Patents by Inventor James A. Sikorski

James A. Sikorski has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 6458785
    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 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: April 18, 2001
    Date of Patent: October 1, 2002
    Assignee: G. D. Searle
    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
  • Use of substituted N, N-bis-phenyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6458852
    Abstract: The invention relates to use of 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. Preferred tertiary-heteroalkylamine compounds are substituted N,N- bis-phenyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: October 1, 2002
    Assignee: 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
  • use of substituted N,N-disubstituted mercapto amino compounds for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6458849
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkyamine 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. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted mercapto amines.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: October 1, 2002
    Assignee: 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 N-phenyl-N-heteroaralkyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6458803
    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. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: November 23, 2001
    Date of Patent: October 1, 2002
    Assignee: 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
  • Combinations of cholesteryl ester transfer protein inhibitors and fibric acid derivatives for cardiovascular indications
    Patent number: 6458850
    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 a fibric acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: October 1, 2002
    Assignee: G.D. Searle, LLC
    Inventors: James A. Sikorski, Kevin C. Glenn
  • Combinations of ileal bile acid transport inhibitors and cholesteryl ester transfer protein inhibitors for cardiovascular indications
    Patent number: 6458851
    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 ileal bile acid transport inhibitor combined with a cholesteryl ester transfer protein (CETP) inhibitor.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: October 1, 2002
    Assignee: G. D. Searle, LLC
    Inventors: Bradley T. Keller, James A. Sikorski, Kevin C. Glenn, Daniel T. Connolly, Mark E. Smith, Joseph R. Schuh
  • Use of substituted N, N-disubstituted fused-heterocyclo amino compounds for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6455519
    Abstract: The invention relates to use of 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. Preferred tertiary-heteroalkylamine compounds are substituted N,N- disubstituted fused-heterocyclo amines.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: September 24, 2002
    Assignee: 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
  • 2-Amino-2-alkyl-5 heptenoic and heptynoic acid derivatives useful as nitric oxide synthase inhibitors
    Publication number: 20020132849
    Abstract: The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Application
    Filed: September 15, 2001
    Publication date: September 19, 2002
    Inventors: Donald W. Hansen, Ronald Keith Webber, Barnett S. Pitzele, James Sikorski, Mark A. Massa, Timothy J. Hagen, Margaret Grapperhaus, Lijuan Jane Wang, Arija A. Bergmanis, Steven W. Kramer, E. Ann Hallinan
  • Use of substituted N-phenoxy-N-phenyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6451823
    Abstract: The invention relates to use of 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. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 17, 2002
    Assignee: 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
  • Use of substituted N,N-disubstituted non-fused heterocyclo amino compounds for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6451830
    Abstract: The invention relates to use of 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. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 17, 2002
    Assignee: 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
  • 2-Amino-2-alkyl-4 hexenoic and hexynoic acid derivatives useful as nitric oxide synthase inhibitors
    Publication number: 20020128510
    Abstract: The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Application
    Filed: September 15, 2001
    Publication date: September 12, 2002
    Inventors: Richard C. Durley, James Sikorski, Donald W. Hansen, Michelle A. Promo, Ronald Keith Webber, Barnett S. Pitzele, Alok K. Awasthi, Alan Moorman
  • Use of substituted N-fused-phenyl-N-benzyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6448295
    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. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 10, 2002
    Assignee: 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 N, N-disubstituted diamino compounds useful for inhibiting cholesteryl ester transfer protein activity
    Publication number: 20020120011
    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. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted diamines.
    Type: Application
    Filed: November 14, 2001
    Publication date: August 29, 2002
    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
  • Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Publication number: 20020111368
    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: April 18, 2001
    Publication date: August 15, 2002
    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
  • Pyrazole substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
    Patent number: 6432999
    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: August 13, 2002
    Assignee: Pharmacia Corporation
    Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Hwang-Fun Lu
  • 2-Amino-2-alky-4 heptenoic and heptynoic acid derivatives useful as nitric oxide synthase inhibitors
    Publication number: 20020103398
    Abstract: The present invention relates to 2-amino-2-alkyl-4 heptenoic and heptynoic ac derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Application
    Filed: September 15, 2001
    Publication date: August 1, 2002
    Inventors: Donald W. Hansen, Mahima Trivedi, Mihaly V. Toth, Ronald Keith Webber, Barnett S. Pitzele, Alok K. Awasthi, James Sikorski
  • Substituted sulfonylphenylheterocycles as cyclooxygenase-2 and 5-lipoxygenase inhibitors
    Publication number: 20020086886
    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-lizoxygenase, such as inflammation.
    Type: Application
    Filed: December 4, 2001
    Publication date: July 4, 2002
    Applicant: G.D. Searle & Co.
    Inventors: John J. Talley, James A. Sikorski, Balekudru Devadas, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Roland S. Rogers, Kathy L. Rogers, Hwang-Fun Lu, David L. Brown
  • 2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
    Publication number: 20020077363
    Abstract: The present invention contains novel compounds useful as nitric oxide synthase inhibitors.
    Type: Application
    Filed: April 13, 2001
    Publication date: June 20, 2002
    Inventors: Barnett S. Pitzele, James A. Sikorski, Ronald Keith Webber
  • Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 6407134
    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: February 5, 2001
    Date of Patent: June 18, 2002
    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
  • 2-amino-2-alkyl-3 heptenoic and heptynoic acid derivatives useful as nitric oxide synthase inhibitors
    Publication number: 20020072630
    Abstract: The present invention relates to 2-amino-2-alkyl-3 heptenoic and heptynoic ac derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors
    Type: Application
    Filed: September 15, 2001
    Publication date: June 13, 2002
    Inventors: Donald W. Hansen, Ronald Keith Webber, Barnett S. Pitzele, Alok K. Awasthi, James Sikorski, Mahima Trivedi