Patents Assigned to G. D. Searle & Co.
  • ?- and ?-amino acid hydroxyethlamino sulfonyl urea derivatives useful as retroviral protease inhibitors
    Patent number: 7232817
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 27, 2005
    Date of Patent: June 19, 2007
    Assignees: G.D. Searle & Co., Monsanto Company
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • ?- and ?-amino acid hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
    Patent number: 7202258
    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 28, 2005
    Date of Patent: April 10, 2007
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Alpha- and beta-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Publication number: 20070078173
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: September 25, 2006
    Publication date: April 5, 2007
    Applicant: G.D. Searle & Co.
    Inventors: Michael Vazquez, Richard Mueller, John Talley, Daniel Getman, Gary DeCrescenzo, John Freskos, Robert Heintz, Deborah Bertenshaw
  • Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
    Patent number: 7199158
    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: Grant
    Filed: July 18, 2005
    Date of Patent: April 3, 2007
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • N-protected/N-substituted-beta-amino hydroxy sulfonates
    Patent number: 7192983
    Abstract: N-protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their preparation and use.
    Type: Grant
    Filed: January 13, 2003
    Date of Patent: March 20, 2007
    Assignee: G.D. Searle & Co.
    Inventor: Joseph J. Wieczorek
  • Method of preparing intermediates useful in synthesis of retroviral protease inhibitors
    Patent number: 7189864
    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
  • Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Publication number: 20070037754
    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
  • Cyclic sulfone containing retroviral protease inhibitors
    Publication number: 20070015818
    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: Application
    Filed: July 5, 2006
    Publication date: January 18, 2007
    Applicants: G.D. Searle & Co. (now G.D. Searle, LLC), Monsanto Company (now Pharmacia Corporation)
    Inventors: Deborah Bertenshaw, Daniel Getman, Robert Heintz, John Talley, Kathryn Reed, Robert Chrusciel, Michael Clare
  • 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
    Publication number: 20070004646
    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
  • alpha- and beta-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Publication number: 20060276493
    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
  • Methods of preparing retroviral proteases inhibitor intermediates
    Publication number: 20060270855
    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
  • 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
  • ?- and ?-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: 7141609
    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
  • Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
    Publication number: 20060264483
    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
  • Substituted benzopyran derivatives for the treatment of inflammation
    Patent number: 7138411
    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
  • 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
  • Immunosuppressive effects of administration of a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor
    Patent number: 7132441
    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
  • Retroviral protease inhibitor combinations
    Publication number: 20060240410
    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
  • ?- and ?-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: 7115618
    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