Patents Represented by Attorney Joseph F. DiPrima

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  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • Method for the production of a modified "8-amino acid" cyclosporin derivative
    Patent number: 5318901
    Abstract: A cyclosporin derivative with incorporated "8-(3-fluoro-D-alanine)" or "8-(2-deutero-3-fluoro-D-alanine)" has been isolated from the fermentation broth of incubating Tolypocladium inflatum MF5080 (NRRL 8044) with 3-fluoro-D-alanine or its 2-deuterated isomer respectively. The modified cyclosporins exhibit immunosuppressive properties.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: June 7, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, Raymond F. White, Robert T. Goegelman
  • N-biphenyl-3-amido substituted benzolactams stimulate growth hormone release
    Patent number: 5317017
    Abstract: There are disclosed certain compounds identified as N-biphenyl-3-amido substituted benzolactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzolactams as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: May 31, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Hyun O. Ok, William R. Schoen, Matthew Wyvratt
  • 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
  • Crystallization method to improve crystal structure and size
    Patent number: 5314506
    Abstract: Impinging fluid jet streams are used in a continuous crystallization process to achieve high intensity micromixing of fluids so as to form a homogeneous composition prior to the start of nucleation. This process permits direct crystallization of high surface area particles of high purity and stability.
    Type: Grant
    Filed: November 18, 1991
    Date of Patent: May 24, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Michael Midler, Jr., Edward L. Paul, Edwin F. Whittington, Mauricio Futran, Paul D. Liu, Jaanpyng Hsu, Shih-Hsie Pan
  • 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
  • Strain of streptomyces avermitilis capable of glycosylating avermectin compounds at the 13- and 14A positions
    Patent number: 5312753
    Abstract: Avermectin compounds are glycosylated at the 4',13- Or 14a-positions by adding the avermectin compounds to the fermentation medium of a novel strain of Streptomyces avermitilis. The 13-hydroxy and 14a-hydroxy methyl groups of the avermectin compound are glycosylated with a glycosyl moiety, specifically an oleandrose group. The new strain offers the added advantage of not producing any C5-O-methylation products. The compounds are potent anthelmintic and antiparasite agents, and compositions for such uses are also disclosed.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: May 17, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Douglas J. MacNeil, Tanya MacNeil
  • Substituted carbamoyl and oxycarbonyl derivatives of biphenylmethylamines
    Patent number: 5312820
    Abstract: Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT.sub.1 and AT.sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ##STR1## where X is --O-- or --N(R.sup.7)--.
    Type: Grant
    Filed: July 17, 1992
    Date of Patent: May 17, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee, Steven M. Hutchins, Ralph A. Rivero
  • Cyclohexapeptide compound
    Patent number: 5310873
    Abstract: A cyclohexapeptide base which is the nucleus of closely related antibiotics obtained by culturing Zalerion arboricola and its salts are described. They are useful intermediates for the preparation of new semisynthetic compounds having antimicrobial activity.
    Type: Grant
    Filed: March 12, 1990
    Date of Patent: May 10, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Dennis M. Schmatz, Jan S. Tkacz, Robert E. Schwartz, Mervyn Turner
  • 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
  • Benzo-fused lactams that promote the release of growth hormone
    Patent number: 5310737
    Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: February 2, 1993
    Date of Patent: May 10, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Michael H. Fisher, William R. Schoen, Matthew J. Wyvratt, Robert J. DeVita
  • Quinazolinones
    Patent number: 5308846
    Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula 1 ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.
    Type: Grant
    Filed: July 22, 1993
    Date of Patent: May 3, 1994
    Assignees: Merck & Co., Inc., E. I. Du Pont de Nemours and Co.
    Inventors: Eric E. Allen, Richard E. Olson
  • Heteroarylnaphthalenes as inhibitors of leukotriene biosynthesis
    Patent number: 5308852
    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: May 3, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Daniel Delorme, Rejean Fortin, Daniel Dube, Pierre Hamel, Carol Lepine, Yves Ducharme