Patents Represented by Attorney, Agent or Law Firm Valerie J. Camara
  • Thrombin inhibitors
    Patent number: 6376499
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is N Y1 or O; c is CY2 or N; d is CY2; e is CY1 or N; f is CY1 or N; g is CY1 or N; Y1 is hydrogen, C1-4 alkyl, or halogen; Y2 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy; A is  and W, X, Z, R3, R4 and R5 are defined in the specification.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: April 23, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Philip E. Sanderson, Terry Lyle, Bruce Dorsey, Matthew G. Stanton, Adel M. Naylor-Olsen
  • Asymmetric conjugate addition reaction
    Patent number: 6353110
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: November 24, 1999
    Date of Patent: March 5, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul N. Devine, Richard D. Tillyer, Richard M. Heid, Jr., David M. Tschaen
  • SRC kinase inhibitor compounds
    Patent number: 6329380
    Abstract: Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of proteins tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.
    Type: Grant
    Filed: June 26, 2000
    Date of Patent: December 11, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Joung L. Goulet, Mark A. Holmes, Julianne A. Hunt, Sander G. Mills, William H. Parsons, Peter J. Sinclair, Dennis M. Zaller
  • SRC kinase inhibitor compounds
    Patent number: 6316444
    Abstract: Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of protein tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.
    Type: Grant
    Filed: June 26, 2000
    Date of Patent: November 13, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Julianne A. Hunt, Sander G. Mills, Peter J. Sinclair, Dennis M. Zaller
  • Synthesis of cyclopropaneacetylene using a catalytic decarboxylation reaction
    Patent number: 6313364
    Abstract: The present invention relates to a process for the preparation of cyclopropaneacetylene by the two step process: (1) an alkylation of propiolic acid with a 1,3-disubstituted propane followed by a cycloalkylation to give a 3-cyclopropaneacetylene carboxylic acid; and (2) decarboxylation of 3-cyclopropaneacetylene carboxylic acid in the presence of copper catalyst.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: November 6, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Karel M. J. Brands
  • Method for decreasing QT dispersion or inhibiting the progression of QT dispersion with an angiotensin II receptor antagonist
    Patent number: 6300356
    Abstract: Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in die risk of experiencing an adverse cardiac event, such as sudden cardiac death, myocardial infarction or arrhythmias, using QT dispersion in patients treated with a therapeutically effective amount of an angiotensin II antagonist.
    Type: Grant
    Filed: August 10, 2000
    Date of Patent: October 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Robert Segal, Paul J. Robinson, Lawrence I. Deckelbaum
  • Method for quantitating an inflammatory response
    Patent number: 6268155
    Abstract: A method for objectively quantitating the cellular infiltration in a tissue biopsy of a warm-blooded animal using a capture ELISA method. This method also allows one to quantitate the cellular infiltration of a tissue biopsy corresponding to an inflammatory response. As such this invention has both research and clinical applications in the analysis of an inflammatory response, and the effectiveness of immunosuppresants in addressing the inflammation.
    Type: Grant
    Filed: September 10, 1996
    Date of Patent: July 31, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Gloria C. Koo, Mai P. Nguyen, Althea D. Talento
  • Cyclohexapeptidyl amine compounds
    Patent number: 6268338
    Abstract: Cyclohexapeptidyl amine compounds are disclosed of the formula: or its acid addition salt, wherein: R1 is H or OH; R2 is H or OH; R3 is QCnH2nNRVRVI, QCnH2nNRVRVIRVII+Y−, or Q(CH2)1-3CRVIIIRIXNHRX.
    Type: Grant
    Filed: April 30, 1993
    Date of Patent: July 31, 2001
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances Aileen Bouffard, James F. Dropinski, Robert A. Zambias
  • Rearrangement process and tricyclic and tetracyclic compounds
    Patent number: 6268510
    Abstract: A rearrangement process for the preparation of a 6,5,5-tricyclic, a 6,6,5-tricyclic and 6,5,5,7-tetracyclic ring system is disclosed.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: July 31, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Lisa F. Frey, Edward J. J. Grabowski, Stephane G. Ouellet, Robert A. Reamer, Richard D. Tillyer
  • Method of improved mixing of a varicella-infected cell culture in roller bottles
    Patent number: 6251653
    Abstract: A method for enhancing the mixing of a varicella-infected cell culture in a roller bottle by the introduction of controlled cross-sectional flow perturbations in roller bottle rotation is disclosed. The effectiveness of the method is demonstrated by achieving higher efficiency in cell culturing and virus propagation in roller bottles by introducing controlled cross-sectional flow perturbations during the process.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: June 26, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Joye L. Bramble, Fernando J. Muzzio, James A. Searles
  • Methods of treating or preventing cardiac arrhythmia
    Patent number: 6214810
    Abstract: This application discloses a method of treating or preventing atrial arrhythmias which utilizes compounds which are blockers of the ultra-rapidly-activating delayed rectifier K+ current (IKur) of the human atrium in a use-dependent and/or rate dependent manner, and which provide the selective block preferentially at fast heart rates so that the effect is realized or maximized when required.
