Patents by Inventor Joshua S. Boger
Joshua S. Boger 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).
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Patent number: 5723459Abstract: The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. 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, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.Type: GrantFiled: January 24, 1995Date of Patent: March 3, 1998Assignee: Vertex Pharmaceuticals IncorporatedInventors: David M. Armistead, Matthew W. Harding, Jeffrey O. Saunders, Joshua S. Boger
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Patent number: 5665774Abstract: 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: March 8, 1993Date of Patent: September 9, 1997Inventors: David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
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Patent number: 5622970Abstract: 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: June 1, 1995Date of Patent: April 22, 1997Assignee: Vertex Pharmaceuticals, IncorporatedInventors: David A. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
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Patent number: 5620971Abstract: The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. 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, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.Type: GrantFiled: March 25, 1994Date of Patent: April 15, 1997Assignee: Vertex Pharmaceuticals IncorporatedInventors: David M. Armistead, Jeffrey O. Saunders, Joshua S. Boger
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Patent number: 5516797Abstract: 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: April 11, 1994Date of Patent: May 14, 1996Assignee: Vertex Pharmaceuticals, IncorporatedInventors: David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
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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
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Patent number: 4994553Abstract: Several distinct peptide regions of the secreted form of purified human interleukin-1 species pI 6.8 have been found to exhibit characteristics associated with highly immunogenic protein moieties and are used to produce specific anti-peptide antibodies. The antibodies raised against the individual peptides are specific for the peptide used for their production and for IL-1, pI 6.8. The individual antibodies bind to both the precursor of IL-1, pI 6.8 and the mature or extracellular IL-1, pI 6.8.Type: GrantFiled: June 17, 1988Date of Patent: February 19, 1991Assignee: Merck & Co., Inc.Inventors: John A. Schmidt, Joshua S. Boger, Ellen B. K. Bayne
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Patent number: 4978679Abstract: Positions 7- and/or 6-substituted 1,2,3,4,4a,9b-Hexahydro-8-hydroxydibenzofuran-3-ols and analogs of that general structure are described.These compounds are found to be potent inhibitors of 5-lipoxygenase, an enzyme crucial to the biosynthesis of leukotrienes and useful in the treatment of a variety of inflammatory conditions.Type: GrantFiled: September 25, 1989Date of Patent: December 18, 1990Assignee: Merck & Co., Inc.Inventors: Kathleen M. Rupprecht, Joshua S. Boger
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Patent number: 4975457Abstract: Certain trans-2,3-disubstituted-2,3-dihydro-5-hydroxybenzofurans are described. The synthesis involves an intramolecular Michael addition to yield the thermodynamic trans isomer. The compounds were found to be inhibitors of 5-lipoxygenase, an enzyme crucial to the biosynthesis of leukotrienes and useful for the treatment of various inflammatory diseases.Type: GrantFiled: September 25, 1989Date of Patent: December 4, 1990Assignee: Merck & Co., Inc.Inventors: Kathleen M. Rupprecht, Joshua S. Boger
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Patent number: 4914188Abstract: Novel cyclosporin analogs containing a MeAla or MeAbu residue at the 6-position of the cyclic undecapeptide have been synthesized and found unexpectedly to exhibit antagonistic activity toward cyclosporin A binding to its cytosolic protein receptor, cyclophilin, without being immunosuppressive.Type: GrantFiled: November 16, 1987Date of Patent: April 3, 1990Assignee: Merck & Co., Inc.Inventors: Francis J. Dumont, Philippe L. Durette, Arsenio A. Pessolano, Joshua S. Boger, Nolan H. Sigal
