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1. 发明授权

US06288068B1 Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US06288068B1
公开(公告)日：2001-09-11
申请号：US09482168
申请日：2000-01-12
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 , Javaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
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 , Javaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
IPC分类号： C07D31495
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, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alheimer'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 enhancing acetylcholine release with acetylcholinesterase inhibitors.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物（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。

2. 发明授权

US06498168B2 Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US06498168B2
公开(公告)日：2002-12-24
申请号：US09902849
申请日：2001-07-11
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
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
IPC分类号： C07D40102
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, R1, 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 enhancing acetylcholine release with acetylcholinesterase inhibitors.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物（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。

3. 发明授权

US6037352A Muscarinic antagonists 失效
公开(公告)号：US6037352A
公开(公告)日：2000-03-14
申请号：US195742
申请日：1998-11-19
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
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
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 , C07D211/00 , C07D211/08
CPC分类号： C07D211/20 , 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 , C07C2101/14
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) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, 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 enhancing acetylcholine release with acetylcholinesterase inhibitors.

4. 发明授权

US5883096A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US5883096A
公开(公告)日：1999-03-16
申请号：US602403
申请日：1996-02-16
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
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
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
CPC分类号： C07D211/20 , 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 , C07C2101/14
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.
摘要翻译：式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物其中Y和Z之一是N，另一个是N，CH或C-烷基; X是-O - ， - SO 2 - ， - 氨基，取代的氨基，-CO - ， - CH 2 - ，单或二取代的亚甲基，-CS-，-CONR 20 - ，-NR 20 SO 2 - ， - -SO 2 NR 20 - ， - CH = CH - ， - C 3 CF 3 - 或-NHC（O）NH-; R是任选取代的苯基，芳基或环烷基，或说明书中定义的其它取代基; R1和R21是H，CN或任选取代的烷基，或说明书中定义的其它取代基; R2是任选取代的环烷基或哌啶基，或说明书中定义的其它取代基; R3，R4，R5，R20，R27和R28如说明书中所定义; 是可用于治疗认知障碍如阿尔茨海默病的毒蕈碱拮抗剂; 还公开了药物组合物和制备方法，以及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。

5. 发明授权

US5889006A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US5889006A
公开(公告)日：1999-03-30
申请号：US700628
申请日：1996-08-08
申请人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
发明人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
IPC分类号： C07D211/58 , A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/02 , C07D403/02 , C07D403/14
CPC分类号： C07D405/14 , 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 , C07C2101/14
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) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, 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 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 R28，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病的毒蕈碱性拮抗剂。还公开了药物组合物和制备方法。还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

6. 发明授权

US6043255A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US6043255A
公开(公告)日：2000-03-28
申请号：US266079
申请日：1999-03-10
申请人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
发明人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
IPC分类号： C07D211/58 , A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/02
CPC分类号： C07D405/14 , 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 , C07C2101/14
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) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, 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 with acetylcholinesterase inhibitors.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物（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。还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

7. 发明授权

US5362728A 4,5-bridged-2,3,4,5-tetrahydro-1H-3-benzazepine-7-ols and derivatives and compositions and methods employing such compounds 失效
标题翻译： 4,5桥连-2,3,4,5-四氢-1H-3-苯并氮杂-7-醇及其衍生物和组合物和方法
公开(公告)号：US5362728A
公开(公告)日：1994-11-08
申请号：US915710
申请日：1992-07-29
申请人： Theodros Asberom , Edward O'Connor , Joel G. Berger , John W. Clader
发明人： Theodros Asberom , Edward O'Connor , Joel G. Berger , John W. Clader
IPC分类号： A61K31/55 , A61P25/04 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/30 , C07D223/18 , C07D223/32
CPC分类号： C07D223/18 , C07D223/32
摘要： Novel benzazepines of the formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R represents H, alkyl, allyl or ##STR2## A represents --[CR.sup.1 R.sup.2].sub.n --; n represents 3 or 4; R.sup.1 and R.sup.2 may be the same or different and each independently represents H, OH, atkyl, alkoxy, phnenyl or substituted phenyl, with the proviso that R.sup.1 and R.sup.2 on the same carbon atom are not both OH, or R.sup.1 and R.sup.2 on the same carbon atom together represent=O;G represents H, R.sup.3 (CO)-- or ArNHCO--;R.sup.3 represents H, alkyl, alkoxy, phenyl or substituted phenyl;Ar represents phenyl or substituted phenyl; andY and Z may be the same or different and each is independently selected from H, halo, alkyl, alkoxy or halpalkyl;the pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, useful in the treatment of psychoses, drug dependence, D1 dependent neurological disorder or pain are disclosed.
摘要翻译： PCT No.PCT / US91 / 00503 Sec。 371日期：1992年7月29日 102（e）日期1992年7月29日PCT PCT 1991年1月31日PCT。式I的新的苯并氮杂：其中R表示H，烷基，烯丙基或A表示 - [CR1R2] n- n表示3或4; R1和R2可以相同或不同，并且各自独立地表示H，OH，烷基，烷氧基，苯基或取代的苯基，条件是相同碳原子上的R 1和R 2不同时为OH，或者R 1和R 2在同一个上碳原子一起代表= O; G表示H，R 3（CO） - 或ArNHCO-; R 3表示H，烷基，烷氧基，苯基或取代的苯基; Ar表示苯基或取代的苯基; 并且Y和Z可以相同或不同，并且各自独立地选自H，卤素，烷基，烷氧基或卤代烷基; 公开了可用于治疗精神病，药物依赖性，D1依赖性神经障碍或疼痛的药学上可接受的盐及其药物组合物。

