Patents Assigned to Vertex Pharmaceutical, Inc.
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Patent number: 5985838Abstract: Disclosed are compounds, compositions and methods for inhi.beta.iting interleukin-1.beta. protease activity, the compounds .alpha.-substituted methyl ketones having the formula (I) set forth herein. These compounds are inhibitors of IL-1.beta. converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.Type: GrantFiled: July 10, 1996Date of Patent: November 16, 1999Assignee: Vertex Pharmaceuticals, Inc.Inventors: Roland E. Dolle, Irennegbe K. Osifo, Stanley J. Schmidt, Denton W. Hoyer, Tina Morgan Ross, Prasad V. Chaturvedula, Catherine P. Prouty, Mohamed M. A. Awad, Joseph M. Salvino, James M. Rinker, Eric P. Lodge, Jasbir Singh, Mark A. Ator
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Patent number: 5976529Abstract: A protein such as an enzyme or antibody is immobilized by crosslinking crystals of the protein with a multifunctional crosslinking agent. The crosslinked protein crystals may be lyophilized for storage. A preferred protein is an enzyme such as thermolysin, elastase, asparaginase, lysozyme, lipase or urease. Crosslinked enzyme crystals preferably retain at least 91% activity after incubation for three hours in the presence of a concentration of Pronase.TM. that causes the soluble uncrosslinked form of the enzyme to lose at least 94% of its initial activity under the same conditions. A preferred enzyme:Pronase.TM. ratio is 1:40. Enzyme crystals that are crosslinked may be microcrystals having a cross-section of 10.sup.-1 mm or less.Type: GrantFiled: June 7, 1995Date of Patent: November 2, 1999Assignee: Vertex Pharmaceuticals, Inc.Inventors: Manuel A. Navia, Nancy L. St. Clair
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Patent number: 5973111Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: March 28, 1997Date of Patent: October 26, 1999Assignee: Vertex Pharmaceuticals, Inc.Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
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Patent number: 5912269Abstract: This invention relates to butyrate prodrugs derived from lactic acid and pharmaceutical compositions and methods employing them, either alone or in combination with other agents, for increasing gamma globin and fetal hemoglobin in a patient. These compounds, compositions and methods are particularly effective in treating .beta.-hemoglobinopathies, including sickle cell syndromes and .beta.-thalassemia syndromes. In addition, this invention relates to the use of these prodrugs, alone or in combination with other agents, to stimulate cell differentiation which prevents proliferation of malignant cells. These methods are particularly useful in treating cancer, especially malignant hematological disorders.Type: GrantFiled: April 30, 1996Date of Patent: June 15, 1999Assignee: Vertex Pharmaceuticals, Inc.Inventors: Roger D. Tung, Biqin Li
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Patent number: 5883123Abstract: This invention relates to butyrate prodrugs derived from lactic acid and pharmaceutical compositions and methods employing them, either alone or in combination with other agents, for increasing gamma globin and fetal hemoglobin in a patient. These compounds, compositions and methods are particularly effective in treating .beta.-hemoglobinopathies, including sickle cell syndromes and .beta.-thalassemia syndromes. In addition, this invention relates to the use of these prodrugs, alone or in combination with other agents, to stimulate cell differentiation which prevents proliferation of malignant cells. These methods are particularly useful in treating cancer, especially malignant hematological disorders.Type: GrantFiled: October 6, 1995Date of Patent: March 16, 1999Assignee: Vertex Pharmaceuticals, Inc.Inventors: Roger D. Tung, Biqin Li
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Patent number: 5880152Abstract: This invention relates to butyrate prodrugs derived from lactic acid and pharmaceutical compositions and methods employing them, either alone or in combination with other agents, for increasing gamma globin and fetal hemoglobin in a patient. These compounds, compositions and methods are particularly effective in treating .beta.-hemoglobinopathies, including sickle cell syndromes and .beta.-thalassemia syndromes. This invention relates to the use of these prodrugs, alone or in combination with other agents, to stimulate cell differentiation which prevents proliferation of malignant cells. These methods are particularly useful in treating cancer, especially malignant hematological disorders. In addition, this invention relates to the use of these prodrugs in treating inflammatory bowel diseases.Type: GrantFiled: March 10, 1997Date of Patent: March 9, 1999Assignee: Vertex Pharmaceuticals, Inc.Inventors: Roger D. Tung, Bigin Li
