Abstract: This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to ?novel! reagents useful therein.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
March 24, 1998
Assignee:
Corvas International, Inc.
Inventors:
Thomas Roy Webb, John Eugene Reiner, Susan Yoshiko Tamura, William Charles Ripka, Raymond Dagnino, Jr., Ruth Foelsche Nutt
Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Type:
Grant
Filed:
June 17, 1994
Date of Patent:
February 3, 1998
Assignee:
Corvas International, Inc.
Inventors:
Joseph E. Semple, Odile E. Levy, Ruth F. Nutt, William C. Ripka
Abstract: Novel compounds having activity against trypsin are disclosed. Specifically, novel peptide aldehyde analogues that have substantial potency and specificity as inhibitors of mammalian pancreatic trypsin are presented. The compounds are useful in the prevention and treatment of the tissue damage or destruction associated with pancreatitis.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
February 3, 1998
Assignee:
Corvas International, Inc.
Inventors:
Terence K. Brunck, Michael G. Pepe, Daniel A. Pearson, Thomas R. Webb
Abstract: Compositions enriched for Neutrophil Inhibitory Factor which inhibit neutrophil activity including adhesion to vascular endothelial cells are provided. Such compositions may comprise a glycoprotein isolated from nematodes, particularly of the genus Ancylostoma. These compositions are useful in the therapy of conditions which involve abnormal or undesired inflammatory responses.
Type:
Grant
Filed:
May 24, 1994
Date of Patent:
January 13, 1998
Assignee:
Corvas International, Inc.
Inventors:
Matthew Moyle, David L. Foster, George P. Vlasuk
Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 30, 1997
Assignee:
Corvas International, Inc.
Inventors:
Joseph Edward Semple, Robert John Ardecky, Ruth Foelsche Nutt, William Charles Ripka, David C. Rowley, Marguerita S. L. Lim-Wilby, Terence Kevin Brunck
Abstract: The present invention discloses peptide aldehydes which are potent inhibitors of factor Xa, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Type:
Grant
Filed:
December 21, 1994
Date of Patent:
December 9, 1997
Assignee:
Corvas International, Inc.
Inventors:
Matthew Mark Abelman, Todd Anthony Miller, Ruth Foelsche Nutt
Abstract: This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
Type:
Grant
Filed:
April 28, 1994
Date of Patent:
October 28, 1997
Assignee:
Corvas International, Inc.
Inventors:
Matthew M. Abelman, Robert J. Ardecky, Ruth F. Nutt
Abstract: a-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions, diagnostic compositions and pharmaceutical compositions, which are useful for preventing or treating in a mammal a pathological condition characterized by thrombosis are described.a-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions and diagnostic compositions, which are useful for in vivo imaging of thrombi in a mammal are also described.Methods of preventing or treating in a mammal a pathological condition characterized by thrombosis and methods of in vivo imaging of thrombi in a mammal are also disclosed.
Type:
Grant
Filed:
March 25, 1994
Date of Patent:
September 23, 1997
Assignee:
Corvas International, Inc.
Inventors:
Matthew M. Abelman, Daniel A. Pearson, George P. Vlasuk, Thomas R. Webb
Abstract: This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
Type:
Grant
Filed:
April 18, 1995
Date of Patent:
August 19, 1997
Assignee:
Corvas International Inc.
Inventors:
Matthew Mark Abelman, Robert John Ardecky, Ruth Foelsche Nutt
Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
August 19, 1997
Assignee:
Corvas International, Inc.
Inventors:
Susan Yoshiko Tamura, Joseph Edward Semple, William Charles Ripka, Robert John Ardecky, Yu Ge, Stephen H. Carpenter, Terence K. Brunck
Abstract: The present invention discloses heterocyclic aromatic peptide aldehydes which have an oxopyrimidine or oxopyridine group and an argininal tail which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
August 12, 1997
Assignee:
Corvas International, Inc.
Inventors:
Susan Yoshiko Tamura, Joseph Edward Semple, William Charles Ripka, Robert John Ardecky, Yu Ge, Stephen H. Carpenter, Terence K. Brunck
Abstract: .alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions, diagnostic compositions and pharmaceutical compositions, which are useful for preventing or treating in a mammal a pathological condition characterized by thrombosis are described..alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions and diagnostic compositions, which are useful for in vivo imaging of thrombi in a mammal are also described.Methods of preventing or treating in a mammal a pathological condition characterized by thrombosis and methods of in vivo imaging of thrombi in a mammal are also disclosed.
Type:
Grant
Filed:
March 25, 1993
Date of Patent:
August 12, 1997
Assignee:
Corvas International, Inc.
Inventors:
Matthew M. Abelman, Daniel A. Pearson, George P. Vlasuk, Thomas R. Webb
Abstract: This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
July 8, 1997
Assignee:
Corvas International, Inc.
Inventors:
Matthew M. Abelman, Robert J. Ardecky, Ruth F. Nutt
Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease slates in mammals characterized by abnormal thrombosis.
Type:
Grant
Filed:
June 17, 1994
Date of Patent:
June 10, 1997
Assignee:
Corvas International, Inc.
Inventors:
Odile E. Levy, Susan Y. Tamura, Ruth F. Nutt, William C. Ripka
Abstract: The present invention is directed to N-sulfonyl arginine alpha-keto-amide derivatives, their pharmaceutically acceptable salts and compositions thereof which are useful as antithrombotic agents in mammals and also the use of these compounds as antithrombotic agents. Also, disclosed are methods of using these inhibitors in their various embodiments as therapeutic agents for disease states characterized by disorders of the blood coagulation process. Further disclosed are compounds useful as intermediates in the preparation of these compounds.
Type:
Grant
Filed:
October 18, 1993
Date of Patent:
January 28, 1997
Assignee:
Corvas International, Inc.
Inventors:
Thomas R. Webb, Todd A. Miller, George P. Vlasuk, Matthew M. Abelman
Abstract: Novel compounds having activity against trypsin are disclosed. Specifically, novel peptide aldehyde analogues that have substantial potency and specificity as inhibitors of mammalian pancreatic trypsin are presented. The compounds are useful in the prevention and treatment of the tissue damage or destruction associated with pancreatitis.
Type:
Grant
Filed:
January 29, 1993
Date of Patent:
July 9, 1996
Assignee:
Corvas International, Inc.
Inventors:
Terence K. Brunck, Michael G. Pepe, Daniel A. Pearson, Thomas R. Webb
Abstract: Coagulation protein antagonists are disclosed, which include monoclonal-type antibodies and related cell lines disclosed for the production of specific, neutralizing antibodies against factors VII and VIIa and the tissue factor/factor VIIa bimolecular complex, which antibodies are useful for the prevention or treatment of thrombotic and related diseases, for immunoaffinity isolation and purification of factors VII and VIIa and the tissue factor/factor VIIa complex, and for determination of factors VII or VIIa and the tissue factor/factors VII or VIIa complex in a biological sample.
Abstract: This invention relates to peptide aldehyde analogs that inhibit the thrombin or Factor Xa. The compounds are thought useful for preventing or treating conditions in mammal characterized by abnormal thrombosis.
Type:
Grant
Filed:
February 14, 1994
Date of Patent:
February 20, 1996
Assignee:
Corvas International, Inc.
Inventors:
George P. Vlasuk, Thomas R. Webb, Daniel A. Pearson, Matthew M. Abelman