Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Imidazolinobenzodiazepines
    Patent number: 5834464
    Abstract: Imidazolinobenzodiazepines are cholecystokinin B (CCK-B) antagonists useful as anxiolytic agents.
    Type: Grant
    Filed: May 6, 1996
    Date of Patent: November 10, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Robert M. DiPardo, Roger M. Freidinger
  • Genes for the subunits of human farnesyl-protein transferase
    Patent number: 5821118
    Abstract: The present invention relates to an assay useful in determining the farnesyl-protein transferase inhibitory activity of pharmaceutical agents. The assay employs purified human farnesyl-protein transferase which is prepared by gene expression in Escherichia coli.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: October 13, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Charles A. Omer, Ronald E. Diehl, Jackson B. Gibbs, Nancy E. Kohl
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5817678
    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: November 15, 1996
    Date of Patent: October 6, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Byeong M. Kim, Anthony W. Shaw, Samuel L. Graham, S. Jane deSolms, Terrence M. Ciccarone
  • Method for treating Meniere's disease
    Patent number: 5817658
    Abstract: A method for the treatment of Meniere's disease comprising the administration of a medicament which modulates the IKs channel of the ear and thereby reducing endolymph production.
    Type: Grant
    Filed: June 24, 1997
    Date of Patent: October 6, 1998
    Assignee: Merck & Company, Inc.
    Inventors: Peter K. S. Siegl, Allan I. Goldberg, Michael R. Goldberg, Paul I. Chang
  • Benzoxazinones as inhibitors of HIV reverse transcriptase
    Patent number: 5811423
    Abstract: Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: March 12, 1997
    Date of Patent: September 22, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Steven D. Young, Linda S. Payne, Susan F. Britcher, Lekhanh O. Tran, William C. Lumma, Jr.
  • Method of preparing phosphodiesterase IV inhibitors
    Patent number: 5808082
    Abstract: A process for the preparation of Phosphodiesterase IV inhibitors is described. The process consists of eight chemical steps involving five isolations to prepare the title compound from readily available isovanillin in 35% overall yield (Scheme 1). The process is highlighted by: a) a highly diastereoselective Michael addition of phenyllithium using (1R, 2S) cis-aminoindanol as a chiral auxiliary, b) highly crystalline intermediates providing for efficient purifications, c) crystallization of the final compound as its CSA salt for excellent enantiomeric purity.
    Type: Grant
    Filed: April 22, 1997
    Date of Patent: September 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Woo-Baeg Choi, Hywyn R. D. Churchill, Joseph E. Lynch, Paul J. Reider, Ralph P. Volante
  • Process for preparing substituted azetidinones
    Patent number: 5808056
    Abstract: The present invention relates to the process for the preparation of the substituted azetidinone having the formula: ##STR1## comprising a convergent synthesis wherein the azetidinone portion of the molecule is coupled to the lower benzodioxole portion via a base catalyzed addition to an isocyanate.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: September 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Joseph S. Amato, Raymond Cvetovich, Frederick W. Hartner
  • Antifungal agent from sporomiella minimoides
    Patent number: 5801172
    Abstract: There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.
    Type: Grant
    Filed: July 11, 1997
    Date of Patent: September 1, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Wendy H. Clapp-Shapiro, Bruce W. Burgess, Robert A. Giacobbe, Guy H. Harris, Suzanne Mandala, Jon Polishook, Mark Rattray, Rosemary A. Thornton, Deborah L. Zink, Angeles Cabello, Maria Teresa Diez, Isabel Martin, Fernando Pelaez
  • Enhanced functional recovery of the heart by losartan treatment after an ischemic attach
    Patent number: 5795904
    Abstract: Losartan, its active metabolite, EXP3174, or the pharmaceutically acceptable salts of these compounds for use in enhancing the functional recovery of the heart after an ischemic attack.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: August 18, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Sheila M. Cohen, Jeffrey G. Werrmann
  • 2-substituted aryl pyrroles, compositions containing such compounds and methods of use
    Patent number: 5792778
    Abstract: The present invention addresses 2-substituted aryl pyrroles, as well as compositions containing such compounds and methods of treatment. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production or activity of one or more cytokines occurs. Interleukin-1 (IL-1), Interleukin-6 (IL-6), Interleukin-8 (IL-8) and Tumor Necrosis Factor (TNF) are cytokines which are involved.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: August 11, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Stephen E. de Laszlo, Nigel J. Liverton, Gerald S. Ponticello, Harold G. Selnick, Nathan B. Mantlo
  • Aza cyclohexapeptide compounds
    Patent number: 5792746
    Abstract: Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.
