Patents Represented by Attorney, Agent or Law Firm David A. Muthard
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5439918
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.
    Type: Grant
    Filed: March 14, 1994
    Date of Patent: August 8, 1995
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Samuel L. Graham
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5436263
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: July 25, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Sheo B. Singh, Barry A. Katz, Russell B. Lingham, Isabel Martin, Keith C. Silverman
  • Inhibitors of farnesyl protein transferase or prodrugs thereof
    Patent number: 5420157
    Abstract: This invention relates to pharmaceutical compounds of structural formulae (I) and (II): ##STR1## and compositions and methods of treatment utilizing these compounds to inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: December 16, 1991
    Date of Patent: May 30, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Sheo B. Singh, Gerald F. Bills, Russell B. Lingham, Keith C. Silverman, Deborah L. Zink
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5420334
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting famesyl-protein transferase and the famesylation of the oncogene protein Ras.
    Type: Grant
    Filed: April 4, 1994
    Date of Patent: May 30, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Sheo B. Singh, Gerald F. Bills, Russell B. Lingham, Isabel Martin, Keith C. Silverman, Jack L. Smith
  • Process for the preparation of antiulcer agents
    Patent number: 5391752
    Abstract: Anti-ulcer agents having a methylsulfinyl bridge between a substituted pyridine moiety and a substituted benzimidazole moiety are prepared by oxidizing the corresponding compounds, having a methylthio bridge, with magnesium monoperoxyphthalate in a suitable solvent. The reaction may be run in an aromatic hydrocarbon solvent, wherein the product may crystallize out of the reaction solution and may be directly isolated by filtration.
    Type: Grant
    Filed: February 22, 1993
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Robert S. Hoerrner, Joel J. Friedman, Joseph S. Amato, Thomas M. Liu, Ichiro Shinkai, Leonard M. Weinstock
  • Farnesyl pyrophosphate analogs
    Patent number: 5362906
    Abstract: The present invention is directed to farnesyl pyrophosphate analogs which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention, and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 18, 1993
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Ta-Jyh Lee, Robert L. Smith, Gerald E. Stokker
  • Inhibitors of farnesyl protein transferase
    Patent number: 5350867
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Sheo B. Singh
  • Cationic-2-heteroarylphenyl-carbapenem antibacterial agents
    Patent number: 5342933
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: August 30, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Susan M. Schmitt, Ravindra N. Guthikonda
  • 2-phenanthridinyl carbaphenem antibacterial agent
    Patent number: 5336674
    Abstract: The present invention relates to antibacterial agents of the carbapenem class, in which the 2-position sidechain is characterized by a phenanthridine moiety typically having a substituent attached to the nitrogen of the phenanthridine and substituted at other positions by various neutral substituents. When there is substitution on the nitrogen of the phenathridine moiety that nitrogen is a charged quaternary nitrogen.
    Type: Grant
    Filed: January 27, 1993
    Date of Patent: August 9, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Mark L. Greenlee, Thomas A. Rano, Wendy Lee
  • 2-phenanthridinyl carbapenem antibacterial agents
    Patent number: 5328904
    Abstract: The present invention relates to antibacterial agents of the carbapenem class, in which the 2-position sidechain is characterized by a phenanthridine moiety, substituted by various neutral substituents.
    Type: Grant
    Filed: January 27, 1993
    Date of Patent: July 12, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Mark L. Greenlee, Thomas A. Rano, Wendy Lee
  • Methods of achieving antitumor activity using 16-membered-macrolide-type compounds
    Patent number: 5324720
    Abstract: Inhibition of renal cancer, melanoma, colon cancer, lung cancer and leukemia cells by administration of compounds from the bafilomycin and hygrolidin groups of compounds.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: June 28, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Tom G. Holt, Richard L. Monaghan
  • HPLC assay for the selective resolution of recombinant proteins
    Patent number: 5322795
    Abstract: Proteins that cannot be resolved by conventional HPLC techniques, including reversed-phase HPLC, can be distinguished, and the quantity of a protein of interest monitored in numerous types of in-process samples, including fermentation and down-stream processing samples, by covalently binding monobromobimane to a protein of interest bearing sulfhydryl groups and chromatographing these in-process samples using reversed-phase HPLC, fluorescence detection and UV absorbance detection.
