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).

  • Patent number: 5723459
    Abstract: 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: Grant
    Filed: January 24, 1995
    Date of Patent: March 3, 1998
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David M. Armistead, Matthew W. Harding, Jeffrey O. Saunders, Joshua S. Boger
  • Patent number: 5665774
    Abstract: 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: Grant
    Filed: March 8, 1993
    Date of Patent: September 9, 1997
    Inventors: David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
  • Patent number: 5622970
    Abstract: 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: Grant
    Filed: June 1, 1995
    Date of Patent: April 22, 1997
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: David A. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
  • Patent number: 5620971
    Abstract: 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: Grant
    Filed: March 25, 1994
    Date of Patent: April 15, 1997
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David M. Armistead, Jeffrey O. Saunders, Joshua S. Boger
  • Patent number: 5516797
    Abstract: 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: Grant
    Filed: April 11, 1994
    Date of Patent: May 14, 1996
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
  • Patent number: 5330993
    Abstract: 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: Grant
    Filed: July 2, 1991
    Date of Patent: July 19, 1994
    Assignee: Vertex Pharmaceuticals, Inc.
    Inventors: David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
  • Patent number: 5192773
    Abstract: 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: Grant
    Filed: July 2, 1990
    Date of Patent: March 9, 1993
    Assignee: Vertex Pharmaceuticals, Inc.
    Inventors: David A. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
  • Patent number: 4994553
    Abstract: 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: Grant
    Filed: June 17, 1988
    Date of Patent: February 19, 1991
    Assignee: Merck & Co., Inc.
    Inventors: John A. Schmidt, Joshua S. Boger, Ellen B. K. Bayne
  • Patent number: 4978679
    Abstract: 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: Grant
    Filed: September 25, 1989
    Date of Patent: December 18, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Kathleen M. Rupprecht, Joshua S. Boger
  • Patent number: 4975457
    Abstract: 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: Grant
    Filed: September 25, 1989
    Date of Patent: December 4, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Kathleen M. Rupprecht, Joshua S. Boger
  • Patent number: 4914188
    Abstract: 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: Grant
    Filed: November 16, 1987
    Date of Patent: April 3, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Francis J. Dumont, Philippe L. Durette, Arsenio A. Pessolano, Joshua S. Boger, Nolan H. Sigal
  • Patent number: 4812442
    Abstract: 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: Grant
    Filed: May 4, 1987
    Date of Patent: March 14, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Joshua S. Boger, Ben E. Evans, Mark G. Bock
  • Patent number: 4782043
    Abstract: 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: Grant
    Filed: October 31, 1985
    Date of Patent: November 1, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Joshua S. Boger, Daniel F. Veber
  • Patent number: 4772685
    Abstract: 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: Grant
    Filed: October 2, 1985
    Date of Patent: September 20, 1988
    Assignee: Merck & Co., Inc.
    Inventors: John A. Schmidt, Joshua S. Boger, Ellen B. K. Bayne
  • Patent number: 4761470
    Abstract: 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: Grant
    Filed: April 10, 1987
    Date of Patent: August 2, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Emilio A. Emini, Vivian M. Larson, Joshua S. Boger
  • Patent number: 4743584
    Abstract: 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: Grant
    Filed: October 7, 1986
    Date of Patent: May 10, 1988
    Assignee: Merck & Co., Inc.
    Inventor: Joshua S. Boger
  • Patent number: 4705892
    Abstract: 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: Grant
    Filed: October 16, 1986
    Date of Patent: November 10, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Joshua S. Boger, Linda S. Payne
  • Patent number: 4668770
    Abstract: 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: Grant
    Filed: May 8, 1984
    Date of Patent: May 26, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Joshua S. Boger, Daniel F. Veber, Ben E. Evans
  • Patent number: 4668663
    Abstract: 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: Grant
    Filed: March 27, 1984
    Date of Patent: May 26, 1987
    Assignee: Merck & Co., Inc.
    Inventor: Joshua S. Boger
  • Patent number: 4665052
    Abstract: 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: Grant
    Filed: March 27, 1984
    Date of Patent: May 12, 1987
    Assignee: Merck & Co., Inc.
    Inventor: Joshua S. Boger