Margaret A Browne

US Patent:

6498168, Dec 24, 2002

Filed:

Jul 11, 2001

Appl. No.:

09/902849

Inventors:

Derek Lowe - Scotch Plains NJ
Wei Chang - Livingston NJ
Joseph Kozlowski - Princeton NJ
Joel G. Berger - Cedar Grove NJ
Robert McQuade - Scotch Plains NJ
Allen Barnett - Pine Brook NJ
Margaret Sherlock - Bloomfield NJ
Wing Tom - Cedar Grove NJ
Sundeep Dugar - Bridgewater NJ
John W Clader - Cranford NJ
Samuel Chackalamannil - East Brunswick NJ
Wang Yuguang - North Brunswick NJ
Stuart W. McCombie - Caldwell NJ
Jayaram R. Tagat - Westfield NJ
Susan F. Vice - Mountainside NJ
Wayne Vaccaro - Yardley PA
Michael J. Green - Skillman NJ
Margaret E. Browne - Bloomfield NJ
Theodros Asberom - West Orange NJ

Assignee:

Schering Corporation - Kenilworth NJ

International Classification:

C07D40102

US Classification:

514316, 546186, 546187, 546188, 546189

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, R , R , R , R , R , R , R , X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimers 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.

US Patent:

58830960, Mar 16, 1999

Filed:

Feb 16, 1996

Appl. No.:

8/602403

Inventors:

Derek Lowe - Scotch Plains NJ
Wei Chang - Livingston NJ
Joseph Kozlowski - Princeton NJ
Joel G. Berger - Cedar Grove NJ
Robert McQuade - Scotch Plains NJ
Allen Barnett - Pine Brook NJ
Margaret Sherlock - Bloomfield NJ
Wing Tom - Cedar Grove NJ
Sundeep Dugar - Bridgewater NJ
John W. Clader - Cranford NJ
Samuel Chackalamannil - East Brunswick NJ
Wang Yuguang - North Brunswick NJ
Stuart W. McCombie - Caldwell NJ
Jayaram R. Tagat - Westfield NJ
Susan F. Vice - Mountainside NJ
Wayne Vaccaro - Yardley PA
Michael J. Green - Skillman NJ
Margaret E. Browne - Bloomfield NJ
Theodros Asberom - West Orange NJ

Assignee:

Schering Corporation - Kenilworth NJ

International Classification:

C07D29508
C07D30781
C07D33358
A61K 31495

US Classification:

514252

Abstract:

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; and R. 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.

US Patent:

60373520, Mar 14, 2000

Filed:

Nov 19, 1998

Appl. No.:

9/195742

Inventors:

Derek Lowe - Scotch Plains NJ
Wei Chang - Livingston NJ
Joseph Kozlowski - Princeton NJ
Joel G. Berger - Cedar Grove NJ
Robert McQuade - Scotch Plains NJ
Allen Barnett - Pine Brook NJ
Margaret Sherlock - Bloomfield NJ
Wing Tom - Cedar Grove NJ
Sundeep Dugar - Bridgewater NJ
John W Clader - Cranford NJ
Samuel Chackalamannil - East Brunswick NJ
Wang Yuguang - North Brunswick NJ
Stuart W. McCombie - Caldwell NJ
Jayaram R. Tagat - Westfield NJ
Susan F. Vice - Mountainside NJ
Wayne Vaccaro - Yardley PA
Michael J. Green - Skillman NJ
Margaret E. Browne - Bloomfield NJ
Theodros Asberom - West Orange NJ

Assignee:

Schering Corporation - Kenilworth NJ

International Classification:

A61K 31445
C07D21100
C07D21108

US Classification:

514316

Abstract:

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.

US Patent:

60432551, Mar 28, 2000

Filed:

Mar 10, 1999

Appl. No.:

9/266079

Inventors:

Derek B. Lowe - Scotch Plains NJ
Wei K. Chang - Livingston NJ
Joseph A. Kozlowski - Princeton NJ
Joel G. Berger - Cedar Grove NJ
Robert McQuade - Scotch Plains NJ
Allen Barnett - Pine Brook NJ
Margaret Sherlock - Bloomfield NJ
Wing Tom - Cedar Grove NJ
Sundeep Dugar - Bridgewater NJ
John W Clader - Cranford NJ
Samuel Chackalamannil - East Brunswick NJ
Yuguang Wang - North Brunswick NJ
Stuart W. McCombie - Caldwell NJ
Jayaram R. Tagat - Westfield NJ
Susan F. Vice - Mountainside NJ
Wayne Vaccaro - Yardley PA
Michael J. Green - Encinitas CA
Margaret E. Browne - Bloomfield NJ
Theodros Asberom - West Orange NJ
Craig D. Boyle - Bridgewater NJ

Assignee:

Schering Corporation - Kenilworth NJ

International Classification:

A61K 31445
C07D40102

US Classification:

514316

Abstract:

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.

US Patent:

62880683, Sep 11, 2001

Filed:

Jan 12, 2000

Appl. No.:

9/482168

Inventors:

Derek Lowe - Scotch Plains NJ
Wei Chang - Livingston NJ
Joseph Kozlowski - Princeton NJ
Joel G. Berger - Cedar Grove NJ
Robert McQuade - Scotch Plains NJ
Allen Barnett - Pine Brook NJ
Margaret Sherlock - Bloomfield NJ
Wing Tom - Cedar Grove NJ
Sundeep Dugar - Bridgewater NJ
John W Clader - Cranford NJ
Samuel Chackalamannil - East Brunswick NJ
Wang Yuguang - North Brunswick NJ
Stuart W. McCombie - Caldwell NJ
Javaram R. Tagat - Westfield NJ
Susan F. Vice - Mountainside NJ
Wayne Vaccaro - Yardley PA
Michael J. Green - Skillman NJ
Margaret E. Browne - Bloomfield NJ
Theodros Asberom - West Orange NJ

Assignee:

Schering Corporation - Kenilworth NJ

International Classification:

C07D 31495
A61K24136

US Classification:

514256

Abstract:

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 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.

US Patent:

58890068, Mar 30, 1999

Filed:

Aug 8, 1996

Appl. No.:

8/700628

Inventors:

Derek B. Lowe - Scotch Plains NJ
Wei K. Chang - Livingston NJ
Joseph A. Kozlowski - Princeton NJ
Joel G. Berger - Cedar Grove NJ
Robert McQuade - Scotch Plains NJ
Allen Barnett - Pine Brook NJ
Margaret Sherlock - Bloomfield NJ
Wing Tom - Cedar Grove NJ
Sundeep Dugar - Bridgewater NJ
John W. Clader - Cranford NJ
Samuel Chackalamannil - East Brunswick NJ
Yuguang Wang - North Brunswick NJ
Stuart W. McCombie - Caldwell NJ
Jayaram R. Tagat - Westfield NJ
Susan F. Vice - Mountainside NJ
Wayne Vaccaro - Yardley PA
Michael J. Green - Encinitas CA
Margaret E. Browne - Bloomfield NJ
Theodros Asberom - West Orange NJ
Craig D. Boyle - Bridgewater NJ

Assignee:

Schering Corporation - Kenilworth NJ

International Classification:

C07D40102
C07D40302
C07D40314
C07D40114

US Classification:

519252

Abstract:

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.