    Type: Grant
    Filed: June 23, 1992
    Date of Patent: June 21, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Donald O'Keefe
  • Process for the preparation of 4-substituted-1,4-dihydropydrines
    Patent number: 5310917
    Abstract: 4-Substituted-1,4-dihydropyridines are prepared by a cycloaddition reaction in which the cyclization is driven to completion, after thermal reaction, by addition of an acid. Felodipine, a vasodilator, is prepared by a cycloaddition reaction of ethyl 3-aminocrotonate with a suitably substituted dichlorobenzylidine under reaction conditions whereby the product crystallizes out of the reaction solution and may be directly isolated by filtration.
    Type: Grant
    Filed: July 28, 1992
    Date of Patent: May 10, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Joseph Auerbach
  • Methods of achieving antileukemia activity using 16-membered-macrolide-type compounds
    Patent number: 5306716
    Abstract: Inhibition of renal cancer, melanoma, colon cancer, lung cancer and leukemia cells by administration of compounds from the bafilomycin and hygrolidin groups of compounds.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: April 26, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Tom G. Holt, Richard L. Monaghan
  • Ibuprofen antacid combinations
    Patent number: 5288507
    Abstract: This invention relates to a pharmaceutical composition for use in the treatment of pain and inflammation and the treatment of acid indigestion, sour stomach, heartburn and symptoms of upset stomach associated with these conditions in a mammalian organism, said composition comprising:(i) an analgesically and anti-inflammatory effective amount of (S)-ibuprofen, or a salt thereof, substantially free of (R)-ibuprofen;(ii) an amount effective in the treatment of acid indigestion, sour stomach and/or heartburn of at least one of the antacids; and(iii) optionally, an amount effective in treating excess gas and flatulence of an anti-gas agent.
    Type: Grant
    Filed: July 29, 1992
    Date of Patent: February 22, 1994
    Assignees: Merck & Co., Inc., McNeill-PPC, Inc.
    Inventors: Robert T. Sims, Thomas N. Gates, William Slivka
  • (Quinolin-2-ylmethoxy)indoles as inhibitors of the biosynthesis of leukotrienes
    Patent number: 5272145
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
    Type: Grant
    Filed: December 14, 1992
    Date of Patent: December 21, 1993
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, Richard Frenette, John Gillard
  • Inhibitors of farnesyl protein transferase
    Patent number: 5260465
    Abstract: This invention relates to pharmaceutical compounds of structural formula (I): ##STR1## and compositions and methods of treatment utilizing these compounds to inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: December 16, 1991
    Date of Patent: November 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Sheo B. Singh, Deborah L. Zink
  • Inhibitors of farnesyl protein transferase
    Patent number: 5260479
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: December 16, 1991
    Date of Patent: November 9, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Sheo B. Singh
  • Heteroarylnaphthalene hydroxy acids as inhibitors of leukotriene biosynthesis
    Patent number: 5252599
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: August 27, 1992
    Date of Patent: October 12, 1993
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Rejean Fortin, Daniel Delorme, Daniel Dube, Pierre Hamel, Yves Ducharme, John W. Gillard
  • Process for aromatic bromination
    Patent number: 5248817
    Abstract: A novel procedure for bromination of aromatic moieties utilizes N-bromosuccinimide or dibromodimethylhydantoin in an aqueous alkali medium. The bromination procedure is employed for the preparation of an intermediate used in the preparation of remoxipride, an antipsychotic compound.
    Type: Grant
    Filed: July 8, 1992
    Date of Patent: September 28, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Joseph Auerbach, Steven A. Weissman