkyl; or R 4 and R 5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR 6 ; R 6 is (C 1-4 )alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C 1-4 )alkyl, (C 1-4 )alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.

  本发明涉及具有通式I的（吡啶/噻吩）-[f]-噁唑烷-5-酮衍生物，其中R1、R2和R3独立地表示H或（C1-4）烷基；Ar代表融合的噻吩或吡啶环，可选地取代一个或多个取代基，所述取代基选择自（C1-4）烷基，（C1-4）烷氧基，（C1-4）烷氧基（C1-4）烷基，CF3，卤素，硝基，氰基，NR4R5，NR4COR6和CONR4R5；R4和R5独立地表示H或（C1-4）烷基；或R4和R5与它们所结合的氮原子一起形成一个5-或6-成员饱和杂环环，可选地含有进一步的杂原子，所述杂原子选择自O、S或NR6；R6为（C1-4）烷基；A表示4-7成员饱和杂环环的残基，可选地含有一个氧原子，所述环可选地用1-3个取代基选择自（C1-4）烷基，（C1-4）烷氧基，羟基，卤素和氧代基取代；或其药学上可接受的盐。本发明还涉及包含所述衍生物的制药组合物以及使用这些（吡啶/噻吩）-[f]-噁唑烷-5-酮衍生物治疗对中枢神经系统中的AMPA受体介导的突触反应增强有响应的神经疾病和精神障碍。
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  申请人：——

  公开号：US7345036B2

  公开（公告）日：2008-03-18
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  公开号：US8034804B2

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