Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders.
Type:
Grant
Filed:
April 17, 2002
Date of Patent:
December 10, 2002
Assignee:
G. D. Searle & Co.
Inventors:
John J Talley, Thomas D Penning, Paul W Collins, Donald J Rogier, Jr., James W Malecha, Julie M Miyashiro, Stephen R Bertenshaw, Ish K Khanna, Matthew J Graneto, Roland S Rogers, Jeffery S Carter, Stephen H. Docter, Stella S Yu
Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′
wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.
Type:
Grant
Filed:
May 24, 2001
Date of Patent:
December 10, 2002
Assignee:
G.D. Searle & Co.
Inventors:
Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan Raj Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz, Donald E Korte
Abstract: A class of amino-isoxazolidone compounds is described for use to improve implicit memory in patients susceptible to or afflicted with Alzheimer's Disease. Preferred compounds of this class are D-cycloserine and its prodrugs.
Type:
Application
Filed:
May 24, 2002
Publication date:
December 5, 2002
Applicant:
G.D. Searle & Co.
Inventors:
Robert L. Herting, Barbara L. Schwartz, Stephen I. Deutsch
Abstract: A class of amino-isoxazolidone compounds is described for use to improve implicit memory in patients susceptible to or afflicted with Alzheimer's Disease. Preferred compounds of this class are D-cycloserine and its prodrugs.
Type:
Application
Filed:
May 22, 2002
Publication date:
December 5, 2002
Applicant:
G.D. Searle & Co.
Inventors:
Robert L. Herting, Barbara L. Schwartz, Stephen I. Deutsch
Abstract: The current invention relates to compounds of Formula I
pharmaceutical compositions and methods of use as nitric oxide synthase inhibitors, wherein the substituents are defined in the application.
Type:
Grant
Filed:
June 10, 1999
Date of Patent:
December 3, 2002
Assignee:
G.D. Searle & Co.
Inventors:
Donald W. Hansen, Jr., R. Keith Webber, E. Ann Hallinan, Mihaly V. Toth, Barnett S. Pitzele, Alok K. Awasthi, Alan E. Moormann, Suzanne Metz, Jeffery S. Snyder, William M. Moore, Jeffrey A. Scholten
Abstract: The invention relates to use of substituted aromatic polycyclic tertiary-heteroalkylamine compounds as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred substituted aromatic polycyclic tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.
Type:
Grant
Filed:
December 20, 1999
Date of Patent:
November 19, 2002
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted diamines.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
November 12, 2002
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-bis-benzyl aminoalcohols.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
November 5, 2002
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted cycloalkyl aminoalcohols.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
November 5, 2002
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: This invention provides a kit for use in a method for detecting gastric damage. The kit comprises: (a) a sealed container of sterilized buffered aqueous sucrose solution; and (b) a urine collection device suitable for collection and storage of human urine.
Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
Type:
Application
Filed:
April 3, 2002
Publication date:
October 31, 2002
Applicant:
G.D. Searle & Co.
Inventors:
John S. Ng, Claire A. Przybyla, Richard A. Mueller, Michael L. Vazquez, Daniel P. Getman
Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
February 22, 2000
Date of Patent:
October 29, 2002
Assignee:
G.D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula I.
wherein A, R2 and R3 are as described in the specification.
Type:
Grant
Filed:
May 21, 2001
Date of Patent:
October 22, 2002
Assignee:
G.D. Searle & Co.
Inventors:
Karen Seibert, Jaime Masferrer, Gary B Gordon
Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
June 20, 2001
Date of Patent:
October 22, 2002
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
October 8, 2002
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include an HMG CoA reductase inhibitor combined with a cholesteryl ester transfer protein (CETP) inhibitor.
Type:
Grant
Filed:
December 17, 1999
Date of Patent:
October 8, 2002
Assignee:
G.D. Searle & Co.
Inventors:
Bradley T. Keller, James A. Sikorski, Kevin C. Glenn, Daniel T. Connolly, Mark E. Smith
Abstract: This invention is in the field of a combination comprising a therapeutically-effective amount of a cyclooxygenase-2 inhibitor, a 5-lipoxygenase inhibitor and an immunosuppressive drug selected from antiproliferative agents, antiinflammatory-acting compounds and inhibitors of leukocyte activation. This combination may be used, for example, to suppress the immune response associated with organ transplantation, graft versus host disease, and conditions with underlying autoimmune or inflammatory reactivities or responses.
Type:
Application
Filed:
March 15, 2002
Publication date:
October 3, 2002
Applicant:
G.D. Searle & Co.
Inventors:
Susan A. Gregory, Peter C. Isakson, Gary Anderson
Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkyamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted mercapto amines.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
October 1, 2002
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
Type:
Grant
Filed:
November 23, 2001
Date of Patent:
October 1, 2002
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel