Patents Represented by Attorney, Agent or Law Firm Curtis C. Panzer
  • 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
    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
  • Bethalactam elastase inhibitors containing phosphorous acid derivatives at the 4-position of the 2-azetidinone
    Patent number: 5104862
    Abstract: New substituted azetidinones of the general formula (A), which have been found to be potent elastase inhibitors and thereby useful as anti-inflammatory and antidegenerative agents, are described.
    Type: Grant
    Filed: March 20, 1991
    Date of Patent: April 14, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Malcolm Maccoss
  • Novel betalactam elastase inhibitors containing phosphorous acid derivatives at the 4-position of the 2-azetidinone
    Patent number: 5100880
    Abstract: New substituted azetidinones of the general formula (A), which have been found to be potent elastase inhibitors and thereby useful as anti-inflammatory and antidegenerative agents, are described.
    Type: Grant
    Filed: March 20, 1991
    Date of Patent: March 31, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Malcolm Maccoss
  • Process of making 2,5-diaryl tetrahydrofurans and analogs thereof useful as PAF antagonists
    Patent number: 5099033
    Abstract: The present invention is directed to a process of making tetrahydrofuran of the formula (D) ##STR1## resulting in 2,5-diaryltetrahydrofuran PAF antagonists of pharmaceutically acceptable purity.
    Type: Grant
    Filed: June 29, 1990
    Date of Patent: March 24, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Ichiro Shinkai, Andrew S. Thompson, Thomas R. Verhoeven
  • Lipophilic macrolide useful as an immunosuppressant
    Patent number: 5093338
    Abstract: Disclosed is a novel lipophilic macrolide of Formula I: ##STR1## The compound of assigned Formula I is an analog of rapamycin which has activity as an antifungal agent and as an immunosuppressant.
    Type: Grant
    Filed: April 23, 1991
    Date of Patent: March 3, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Kevin Byrne, Robert T. Goegelman, Otto Hensens, Louis Kaplan, Jerrold M. Liesch
  • Lipophilic macrolide useful as an immunosuppressant
    Patent number: 5091389
    Abstract: Disclosed is a novel lipophilic macrolide of assigned Formula I: ##STR1## The compound of assigned Formula I is an analog of rapamycin which has activity as an antifungal agent and as an immunosuppressant.
    Type: Grant
    Filed: April 23, 1991
    Date of Patent: February 25, 1992
    Assignee: Merck & Co., Inc.
    Inventors: John Ondeyka, Otto Hensens, Jerrold Liesch
  • N-alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives as dual cyclooxygenase and lipoxygenase inhibitors
    Patent number: 5068248
    Abstract: Method for increasing resistance to gastro-intestinal irritation, and for the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandin and/or leukotriene mediated diseases comprising the administration to a subject in need of such treatment, a non-toxic therapeutically effective amount of compound of formula I: ##STR1##
    Type: Grant
    Filed: June 22, 1989
    Date of Patent: November 26, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Allan N. Tischler, Philippe L. Durette, Bruce E. Witzel, Kathleen M. Rupprecht, Timothy F. Gallagher, Marvin M. Goldenberg, Debra L. Allison
  • 1,3-diaryl cyclopentanes and derivatives thereof as PAF antagonists
    Patent number: 5047420
    Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.
    Type: Grant
    Filed: August 21, 1989
    Date of Patent: September 10, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
  • 5-amino or substituted amino 1,2,3-triazoles useful as antimetastatic agents
    Patent number: 5045543
    Abstract: This invention is directed to the method of treating patients with surgically excised tumors with a high probability of metastasis, such as melanoma and breast cancer, by administering to such patient a nontoxic therapeutically effective amount of a 5-amino or substituted amino, 1,2,3-triazoles which are disclosed as a new class of antimetastatic agents useful in such treatment.
    Type: Grant
    Filed: May 8, 1989
    Date of Patent: September 3, 1991
    Assignee: Merck & Co., Inc.
    Inventor: Donald Hupe
  • 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
    Patent number: 5011847
    Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein Ar is a pyridyl, dimethoxy-pyridyl or a dimethoxy-pyrazinyl group, R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group, Y is an alkyl or substituted alkyl group, R.sup.6 is an alkyl or a substituted alkyl and the substituents at positions 3, 4 and 5 are acyclic.
    Type: Grant
    Filed: June 8, 1989
    Date of Patent: April 30, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Mitree M. Ponpipom, Nirindar N. Girotra
  • Certain 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
    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
  • Novel 7-aroyl-4-hydroxy-3-methyl-benzofurans as dual inhibitors of cyclooxygenase and 5-lipoxygenase
    Patent number: 5006549
    Abstract: Novel 7-Aroyl-4-Hydroxy-3-Methyl-Benzofurans of the following general formula (I) are disclosed: ##STR1##The compounds are found to be potent dual inhibitors of cyclooxygenase and 5-lipoxygenase.
    Type: Grant
    Filed: May 24, 1989
    Date of Patent: April 9, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Robert A. Zambias, Milton L. Hammond
  • Derivatives of 3-hydroxyazabenzo(beta)thiophene useful as 5-lipoxygenase inhibitors
    Patent number: 5006532
    Abstract: 3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthio-alkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory diseases and other leukotriene mediated diseases.
    Type: Grant
    Filed: December 8, 1989
    Date of Patent: April 9, 1991
    Assignee: Merck & Co. Inc., Inc.
    Inventors: Robert K. Baker, Arsenio A. Pessolano, Kathleen M. Rupprecht, Philippe L. Durette
  • Welan gum in cement compositions
    Patent number: 5004506
    Abstract: Cement compositions, i.e., mortar, structured concrete, pre-cast concrete, and oilfield cement, comprising 0.01-0.9% (wt/wt) welan gum are described.
    Type: Grant
    Filed: April 2, 1990
    Date of Patent: April 2, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Floyd L. Allen, Glen H. Best, Thomas A. Lindroth
  • 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
    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
  • 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
    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
  • Process for the preparation of 1,1-dioxo-7-substituted cephems
    Patent number: 4992541
    Abstract: The present invention relates to an improved process for the preparation of the compounds of formula (I) ##STR1## which involve the direct oxidation without N-protection of the compound of the formula (II) ##STR2##
    Type: Grant
    Filed: August 1, 1989
    Date of Patent: February 12, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, John W. Butcher, Paul Sohar, Theresa Lamanec
  • 6- and/or 7-substituted-1,2,3,4,4A,9B-hexahydro-8-hydroxydibenzofuran-3-ols as inhibitors of leukotriene biosynthesis
    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
  • 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
    Patent number: 4977146
    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, R.sup.6 is an alkyl or a substituted alkyl group and the substituents at positions 3, 4 or 5 are acyclic.
    Type: Grant
    Filed: April 11, 1990
    Date of Patent: December 11, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Mitree M. Ponpipom, Nirindar N. Girotra
  • Trans 2,3-disubstituted-2,3-dihydro-5-hydroxy-benzofurans as inhibitors of leukotriene biosynthesis
    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