    Type: Grant
    Filed: April 19, 1999
    Date of Patent: April 10, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Bernard Fermini, Joseph J. Lynch, Jr., Joseph J. Salata, Richard J. Swanson
  • Methods of treating or preventing cardiac arrhythmia
    Patent number: 6214809
    Abstract: A method of treating or preventing supraventricular tachyarrhythmias is disclosed which comprises the use of a compound which selectively blocks the ultra-rapidly-activating delayed rectifier K+ current (IKur) of the human atrium.
    Type: Grant
    Filed: April 19, 1999
    Date of Patent: April 10, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Bernard Fermini, Joseph J. Lynch, Jr., Joseph J. Salata, Richard J. Swanson
  • Benzodiazepine derivatives as antiarrhythmic agents
    Patent number: 6214823
    Abstract: This invention is concerned with novel compounds represented by structural formula I which are useful in the treatment of arrhythmia.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: April 10, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Nigel J. Liverton, John W. Butcher, David A. Claremon, Harold G. Selnick
  • Method for reducing mortality with an angiotensin II antagonist
    Patent number: 6201002
    Abstract: Angiotensin II receptor antagonists are useful in reducing and preventing mortality and sudden cardiac death in symptomatic heart failure patients. Losartan potassium has been shown to reduce mortality and sudden cardiac death in this patient population. Additionally, losartan potassium has been shown to reduce the need for hospitalization of symptomatic heart failure patients.
    Type: Grant
    Filed: January 6, 1998
    Date of Patent: March 13, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Polly A. Beere, Paul I. Chang, Bertram Pitt, Eva J. Rucinska, Robert Segal, Divakar Sharma, Duane B. Snavely
  • Asymmetric conjugate addition reaction
    Patent number: 6172235
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: April 27, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Model of heart failure
    Patent number: 6158438
    Abstract: A method of chronically instrumenting an animal enabling one to simulate congestive heart failure. This invention also relates to method for assessing the effects of a test compound on cardiac function and systemic vascular dynamics.
    Type: Grant
    Filed: February 4, 1999
    Date of Patent: December 12, 2000
    Assignee: Merck & Co., Inc.
    Inventor: You-Tang Shen
  • Potassium channel agonists
    Patent number: 6150357
    Abstract: This application discloses a method of treating cardiac ventricular arrhythmias and repolarization abnormalities associated with long QT syndrome and/or congestive heart failure comprising the adminstration of an agonist of the slowly activating cardiac delayed rectifier potassium current (I.sub.Ks).
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: November 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Joseph J. Salata, Jixin Wang, Michael C. Sanguinetti, Nancy K. Jurkiewicz
  • Oxidation process using periodic acid
    Patent number: 6150554
    Abstract: The present invention relates to an oxidation which converts a primary or secondary alcohol of Formula II: ##STR1## to an acid or ketone of Formula I: ##STR2## with periodic acid and a catalytic amount of a chromium reagent.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: November 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jing Li, David M. Tschaen, Zhiguo Song, Mangzu Zhao
  • Oxidaton of primary alcohols to carboxylic acids with a TEMPO catalyst using NaClO.sub.2 and NaClO
    Patent number: 6127573
    Abstract: The present invention relates to a TEMPO-catalyzed oxidation of primary alcohols, RCH.sub.2 OH to corresponding carboxylic acids, RCOOH in the presence of catalytic in the presence of catalytic amount of NaClO and stoichiometric amount of NaClO.sub.2 as an oxidant.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jing Li, Zhiguo Song, David M. Tschaen, Mangzu Zhao
  • Enantioselective bioreduction using yeast
    Patent number: 6121026
    Abstract: The invention relates to a class of enantiomerically pure intermediates represented by Formula I, where X is F, Cl, Br, or I, and a novel enantioselective bioreductive process using yeast to form these intermediates, which are useful in the synthesis of endothelin antagonists, and the like.
    Type: Grant
    Filed: July 23, 1999
    Date of Patent: September 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Michel M. Chartrain, Barbara A. Krulewicz, Paul N. Devine, David M. Tschaen