Patents Assigned to G. D. Searle & Co.
  • 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
  • Patent number: 7112683
    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
  • Publication number: 20060199822
    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
  • 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
  • Publication number: 20060189611
    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: Application
    Filed: January 24, 2006
    Publication date: August 24, 2006
    Applicant: G.D. Searle & Co.
    Inventors: Daniel Getman, Gary DeCrescenzo, John Freskos, Michael Vazquez, James Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David Brown, Joseph McDonald
  • 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
  • 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
  • Patent number: 7060851
    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: Grant
    Filed: October 12, 2004
    Date of Patent: June 13, 2006
    Assignee: G.D. Searle & Co.
    Inventors: John S Ng, Claire A Przybyla, Shu-Hong Zhang
  • Patent number: 7045518
    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: Grant
    Filed: October 3, 2003
    Date of Patent: May 16, 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 Raj Nagarajan, Joseph J. McDonald
  • Publication number: 20060094789
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: September 27, 2005
    Publication date: May 4, 2006
    Applicant: G.D. Searle & Co.
    Inventors: Michael Vazquez, Richard Mueller, John Talley, Daniel Getman, Gary DeCrescenzo, Eric Sun
  • Patent number: 7038084
    Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: February 24, 2004
    Date of Patent: May 2, 2006
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 7038040
    Abstract: Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I wherein: -A-A- represents the group —CHR4—CHR5— or CR4?CR5— R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy, R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical, -B-B- represents the group —CHR6—CHR7— or an alpha- or beta-oriented group: ?where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and R8 and R9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, or R8 and R9 together comprise a carbocyclic or h
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: May 2, 2006
    Assignee: G.D. Searle & Co.
    Inventors: John S. Ng, Ping T. Wang, Julio A. Baez, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Gennaro Mucciariello, Fortunato Vanzanella, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
  • 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
  • Patent number: 7030161
    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: October 21, 2003
    Date of Patent: April 18, 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
  • Patent number: 7030153
    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.
    Type: Grant
    Filed: December 27, 2002
    Date of Patent: April 18, 2006
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Roland S. Rogers
  • 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
  • Patent number: 7026485
    Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: March 5, 2004
    Date of Patent: April 11, 2006
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
  • Publication number: 20060074247
    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: Application
    Filed: January 13, 2003
    Publication date: April 6, 2006
    Applicant: G.D. Searle & Co.
    Inventor: Joseph Wieczorek
  • 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
  • Publication number: 20060040974
    Abstract: HIV protease inhibitors are disclosed which are characterized as having both hydroxyethylamine and N-heterocyclic moieties.
    Type: Application
    Filed: August 9, 2005
    Publication date: February 23, 2006
    Applicant: G.D. Searle & Co.
    Inventors: Richard Mueller, Daniel Getman