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).

  • Patent number: 7479504
    Abstract: 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: Grant
    Filed: January 15, 2003
    Date of Patent: January 20, 2009
    Assignee: 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
  • Patent number: 6528531
    Abstract: 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: Grant
    Filed: November 10, 2000
    Date of Patent: March 4, 2003
    Assignee: 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
  • Patent number: 5985892
    Abstract: 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: Grant
    Filed: March 25, 1999
    Date of Patent: November 16, 1999
    Assignee: Merck & Co., Ltd.
    Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla, Robert L. Bugianesi
  • Patent number: 5756507
    Abstract: 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: Grant
    Filed: December 5, 1996
    Date of Patent: May 26, 1998
    Assignee: 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
  • Patent number: 5506262
    Abstract: 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: Grant
    Filed: November 10, 1993
    Date of Patent: April 9, 1996
    Assignee: 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
  • Patent number: 5369125
    Abstract: 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: Grant
    Filed: March 19, 1993
    Date of Patent: November 29, 1994
    Assignee: 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
  • Patent number: 5114961
    Abstract: 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: Grant
    Filed: December 10, 1990
    Date of Patent: May 19, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Robert L. Bugianesi, Nirindar N. Girotra, Mitree M. Ponpipom, Soumya P. Sahoo, Chan H. Kuo
  • Patent number: 5010100
    Abstract: 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: Grant
    Filed: June 8, 1989
    Date of Patent: April 23, 1991
    Assignee: Merck & Co. Inc.
    Inventors: Tesfaye Biftu, John C. Chabala, Robert L. Bugianesi, Mitree M. Ponpipom, Soumya P. Sahoo
  • Patent number: 5001123
    Abstract: 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: Grant
    Filed: June 8, 1989
    Date of Patent: March 19, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Nirindar N. Girotra, Robert L. Bugianesi, Mitree M. Ponpipom, Soumya P. Sahoo, Chan H. Kuo
  • Patent number: 4996203
    Abstract: 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: Grant
    Filed: June 8, 1989
    Date of Patent: February 26, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Robert L. Bugianesi, Nirindar N. Girotra, Mitree M. Ponpipom, Soumya P. Sahoo, Chan H. Kuo
  • Patent number: 4761404
    Abstract: 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: Grant
    Filed: July 1, 1985
    Date of Patent: August 2, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Robert L. Bugianesi, Mitree M. Ponpipom, Kathleen M. Rupprecht
  • Patent number: 4704462
    Abstract: 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: Grant
    Filed: August 22, 1985
    Date of Patent: November 3, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, San-Bao Hwang, Mitree M. Ponpipom, Robert L. Bugianesi
  • Patent number: 4554349
    Abstract: 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: Grant
    Filed: October 11, 1983
    Date of Patent: November 19, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Mitree M. Ponpipom, Tsung-Ying Shen, Robert L. Bugianesi
  • Patent number: 4386026
    Abstract: 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: Grant
    Filed: April 20, 1981
    Date of Patent: May 31, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Mitree M. Ponpipom, Robert L. Bugianesi, James C. Robbins, Tsung-Ying Shen
  • Patent number: 4259324
    Abstract: 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: Grant
    Filed: July 31, 1979
    Date of Patent: March 31, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Mitree M. Ponpipom, Tsung-Ying Shen, Robert L. Bugianesi
  • Patent number: 4229441
    Abstract: Glycolipid compounds of the formulae ##STR1## wherein R is ##STR2## are useful immunologic adjuvants in vaccines.
    Type: Grant
    Filed: December 1, 1978
    Date of Patent: October 21, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Robert L. Bugianesi, Mitree M. Ponpipom, Tsung-Ying Shen
  • Patent number: 4228274
    Abstract: 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: Grant
    Filed: July 10, 1978
    Date of Patent: October 14, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Mitree M. Ponpipom, Robert L. Bugianesi, Philippe L. Durette, Howard M. Katzen, Tsung-Ying Shen