Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA
wherein R1, R2, R3 and R4 are as described in the specification.
Type:
Grant
Filed:
November 20, 1998
Date of Patent:
February 4, 2003
Assignee:
G.D. Searle & Company
Inventors:
Ashok Anantanarayan, Michael Clare, Paul W. Collins, Joyce Zuowu Crich, Rajesh Devraj, Daniel L. Flynn, Lifeng Geng, Matthew J. Graneto, Cathleen E. Hanau, Gunnar J. Hanson, Susan J. Hartmann, Michael Hepperle, He Huang, Francis J. Koszyk, Shuyuan Liao, Suzanne Metz, Richard A. Partis, Thao D. Perry, Shashidhar N. Rao, Shaun Raj Selness, Michael S. South, Michael A. Stealey, John Jeffrey Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xu, Ish K. Khanna, Yi Yu
Abstract: Novel 5&bgr;-cyano steroid compounds including compounds of Formula VII:
wherein A—A, B—B, R3, R8 and R9 are as defined in the specification.
Type:
Grant
Filed:
May 30, 2000
Date of Patent:
January 1, 2002
Assignee:
G.D. Searle & Co.
Inventors:
John S. Ng, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
Abstract: A process for the formation of an epoxy compound comprising contacting a substrate compound having an olefinic double bond with a peroxide compound in the presence of a peroxide activator, said peroxide activator corresponding to the formula:
where Ro is a substituent having an electron withdrawing strength not less than that of monochloromethyl.
Type:
Grant
Filed:
February 8, 1999
Date of Patent:
December 18, 2001
Assignee:
G.D. Searle & Co.
Inventors:
John S. Ng, Ping T. Wang, Julio A. Baez, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Gennaro Mucciariello, Fortunato Vanzanella, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
Abstract: Novel urea derivatives of the formula are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.
Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and EG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
Type:
Grant
Filed:
March 9, 1998
Date of Patent:
July 31, 2001
Assignee:
G. D. Searle & Co.
Inventors:
Bradley T. Keller, Kevin C. Glenn, Robert E. Manning
Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
Type:
Grant
Filed:
November 19, 1999
Date of Patent:
July 17, 2001
Assignee:
G.D. Searle and Company
Inventors:
Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
Abstract: Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other compounds of Formula I
wherein the variables are as defined by the specification.
Type:
Grant
Filed:
May 30, 2000
Date of Patent:
July 10, 2001
Assignee:
G. D. Searle & Co.
Inventors:
John S. Ng, Ping T. Wang, Julio A. Baez, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Gennaro Mucciariello, Fortunato Vanzanella, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
Abstract: Multiple reaction schemes, process steps and intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other compounds of Formula I
wherein the variables are as defined by the specification.
Type:
Grant
Filed:
February 9, 1999
Date of Patent:
January 30, 2001
Assignee:
G.D. Searle & Co.
Inventors:
John S. Ng, Ping T. Wang, Julio A. Baez, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Gennaro Mucciariello, Fortunato Vanzanella, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
Abstract: A class of substituted pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II wherein R.sup.1 is selected from hydrido, halo, alkoxy, haloalkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R.sup.2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R.sup.5 and R.sup.6 are one or more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R.sup.5 and R.sup.6 is substituted with alkylsulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.
Type:
Grant
Filed:
August 8, 1997
Date of Patent:
June 29, 1999
Assignee:
G. D. Searle & Co.
Inventors:
Richard M Weier, Len F Lee, Richard A Partis, Francis J Koszyk