8. 发明授权

US5416118A Bicyclic amides as inhibitors of acyl-coenzyme A: cholesterol acyl transferase 失效
标题翻译：作为酰基辅酶A：胆固醇酰基转移酶的抑制剂的双环酰胺
公开(公告)号：US5416118A
公开(公告)日：1995-05-16
申请号：US122537
申请日：1993-09-28
申请人： John W. Clader , Thomas Fevig , Wayne Vaccaro , Joel G. Berger
发明人： John W. Clader , Thomas Fevig , Wayne Vaccaro , Joel G. Berger
IPC分类号： C07C233/11 , C07C233/23 , C07C275/24 , C07D213/40 , A61K31/165 , A61K31/35 , A61K31/44
CPC分类号： C07D213/40 , C07C233/11 , C07C233/23 , C07C275/24 , C07C2102/08 , C07C2102/10 , C07C2102/12
摘要： Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.2 -substituted heteroarylene groups; an interrupted alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain of 4 to 25 carbon atoms, interrupted by one or more --NH--, --C(O)-- or --N(lower alkyl)-- groups; an interrupted alkyl chain of 4 to 25 carbon atoms substituted by one or more phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl groups; a diphenylamino group; a di-(R.sup.2 -substituted phenyl)amino group; a diheteroarylamino group; or a di-(R.sup.2 -substituted heteroaryl)amino group;or a pharmaceutically acceptable salt thereof, useful in the treatment of artherosclerosis are disclosed.
摘要翻译： PCT No.PCT / US92 / 02662 Sec。 371日期：1993年9月28日 102（e）日期1993年9月28日PCT提交1992年4月9日PCT公布。第WO92 / 18462号公报日期：1992年10月29日。式IMA IMA的新型双环酰胺其中Ar 1和Ar 2是苯基，R 2取代的苯基，杂芳基或R 2取代的杂芳基，其中R 2是1至3个独立地选自卤代，羟基，低级烷基，低级烷氧基，硝基，氨基，低级烷基氨基和低级二烷基氨基; X，Y和Z是-CH 2 - ， - CH（烷基） - ， - C（烷基）2 - ， - NH - ， - N（烷基） - ， - O-或-SOr，其中r是0,1或 2，m，n和p为0或1; R1是1〜25个碳原子的烷基链; 被一个或多个任选取代的苯基或杂芳基取代的烷基链; 烷基链-O-，-SOr，亚苯基，R 2取代的亚苯基，亚杂芳基或R 2取代的亚杂芳基; 被一个或多个任选取代的苯基或杂芳基取代的间断烷基链; 4个至25个碳原子的烷基链，被一个或多个-NH-，-C（O） - 或-N（低级烷基）基团间隔; 被一个或多个苯基，R 2取代的苯基，杂芳基或R 2取代的杂芳基取代的具有4至25个碳原子的中断的烷基链; 二苯基氨基; 二（R 2取代苯基）氨基; 二杂芳基氨基; 或二（R 2取代的杂芳基）氨基; 或其药学上可接受的盐，其可用于治疗动脉粥样硬化。

9. 发明授权

US4973586A Fused benzazepines, compositions of, and medical use thereof 失效
标题翻译：熔融苯并氮杂，其组成和医疗用途
公开(公告)号：US4973586A
公开(公告)日：1990-11-27
申请号：US223739
申请日：1988-07-18
申请人： Joel G. Berger , Wei K. Chang , Elijah H. Gold , John W. Clader
发明人： Joel G. Berger , Wei K. Chang , Elijah H. Gold , John W. Clader
IPC分类号： C07D223/14 , A61K31/55 , A61K31/675 , A61P25/30 , A61P39/02 , C07D223/32 , C07D401/12 , C07D403/06 , C07D403/12 , C07D491/04 , C07D491/044 , C07D491/052 , C07D495/04 , C07D495/14 , C07F9/553 , C07F9/6561
CPC分类号： C07D223/14 , A61K31/55 , C07D491/04
摘要： Disclosed are fused benzazepine compounds, pharmaceutical compositions including such compounds, methods of using such compounds, for example, in the treatment of psychoses and/or depression, and intermediates useful in the preparation of such compounds.
摘要翻译：公开了稠合苯并氮杂化合物，包括这些化合物的药物组合物，使用这些化合物的方法，例如治疗精神病和/或抑郁症，以及可用于制备这些化合物的中间体。

10. 发明授权

US5374722A Bridged benzazepines 失效
标题翻译：桥接苯并氮杂
公开(公告)号：US5374722A
公开(公告)日：1994-12-20
申请号：US27167
申请日：1993-03-16
申请人： Joel G. Berger , Wei K. Chang , John W. Clader
发明人： Joel G. Berger , Wei K. Chang , John W. Clader
IPC分类号： A61K31/55 , A61P25/18 , C07D223/14 , C07D223/32 , C07D223/16 , C07D223/18
CPC分类号： C07D223/32 , C07D223/14
摘要： The compound ##STR1## is useful as an agent in the treatment of psychoses and drug dependence and for providing an analgesic effect.
摘要翻译： PCT No.PCT / US91 / 06705 Sec。 371日期1993年3月16日 102（e）1993年3月16日PCT 1991年9月20日PCT。化合物II可用作治疗精神病药物依赖和提供镇痛作用的药剂。

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