Abstract: Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antivirals agents, nucleotide antiviral agents, or mixtures thereof, and immunomodulating/immunostimulating agents.
Type:
Grant
Filed:
January 19, 2000
Date of Patent:
February 10, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Gary S. Jacob, Timothy M. Block, Raymond A. Dwek
Abstract: The present invention relates to a class of compounds represented by the Formula I
or a pharmaceutically acceptable salts thereof, pharmaceutical compositions containing such compounds and methods of treating conditions mediated by the &agr;v&bgr;3 integrin.
Type:
Grant
Filed:
April 8, 1999
Date of Patent:
February 10, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Nizal Samuel Chandrakumar, Bipinchandra Nanubhai Desai, Balekudru Devadas, Alan Frank Gasiecki, Renee Huff, Ish K. Khanna, James W. Malecha, Julie M. Miyashiro, Shashidhar N. Rao, Joseph Gerace Rico, Thomas Edward Rogers, Peter Gerrard Ruminski, Mark Andrew Russell, Yi Yu
Abstract: &agr;-and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
May 6, 2002
Date of Patent:
January 27, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
March 15, 2002
Date of Patent:
January 27, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
Abstract: A class of compounds for the treatment of viral infections. Compounds of particular interest are defined by Formula I
wherein R-R4 are as defined herein, or a pharmaceutically-acceptable salt thereof.
Type:
Grant
Filed:
January 4, 2002
Date of Patent:
January 27, 2004
Assignee:
G.D. Searle & Co.
Inventors:
Norman Abood, Daniel L. Flynn, Daniel P. Becker, Brian M. Bax, Hui Li, Roger A. Nosal, Lori A. Schretzman, Clara I. Villamil
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:
Application
Filed:
February 8, 2002
Publication date:
January 22, 2004
Applicant:
G.D. Searle & Co.
Inventors:
Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
Abstract: The present invention relates to a class of compounds represented by the Formula I
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 integrin.
Type:
Grant
Filed:
August 28, 1998
Date of Patent:
January 13, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Nizal Chandrakumar, Michael Clare, Wendell Doubleday, Alan F. Gasiecki, Mark A. Russell
Abstract: A class of substituted biphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III:
wherein each of R11 through R13 is independently selected from hydrido, halo, lower alkoxy, lower haloalkyl, amino, lower alkylamino, lower dialkylamino, and lower haloalkoxy; or wherein R11 and R12 together form —O(CH2)nO—; wherein n is 1-2, inclusive; or a pharmaceutically-acceptable salt thereof.
Type:
Grant
Filed:
January 30, 2001
Date of Patent:
January 13, 2004
Assignee:
G.D. Searle & Co.
Inventors:
David B Reitz, James J Li, Monica B Norton
Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
Type:
Grant
Filed:
December 4, 2001
Date of Patent:
January 13, 2004
Assignee:
G.D. Searle & Co.
Inventors:
John J. Talley, James A. Sikorski, Balekudru Devadas, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Roland S. Rogers, Hwang-Fun Lu, David L. Brown
Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
April 12, 2002
Date of Patent:
January 6, 2004
Assignee:
G.D. Searle & Co.
Inventors:
Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II
wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and
wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.
Type:
Grant
Filed:
November 14, 2000
Date of Patent:
January 6, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II:
wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; wherein Y is selected from fluoroalkyl, and
and
wherein R9 is alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.
Type:
Grant
Filed:
November 25, 2002
Date of Patent:
January 6, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
December 10, 2002
Publication date:
January 1, 2004
Applicant:
G.D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension.
Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
February 26, 2002
Date of Patent:
December 23, 2003
Assignee:
G.D. Searle & Co.
Inventors:
Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
Abstract: The invention relates to substituted aromatic polycyclic 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:
September 26, 2002
Publication date:
December 4, 2003
Applicant:
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: 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:
February 10, 2003
Publication date:
December 4, 2003
Applicant:
G.D. Searle & Co.
Inventors:
John S. Ng, Claire A. Przybyla, Richard A. Mueller, Michael L. Vazquez, Daniel P. Getman