Abstract: The invention provides a process to restore platelet aggregation by the administration of antibody combining site-containing molecules that specifically bind to a specific class of reversibly-bound GPIIb/IIIa fibrinogen receptor antagonist compounds.
Type:
Application
Filed:
December 24, 2002
Publication date:
June 26, 2003
Applicant:
G.D. Searle & Co.
Inventors:
Kevin C. Glenn, Chris P. Carron, Larry P. Feigen, Jimmy D. Page, Jodi A. Pegg
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.
Type:
Application
Filed:
May 23, 2002
Publication date:
June 26, 2003
Applicant:
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: A family of molecules is disclosed that inhibit matrix metalloprotease (MMP) activity, and particularly inhibit the activity of one or more of MMP-2, MMP-9, or MMP-13, while generally exhibiting little activity against MMP-1. A contemplated compound also exhibits little inhibition of the production of TNF. A contemplated compound is an &agr;-amino-&bgr;-sulfonyl carbocyclo, heterocyclo, aryl, or heteroaryl hydroxamic acid. Also disclosed are processes for preparing a contemplated compound and for treating a mammal having a condition associated with pathological matrix metalloprotease activity.
Type:
Grant
Filed:
May 16, 2000
Date of Patent:
June 24, 2003
Assignee:
G.D. Searle & Co.
Inventors:
Susan L Hockerman, Daniel P. Becker, Louis J Bedell, Gary A DeCrescenzo, John N Freskos, Daniel P Getman, Robert M Heintz, Madeleine H Li, Brent V Mischke, Clara I Villamil, Thomas E Barta
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.
Type:
Application
Filed:
May 23, 2002
Publication date:
June 19, 2003
Applicant:
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.
Type:
Application
Filed:
May 23, 2002
Publication date:
June 12, 2003
Applicant:
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.
Type:
Application
Filed:
May 23, 2002
Publication date:
June 5, 2003
Applicant:
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.
Type:
Application
Filed:
May 23, 2002
Publication date:
May 29, 2003
Applicant:
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: 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:
Grant
Filed:
April 3, 2002
Date of Patent:
May 27, 2003
Assignee:
G. D. Searle & Co.
Inventors:
John S Ng, Claire A. Przybyla, Richard A Mueller, Michael L Vazquez, Daniel P Getman
Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula:
or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
Type:
Grant
Filed:
February 19, 2002
Date of Patent:
May 27, 2003
Assignee:
G. D. Searle & Co.
Inventors:
John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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.
Type:
Application
Filed:
May 23, 2002
Publication date:
May 22, 2003
Applicant:
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 ileal bile acid transport inhibitor combined with a bile acid sequestrant.
Type:
Grant
Filed:
December 17, 1999
Date of Patent:
May 13, 2003
Assignee:
G. D. Searle & Co.
Inventors:
Bradley T. Keller, Kevin C. Glenn, Joseph R. Schuh
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.
Type:
Application
Filed:
May 23, 2002
Publication date:
May 8, 2003
Applicant:
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: Use of low dosages of an aldosterone receptor antagonist, spironolactone, is described for treatment of circulatory disorders. This therapy would be particularly useful to treat or retard the development of congestive heart failure, while avoiding or reducing aldosterone-antagonist-induced side effects, such as hyperkalemia.
Abstract: The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.
Type:
Grant
Filed:
March 19, 2002
Date of Patent:
May 6, 2003
Assignee:
G. D. Searle & Co.
Inventors:
Shilpa S. Thosar, Rajeev D. Gokhale, Dwain S. Tolbert
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.
Type:
Application
Filed:
May 23, 2002
Publication date:
May 1, 2003
Applicant:
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 is a process for producing N-substituted glucamines, a process for oxidizing an N-substituted glucamine with an oxidizing microbe or extract thereof, and a process for oxidizing an N-substituted glucamine with an oxidizing microbe or extract thereof and reducing the oxidized N-substituted glucamine to an N-substituted-1-deoxynojirimycin. In addition, a one pot process for producing N-substituted-1-deoxynojirimycin from D-glucose is disclosed.
Type:
Grant
Filed:
April 14, 1999
Date of Patent:
April 22, 2003
Assignee:
G. D. Searle & Co.
Inventors:
Roy Walter Grabner, Bryan Hayden Landis, Ping Tu Wang, Michael Lee Prunier, Mike G. Scaros
Abstract: A class of amino-isoxazolidone compounds is described for use in treatment of memory impairment associated with Traumatic Brain Injury (“TBI”). Preferred compounds of this class are D-cycloserine and its prodrugs.
Type:
Application
Filed:
October 16, 2002
Publication date:
April 17, 2003
Applicant:
G.D. Searle & Co.
Inventors:
Daniel T. Fakouhi, Robert L. Herting, J. Michael Williams
Abstract: N-Substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections, the compounds of Formula I may be used alone, or in combination with another antiviral agent selected from among nucleosides, nucleotides, immunomodulators, immunostimulats or various combinations of such other agents.
Type:
Grant
Filed:
February 14, 2000
Date of Patent:
April 8, 2003
Assignee:
G.D. Searle & Co.
Inventors:
Richard A. Mueller, Martin L. Bryant, Richard A. Partis
Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol 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. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino(n+1)-Alkanol compounds are substituted (R)-Chiral fused heterocyclic amino compounds.
Type:
Grant
Filed:
December 12, 2001
Date of Patent:
April 8, 2003
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel