Patent number: 6784167
Abstract: 17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula
wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl.
Type:
Grant
Filed:
September 28, 2001
Date of Patent:
August 31, 2004
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Jill E. Wood, Jeremy L. Baryza, Catherine R. Brennan, Soongyu Choi, James H. Cook, Brian R. Dixon, Paul P. Ehrlich, David E. Gunn, Ian McAlexander, Peiying Liu, Derek B. Lowe, Anikó M. Redman, William J. Scott, Yamin Wang
Patent number: 6043255
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.
Type:
Grant
Filed:
March 10, 1999
Date of Patent:
March 28, 2000
Assignee:
Schering Corporation
Inventors:
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
Patent number: 5952349
Abstract: 1,4 Di-substituted piperidine muscarinic antagonists of formula I ##STR1## or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, --O--, --SO.sub.0-2 --, --CO--, --C(OR.sup.7).sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --, --CH(C.sub.1 --C.sub.6 alkyl)--, --C(C.sub.1 --C.sub.6 alkyl).sub.2 --, --CONR.sup.17 --, --NR.sup.17 CO--, --SO.sub.2 NR.sup.17 -- or --NR.sup.17 SO.sub.2 --; R is C.sub.3 --C.sub.6 cycloalkyl, optionally substituted phenyl or optionally substituted pyridyl; R.sup.1 is H, --CN, --CF.sub.3, alkyl, cycloalkyl, cycloalkenyl, alkenyl, --COR.sup.15, --COO(alkyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl), alkylaryl, alkylheteroaryl or --CON(R.sup.13).sub.2 ; R.sup.2 is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; and R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.13, R.sup.15 and R.sup.
Type:
Grant
Filed:
July 8, 1997
Date of Patent:
September 14, 1999
Assignee:
Schering Corporation
Inventors:
Theodros Asberom, Derek B. Lowe, Michael J. Green
