Patents Assigned to G. D. Searle
  • Formulation, Solubilization, Purification, and Refolding of Tissue Factor Pathway Inhibitor
    Publication number: 20080281084
    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
  • Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 7161033
    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
  • Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 7141594
    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
  • Crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl] benzenesulfonamide
    Patent number: 7135489
    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
  • Sulfonyl aryl or heteroaryl hydroxamic acid compounds
    Patent number: 7115632
    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
  • Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 7098202
    Abstract: Selected 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 20, 2004
    Date of Patent: August 29, 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
  • Bis-sulfonamide hydroxyethyl-amino retroviral protease inhibitors
    Patent number: 7091219
    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: April 17, 2003
    Date of Patent: August 15, 2006
    Assignee: G. D. Searle & Co.
    Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
  • Formulation, solubilization, purification, and refolding of tissue factor pathway inhibitor
    Publication number: 20060128947
    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: January 24, 2006
    Publication date: June 15, 2006
    Applicants: Chiron Corporation, G. D. Searle & Co.
    Inventors: Glenn Dorin, Bo Arve, Gregory Pattison, Robert Halenbeck, Kirk Johnson, Bao-Lu Chen, Rajsharan Rana, Maninder Hora, Hassan Madani, Michael Tsang, Mark Gustafson, Gary Bild, Gary Johnson
  • Alpha-and Beta-amino acid hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
    Patent number: 7037941
    Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors:
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: May 2, 2006
    Assignee: G. D. Searle & Co.
    Inventors: Michael L Vazquez, Richard A Mueller, John J Talley, Daniel P Getman, Gary A DeCrescenzo, Eric T Sun
  • Retroviral protease inhibitors
    Patent number: 7026333
    Abstract: HIV protease inhibitors are disclosed which are characterized as having both hydroxyethylamine and N-heterocyclic moieties.
    Type: Grant
    Filed: July 26, 2000
    Date of Patent: April 11, 2006
    Assignee: G. D. Searle & Co.
    Inventors: Richard A Mueller, Daniel P. Getman
  • Formulation, solubilization, purification, and refolding of tissue factor pathway inhibitor
    Patent number: 7022672
    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
  • 3 (5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors
    Patent number: 7019005
    Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I wherein R1, R2, Ar1 and HetAr2 are as described in the specification.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: March 28, 2006
    Assignee: G. D. Searle & Co.
    Inventors: Ashok S. Naraian, Michael Clare, Lifeng Geng, Gunnar J. Hanson, Richard A. Partis, Michael A. Stealey, Richard M. Weier
  • Processes for preparation of 9, 11-epoxy steroids and intermediates useful therein
    Publication number: 20050256094
    Abstract: Intermediates in the preparation of 9,11-epoxy steroids are disclosed. Particularly, disclosed are 11,12-epoxy steroid, 4,5-9,11-diepoxy steroid and 12-keto steroid intermediates.
    Type: Application
    Filed: February 7, 2005
    Publication date: November 17, 2005
    Applicant: G. D. Searle & Company
    Inventors: John Ng, Chin Liu, Dennis Anderson, Jon Lawson, Joseph Wieczorek, Sastry Kunda, Leo Letendre, Mark Pozzo, Yuen-Lung Sing, Ping Wang, Edward Yonan, Richard Weir, Thomas Kowar, Julio Baez, Bernhard Erb
  • Combination therapy of angiotensin converting enzyme inhibitor and eplerenone for treatment of cardiovascular disease
    Publication number: 20050250748
    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
  • Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
    Patent number: 6951886
    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
  • Meta-substituted phenylene sulphonamide derivatives
    Publication number: 20050176821
    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
  • ?- and ?-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: 6924286
    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
  • Processes for preparation of 9, 11-epoxy steroids and intermediates useful therein
    Patent number: 6887991
    Abstract: Processes for the preparation of 4,5-dihydro-5,7-lactone steroid compounds are provided.
    Type: Grant
    Filed: August 25, 2003
    Date of Patent: May 3, 2005
    Assignee: G. D. Searle & Company
    Inventors: John S. Ng, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Joseph Wieczorek, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Ping T. Wang, Edward E. Yonan, Richard M. Weier, Thomas R. Kowar, Julio A. Baez, Bernhard Erb
  • Cyclic sulfone containing retroviral protease inhibitors
    Patent number: 6875790
    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
  • Immediate release eplerenone compositions
    Patent number: 6863902
    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