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Patent number: 4812442Abstract: Enzyme tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems employing the novel tripeptides.Type: GrantFiled: May 4, 1987Date of Patent: March 14, 1989Assignee: Merck & Co., Inc.Inventors: Joshua S. Boger, Ben E. Evans, Mark G. Bock
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Patent number: 4782043Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.Type: GrantFiled: October 31, 1985Date of Patent: November 1, 1988Assignee: Merck & Co., Inc.Inventors: Joshua S. Boger, Daniel F. Veber
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Patent number: 4772685Abstract: Several distinct peptide regions of the secreted form of purified human interleukin-1 species pI 6.8 have been found to exhibit characteristics associated with highly immunogenic protein moieties and are used to produce specific anti-peptide antibodies. The antibodies raised against the individual peptides are specific for the peptide used for their production and for IL-1, pI 6.8. The individual antibodies bind to both the precursor of IL-1, pI 6.8 and the mature or extracellular IL-1, pI 6.8.Type: GrantFiled: October 2, 1985Date of Patent: September 20, 1988Assignee: Merck & Co., Inc.Inventors: John A. Schmidt, Joshua S. Boger, Ellen B. K. Bayne
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Patent number: 4761470Abstract: A synthetic peptide, containing the predicted amino acid residues 64 to 77 of the herpes simplex virus type 1 (HSV1) gB structural glycoprotein open reading frame, a synthetic subunit immunogen that stimulates an immune response against HSV1 and which, when prepared, and chemically-conjugated to a protein carrier molecule, and inoculated into test animals, gives rise to a specific anti-peptide IgG response, such that these anti-peptide antibodies react with a purified HSV-specific structural glycoprotein preparation and are capable of neutralizing the infectivity of HSV1.Type: GrantFiled: April 10, 1987Date of Patent: August 2, 1988Assignee: Merck & Co., Inc.Inventors: Emilio A. Emini, Vivian M. Larson, Joshua S. Boger
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Patent number: 4743584Abstract: Cyclic renin-inhibitory peptides of the formula ##STR1## wherein G is an isostere component substituted into the substrate analogy at the cite of the enzyme cleavage, and analogs thereof, which inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.Type: GrantFiled: October 7, 1986Date of Patent: May 10, 1988Assignee: Merck & Co., Inc.Inventor: Joshua S. Boger
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Patent number: 4705892Abstract: An improved process for preparing .alpha.,.omega.-diamino acids, such as D,L-homolysine, 2,8-diaminooctanoic acid, ornithine, lysine, or the like, comprising reaction of phthalic anhydride and an amino alcohol in a hydrocarbon solvent; treatment of the resulting phthalimide--N--(CH.sub.2).sub.n --OH derivative, without isolation thereof, with phosphorus tribromide or phosphorous pentachloride; alkylation of diethyl acetamidomalonate with the phthalimide--N--(CH.sub.2).sub.n --chloride or --bromide of the previous step, in the presence of, particularly, sodium hydride/dimethylformamide; standard acid hydrolysis and decarboxylation; selective protection via copper(II) chelation, N-specific acylation with benzyl chloroformate, and decomposition of the amino acid-copper(II) complex with alkaline thioacetamide; standard t-butoxycarbonyl acylation; and deprotection to obtain the desired .alpha.,.omega.-diamino acids.Type: GrantFiled: October 16, 1986Date of Patent: November 10, 1987Assignee: Merck & Co., Inc.Inventors: Joshua S. Boger, Linda S. Payne
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Patent number: 4668770Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.Type: GrantFiled: May 8, 1984Date of Patent: May 26, 1987Assignee: Merck & Co., Inc.Inventors: Joshua S. Boger, Daniel F. Veber, Ben E. Evans
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Patent number: 4668663Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.Type: GrantFiled: March 27, 1984Date of Patent: May 26, 1987Assignee: Merck & Co., Inc.Inventor: Joshua S. Boger
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Patent number: 4665052Abstract: Renin inhibitory peptides of the formula ##EQU1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.Type: GrantFiled: March 27, 1984Date of Patent: May 12, 1987Assignee: Merck & Co., Inc.Inventor: Joshua S. Boger