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:
October 13, 2004
Date of Patent:
March 13, 2007
Assignee:
G.D. Searle & Co.
Inventors:
John S. Ng, Claire A. Przybyla, Richard A. Mueller, Michael L. Vazquez, Daniel P. Getman
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, compositions, and methods for inhibiting retroviral proteases, such as human inmmunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Application
Filed:
August 10, 2006
Publication date:
February 15, 2007
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: 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: 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:
January 18, 2005
Date of Patent:
January 9, 2007
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: 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, compositions, and methods 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:
June 12, 2006
Publication date:
January 4, 2007
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: 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:
April 2, 2004
Date of Patent:
January 2, 2007
Assignee:
G.D. Searle, LLC
Inventors:
Shilpa S. Thosar, Rajeev D. Gokhale, Dwain S. Tolbert
Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as-inhibitors of HIV protease.
Type:
Application
Filed:
May 15, 2006
Publication date:
December 7, 2006
Applicant:
G.D Searle & Co.
Inventors:
Michael Vasquez, Richard Mueller, John Talley, Daniel Getman, Gary DeCrescenzo, John Freskos, Deborah Bertenshaw, Robert 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, diastereomerically 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:
May 16, 2006
Publication date:
November 30, 2006
Applicant:
G.D. Searle & Co.
Inventors:
John Ng, Claire Przybyla, Shu-Hong Zhang
Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
April 21, 2005
Date of Patent:
November 28, 2006
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: 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:
November 19, 2003
Date of Patent:
November 28, 2006
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: 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:
Application
Filed:
April 4, 2006
Publication date:
November 23, 2006
Applicant:
G.D. Searle & Co.
Inventors:
Daniel Getman, Gary DeCrescenzo, John Freskos, Michael Vazquez, James Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph McDonald
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:
November 22, 2002
Date of Patent:
November 21, 2006
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 stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.
Type:
Grant
Filed:
July 26, 2002
Date of Patent:
November 14, 2006
Assignee:
G. D. Searle & Co.
Inventors:
John J Talley, John R Medich, Kathleen T McLaughlin, Henry T Gaud, Edward E Yonan
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:
Grant
Filed:
March 15, 2002
Date of Patent:
November 7, 2006
Assignee:
G.D. Searle & Co.
Inventors:
Susan A. Gregory, Peter C. Isakson, Gary Anderson
Abstract: Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney.
Abstract: The present invention is directed to a method for the treatment of mammalian retrovirus infections, such as HIV, using combinations of retroviral protease inhibitors which are effective in preventing the replication of the retroviruses in vitro or in vivo. This invention, in particular, relates to protease inhibitor compounds used in combination therapy with other protease inhibitor compounds. This invention also relates to combination therapy with a combination of protease inhibitors and antiviral agents other than protease inhibitors.
Type:
Application
Filed:
April 4, 2006
Publication date:
October 26, 2006
Applicant:
G.D. Searle & Co.
Inventors:
Martin Bryant, Karen Potts, Mary Smidt, Simon Tucker
Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
March 30, 2004
Date of Patent:
October 3, 2006
Assignee:
G.D. Searle & Co.
Inventors:
Michael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.
Type:
Grant
Filed:
May 11, 2000
Date of Patent:
October 3, 2006
Assignee:
G. D. Searle & Co.
Inventors:
Louis J Bedell, Joseph J McDonald, Thomas E Barta, Daniel P Becker, Rao N Shashidhar, John N Freskos, Brent V Mischke, Daniel P Getman, Gary A DeCrescenzo, Clara I Villamil
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:
September 2, 2004
Date of Patent:
September 26, 2006
Assignees:
G.D. Searle & Co., Monsanto Company
Inventors:
Deborah E. Bertenshaw, Daniel P. Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert A. Chrusciel, Michael Clare
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:
Application
Filed:
February 8, 2006
Publication date:
September 7, 2006
Applicant:
G.D. Searle & Co.
Inventors:
John Freskos, Daniel Getman, John Talley, James Sikorski