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公开(公告)号：WO9805292A3
公开(公告)日：1998-04-02
申请号：PCT/US9713383
申请日：1997-08-06
Applicant: SCHERING CORP
Inventor： 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 , ASBEROM THEODROS , BOYLE CRAIG D , JOSIEN HUBERT B
IPC: 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 , A61K
CPC classification number: 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
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：JP2009040778A
公开(公告)日：2009-02-26
申请号：JP2008194199
申请日：2008-07-28
Applicant: Schering Corp , シェーリング コーポレイションSchering Corporation
Inventor： KOZLOWSKI JOSEPH A , LOWE DEREK B , CHANG WEI K , DUGAR SUNDEEP
IPC: C07D211/58 , C07D295/08 , A61K31/445 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61P25/28 , A61P43/00 , C07D239/34 , C07D241/04 , C07D295/088 , C07D295/096 , C07D311/68 , C07D317/58 , C07D317/62 , C07D405/14
CPC classification number: C07D317/62 , C07B2200/07 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D211/58 , C07D239/34 , C07D295/088 , C07D295/096 , C07D311/68 , C07D317/58
Abstract: PROBLEM TO BE SOLVED: To provide a muscarinic antagonist.
SOLUTION: A di-N-substituted piperazine compound or a 1,4-substituted piperazine compound in accordance with formula (I) is a muscarinic antagonist useful to treat cognitive disorders such as Alzheimer's disease. A synergistic combination of a compound of the above formula with an acetylcholine esterase inhibitor is also disclosed.
COPYRIGHT: (C)2009,JPO&INPITAbstract translation: 要解决的问题：提供毒蕈碱拮抗剂。 解决方案：根据式（I）的二-N-取代的哌嗪化合物或1,4-取代的哌嗪化合物是用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。 版权所有（C）2009，JPO＆INPIT
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公开(公告)号：CA2261725C
公开(公告)日：2005-10-25
申请号：CA2261725
申请日：1997-08-06
Applicant: SCHERING CORP
Inventor： BARNETT ALLEN , SHERLOCK MARGARET , MCQUADE ROBERT , VICE SUSAN F , GREEN MICHAEL J , WANG YUGUANG , BERGER JOEL G , TOM WING , ASBEROM THEODROS , BROWNE MARGARET E , BOYLE CRAIG D , JOSIEN HUBERT B , DUGAR SUNDEEP , KOZLOWSKI JOSEPH A , CLADER JOHN W , MCCOMBIE STUART W , LOWE DEREK B , TAGAT JAYARAM R , CHEN LIAN-YONG , CHACKALAMANNIL SAMUEL , CHANG WEI K , VACCARO WAYNE D
IPC: 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 , C07D417/14 , A61K31/53
Abstract: 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, R1, R2, R3, R4, R21, R22, R28, X, Y and Z a s 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.
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公开(公告)号：CO4900068A1
公开(公告)日：2000-03-27
申请号：CO97045104
申请日：1997-08-06
Applicant: SCHERING CORP
Inventor： LOWE DEREK B , WEI K CHANG , KOZLOWSKI JOSEPH A , BERGER JOEL G , MCQUADE ROBERT , BARNETT ALLEN , SHERLOCK MARGARET , WING TOM , DUGAR SUNDEEP , CHEN LIAN-YONG , CLADER JOHN W
IPC: 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
Abstract: Compuestos de piperazina di-N-sustituida o piperidina1,4-di-sustituida de acuerdo con la fórmula I (incluyendo todos los isómeros, sales, ésteres y solvatos) en donde R, R1 , R2 , R3 , R4 , R21 , R27 , R28 , X, Y y Z son como se definen en la presente, antagonistas muscarínicos útiles para el tratamiento de trastornos cognitivos como ser la enfermedad de Alzheimer. También se describen composiciones farmacéuticas y métodos de preparación. Se describen además combinaciones de compuestos sinérgicas de la fórmula que figura anteriormente con inhibidores de acetilcolinesterasa.
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公开(公告)号：TR9900255T2
公开(公告)日：1999-07-21
申请号：TR9900255
申请日：1997-08-06
Applicant: SCHERING CORP
Inventor： 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 , ASBEROM THEODROS , BOYLE CRAIG D , JOSIEN HUBERT B
IPC: 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
CPC classification number: 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
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Patent Agency Ranking
公开(公告)号：TR199900255T2
公开(公告)日：1999-07-21
申请号：TR9900255
申请日：1997-08-06
Applicant: SCHERING CORP
Inventor： 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 , ASBEROM THEODROS , BOYLE CRAIG D , JOSIEN HUBERT B
IPC: A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , C07D211/58 , 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
Abstract: 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 with acetylcholinesterase inhibitors.
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公开(公告)号：NO990551D0
公开(公告)日：1999-02-05
申请号：NO990551
申请日：1999-02-05
Applicant: SCHERING CORP
Inventor： 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 , ASBEROM THEODROS , BOYLE CRAIG D , JOSIEN HUBERT B
IPC: A61K31/00 , A61K31/435 , C07D211/58 , 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 , C07D
Abstract: 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 with acetylcholinesterase inhibitors.
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公开(公告)号：AT224884T
公开(公告)日：2002-10-15
申请号：AT97931281
申请日：1997-06-26
Applicant: SCHERING CORP
Inventor： KOZLOWSKI JOSEPH A , LOWE DEREK B , CHANG WEI K , DUGAR SUNDEEP
IPC: C07D295/08 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61P25/28 , A61P43/00 , C07D211/58 , C07D239/34 , C07D241/04 , C07D295/088 , C07D295/096 , C07D311/68 , C07D317/58 , C07D317/62 , C07D405/14 , C07D213/643 , C07D405/12 , A61K31/44 , A61K31/35
Abstract: Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula (I) (including all isomers, salts, esters, and solvates), wherein Q, n, R, R , R , R , R , R , R , R , X, 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 with acetylcholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.
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公开(公告)号：AU717431B2
公开(公告)日：2000-03-23
申请号：AU3495397
申请日：1997-06-26
Applicant: SCHERING CORP
Inventor： KOZLOWSKI JOSEPH A , LOWE DEREK B , CHANG WEI K , DUGAR SUNDEEP
IPC: C07D295/08 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61P25/28 , A61P43/00 , C07D211/58 , C07D239/34 , C07D241/04 , C07D295/088 , C07D295/096 , C07D311/68 , C07D317/58 , C07D317/62 , C07D405/14 , C07D213/643 , C07D405/12 , A61K31/44 , A61K31/35
Abstract: Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula (I) (including all isomers, salts, esters, and solvates), wherein Q, n, R, R , R , R , R , R , R , R , X, 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 with acetylcholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.
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公开(公告)号：CZ36699A3
公开(公告)日：1999-06-16
申请号：CZ36699
申请日：1997-08-06
Applicant: SCHERING CORP
Inventor： 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 , ASBEROM THEODROS , BOYLE CRAIG D , JOSIEN HUBERT B
IPC: 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 , C07D417/14
Abstract: 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 with acetylcholinesterase inhibitors.
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