Patents by Inventor Robert W. Marquis
Robert W. Marquis 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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Publication number: 20040229863Abstract: The present invention provides methods which use 4-amino-azepan-3-one protease inhibitors of cathepsin S in the treatment of diseases in which cathepsin S is implicated, especially treatment or prevention of autoimmune disease; treatment or prevention of a disease state caused by the formation of atherosclerotic lesions and complications arising therefrom; and diseases requiring inhibition, for therapy, of a class II MHC-restricted immune response, inhibition of an asthmatic response, inhibition of an allergic response, inhibition of immune response against a transplanted organ or tissue, or inhibition of elastase activity in atheroma, and novel compounds for use therewith.Type: ApplicationFiled: March 10, 2004Publication date: November 18, 2004Applicant: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
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Publication number: 20040192674Abstract: The present invention provides methods which uses certain 4-amino-azepan-3-ones to inhibit cathepsin L. Consequently they are useful for preventing or treating diseases in which cathepsin L is implicated, such as rheumatoid arthritis or inhibition of positive selection of CD4+T-cells by cortical thymic epithelial cells.Type: ApplicationFiled: February 5, 2004Publication date: September 30, 2004Inventor: Robert W. Marquis
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Publication number: 20040180927Abstract: The present invention relates to compounds of formula (I): 1Type: ApplicationFiled: February 27, 2004Publication date: September 16, 2004Applicant: SmithKline Beecham CorporationInventors: Robert W. Marquis, Daniel F. Veber, Yu Ru, Stephen Lo Castro
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Publication number: 20040044201Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: ApplicationFiled: September 20, 2002Publication date: March 4, 2004Inventors: Maxwell D. Cummings, Robert W. Marquis Jr., Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
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Publication number: 20040038965Abstract: The present invention provides C3-C6 1-amino-1-acyl cycloalkane-substituted 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: ApplicationFiled: May 22, 2003Publication date: February 26, 2004Inventors: Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
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Publication number: 20040034013Abstract: The present invention provides methods which use 4-amino-azepan-3-one protease inhibitors of cathepsin L in the treatment of diseases in which cathepsin L is implicated, especially treatment or prevention of rheumatoid arthritis; treatment or prevention of cancer metastasis; treatment or prevention of diseases requiring inhibition of tissue destruction by macrophage, particularly lung macrophage, such as asthma, chronic obstructive pulmonary disease (COPD), and emphysema; treatment or prevention of diseases requiring, for therapy, inhibition of positive selection of CD4+ T-cells by cortical thymic epithelial cells.Type: ApplicationFiled: October 17, 2002Publication date: February 19, 2004Inventors: Maxwell D Cummings, Robert W Marquis, Yu Ru, Scott K Thompson, Daniel F Veber, Dennis S Yamashita
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Patent number: 6596715Abstract: This invention relates to the compound of Formula (I): or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor.Type: GrantFiled: May 6, 2002Date of Patent: July 22, 2003Assignee: SmithKline Beecham CorporationInventors: Robert W. Marquis, Jr., Daniel Frank Veber
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Publication number: 20030114437Abstract: The present invention provides methods which use 4-amino-azepan-3-one protease inhibitors of cathepsin S in the treatment of diseases in which cathepsin S is implicated, especially treatment or prevention of autoimmune disease; treatment or prevention of a disease state caused by the formation of atherosclerotic lesions and complications arising therefrom; and diseases requiring inhibition, for therapy, of a class II MHC-restricted immune response, inhibition of an asthmatic response, inhibition of an allergic response, inhibition of immune response against a transplanted organ or tissue, or inhibition of elastase activity in atheroma, and novel compounds for use therewith.Type: ApplicationFiled: October 17, 2002Publication date: June 19, 2003Inventors: Maxwell D. Cummings, Robert W. Marquis Jr, Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
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Patent number: 6566373Abstract: The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.Type: GrantFiled: July 30, 2001Date of Patent: May 20, 2003Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: Andrew D Gribble, Ashley Edward Fenwick, Robert W Marquis, Daniel F Veber, Jason Witherington
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Patent number: 6534498Abstract: This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor.Type: GrantFiled: May 6, 2002Date of Patent: March 18, 2003Assignee: SmithKline Beecham CorporationInventors: Robert W. Marquis, Jr., Yu Ru, Daniel Frank Veber
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Publication number: 20020128476Abstract: This invention relates to compounds of formula (I): 1Type: ApplicationFiled: April 17, 2001Publication date: September 12, 2002Applicant: SmithKline Beecham corporationInventors: Robert W. Marquis, Daniel F. Veber, Yu Ru, Stephen Lo Castro
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Publication number: 20020082426Abstract: 1Type: ApplicationFiled: February 27, 2002Publication date: June 27, 2002Applicant: SmithKline Beecham CorporationInventors: Ashley E. Fenwick, Andrew D. Gribble, Robert W. Marquis, Jason Witherington
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Patent number: 6369077Abstract: This invention relates to compounds of formula (I): wherein: Y is Ar or NR1R2; R1 is R″, R″C(O), R″C(S), R″SO2, R″OC(O), R″R′NC(O), or R″R′NC(S); R2 is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R3 is H, C2-6alkenyl, C2-6alkynyl, Het, Ar or C1-6alkyl optionally substituted by OR′, SR′, NR′2, N(R′)C(O)OR″, CO2R′, CO2NR′2, N(C═NH)NH2, Het or Ar; R4 is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R5 is Ar-C0-6alkyl, Het-C0-6alkyl, adamantyl-C(O)—, Ar-C(O)—, Het-C(O)— or; R6 is R″, R″C(O), R″C(S), R″SO2, R″OC(O), R″R′NC(O), R″R′NC(S), or R″OC(O)NR′CH(R*)C(O); R7 is C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, Ar-C0-6alkoxy, Het-C0-6alkoxy, or C1-6alkyl optionally substituted by OR′, SR′, NR′2, N(R′)C(O)OR″, CO2R&pType: GrantFiled: November 4, 1999Date of Patent: April 9, 2002Assignee: SmithKline Beecham CorporationInventors: Robert W. Marquis, Yu Ru, Daniel F. Veber, Stephen M. LoCastro
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Publication number: 20020013360Abstract: The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.Type: ApplicationFiled: July 30, 2001Publication date: January 31, 2002Applicant: SmithKline Beecham CorporationInventors: Andrew D. Gribble, Ashley Edward Fenwick, Robert W. Marquis, Daniel F. Veber, Jason Witherington
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Patent number: 5559128Abstract: The present invention is directed to certain novel compounds identified as 3-substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.4, R.sup.5, A, X, and Y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing these compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: April 18, 1995Date of Patent: September 24, 1996Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Ravi Nargund, Robert W. Marquis, Arthur A. Patchett, Lihu Yang
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Patent number: 5506262Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthetase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: November 10, 1993Date of Patent: April 9, 1996Assignee: Merck & Co., Inc.Inventors: Robert M. Burk, William H. Parsons, John J. Acton, III, Gregory D. Berger, Tesfaye Biftu, Robert L. Bugianesi, Yuan-Ching P. Chiang, Claude Dufresne, Narindar N. Girotra, Robert W. Marquis, Jr., Chan-Hwa Kuo, Sandra P. Plevyak, Mitree M. Ponpipom, Lori L. Whiting, James D. Bergstrom, Conrad Santini
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Patent number: 5258401Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: September 10, 1992Date of Patent: November 2, 1993Assignee: Merck & Co., Inc.Inventors: Gregory D. Berger, Robert W. Marquis, Jr., Albert J. Robichaud, Edward M. Scolnick