Patents by Inventor Robert L. Bugianesi
Robert L. Bugianesi 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: 7479504Abstract: The present invention encompasses compounds of Formula 1: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.Type: GrantFiled: January 15, 2003Date of Patent: January 20, 2009Assignee: Merck & Co., Inc.Inventors: Robert L. Bugianesi, George A. Doherty, Amy Gentry, Jeffrey J. Hale, Christopher L. Lynch, Sander G. Mills, William E. Neway, III
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Patent number: 6528531Abstract: Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.Type: GrantFiled: November 10, 2000Date of Patent: March 4, 2003Assignee: Merck & Co., Inc.Inventors: Tesfaye Bitfu, Danqing D. Feng, Gui-Bai Liang, Mitree M. Ponpipom, Xiaoxia Qian, Michael H. Fisher, Matthew J. Wyvratt, Robert L. Bugianesi
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Patent number: 5985892Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: March 25, 1999Date of Patent: November 16, 1999Assignee: Merck & Co., Ltd.Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla, Robert L. Bugianesi
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Patent number: 5756507Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: December 5, 1996Date of Patent: May 26, 1998Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Lin Chu, Wallace T. Ashton, Michael H. Fisher, Matthew J. Wyvratt, Roy G. Smith, Robert L. Bugianesi, Mitree M. Ponpipom, Yi Tien Yang, Peter Lin
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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: 5369125Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.Type: GrantFiled: March 19, 1993Date of Patent: November 29, 1994Assignee: Merck & Co., Inc.Inventors: Gregory D. Berger, James D. Bergstrom, Tesfaye Biftu, Robert L. Bugianesi, Robert M. Burk, Narindar N. Girotra, C. H. Kuo, William H. Parsons, Mitree M. Ponpipom, Lori L. Whiting
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Patent number: 5114961Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3, 4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio moiety.Type: GrantFiled: December 10, 1990Date of Patent: May 19, 1992Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Robert L. Bugianesi, Nirindar N. Girotra, Mitree M. Ponpipom, Soumya P. Sahoo, Chan H. Kuo
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Patent number: 5010100Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group, Y is an alkyl or substituted alkyl group and R.sup.6 is an alkoxy or a substituted alkoxy or alkyl group.Type: GrantFiled: June 8, 1989Date of Patent: April 23, 1991Assignee: Merck & Co. Inc.Inventors: Tesfaye Biftu, John C. Chabala, Robert L. Bugianesi, Mitree M. Ponpipom, Soumya P. Sahoo
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Patent number: 5001123Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein Ar is a pyridyl, a dimethoxy-pyridyl or dimethoxy-pyrazyl group, R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3,4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio group.Type: GrantFiled: June 8, 1989Date of Patent: March 19, 1991Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Nirindar N. Girotra, Robert L. Bugianesi, Mitree M. Ponpipom, Soumya P. Sahoo, Chan H. Kuo
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Patent number: 4996203Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3,4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio moiety.Type: GrantFiled: June 8, 1989Date of Patent: February 26, 1991Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Robert L. Bugianesi, Nirindar N. Girotra, Mitree M. Ponpipom, Soumya P. Sahoo, Chan H. Kuo
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Patent number: 4761404Abstract: There are disclosed phospholipid analogs which are useful as PAF synthesis inhibitors. These compounds inhibit PAF (platelet-activating factor) biosynthesis and are thereby useful in the treatment of various diseases or disorders mediated by the PAF such as, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, and adult respiratory distress syndrome.Type: GrantFiled: July 1, 1985Date of Patent: August 2, 1988Assignee: Merck & Co., Inc.Inventors: Robert L. Bugianesi, Mitree M. Ponpipom, Kathleen M. Rupprecht
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Patent number: 4704462Abstract: Substituted 2,3,3a,6-tetrahydro-6-oxobenzofuran derivatives have been prepared. These neolignans are found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by PAF, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, toxic shock syndrome and adult respiratory distress syndrome.Type: GrantFiled: August 22, 1985Date of Patent: November 3, 1987Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, San-Bao Hwang, Mitree M. Ponpipom, Robert L. Bugianesi
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Patent number: 4554349Abstract: The invention disclosed herein relates to novel 1-deoxyglycosides, preferably 1-deoxy-D-mannopyranosides and 1-deoxy-L-rhamnopyranosides, having in the 1-position of the pyranose ring an aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy or aralkanoylamino/aralkenoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxyglycosides starting with the corresponding tetra-O-acetylglycopyranosyl bromide or amine. The 6-hydroxy group of 1-substituted-1 deoxyglycopyranosides can also be replaced by other functional groups. These aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy and aralkanoylamino/aralkenoylamino 1-deoxyglycosides are potent inhibitors of antigen-specific T-cell proliferation and are also useful as inhibitors of delayed-type hypersensitivity reactions.Type: GrantFiled: October 11, 1983Date of Patent: November 19, 1985Assignee: Merck & Co., Inc.Inventors: Mitree M. Ponpipom, Tsung-Ying Shen, Robert L. Bugianesi
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Patent number: 4386026Abstract: Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release. Other examples include the macrophage ligand N.sup.2 -N.sup.2, N.sup.6 -Bis-[3-(.alpha.-D-mannopyranosylthio)propionyl]-6-lysyl-N.sup.6 -[3-(.alpha.-D-mannopyranosylthio)propionyl]-L-lysine, 5, which when coupled to .beta.Type: GrantFiled: April 20, 1981Date of Patent: May 31, 1983Assignee: Merck & Co., Inc.Inventors: Mitree M. Ponpipom, Robert L. Bugianesi, James C. Robbins, Tsung-Ying Shen
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Patent number: 4259324Abstract: Compounds of the formulae Y--R wherein Y is 1-thio-.beta.-L-fucose, 1-thio-.beta.-D-galactose or 1-thio-.beta.-lactose and R is 2-(1-adamantyl)ethyl, 3-[(p-tetrafluorophenethyl)phenyl]propyl, 6-(5-cholesten-3.beta.-yloxy)hex-3-ynl, oleyl, or hexadecyl are useful immunologic adjuvants in vaccines.Type: GrantFiled: July 31, 1979Date of Patent: March 31, 1981Assignee: Merck & Co., Inc.Inventors: Mitree M. Ponpipom, Tsung-Ying Shen, Robert L. Bugianesi
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Patent number: 4229441Abstract: Glycolipid compounds of the formulae ##STR1## wherein R is ##STR2## are useful immunologic adjuvants in vaccines.Type: GrantFiled: December 1, 1978Date of Patent: October 21, 1980Assignee: Merck & Co., Inc.Inventors: Robert L. Bugianesi, Mitree M. Ponpipom, Tsung-Ying Shen
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Patent number: 4228274Abstract: The invention disclosed herein relates to novel 1-deoxy-glycopyranosides, preferably 1-deoxy-D-mannopyranosides, having in the 1-position of the pyranoside ring an .omega.-aminoalkylthio, .omega.-aminoalkyloxy or .omega.-aminoalkanoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxy-glycopyranosides starting with the corresponding tetra-O-acetyl-glycopyranosyl bromide or amine. These .omega.-amino(alkylthio, alkyloxy or alkanoylamino)-1-deoxy-glycopyranosides, and in particular 1-[(6'-aminohexyl)thio or oxy]-1-deoxy-D-mannopyranosides, possess insulin-like activity.Type: GrantFiled: July 10, 1978Date of Patent: October 14, 1980Assignee: Merck & Co., Inc.Inventors: Mitree M. Ponpipom, Robert L. Bugianesi, Philippe L. Durette, Howard M. Katzen, Tsung-Ying Shen