Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Bicyclic(azaaromatic)indoles as inhibitors of leukotriene bisynthesis
    Patent number: 5334719
    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: June 17, 1992
    Date of Patent: August 2, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventor: Richard Frenette
  • Indole carbamates as leukotriene antagonists
    Patent number: 5334597
    Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. 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.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: August 2, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Petpiboon Prasit, Marc Blouin
  • Tricyclic thienothiopyran carbonic anhydrase inhibitors
    Patent number: 5334591
    Abstract: Conformationally constrained tricyclic thienothiopyran compounds are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
    Type: Grant
    Filed: March 4, 1993
    Date of Patent: August 2, 1994
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Kenneth L. Shepard, Gerald S. Ponticello, Theresa M. Williams
  • Substituted imidazo-fused 6-membered heterocycles as angiotensin II antagonists
    Patent number: 5332744
    Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: May 4, 1990
    Date of Patent: July 26, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Thomas F. Walsh
  • Process of producing 8A- and 9A-azalide antibiotics
    Patent number: 5332807
    Abstract: A process of producing 8a- and 9a- azalide compounds is disclosed, comprised of reacting an 8a- aza or 9a- aza azalide eastern fragment or a derivative thereof with a compound of the formula:X--A'--Ywherein X and Y are appropriate reactive groups and A' is a fragment or compound which forms the western portion of the azalide, andcyclizing this intermediate to form the target 8a- or 9a-azalide compound. Compounds of formula I, II and III as well as other azalides can be synthesized according to this process.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: July 26, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Sherman T. Waddell, Timothy A. Blizzard
  • Lipopeptide derivatives
    Patent number: 5330973
    Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: July 19, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Milton L. Hammond, Robert E. Schwartz, James M. Balkovec
  • 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
  • Processes for making proteins having anticoagulant properties
    Patent number: 5328997
    Abstract: Proteins which specifically inhibit coagulation Factor Xa. The inhibitors, which do not inhibit Factor VIIa, kallikrein, trypsin, chymotrypsin, thrombin, urokinase, tissue plasminogen activator, plasmin, elastase, Factor XIa or S. aureus V8 protease, are polypeptides of 60 amino acid residues. The inhibitors may be purified from Ornithodoros moubata extract, synthesized, or produced using a recombinant DNA yeast expression system.
    Type: Grant
    Filed: April 28, 1993
    Date of Patent: July 12, 1994
    Assignee: Merck & Co., Inc.
    Inventors: George P. Vlasuk, Lloyd H. Waxman, Victor M. Garsky, Michael P. Neeper
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5326773
    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: October 29, 1992
    Date of Patent: July 5, 1994
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane de Solms, Samuel L. Graham
  • Fluid ophthalmic composition based on lipid microparticles containing at least one active principle
    Patent number: 5326761
    Abstract: There is described a fluid ophthalmic composition which comprises a suspension in a fluid dispersant medium of lipid microparticles containing at least one active principle. The composition enables improved availability of the active principle to be obtained as a result of high intraocular levels.
    Type: Grant
    Filed: January 10, 1991
    Date of Patent: July 5, 1994
    Assignee: Merck Sharp & Dohme-Chibret
    Inventor: Annouk Rozier
  • Substituted pyrimidines, pyrimidinones and pyridopyrimidines
    Patent number: 5324729
    Abstract: Substituted pyrimidines, pyrimidinones and pyridopyrimidines of formula (I) are as angiotensin II antagonists useful in the treatment of hypertension, ocular hypertension and certain CNS ailments: ##STR1## wherein K is --N(R.sup.8a)--C(.dbd.M) or --N.dbd.C(R.sup.8b) where M is O or NR.sup.22.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: June 28, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Malcolm MacCoss, Arthur A. Patchett
  • Benzodiazepine analogs
    Patent number: 5324726
    Abstract: Benzodiazepine analogs of the formula: ##STR1## wherein: R.sup.3 is ##STR2## --NH(CH.sub.2).sub.2 --.sub.3 NHCOR.sup.7, ##STR3## or --X.sup.11 NR.sup.18 SO.sub.2 (CH.sub.2).sub.q R.sup.7 ; R.sup.7 is O,S,HH, or NR.sup.15 with the proviso that X.sup.7 can be NR.sup.15 only when R.sup.1 is not H.are disclosed which are antagonists of gastrin and cholecystokinin (CCK) with enhanced aqueous solubility and have properties useful in the treatment of disorders of gastric secretion, appetite regulation, gastrointestinal motility, pancreatic secretion, and dopaminergic function, as well as in treatment producing potentiation of morphine and other opiate analgesics.
    Type: Grant
    Filed: October 29, 1992
    Date of Patent: June 28, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger
  • 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 benzylformimidate
    Patent number: 5319122
    Abstract: This invention relates to a novel process for preparing benzylformimidates which are useful in the production of certain carbapenem antibiotics. The process of this invention provides a means of producing a high-yield, high-purity product.
    Type: Grant
    Filed: November 12, 1992
    Date of Patent: June 7, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Joel J. Friedman
  • Aryl thiopyrano[2,3,4-C,D]indoles as inhibitors of leukotriene biosynthesis
    Patent number: 5314900
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of 5-lipoxygenase and 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, psoriasis, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: November 19, 1992
    Date of Patent: May 24, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, John H. Hutchinson, Michel Therien, Daniel Delorme
  • Use of non-steroidal antiiflammatory agents in macular degeneration
    Patent number: 5314909
    Abstract: Topically applied non-steroidal antiinflammatory agents (NSAID's) are useful in the treatment of macular degeneration.
    Type: Grant
    Filed: March 17, 1993
    Date of Patent: May 24, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Jens Dollerup
  • LTD.sub.4 receptor and photoaffinity probe
    Patent number: 5310884
    Abstract: The LTD.sub.4 receptor has been defined by radioligand binding studies as a member of the family of G-protein coupled receptors. A photoactivable azido derivative of LTD.sub.4 ([.sup.125 I]Azido-LTD.sub.4) has been synthesized for use as a photoaffinity probe. Photoactivation of ([.sup.125 I]Azido-LTD.sub.4 under equilibrium binding conditions revealed the selective radiolabeling of a 45 kDa protein in guinea-pig lung membranes, as visualized by SDS-PAGE and autoradiography.
    Type: Grant
    Filed: April 3, 1992
    Date of Patent: May 10, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert Zamboni, Kathleen M. Metters
  • Lipopeptide compounds
    Patent number: 5310726
    Abstract: Antifungal and antiparasital lipopeptide compounds stable in aqueous media are described. Stability in aqueous media render lipopeptides more useful for compositions for therapeutic applications.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: May 10, 1994
    Assignee: Merck & Co., Inc.
    Inventor: James M. Balkovec
  • Substituted aromatic sulfonamides as antiglaucoma agents
    Patent number: 5308863
    Abstract: Thieno[2,3-b]thiopyran-2-sulfonamides and ring homologs with a hydrophilic substituted-alkyl group adjacent to the thiopyran sulfur are carbonic anhydrase inhibitors topically effective in lowering intraocular pressure.
    Type: Grant
    Filed: June 16, 1992
    Date of Patent: May 3, 1994
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Charles N. Habecker, Harold G. Selnick