发明公开
- 专利标题: HETEROCYCLIC MGLU5 ANTAGONISTS
- 专利标题(中): 杂环的mGlu5拮抗剂
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申请号: EP10759812.0申请日: 2010-09-14
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公开(公告)号: EP2477981A1公开(公告)日: 2012-07-25
- 发明人: LEONARDI, Amedeo , MOTTA, Gianni , RIVA, Carlo , GUARNERI, Luciano , GRAZIANI, Davide , MARINONI, Fabio , BETTINELLI, Ilaria
- 申请人: Recordati Ireland Limited
- 申请人地址: Raheens East Ringaskiddy County Cork IE
- 专利权人: Recordati Ireland Limited
- 当前专利权人: Recordati Ireland Limited
- 当前专利权人地址: Raheens East Ringaskiddy County Cork IE
- 代理机构: McKelvey, Ian Edward
- 优先权: US242208P 20090914
- 国际公布: WO2011029633 20110317
- 主分类号: C07D403/14
- IPC分类号: C07D403/14 ; C07D405/14 ; C07D409/14 ; C07D413/14 ; C07D417/14 ; A61K31/4523 ; A61P13/00
摘要:
Compounds (I) (R
1 is an optionally substituted C
1 -C
13 heteromonocyclic, heterobicyclic or heterotri cyclic group containing from 1 to 5 heteroatoms selected from N, O and S; R
2 is H, an optionally substituted monocyclic aromatic group, or a C
1 -C
5 heteroaromatic group containing from 1 to 4 heteroatoms selected from N, O and S; R
3 is an optionally substituted C
1 -C
13 heteromonocyclic, heterobicyclic or heterotri cyclic group containing from 1 to 5 heteroatoms selected from N, O and S; an optionally substituted mono-, bi- or tricyclic C
6 -C
14 aryl group, an optionally substituted C
3 -C
6 cycloalkyl group, or an optionally substituted C
3 -C
6 cycloalkenyl group; each R
4 , independently for each position capable of substitution, is H or C
1 -C
6 alkyl; R
5 is H, halogen or C
1 -C
6 alkyl; m is 0, 1 or 2; n is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, or 6; and --- is an optional double bond) and their enantiomers, diastereomers, N-oxides and pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful for the treatment of neuromuscular dysfunction of the lower urinary tract and also for the treatment of gastrooesophageal reflux disease; anxiety disorder; abuse, substance dependence and substance withdrawal disorders; neuropathic pain disorder, migraine and fragile X syndrome disorders.
1 is an optionally substituted C
1 -C
13 heteromonocyclic, heterobicyclic or heterotri cyclic group containing from 1 to 5 heteroatoms selected from N, O and S; R
2 is H, an optionally substituted monocyclic aromatic group, or a C
1 -C
5 heteroaromatic group containing from 1 to 4 heteroatoms selected from N, O and S; R
3 is an optionally substituted C
1 -C
13 heteromonocyclic, heterobicyclic or heterotri cyclic group containing from 1 to 5 heteroatoms selected from N, O and S; an optionally substituted mono-, bi- or tricyclic C
6 -C
14 aryl group, an optionally substituted C
3 -C
6 cycloalkyl group, or an optionally substituted C
3 -C
6 cycloalkenyl group; each R
4 , independently for each position capable of substitution, is H or C
1 -C
6 alkyl; R
5 is H, halogen or C
1 -C
6 alkyl; m is 0, 1 or 2; n is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, or 6; and --- is an optional double bond) and their enantiomers, diastereomers, N-oxides and pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful for the treatment of neuromuscular dysfunction of the lower urinary tract and also for the treatment of gastrooesophageal reflux disease; anxiety disorder; abuse, substance dependence and substance withdrawal disorders; neuropathic pain disorder, migraine and fragile X syndrome disorders.
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