Patents Assigned to G. D. Searle & Co.
  • Epoxy-steroidal aldosterone antagonist and calcium channel blocker combination therapy for treatment of congestive heart failure
    Publication number: 20030055027
    Abstract: A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a calcium channel blocker is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred calcium channel blockers are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 2O-spiroxane steroidal compounds characterized by the presence of a 9&agr;,11&agr;-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker verapamil HC1 (Benzenacetonitrile, (±) -&agr;[3[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-3,4-dimethoxy-&agr;-(1-methylethyl)hydrochloride) and the aldosterone receptor antagonist epoxymexrenone.
    Type: Application
    Filed: April 19, 2002
    Publication date: March 20, 2003
    Applicant: G. D. Searle & Co.
    Inventor: Joseph R. Schun
  • Immediate release eplerenone compositions
    Patent number: 6534093
    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: March 19, 2002
    Date of Patent: March 18, 2003
    Assignee: G.D. Searle & Co.
    Inventors: Shilpa S. Thosar, Rajeev D. Gokhale, Dwain S. Tolbert
  • 4,5-subtstituted imdazolyl compounds for the treatment of inflammation
    Publication number: 20030050330
    Abstract: A class of compounds is described for treating inflammation and inflammation-related disorders.
    Type: Application
    Filed: June 21, 2002
    Publication date: March 13, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Richard M. Weier, Paul W. Collins, Michael A. Stealey, Thomas E. Barta, Renee M. Huff
  • Heterocyclo-substituted imidazoles for the treatment of inflammation
    Publication number: 20030036557
    Abstract: A class of imidazolyl compounds is described for use in treating inflammation.
    Type: Application
    Filed: December 5, 2001
    Publication date: February 20, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Ish K. Khanna, Richard M. Weier, Paul W. Collins, Yi Yu, Xiangdong Xu, Richard A. Partis, Francis J. Koszyk, Renee M. Huff
  • Substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity
    Publication number: 20030032644
    Abstract: Substituted Polycyclic Aryl and Heteroaryl tetiary-leteroalkylamines Useful for Inhibiting Cholesteryl Ester Transfer Protein Activity Abstract The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.
    Type: Application
    Filed: February 7, 2002
    Publication date: February 13, 2003
    Applicant: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
    Patent number: 6515024
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: February 4, 2003
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Method of preparing retroviral protease inhibitor intermediates
    Patent number: 6515162
    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: December 21, 2000
    Date of Patent: February 4, 2003
    Assignee: G.D. Searle & Co.
    Inventors: John S Ng, Claire S. Przybyla, Shu-Hong Zhang
  • Thiophene substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
    Patent number: 6515014
    Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
    Type: Grant
    Filed: June 11, 2001
    Date of Patent: February 4, 2003
    Assignee: G. D. Searle & Co.
    Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Lu Hwang-Fun
  • Glucamine compounds for treating hepatitis virus infections
    Patent number: 6515028
    Abstract: N-Substituted glucamine compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections, the compounds of Formula I may be used alone, or in combination with another antiviral agents selected from among nucleosides, nucleotides, immunomodulators, immunostimulants or various combinations of such other agents.
    Type: Grant
    Filed: February 14, 2000
    Date of Patent: February 4, 2003
    Assignee: G.D. Searle & Co.
    Inventors: Richard A. Mueller, Martin L. Bryant, Richard A. Partis
  • 2-Amino-benzoxazinones for the treatment of viral infections
    Publication number: 20030022895
    Abstract: A class of compounds for the treatment of viral infections.
    Type: Application
    Filed: January 4, 2002
    Publication date: January 30, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Norman Abood, Daniel L. Flynn, Daniel P. Becker, Brian M. Bax, Hui Li, Roger A. Nosal, Lori A. Schretzman, Clara I. Villamil
  • Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
    Patent number: 6512121
    Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
    Type: Grant
    Filed: June 11, 2001
    Date of Patent: January 28, 2003
    Assignee: G.D. Searle & Co.
    Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Hwang-Fun Lu
  • 3,4-diaryl thiophenes and analogs thereof having use as anti-inflammatory agents
    Publication number: 20030013744
    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.
    Type: Application
    Filed: July 1, 2002
    Publication date: January 16, 2003
    Applicant: G.D. Searle & Co.
    Inventors: John J. Talley, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Roland S. Rogers
  • Bis-sulfonamide hydroxyethyl-amino retroviral protease inhibitors
    Publication number: 20030013751
    Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: February 19, 2002
    Publication date: January 16, 2003
    Applicant: G.D. Searle & Co.
    Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
  • LTA4 hydrolase inhibitor pharmaceutical compositions and methods of use
    Patent number: 6506876
    Abstract: The present invention provides compounds of the formula Ar1—Q—Ar2—Y—R—Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention 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: October 11, 1994
    Date of Patent: January 14, 2003
    Assignee: G.D. Searle & Co.
    Inventors: Nizal Samuel Chandrakumar, Barbara Baosheng Chen, Michael Clare, Bipinchandra Nanubhai Desai, Stevan Wakefield Djuric, Stephen Hermann Docter, Alan Frank Gasiecki, Richard Arthur Haack, Chi-Dean Liang, Julie Marion Miyashiro, Thomas Dale Penning, Mark Andrew Russell, Stella Siu-tzyy Yu
  • Crystalline form of 4-[5-methyl-3-phenylisoxazol-4-YL] benzenesulfonamide
    Publication number: 20030004200
    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: July 26, 2002
    Publication date: January 2, 2003
    Applicant: G.D. Searle & Co.
    Inventors: John J. Talley, John R. Medich, Kathleen T. McLaughlin, Henry T. Gaud, Edward E. Yonan
  • &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: 6500832
    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: March 14, 2000
    Date of Patent: December 31, 2002
    Assignee: G. D. Searle & Co.
    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
  • Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
    Publication number: 20020198378
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: December 11, 2001
    Publication date: December 26, 2002
    Applicant: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Combination drug therapy for glycolipid storage diseases
    Patent number: 6495570
    Abstract: A novel combination drug therapy is disclosed for the treatment of a patient affected with Gaucher's disease or other such glycolipid storage diseases. The method comprises administering to said patient a therapeutically effective amount of both a N-alkyl derivative of deoxynojirimycin (DNJ) and a glucocerebrosidase enzyme to alleviate or inhibit the glycolipid storage disease. The alkyl group has from about two to about 20 carbon atoms and preferably is butyl, nonyl or decyl.
    Type: Grant
    Filed: May 17, 2001
    Date of Patent: December 17, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Gary S. Jacob, Raymond A. Dwek
  • Eplerenone compositions having improved bioavailability
    Patent number: 6495165
    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: March 19, 2002
    Date of Patent: December 17, 2002
    Assignee: G.D. Searle & Co.
    Inventors: Shilpa S. Thosar, Rajeev D. Gokhale, Dwain S. Tolbert
  • 3.4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
    Patent number: 6492413
    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: March 20, 2000
    Date of Patent: December 10, 2002
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Stephen R Bertenshaw, Paul W Collins, Thomas D. Penning, David B. Reitz, Roland S Rogers