发明授权
- 专利标题： Muscarinic antagonists
- 专利标题（中）： 毒蕈碱拮抗剂
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申请号： US602403申请日： 1996-02-16
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公开(公告)号： US5883096A公开(公告)日： 1999-03-16
- 发明人: Derek Lowe , Wei Chang , Joseph Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Wang Yuguang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
- 申请人： Derek Lowe , Wei Chang , Joseph Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Wang Yuguang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
- 申请人地址： NJ Kenilworth
- 专利权人： Schering Corporation
- 当前专利权人： Schering Corporation
- 当前专利权人地址： NJ Kenilworth
- 主分类号： C07D295/08
- IPC分类号： C07D295/08 ; A61K31/335 ; A61K31/357 ; A61K31/36 ; A61K31/365 ; A61K31/4427 ; A61K31/443 ; A61K31/445 ; A61K31/4468 ; A61K31/451 ; A61K31/495 ; A61K31/496 ; A61K31/505 ; A61K31/535 ; A61K31/5375 ; A61K31/5377 ; A61P25/28 ; C07D211/14 ; C07D211/22 ; C07D211/24 ; C07D211/26 ; C07D211/32 ; C07D211/58 ; C07D211/62 ; C07D239/34 ; C07D257/04 ; C07D271/06 ; C07D295/02 ; C07D295/03 ; C07D295/084 ; C07D295/088 ; C07D295/096 ; C07D295/112 ; C07D295/116 ; C07D295/12 ; C07D295/125 ; C07D295/13 ; C07D295/135 ; C07D295/14 ; C07D295/145 ; C07D295/15 ; C07D307/33 ; C07D309/12 ; C07D317/28 ; C07D317/62 ; C07D401/12 ; C07D401/14 ; C07D403/12 ; C07D405/12 ; C07D405/14 ; C07D409/14 ; C07D307/81 ; C07D333/58
摘要：
Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds of formula I ##STR1## wherein one of Y and Z is N and the other is N, CH, or C-alkyl;X is --O--, --SO.sub.0-2 --, amino, substituted amino, --CO--, --CH.sub.2 --, mono or di-substituted methylene, --CS--, --CONR.sup.20 --, --NR.sup.20 --SO.sub.2 --, --NR.sup.20 CO--, --SO.sub.2 NR.sup.20 --, --CH.dbd.CH--, --C.tbd.C-- or --NHC(O)NH--;R is optionally substituted phenyl, aryl or cycloalkyl, or other substituents as defined in the specification;R.sup.1 and R.sup.21 are H, CN or optionally substituted alkyl, or other substituents as defined in the specification;R.sup.2 is optionally substituted cycloalkyl or piperidyl, or other substituents as defined in the specification; andR.sup.3, R.sup.4, R.sup.5, R.sup.20, R.sup.27 and R.sup.28 are as defined in the specification; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease; pharmaceutical compositions and methods of preparation are also disclosed, as well as synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.
公开/授权文献
- US5161912A Apparatus and methods for agricultural irrigation 公开/授权日：1992-11-10
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