发明授权
US07803820B2 3-triazolylthiaalkyl-3-azabicyclo (3-1-O) hexanes and their use as dopamine D3 receptor ligands
失效
3-三唑基硫杂烷基-3-氮杂双环(3-1-O)己烷及其作为多巴胺D3受体配体的用途
- 专利标题: 3-triazolylthiaalkyl-3-azabicyclo (3-1-O) hexanes and their use as dopamine D3 receptor ligands
- 专利标题(中): 3-三唑基硫杂烷基-3-氮杂双环(3-1-O)己烷及其作为多巴胺D3受体配体的用途
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申请号: US11911035申请日: 2006-04-12
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公开(公告)号: US07803820B2公开(公告)日: 2010-09-28
- 发明人: Daniele Andreotti , Anna Checchia , Dieter Hamprecht , Fabrizio Micheli
- 申请人: Daniele Andreotti , Anna Checchia , Dieter Hamprecht , Fabrizio Micheli
- 申请人地址: GB Middlesex
- 专利权人: Glaxo Group Limited
- 当前专利权人: Glaxo Group Limited
- 当前专利权人地址: GB Middlesex
- 代理商 James N. Kanagy; Edward R. Gimmi; Charles M. Kinzig
- 优先权: GB0507601.3 20050414
- 国际申请: PCT/EP2006/003553 WO 20060412
- 国际公布: WO2006/108700 WO 20061019
- 主分类号: A61K31/41
- IPC分类号: A61K31/41 ; C07D249/08 ; C07D257/00
摘要:
The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R3 comprises at least one SF5 group as a substituent; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
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