公开(公告)号：EP1319003A1

公开(公告)日：2003-06-18

申请号：EP01971092.0

申请日：2001-09-17

申请人： SCHERING CORPORATION

发明人： CHACKALAMANNIL, Samuel ,  WANG, Yuguang ,  BOYLE, Craig, D. ,  STAMFORD, Andrew, W.

IPC分类号： C07D473/04 ,  C07D473/06 ,  C07D473/08 ,  A61K31/522 ,  A61P15/00 ,  A61P9/00

CPC分类号： C07D473/04 ,  C07D473/06 ,  C07D473/08

摘要： A xanthine phosphodiesterase V inhibitor having the formula (I), where R4 is a C¿3-15? cycloalkyl group, with or without one or more substituents, C3-15 cycloalkenyl group, with or without one or more substituents, or a heterocycloalkyl group of 3 to 15 members, with or without one or more substituents; useful for treating male (erectile) and female sexual dysfunction and other physiological disorders. For example, a representative compound of the invention is formula (II).

公开(公告)号：EP0938483A2

公开(公告)日：1999-09-01

申请号：EP97936296.0

申请日：1997-08-06

申请人： SCHERING CORPORATION

发明人： LOWE, Derek, B. ,  CHANG, Wei, K. ,  KOZLOWSKI, Joseph, A. ,  BERGER, Joel, G. ,  McQUADE, Robert ,  BARNETT, Allen ,  SHERLOCK, Margaret ,  TOM, Wing ,  DUGAR, Sundeep ,  CHEN, Lian-Yong ,  CLADER, John, W. ,  CHACKALAMANNIL, Samuel ,  WANG, Yuguang ,  McCOMBIE, Stuart, W. ,  TAGAT, Jayaram, R. ,  VICE, Susan, F. ,  VACCARO, Wayne, D. ,  GREEN, Michael, J. ,  BROWNE, Margaret, E. ,  BOYLE, Craig, D. ,  JOSIEN, Hubert, B. ,  ASBEROM, Theodros

IPC分类号： C07D211 ,  A61K31 ,  A61K45 ,  A61P25 ,  C07D239 ,  C07D257 ,  C07D295 ,  C07D401 ,  C07D405 ,  C07D409 ,  C07D413

CPC分类号： C07D405/14 ,  C07C2601/14 ,  C07D211/24 ,  C07D211/32 ,  C07D239/34 ,  C07D257/04 ,  C07D295/03 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096 ,  C07D295/112 ,  C07D295/116 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/145 ,  C07D295/15 ,  C07D405/12 ,  C07D409/14

摘要： Di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R?1, R2, R3, R4, R21, R27, R28¿, X, Y and Z as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

公开(公告)号：EP0811002A2

公开(公告)日：1997-12-10

申请号：EP96906286.0

申请日：1996-02-16

申请人： SCHERING CORPORATION

发明人： LOWE, Derek ,  CHANG, Wei ,  KOZLOWSKI, Joseph ,  BERGER, Joel, G. ,  McQUADE, Robert ,  BARNETT, Allen ,  SCHERLOCK, Margaret ,  TOM, Wing ,  DUGAR, Sundeep ,  CHEN, Lian-Yong ,  CLADER, John, W. ,  CHACKALAMANNIL, Samuel ,  MCCOMBIE, Stuart W. ,  TAGAT, Jayaram R. ,  VICE, Susan F. ,  VACCARO, Wayne ,  WANG, Yuguang ,  GREEN, Michael J. ,  BROWNE, Margaret E. ,  ASBEROM, Theodros

IPC分类号： C07D295 ,  A61K31 ,  A61P25 ,  C07D211 ,  C07D239 ,  C07D257 ,  C07D271 ,  C07D307 ,  C07D309 ,  C07D317 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409

CPC分类号： C07D211/20 ,  C07C2601/14 ,  C07D211/22 ,  C07D211/24 ,  C07D211/32 ,  C07D211/58 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68 ,  C07D237/14 ,  C07D239/34 ,  C07D239/38 ,  C07D257/04 ,  C07D277/34 ,  C07D295/03 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096 ,  C07D295/112 ,  C07D295/116 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/145 ,  C07D295/15 ,  C07D295/26 ,  C07D307/33 ,  C07D333/20 ,  C07D335/02 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14

摘要： Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula (I) (including all isomers, salts, esters, and solvates) wherein R, R?1, R2, R3, R4, R21, R27, R28¿, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhan cing acetylcholine release with acetylcholinesterase inhibitors.

摘要翻译： 根据式I的二-N-取代哌嗪或1,4-二取代哌啶化合物（包括所有异构体，盐，酯和溶剂合物），其中R，R 1，R 2，R 3，R 4，R 21，R 27，R 28，X ，Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了药物组合物和制备方法。 还公开了上述化合物或能够与乙酰胆碱酯酶抑制剂一起增强乙酰胆碱释放的其它化合物的协同组合。