Abstract: ?-and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
December 7, 2007
Date of Patent:
November 9, 2010
Assignee:
G.D. Searle LLC
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
May 15, 2006
Date of Patent:
May 12, 2009
Assignee:
G.D. Searle LLC
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: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
December 7, 2007
Publication date:
January 22, 2009
Applicant:
G.D. SEARLE LLC
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Abstract: Compositions are described that are suitable for formulating TFPI. Solubilizers and stabilizers facilitate the preparation of pharmaceutically acceptable compositions of TFPI at various concentrations.
Type:
Application
Filed:
April 5, 2007
Publication date:
November 13, 2008
Applicants:
Novartis Vaccines and Diagnostics, Inc., G. D. Searle LLC
Inventors:
Glenn J. Dorin, Bo H. Arve, Gregory L. Pattison, Robert F. Halenbeck, Kirk Johnson, Bao-Lu Chen, Raisharan K. Rana, Maninder S. Hora, Hassan Madani, Michael Tsang, Mark E. Gustafson, Gary S. Bild, Gary V. Johnson
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:
November 14, 2007
Publication date:
July 24, 2008
Applicant:
G.D. SEARLE LLC
Inventors:
John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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 immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Application
Filed:
January 29, 2008
Publication date:
May 22, 2008
Applicant:
G.D. Searle LLC
Inventors:
Daniel Getman, Gary DeCrescenzo, John Freskos, Michael Vazquez, James Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David Brown, Joseph McDonald
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 immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
August 10, 2006
Date of Patent:
March 4, 2008
Assignee:
G.D. Searle LLC
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: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
September 25, 2006
Date of Patent:
January 22, 2008
Assignee:
G.D. Searle LLC
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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 8, 2006
Date of Patent:
November 20, 2007
Assignee:
G.D. Searle, LLC
Inventors:
John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
Abstract: Oral pharmaceutical formulation which improves the bioavailability of pharmaceuticals which are substantially water and oil insoluble is disclosed. In addition to the pharmaceutical, the formulation includes an emulsifier, an oil and an solubilizer. Alternatively, the formulation includes an aqueous solution of solubilizer.
Type:
Grant
Filed:
April 29, 2003
Date of Patent:
June 5, 2007
Assignee:
G.D. Searle LLC
Inventors:
Rajeev Gokhale, Martin J. Griffin, James E. Truelove, James C. Stolzenbach, Aziz Karim, Ajit K. Roy
Abstract: Compositions are described that are suitable for formulating TFPI. Solubilizers and stabilizers facilitate the preparation of pharmaceutically acceptable compositions of TFPI at various concentrations.
Type:
Grant
Filed:
January 24, 2006
Date of Patent:
June 5, 2007
Assignees:
G.D. Searle LLC, Novartis Vaccines and Diagnostics, Inc.
Inventors:
Glenn J. Dorin, Bo H. Arve, Gregory L. Pattison, Robert F. Halenbeck, Kirk Johnson, Bao-Lu Chen, Raisharan K. Rana, Maninder S. Hora, Hassan Madani, Michael Tsang, Mark E. Gustafson, Gary S. Bild, Gary V. Johnson
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 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: A method of modifying protein solubility employs polyionic polymers. These facilitate the solubilization, formulation, purification and refolding of proteins especially incorrectly folded proteins and aggregated proteins. Compositions are described that are suitable for formulating TFPI. The compositions allow preparation of pharmaceutically acceptable compositions of TFPI at concentrations above 0.2 mg/mL and above 10 mg/mL.
Type:
Grant
Filed:
November 30, 2001
Date of Patent:
April 4, 2006
Assignees:
Chiron Corporation, G. D. Searle, LLC
Inventors:
Glenn J. Dorin, Bo H. Arve, Gregory L. Pattison, Robert F. Halenbeck, Kirk Johnson, Bao-Lu Chen, Rejsharan K. Bana, Maninder S. Hoba, Hassan Madani, Michael Tsang, Mark E. Gustafson, Gary S. Bild, Gary V. Johnson
Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
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 a nicotinic acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.
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 23, 2007
Date of Patent:
November 1, 2011
Assignee:
G.D. Searle LLC
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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 23, 2007
Date of Patent:
August 21, 2012
Assignee:
G.D. Searle LLC
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
September 21, 2011
Date of Patent:
November 13, 2012
Assignee:
G.D. Searle LLC
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: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: or a pharmaceutically-acceptable salt thereof. A method of treating inflammation or an inflammation-associated disorder in a subject by administering a therapeutically-effective dose of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide, or a pharmaceutically-acceptable salt thereof, to the subject.
Type:
Grant
Filed:
November 14, 1994
Date of Patent:
March 5, 2013
Assignee:
G.D. Searle LLC
Inventors:
John J. Talley, Stephen R. Bertenshaw, Julie M. Miyashiro