Patents Assigned to G. D. Searle & Co.
  • Method of preparing retroviral protease inhibitor intermediates
    Publication number: 20030171612
    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: December 23, 2002
    Publication date: September 11, 2003
    Applicant: G.D. Searle & Co.
    Inventors: John S. Ng, Claire A. Przybyla, Shu-Hong Zhang
  • Combination therapy employing ileal bile acid transport inhibiting benzothiepiens and HMG Co-A reductase inhibitors
    Publication number: 20030171426
    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 HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
    Type: Application
    Filed: February 15, 2002
    Publication date: September 11, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Bradley T. Keller, Kevin C. Glenn, Robert E. Manning
  • Immunosuppressive effects of administration of a cyclooxygenase-2 inhibitor, a leukotriene B4 receptor inhibitor and a cyclosporin
    Patent number: 6617345
    Abstract: Treatment with a cyclooxygenase-2 inhibitor and a leukotriene B4 receptor antagonist is described as being useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune diseases.
    Type: Grant
    Filed: September 12, 2000
    Date of Patent: September 9, 2003
    Assignee: G.D. Searle & Co.
    Inventors: Susan A Gregory, Peter C Isakson, Gary Anderson
  • Combinations of cholesteryl ester transfer protein inhibitors and HMG CoA reductase inhibitors for cardiovascular indications
    Publication number: 20030166712
    Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include an HMG CoA reductase inhibitor combined with a cholesteryl ester transfer protein (CETP) inhibitor.
    Type: Application
    Filed: July 23, 2002
    Publication date: September 4, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Bradley T. Keller, James A. Sikorski, Kevin C. Glenn, Daniel T. Connolly, Mark E. Smith
  • DNA clone of human tissue factor inhibitor
    Publication number: 20030166194
    Abstract: A cDNA clone having a base sequence for human tissue factor inhibitor (TFI) has been developed and characterized and the amino acid sequence of the TFI has been determined.
    Type: Application
    Filed: March 4, 2003
    Publication date: September 4, 2003
    Applicant: G. D. SEARLE & CO.
    Inventors: Tze Chein Wun, Kuniko K. Kretzmer, George J. Broze
  • Heterocyclo-substituted imidazoles for the treatment of inflammation
    Patent number: 6613789
    Abstract: A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by Formula V: and pharmaceutically-acceptable salts thereof.
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: September 2, 2003
    Assignee: 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
  • Method for treatment of glycolipid storage diseases
    Patent number: 6610703
    Abstract: A novel method 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 a long-chain N-alkyl derivative of deoxynojirimycin to alleviate or inhibit the glycolipid storage disease. The long-chain alkyl group has from nine to about 20 carbon atoms and preferably is nonyl or decyl.
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: August 26, 2003
    Assignees: G.D. Searle & Co., Oxford University
    Inventors: Gary S. Jacob, Frances M. Platt, Terry D. Butters, Raymond A. Dwek
  • Alpha-and beta-amino acid hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
    Publication number: 20030158236
    Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors: 1
    Type: Application
    Filed: June 25, 2002
    Publication date: August 21, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
    Publication number: 20030153602
    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: December 27, 2002
    Publication date: August 14, 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
  • Combination therapy of angiotensin converting enzyme inhibitor and side-effect-reduced amount of aldosterone antagonist for treatment of cardiovascular disease
    Publication number: 20030148960
    Abstract: Combinations of an ACE inhibitor and an aldosterone receptor antagonist are described for use in treatment of circulatory disorders. Of particular interest are therapies using captopril or enalapril co-administered with a low-dose of spironolactone. This co-therapy would be particularly useful to treat or prevent the progression of congestive heart failure while avoiding or reducing aldosterone-antagonist-induced side effects such as hyperkalemia.
    Type: Application
    Filed: October 4, 2002
    Publication date: August 7, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Todd E. MacLaughlan, Alfonso T. Perez
  • Combination therapy of angiotensin converting enzyme inhibitor, side-effect reduced amount of aldosterone antagonist and diuretic for treatment of cardiovascular disease
    Publication number: 20030144213
    Abstract: Combinations of an ACE inhibitor, an aldosterone receptor antagonist and a diuretic are described for use in treatment of circulatory disorders. Of particular interest are therapies using captopril or enalapril co-administered with a low-dose of spironolactone and furosemide. 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: October 8, 2002
    Publication date: July 31, 2003
    Applicant: G.D. Searle & Co.
    Inventor: Alfonso T. Perez
  • alpha- and beta-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
    Publication number: 20030144342
    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: Application
    Filed: May 6, 2002
    Publication date: July 31, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • 3,4-diaryl thiopenes and analogs thereof having use as antiinflammatory agents
    Patent number: 6599934
    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: November 13, 2000
    Date of Patent: July 29, 2003
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Stephen R Bertenshaw, Paul W Collins, Thomas D. Penning, David B. Reitz, Roland S Rogers
  • Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Publication number: 20030130202
    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: Application
    Filed: April 12, 2002
    Publication date: July 10, 2003
    Applicant: 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
  • Imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
    Publication number: 20030130329
    Abstract: Compounds characterized generally as imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension.
    Type: Application
    Filed: November 8, 2002
    Publication date: July 10, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity
    Publication number: 20030125328
    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: May 23, 2002
    Publication date: July 3, 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
  • Substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity
    Publication number: 20030125329
    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: May 23, 2002
    Publication date: July 3, 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
  • Process for preparation of 9,11-epoxy steroids and intermediates useful therein
    Patent number: 6586591
    Abstract: A process for the formation of compounds of Formula VI: comprising hydrolyzing a compound corresponding to Formula VII: wherein —A—A—, —B—B—, R3, R8 and R9 are as defined in the specification.
    Type: Grant
    Filed: August 31, 2001
    Date of Patent: July 1, 2003
    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
  • N-protected/N-substituted-beta-amino hydroxy sulfonates
    Patent number: 6586627
    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: March 20, 2002
    Date of Patent: July 1, 2003
    Assignee: G. D. Searle & Co.
    Inventor: Joseph J. Wieczorek
  • Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation
    Patent number: 6586603
    Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders.
    Type: Grant
    Filed: October 21, 2002
    Date of Patent: July 1, 2003
    Assignee: G.D. Searle & Co.
    Inventors: John J Talley, Thomas D Penning, Paul W Collins, Donald J Rogier, Jr., James W Malecha, Julie M Miyashiro, Stephen R. Bertenshaw, Ish K Khanna, Matthew J Graneto, Roland S Rogers, Jeffery S Carter, Stephen H Docter, Stella S Yu