Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1-R6, R7, R7?, R8, R30-R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
July 18, 2005
Publication date:
January 26, 2006
Applicant:
G.D. Searle & Co.
Inventors:
Michael Vazquez, Richard Mueller, John Talley, Daniel Getman, Gary DeCrescenzo, Eric Sun
Abstract: A therapeutic method is described for treating cardiofibrosis or cardiac hypertrophy using a combination therapy comprising a therapeutically-effective amount of an angiotensin II receptor antagonist and a therapeutically-effective amount of expoxymexrenone.
Type:
Grant
Filed:
February 21, 2003
Date of Patent:
January 10, 2006
Assignee:
G.D Searle & Co.
Inventors:
James J. Egan, Ellen G. McMahon, Gillian M. Olins, Joseph R. Schuh
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:
February 10, 2003
Date of Patent:
December 13, 2005
Assignee:
G.D. Searle & Co.
Inventors:
John S Ng, Claire A. Przybyla, Richard A Mueller, Michael L Vazquez, Daniel P Getman
Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors:
Type:
Application
Filed:
June 28, 2005
Publication date:
December 1, 2005
Applicant:
G.D. Searle & Co.
Inventors:
Michael Vazquez, Richard Mueller, John Talley, Daniel Getman, Gary DeCrescenzo, Eric Sun
Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
April 21, 2005
Publication date:
December 1, 2005
Applicant:
G.D. Searle & Co.
Inventors:
Michael Vazquez, Richard Mueller, John Talley, Daniel Getman, Gary DeCrescenzo, John Freskos, Deborah Bertenshaw, Robert Heintz
Abstract: A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
Type:
Application
Filed:
December 4, 2003
Publication date:
December 1, 2005
Applicant:
G.D. Searle & Co.
Inventors:
Kathleen Barton, Thomas Borchardt, Marlon Carlos, Subhash Desai, Leonard Ferro, Henry Gaud, Scott Ganser, Clay Little, Partha Mudipalli, Mark Pietz, Daniel Pilipauskas, Yuen-Lung Sing, Glenn Stahl, Joseph Wieczorek, Chris Yan
Abstract: Combinations of an ACE inhibitor and an epoxy-steroidal aldosterone receptor antagonist are described for use in treatment of circulatory disorders. Of particular interest are therapies using epoxy-steroidal-type aldosterone receptor antagonist compounds, such as eplerenone, in combination with an angiotensin converting enzyme inhibitor. This co-therapy would be particularly useful to treat congestive heart failure while avoiding or reducing aldosterone-antagonist-induced side effects such as hyperkalemia.
Type:
Application
Filed:
August 6, 2003
Publication date:
November 10, 2005
Applicant:
G. D. Searle & Co.
Inventors:
John Alexander, Barbara Roniker, Subhash Desai
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:
Application
Filed:
January 18, 2005
Publication date:
October 13, 2005
Applicant:
G.D. Searle & Co.
Inventors:
Daniel Getman, Gary DeCrescenzo, John Freskos, Michael Vazquez, James Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David Brown, Joseph McDonald
Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
December 10, 2002
Date of Patent:
October 4, 2005
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: 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 HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
Type:
Grant
Filed:
July 17, 2003
Date of Patent:
September 13, 2005
Assignee:
G.D. Searle & Co.
Inventors:
Bradley T. Keller, Kevin C. Glenn, Robert E. Manning
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 ?v?3 integrin.
Type:
Application
Filed:
September 8, 2003
Publication date:
August 11, 2005
Applicant:
G. D. Searle & Co.
Inventors:
Nizal Chandrakumar, Michael Clare, Wendell Doubleday, Alan Gasiecki, Mark Russell
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:
October 13, 2004
Publication date:
August 4, 2005
Applicant:
G.D. Searle & Co.
Inventors:
John Ng, Claire Przybyla, Richard Mueller, Michael Vazquez, Daniel Getman
Abstract: The present invention relates to carcinogenesis biomarkers produced by phenobarbital-treated rat hepatocytes, nucleic acid molecules that encode carcinogenesis biomarkers or a fragment thereof and nucleic acid molecules that are useful as probes or primers for detecting or inducing carcinogenesis, respectively. The invention also relates to applications of the factor or fragment such as forming antibodies capable of binding the carcinogenesis biomarkers or fragments thereof.
Type:
Grant
Filed:
January 25, 2000
Date of Patent:
August 2, 2005
Assignee:
G.D. Searle & Co.
Inventors:
Roderick T Bunch, Dale L Morris, Sandra W. Curtiss, Charles P. Rodi
Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
August 4, 2003
Date of Patent:
August 2, 2005
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
Abstract: Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diasteredmerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.
Type:
Application
Filed:
October 12, 2004
Publication date:
June 16, 2005
Applicant:
G.D. Searle & Co.
Inventors:
John Ng, Claire Przybyla, Shu-Hong Zhang
Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders.
Type:
Application
Filed:
January 31, 2005
Publication date:
June 16, 2005
Applicant:
G.D. Searle & Co.
Inventors:
John Talley, Thomas Penning, Paul Collins, Donald Rogier, James Malecha, Julie Miyashiro, Stephen Bertenshaw, Ish Khanna, Matthew Graneto, Roland Rogers, Jeffery Carter, Stephen Docter, Stella Yu
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 cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
Type:
Grant
Filed:
February 20, 2003
Date of Patent:
April 5, 2005
Assignees:
G. D. Searle & Co., Pharmacia Corporation (Monsanto Corporation)
Inventors:
Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
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:
November 6, 2002
Date of Patent:
March 8, 2005
Assignee:
G. D. Searle & Co.
Inventors:
Shilpa S. Thosar, Rajeev D. Gokhale, Dwain S. Tolbert
Abstract: A class of benzopyran, derivatives 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:
Application
Filed:
August 19, 2004
Publication date:
March 3, 2005
Applicant:
G.D. Searle & Co.
Inventors:
Jeffery Carter, Mark Obukowicz, Balekudru Devadas, John Talley, David Brown, Matthew Graneto, Stephen Bertenshaw, Donald Rogier, Srinivasan Nagarajan, Cathleen Hanau, Susan Hartmann, Cindy Ludwig, Suzanne Metz, Donald Korte