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Patent number: 5849296Abstract: A protein such as an enzyme or antibody is immobilized by crosslinking crystals of the protein with a multifunctional crosslinking agent. The crosslinked protein crystals may be lyophilized for storage. A preferred protein is an enzyme such as thermolysin, elastase, asparaginase, lysozyme, lipase or urease. Crosslinked enzyme crystals preferably retain at least 91% activity after incubation for three hours in the presence of a concentration of Pronase.TM. that causes the soluble uncrosslinked form of the enzyme to lose at least 94% of its initial activity under the same conditions. A preferred enzyme:Pronase.TM. ratio is 1:40. Enzyme crystals that are crosslinked may be microcrystals having a cross-section of 10.sup.-1 mm or less.Type: GrantFiled: June 7, 1995Date of Patent: December 15, 1998Assignee: Vertex Pharmaceuticals, Inc.Inventors: Manuel A. Navia, Nancy L. St. Clair
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Patent number: 5843904Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 and apoptosis-mediated diseases, including inflammatory diseases, autoimmune diseases, proliferative, infectious, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: December 20, 1995Date of Patent: December 1, 1998Assignee: Vertex Pharmaceuticals, Inc.Inventors: Guy W. Bemis, John P. Duffy, Wolf Herman Fridman, Julian M. C. Golec, David J. Livingston, Michael D. Mullican, Mark A. Murcko, Robert E. Zelle
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Patent number: 5763590Abstract: An FK506 binding protein of mammalian origin of approximate size (M.sub.r) 52,000, isolated by FK506 affinity chromatography and a corresponding human cDNA of approximate size 2.2 Kb, isolated by screening a human placenta cDNA library with a DNA probe whose sequence predicts a consensus amino acid sequence present in five FKBP12 sequences and in the human FKBP13 sequence.Type: GrantFiled: November 9, 1994Date of Patent: June 9, 1998Assignee: Vertex Pharmaceuticals, Inc.Inventors: Debra A. Peattie, Matthew W. Harding, David J. Livingston
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Patent number: 5756466Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: June 17, 1994Date of Patent: May 26, 1998Assignee: Vertex Pharmaceuticals, Inc.Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko
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Patent number: 5717092Abstract: The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.Type: GrantFiled: March 29, 1996Date of Patent: February 10, 1998Assignee: Vertex Pharmaceuticals Inc.Inventors: David M. Armistead, Jeffrey O. Saunders
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Patent number: 5716929Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: June 5, 1995Date of Patent: February 10, 1998Assignee: Vertex Pharmaceuticals, Inc.Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
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Patent number: 5656627Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: March 17, 1995Date of Patent: August 12, 1997Assignee: Vertex Pharmaceuticals, Inc.Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
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Patent number: 5618710Abstract: A protein such as an enzyme of antibody is immobilized by crosslinking crystals of the protein with a multifunctional crosslinking agent. The crosslinked protein crystals may be lyophilized for storage. A preferred protein is an enzyme such as thermolysin, elastase, asparaginase, lysozyme, lipase or urease. Crosslinked enzyme crystals preferably retain at least 91% activity after incubation for three hours in the presence of a concentration of Pronase.TM. that causes the soluble uncrosslinked form of the enzyme to lose at least 94% of its initial activity under the same conditions. A preferred enzyme:Pronase.TM. ratio is 1:40. Enzyme crystals that are crosslinked may be microcrystals having a cross-section of 10.sup.-1 mm or less.Type: GrantFiled: February 12, 1993Date of Patent: April 8, 1997Assignee: Vertex Pharmaceuticals, Inc.Inventors: Manuel A. Navia, Nancy L. St. Clair
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Patent number: 5330993Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamass) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.Type: GrantFiled: July 2, 1991Date of Patent: July 19, 1994Assignee: Vertex Pharmaceuticals, Inc.Inventors: David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
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Patent number: 5192773Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.Type: GrantFiled: July 2, 1990Date of Patent: March 9, 1993Assignee: Vertex Pharmaceuticals, Inc.Inventors: David A. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung