发明申请
US20030195185A1 Azetidinyl diamines useful as ligands of the nociceptin receptor ORL-1
审中-公开
可用作伤害感受肽受体ORL-1的配体的氮杂环丁烷二胺
- 专利标题： Azetidinyl diamines useful as ligands of the nociceptin receptor ORL-1
- 专利标题（中）： 可用作伤害感受肽受体ORL-1的配体的氮杂环丁烷二胺
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申请号： US10294814申请日： 2002-11-14
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公开(公告)号： US20030195185A1公开(公告)日： 2003-10-16
- 发明人: Duane A. Burnett , Mary Ann Caplen , Michael F. Czarniecki , Martin S. Domalksi , Ginny D. Ho , Deen Tulshian , Wen-Lian Wu
- 申请人： Schering Corporation
- 申请人地址： null
- 专利权人： Schering Corporation
- 当前专利权人： Schering Corporation
- 当前专利权人地址： null
- 主分类号： A61K031/506
- IPC分类号： A61K031/506 ; A61K031/454 ; A61K031/397 ; C07D43/02 ; C07D205/00
摘要：
Disclosed are nociceptin ORL-1 receptor agonists of the formula 1 wherein: (a) R1 is optionally substituted alkyl, fluorenyl, pyrimidinyl or optionally substituted piperidinyl; R2 is H; and R3 is nullC(H)(R)nullNR7R8; R is H, optionally substituted aryl or arylalkyl, or heteroaryl; R7 is null(CH2)xR9, optionally substituted tetrahydronaphthyl, or cycloalkyl; and R8 is H; or R7 and R8 together form a substituted piperidinyl or piperazinyl ring; x is 0-10; and R9 is H, alkoxy, optionally substituted phenyl, naphthyl, heteroaryl, pyrrolidinyl, pyrrolidonyl, optionally substituted piperidinyl or diphenylmethyl; or (b) R2is nullNHR7or 2 and R3 is H; pharmaceutical compositions; and methods of using the compounds to treat cough and pain.
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