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HETEROCYCLIC M-GLU5 ANTAGONISTS
专利权人:
Luciano Guarneri;Amedeo Leonardi;Carlo Riva;Fabio Marinoni;Gianni Motta;Davide Graziani;Ilaria Bettinelli
发明人:
Amedeo Leonardi,Carlo Riva,Luciano Guarneri,Davide Graziani,Fabio Marinoni,Gianni Motta,Ilaria Bettinelli
申请号:
US12882169
公开号:
US20120028931A1
申请日:
2010.09.14
申请国别(地区):
US
年份:
2012
代理人:
摘要:
Compounds I(R1 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotricyclic group containing from 1 to 5 heteroatoms selected from N, O and S;R2 is H, an optionally substituted monocyclic aromatic group, or a C1-C5 heteroaromatic group containing from 1 to 4 heteroatoms selected from N, O and S;R3 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotricyclic group containing from 1 to 5 heteroatoms selected from N, O and S; an optionally substituted mono-, bi- or tricyclic C6-C14 aryl group, an optionally substituted C3-C6 cycloalkyl group, or an optionally substituted C3-C6 cycloalkenyl group;each R4, independently for each position capable of substitution, is H or C1-C6 alkyl;R5 is H, halogen or C1-C6 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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