    Type: Grant
    Filed: October 28, 1996
    Date of Patent: August 11, 1998
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances Aileen Bouffard, Regina M. Black
  • P5C reductase gene from zalerion arboricloa
    Patent number: 5789222
    Abstract: There is disclosed an isolated gene coding for an enzyme involved in proline biosynthesis in Zalerion arboricola. There is also disclosed a method of using the gene to produce a strain of Z. arboricola containing high titers of a desirable fermentation product.
    Type: Grant
    Filed: June 18, 1996
    Date of Patent: August 4, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Rosemarie Kelly, Prakash S. Masurekar, Elizabeth A. Register
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5789438
    Abstract: The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). 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: September 5, 1997
    Date of Patent: August 4, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Sheo B. Singh, Russell B. Lingham, Keith C. Silverman, Deborah L. Zink, Isabel Martin, Fernando Pelaez, Manuel Sanchez
  • Protein prenyltransferase
    Patent number: 5789558
    Abstract: The present invention relates, in general, to a protein prenyltransferase and, in particular, to protein geranylgeranyltransferase (GGTase-I) and to a nucleic acid sequence encoding same. The invention also relates to methods of producing GGTase-I and geranylgeranyl modified polypeptides. The invention further relates to a method of screening compounds for the ability to alter GGTase-I activity.
    Type: Grant
    Filed: January 31, 1994
    Date of Patent: August 4, 1998
    Assignees: Merck & Co., Inc., Duke University
    Inventors: Patrick J. Casey, Fang Zhang, Ronald E. Diehl, Nancy E. Kohl, Charles A. Omer
  • High throughput assay using fusion proteins
    Patent number: 5783398
    Abstract: This application describes a high throughput assay for screening for compounds capable of binding to a fusion protein which consists of a target protein and an FK506-binding protein. The method for preparing the DNA encoding for the fusion protein and for expressing that DNA is also described in the application. The invention also discloses the recombinant DNA and protein sequences for several fusion proteins.
    Type: Grant
    Filed: September 4, 1996
    Date of Patent: July 21, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Alice Marcy, Scott P. Salowe, Douglas Wisniewski
  • Stereoselective process for making substituted amino acid derivatives
    Patent number: 5783709
    Abstract: The invention encompasses a method for the stereoselective synthesis of alkyl proline and other amino acid derivatives which are intermediates of the farnesyl-protein transferase inhibiting CA.sup.1 A.sup.2 X motif of the protein Ras. The instant process employs an efficient diastereoselective ?2,3!-Wittig rearrangement of .alpha.-allyloxy amide enolates mediated by a chiral auxiliary to provide acyclic and cyclic precursors.
    Type: Grant
    Filed: August 25, 1997
    Date of Patent: July 21, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Michael Kress, Chunhua Yang, Nobuyoshi Yasuda
  • Process for producing a plurality of holes in dosage forms using a laser beam deflected by an acousto-optic deflector
    Patent number: 5783793
    Abstract: A laser drilling process capable of producing a plurality of holes in a pharmaceutical dosage form, at high speed, is presented. The process utilizes a high power CO.sub.2 laser steered by an acousto-optic deflector together with various mirrors and optical components to achieve the correct beam path geometry, in order to produce an unlimited number of holes through the surface or coating of a dosage form, at rates up to 100,000 units or more per hour.
    Type: Grant
    Filed: February 26, 1997
    Date of Patent: July 21, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Neil Emerton, Graham S. Gutsell, Timothy A. Large, Stephen Owen
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5780492
    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: March 27, 1997
    Date of Patent: July 14, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Theresa M. Williams
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5780488
    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: March 26, 1997
    Date of Patent: July 14, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Jeffrey Bergman, Christopher Dinsmore
  • Antagonists of gonadotropin releasing hormone
    Patent number: 5780437
    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: July 14, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Wallace T. Ashton, Lin Chu, Michael H. Fisher, Narindar N. Girotra, Peter Lin, Matthew J. Wyvratt