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1. 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。

2. 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。

3. 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。

4. 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.

5. 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。

6. 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。

7. 发明授权

US08114879B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US08114879B2
公开(公告)日：2012-02-14
申请号：US12055900
申请日：2008-03-26
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31/497 , C07D403/00
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是氢或烷基; R 2是取代的苯基，取代的杂芳基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R4，R5和R7是氢或烷基; R6是氢，烷基或烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

8. 发明授权

US06689765B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：可用作CCR5拮抗剂的哌嗪衍生物
公开(公告)号：US06689765B2
公开(公告)日：2004-02-10
申请号：US10061011
申请日：2002-01-30
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31695
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v, host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5，R 5和R 5独立地选自氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基， R 7为氢或烷基; R 6为氢，烷基或烯基;用于治疗HIV，实体器官移植排斥，移植物v，宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，公开了牛皮癣，哮喘，过敏或多发性硬化，以及新化合物，包含它们的药物组合物，以及本发明的CCR5拮抗剂与用于治疗可用于治疗炎性疾病的HIV或药物。

9. 发明授权

US06391865B1 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US06391865B1
公开(公告)日：2002-05-21
申请号：US09562814
申请日：2000-05-01
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Eric Gilbert , Marc A. Labroli
IPC分类号： A01N5500
CPC分类号： A61K31/496 , A61K45/06 , C07D211/58 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用式5的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基 - R 4是氢或烷基; R 6是氢，烷基或链烯基; R 4是氢或烷基; R 3是氢，烷基或烷氧基烷基，公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

10. 发明授权

US06387930B1 Piperidine derivatives useful as CCR5 antagonists 有权
标题翻译：哌啶衍生物可用作CCR5拮抗剂
公开(公告)号：US06387930B1
公开(公告)日：2002-05-14
申请号：US09562815
申请日：2000-05-01
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
IPC分类号： C07D40104
CPC分类号： C07D401/14 , C07D211/58 , C07D413/14 , C07D417/14
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—, R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中X是-C（R 13）2 - ， - C（R 13）（R 19） - ， - C（O） - ， - O - N（烷基） - ，R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是H，烷基或烯基; R2是任选取代的苯基，苯基烷基，杂芳基或杂芳基烷基，萘基，芴基或二苯基甲基; R 3是任选取代的苯基，杂芳基或萘基; R4是H，烷基，氟代烷基，环丙基甲基，-CH2CH2OH，-CH2CH2-O-烷基，-CH2C（O）-O-烷基，-CH2C（O）NH2，-CH2C（O）或-CH 2 C（O）-N（烷基）2; R 19是任选取代的苯基，杂芳基或萘基，环烷基，环烷基烷基或烷氧基烷基; 和R 5，R 13，R 14，R 15和R 16是氢或烷基，用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化以及新化合物，包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

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