Patents Assigned to G. D. Searle
  • Method of treating skin related conditions
    Patent number: 6274590
    Abstract: A class of 3,4-diaryl substituted thiophene, 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 S; wherein X is one or two substituents 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 with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: August 14, 2001
    Assignee: G. D. Searle & Co.
    Inventors: John J. Talley, Stephen R Bertenshaw, Paul W Collins, Thomas D. Penning, David B. Reitz, Roland S Rogers
  • Substituted benzopyran derivatives for the treatment of inflammation
    Patent number: 6271253
    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: May 11, 2000
    Date of Patent: August 7, 2001
    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
  • Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors
    Patent number: 6268392
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and EG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
    Type: Grant
    Filed: March 9, 1998
    Date of Patent: July 31, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Bradley T. Keller, Kevin C. Glenn, Robert E. Manning
  • Urea derivatives useful as platelet aggregation inhibitors
    Patent number: 6268380
    Abstract: Novel urea derivatives of the formula are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: July 31, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Foe S. Tjoeng, Mihaly V. Toth
  • LTA4 hydrolase inhibitors
    Patent number: 6265433
    Abstract: The present invention provides compounds having the structure: and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.
    Type: Grant
    Filed: May 14, 1999
    Date of Patent: July 24, 2001
    Assignee: G. D. Searle & Company
    Inventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell, Julie Marion Miyashiro, James Malecha, Thomas Dale Penning
  • Cyclic sulfone containing retroviral protease inhibitors
    Patent number: 6265583
    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: October 22, 1998
    Date of Patent: July 24, 2001
    Assignees: G. D. Searle & Co., Monsanto Company
    Inventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
  • Halogenated phenylacetonitrile alkylaminoalkylphenyl compounds as immunosuppressives
    Patent number: 6265439
    Abstract: A class of halogenated phenylacetonitrile alkylaminoalkylphenyl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: July 24, 2001
    Assignee: G.D. Searle & Co.
    Inventors: Richard A Mueller, Thomas E Barta, John P McKearn, Susan A Gregory, Richard A Partis, Francis J Koszyk
  • Intermediates and processes for the preparation of benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
    Patent number: 6262277
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
    Type: Grant
    Filed: November 19, 1999
    Date of Patent: July 17, 2001
    Assignee: G.D. Searle and Company
    Inventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
  • Keto-Substituted Steroid Compounds
    Patent number: 6258946
    Abstract: Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other compounds of Formula I wherein the variables are as defined by the specification.
    Type: Grant
    Filed: May 30, 2000
    Date of Patent: July 10, 2001
    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
  • Thrombopoietin: IL-3 fusion protein
    Patent number: 6254870
    Abstract: The present invention relates to variants of human c-mpl ligands (thrombopoietin) with activity on hematopoietic differentiation and expansion.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: July 3, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Nicholas R. Staten, Jean P. Favara, Larry E. Kahn, Lyle E. Pegg, John P. McKearn, Charles M. Baum
  • Para-substituted phenylene derivatives
    Patent number: 6251944
    Abstract: The present invention relates to a class of compounds represented by Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 integrin.
    Type: Grant
    Filed: April 8, 1999
    Date of Patent: June 26, 2001
    Assignee: G. D. Searle & Company
    Inventors: Barbara B. Chen, Helen Y. Chen, Glen J. Gesicki, Richard A. Haack, James W. Malecha, Thomas D. Penning, Joseph G. Rico, Thomas E. Rogers, Peter G. Ruminski, Mark A. Russell, Stella S. Yu
  • &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: 6248775
    Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: April 8, 1999
    Date of Patent: June 19, 2001
    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
  • Crystalline form of 4- [ 5-methyl-3-phenylisoxazol-4-yl ] benzenesulfonamide
    Publication number: 20010003752
    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: Application
    Filed: December 19, 2000
    Publication date: June 14, 2001
    Applicant: G.D. Searle & Co.
    Inventors: John J. Talley, John R. Medich, Kathleen T. McLaughlin, Henry T Gaud, Edward E. Yonan
  • Process for making substituted pyrazoles
    Patent number: 6242612
    Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: June 5, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Matthew J. Graneto, Michael L. Vazquez, Susan J. Hartmann, Suzanne Metz, John J. Talley, David L. Brown, Richard M. Weier, Michael A. Stealey, Xiangdong Xu
  • Use of low dose amount of spironolactone for treatment of cardiovascular disease
    Publication number: 20010002399
    Abstract: Use of low dosages of an aldosterone receptor antagonist, spironolactone, is described for treatment of circulatory disorders. This therapy would be particularly useful to treat or retard the development of congestive heart failure, while avoiding or reducing aldosterone-antagonist-induced side effects, such as hyperkalemia.
    Type: Application
    Filed: January 9, 2001
    Publication date: May 31, 2001
    Applicant: G.D. Searle & Co.
    Inventors: Todd E. MacLaughlan, Alfonso T. Perez
  • Primer sets for analyzing fatty acyl-CoA oxidase expression
    Patent number: 6228595
    Abstract: Hepatocyte culturing system, primer sets and an analytical method for selectively detecting and quantitatively assessing the levels of mRNA expression of the major isoenzymes of cytochrome P450 (CYP450 1A1, 1A2, 2B1/2, 2C11, 2E1, 3A1, 3A2 and 4A1), fatty acyl-CoA oxidase (FACO) and select Phase II conjugating enzymes (UDPGT, GST and ST) in the rat using specific 5′ and 3′ oligonucleotide primers and reverse transcriptase-polymerase chain reaction. The method closely reproduces the expression obtained from rat liver tissue following treatment with the same enzyme inducers. Constitutive and inducible expression was maintained by resuspending, culturing and then overlaying adult rat hepatocytes with an extracellular matrix such as Matrigel®.
    Type: Grant
    Filed: July 19, 2000
    Date of Patent: May 8, 2001
    Assignee: G.D. Searle & Co.
    Inventors: Dale Lynn Morris, Julio Cesar Davila
  • Use of alkylated iminosugars to treat multidrug resistance
    Patent number: 6225325
    Abstract: Methods and compositions for preventing, reducing, or reversing multidrug resistance (MDR) during cancer chemotherapy in patients undergoing treatment with therapeutically effective amounts of chemotherapeutic agents are provided. The methods comprise administering an anti-MDR effective amount of an N-substituted-1,5-dideoxy-1,5-imino-D-glucitol or galactitol iminosugar to a patient.
    Type: Grant
    Filed: November 10, 1998
    Date of Patent: May 1, 2001
    Assignee: G.D. Searle & Company
    Inventor: Gary S. Jacob
  • Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 6214861
    Abstract: Selected heterocycle carbonyl 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: February 9, 2000
    Date of Patent: April 10, 2001
    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
  • &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
    Patent number: 6211176
    Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 1, 1999
    Date of Patent: April 3, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Hydroxyamidino derivatives useful as nitric oxide synthase inhibitors
    Patent number: 6207708
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: March 11, 1998
    Date of Patent: March 27, 2001
    Assignee: G. D. Searle & Company
    Inventors: Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth