Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Detergent-free hepatitis C protease
    Patent number: 5861297
    Abstract: The protease of Hepatitis C virus (HCV) is purified without detergent, and is useful as a screening tool for HCV antivirals as well as a diagnostic tool for diseases resulting from HCV infection.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: January 19, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Vinod V. Sardana, Jeffrey T. Blue
  • Substituted imidazoles having cytokine inhibitory activity
    Patent number: 5859041
    Abstract: Compounds represented by formula I: ##STR1## are disclosed. .sup.AR represents an aromatic group containing 6-10 atoms; and ##STR2## represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional N atoms and 0-1 O or S atom. A pharmaceutical composition is also included. Methods of treating cancer and cytokine mediated diseases are also included.
    Type: Grant
    Filed: June 9, 1997
    Date of Patent: January 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Nigel J. Liverton, David A. Claremon, John W. Butcher, Mark T. Bilodeau
  • N-heterocyclic piperazinyl and H-heterocyclic piperazinonyl inhibitors of farnesyl-protein transferase
    Patent number: 5859015
    Abstract: The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## 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: January 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, Theresa M. Williams
  • Process for the crystalization of losartan
    Patent number: 5859258
    Abstract: Losartan potassium is an angiotensin II antagonist useful in the treatment of hypertension and congestive heart failure. ##STR1## This invention relates to the process for the controlled crystallization of losartan potassium utilizing anti-solvent addition combined with massive seeding in order to obtain the desired crystal morphology and bulk physical properties necessary for successful formulation.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: January 12, 1999
    Assignee: Merck & Company, Inc.
    Inventors: Patrick Breen, Erik A. Dienemann, Albert D. Epstein, Karen A. Larson, Michael T. Kennedy, Hari Mahadevan
  • Arylheteroaryl inhibitors of farnesyl-protein transferase
    Patent number: 5859035
    Abstract: The present invention is directed to compounds which inhibit famesyl-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 famesyl-protein transferase and the famesyl of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: January 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5859012
    Abstract: The present invention is directed to piperazine-2,3-dione 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 25, 1997
    Date of Patent: January 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Theresa M. Williams
  • Method of preparing phosphodiesterase IV inhibitors
    Patent number: 5856498
    Abstract: This invention is concerned with a novel process for the preparation of a compound of structural formula I ##STR1## wherein R.sup.1 and R.sup.2 independently are aryl, C.sub.2-15 alkenyl or C.sub.1-15 alkyl, either unsubstituted or substituted with one or three substituents, which can be the same or different, selected from the group consisting of R.sup.a, wherein R.sup.a belongs to a group consisting of C.sub.1-6 alkyl, aryl, halo, --N(R.sup.3).sub.2, --NO.sub.2, --CN, --OR.sup.3, --C.sub.3-6 cycloalkoxy, --CO(R.sup.3), --COOR.sup.3, SO.sub.2 R.sup.3 and --SR.sup.3 ; wherein R3 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl and aryl, said alkyl, alkenyl or aryl optionally substituted with 1 to 3 groups of R.sup.a, which is an important antiasthmatic agent.
    Type: Grant
    Filed: September 16, 1997
    Date of Patent: January 5, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Ilias K. Dorziotis, Ioannis N. Houpis, Jaemoon Lee, Ralph P. Volante
  • Chiral auxilary for stereoselective alkylations
    Patent number: 5856519
    Abstract: This invention relates to a method for the stereoselective synthesis of a 2-aryloxycarboxylic acid using a chiral auxiliary to enhance the stereoselectivity of the alkylation of the .alpha.-halo acid with an aryloxy group.
    Type: Grant
    Filed: September 23, 1997
    Date of Patent: January 5, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Paul N. Devine, Richard M. Heid, Jr., David M. Tschaen
  • Efficient synthesis of a chiral mediator
    Patent number: 5856492
    Abstract: An efficient method for the quantitative preparation and isolation of a compound of formula I ##STR1## or its enantiomer, a chiral mediator used in enantioselective synthesis.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: January 5, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Cheng Yi Chen, Feng Xu, Richard D. Tillyer, Dalian Zhao
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5856326
    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 1, 1996
    Date of Patent: January 5, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Terrence M. Ciccarone, Christopher J. Dinsmore, Robert P. Gomez, Theresa M. Williams, George D. Hartman
  • Biheteroaryl inhibitors of farnesyl-protein transferase
    Patent number: 5854265
    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: December 29, 1998
    Assignee: Merck & Co., Inc.
    Inventor: Neville J. Anthony
  • Cyclohexapeptidyl bisamine compound, compositions containing said compound and methods of use
    Patent number: 5854212
    Abstract: A compound of the formula ##STR1## is disclosed which is useful for the treatment of fungal infections and for the treatment of infections caused by Pneumocystis carinii.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: December 29, 1998
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, James F. Dropinski
  • Antifungal cyclohexapeptides
    Patent number: 5854213
    Abstract: The present invention is directed to novel carba cyclohexapeptide compounds of the formula ##STR1## where all substituents are defined herein, which are useful as antifungal agents and for the treatment of Pneumocystis carinii infections. Compositions containing the compounds of the invention are also disclosed.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: December 29, 1998
    Assignee: Merck & Co., Inc.
    Inventor: Frances A. Bouffard
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5854264
    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: December 29, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5852010
    Abstract: The present invention is directed to substituted benozdiazepine 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 25, 1997
    Date of Patent: December 22, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, Neville J. Anthony, John S. Wai
  • Compounds formed by an asymmetric conjugate addition reaction
    Patent number: 5849914
    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: August 4, 1997
    Date of Patent: December 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Antagonists of gonadotropin releasing hormone
    Patent number: 5849764
    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: December 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Lin Chu, Thomas F. Walsh, Michael H. Fisher, Narindar N. Girotra, Matthew J. Wyvratt, Peter Lin, Wallace T. Ashton
  • Bioerodible implants
    Patent number: 5837228
    Abstract: A bioerodible controlled release dosage form is disclosed comprising a polymer formed by condensing beneficial agents having a hydroxyl functionality of two or more with diketene acetals or divinyl ethers which delivers beneficial agents to a biological environment of use. A statistically significant portion of the beneficial agent is covalently bonded within the polymer matrix.
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: November 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Chung Shih, Gaylen M. Zentner, Randall V. Sparer, R. Lee Seward
  • Method for analyzing the immunosuppressant activity of ion channel blockers using the mini-pig
    Patent number: 5837220
    Abstract: A method for analyzing the immunosuppressant activity of Kv1.3 inhibitors using the mini- and micro-pig. These pig models have been found to have K.sub.v 1.3 channels very similar to man both in function and setting of membrane potential of T-lymphocytes, and respond similarly in a mixed lymphocyte reaction (MLR) to the K.sub.v 1.3 channel blockers. The mini-pig and micro-pig provide useful in vivo animal models for studying the immunosuppressant activity of Kv1.3 channel blockers that would be expected to function in man.
    Type: Grant
    Filed: September 10, 1996
    Date of Patent: November 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: J. Thomas Blake, William P. Feeney, Gloria C. Koo, Althea D. