Patents Represented by Attorney, Agent or Law Firm Melvin Winokur
  • Patent number: 6538134
    Abstract: The present invention is concerned with 4-benzyl-2-hydroxy-1,4-oxazin-3-one, and novel processes for the preparation therof. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: March 25, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Louis S. Crocker, Karel M. Jos Brands, Todd D. Nelson, Philip J. Pye, Jonathan D. Rosen, Kai Rossen
  • Patent number: 6534510
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of: or a pharmaceutically acceptable salt thereof, wherein A is
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: March 18, 2003
    Assignee: Merck & Co., Inc.
    Inventors: James C. Barrow, Bruce D. Dorsey, Harold G. Selnick, Phung L. Ngo
  • Patent number: 6534505
    Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
    Type: Grant
    Filed: November 30, 2000
    Date of Patent: March 18, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Kaufman, Daniel J. Rush
  • Patent number: 6531484
    Abstract: Pyrrolidine compounds of Formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, j, k, 1, m, and n are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally 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: October 10, 2001
    Date of Patent: March 11, 2003
    Assignee: Merck & co., Inc.
    Inventors: Christopher A. Willoughby, Keith Rosauer, Kevin T. Chapman, Sander G. Mills, Dong-Ming Shen, Min Shu
  • Patent number: 6525073
    Abstract: A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: February 25, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Carl M. Mendel, Joanne Waldstreicher
  • Patent number: 6525205
    Abstract: Crystalline 3-hydroxylactone-containing products can be prepared in high yield and purity in a one-pot process by treating the corresponding 3,5-dihydroxy acid with a strong mineral acid in a cold, aprotic, water-miscible solvent to effect lactonization, followed by addition of excess acid to effect crystallization of the lactonized product from the reaction mixture.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: February 25, 2003
    Assignee: Merck & Co., Inc.
    Inventors: James McManus, Nicholas Anousis, John F. Genus, Christopher Hancock
  • Patent number: 6525083
    Abstract: Certain N-substituted indoles having aryloxyacetic acid, substituents are agonists or partial agonists of PPAR gamma, and are useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR mediated diseases, disorders and conditions.
    Type: Grant
    Filed: July 25, 2001
    Date of Patent: February 25, 2003
    Assignee: Merck & Co., Inc.
    Inventors: John J. Acton, III, Regina Marie Black, Anthony Brian Jones, Harold Blair Wood
  • Patent number: 6521625
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline Anhydrous Form B, 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline form Type A Monohydrate, and 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline form Type B monohydrate, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: February 18, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Cameron J. Cowden, V. Brett Cooper, Daniel J. Rush, Patricia Frech
  • Patent number: 6518273
    Abstract: The present invention relates to compounds of the formula (I): wherein R1a, R1b, R2, R3, R4, R5, X and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: September 4, 2001
    Date of Patent: February 11, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Kevin Tyler Chapman, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Steven Michael Hutchins, Duncan Edward Shaw, Christopher Alan Willoughby
  • Patent number: 6515015
    Abstract: The instant invention is concerned with aryl and heteroaryl acetic acid and oxyacetic acid compounds, which are useful as antidiabetic compounds. Compositions and methods for their use in the treatment of diabetes and related diseases and for lowering triglyceride levels are disclosed.
    Type: Grant
    Filed: October 24, 2000
    Date of Patent: February 4, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Alan Adams, Derek Von Langen, Hiroo Koyama, Richard Tolman
  • Patent number: 6515011
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.
    Type: Grant
    Filed: December 18, 2001
    Date of Patent: February 4, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Harold G. Selnick, James C. Barrow, Philippe G. Nantermet, Peter D. Williams, Kenneth J. Stauffer, Philip E. Sanderson, Kenneth E. Rittle, Matthew M. Morrissette, Catherine M. Wiscount, Lekhanh O. Tran, Terry A. Lyle, Donnette D. Staas
  • Patent number: 6515126
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein Ts is a tosylate group and R is an alkyl group, an unsubstituted phenyl or substituted phenyl ring, or a benzyl or substituted benzyl group; which comprises: (i) cyclising a compound of formula (II) in the presence of a suitable catalyst; and (ii) purifying and collecting the resultant compound of formula (I).
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: February 4, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Michael Stewart Ashwood, Ian Frank Cottrell, Cameron John Cowden, Debra Jane Wallace
  • Patent number: 6515023
    Abstract: A thrombin receptor antagonist having the formula useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.
    Type: Grant
    Filed: January 30, 2001
    Date of Patent: February 4, 2003
    Assignee: Merck & Co., Inc.
    Inventors: James C. Barrow, Philippe G. Nantermet, Harold G. Selnick, John H. Hutchinson, Michael J. Breslin, Kristen L. Glass, Thomas M. Connolly, Andrew Stern
  • Patent number: 6511994
    Abstract: Compounds of Formula I: (wherein R1, R2, R3, R4, Q, and X are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally 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: October 10, 2001
    Date of Patent: January 28, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Ronald M. Kim, Jiang Chang, Kevin T. Chapman, Sander G. Mills
  • Patent number: 6511968
    Abstract: The invention provides a method for treating, preventing, or reducing the risk of developing a condition selected from the group consisting of acute coronary ischemic syndrome, thrombosis, thromboembolism, thrombotic occlusion and reocclusion, restenosis, transient ischemic attack, and first or subsequent thrombotic stroke, in a patient, comprising administering to the patient a therapeutically effective amount of an antiplatelet agent in combination with a therapeutically effective amount of a COX-2 inhibitor. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a COX-2 inhibitor, or a pharmaceutically acceptable salt thereof, and an antiplatelet agent, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: January 28, 2003
    Assignee: Merck & Co., Inc.
    Inventor: Steven A. Nichtberger
  • Patent number: 6506777
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: January 14, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Jennifer L. Loebach, Malcolm Maccoss, Sander G. Mills
  • Patent number: 6506908
    Abstract: Processes are disclosed for preparing 3-hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists. A process is described in which the compounds are prepared by opening the cyclopropyl ring of a (1-alkoxycarbonyl-2-oxo)-trans-bicyclo[3.1.0]hexane compound by addition of a nucleophile to the cyclopropyl ring, and then decarboxylating the resulting 2-alkoxycarbonyl-3-(Nu-methyl)-cyclopentanone (Nu=the added nucleophilic group) via base solvolysis. Also described is a process for preparing the bicyclo[3.1.0]hexane precursors by the catalyzed cyclopropanation of a suitable alpha-diazo-beta-ketoester. The preparation of the alpha-diazo-beta-ketoesters and precursors thereto are also disclosed.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: January 14, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Nobuyoshi Yasuda, Michael Palucki, Joann M. Um, David Alan Conlon, Barry M. Trost
  • Patent number: 6504066
    Abstract: The present invention is concerned with novel processes for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: January 7, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Paul Devine, Hansen Karl
  • Patent number: 6500828
    Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a difluoro-or tri-fluoro-substituted phenyl ring at the 3-position, a triazolyl moiety at the 6-position, and a tert-butyl group at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are useful in the treatment of anxiety and convulsions.
    Type: Grant
    Filed: July 23, 2001
    Date of Patent: December 31, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Jose Luis Castro Pineiro, Richard Thomas Lewis, Kevin William Moore, Leslie Joseph Street
  • Patent number: 6500844
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R7, R8, X, Y, Z, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: December 31, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Kevin T. Chapman, Malcolm Maccoss, Sander G. Mills, Bryan Oates