发明公开
EP2477981A1 HETEROCYCLIC MGLU5 ANTAGONISTS 审中-公开
杂环的mGlu5拮抗剂

HETEROCYCLIC MGLU5 ANTAGONISTS
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.
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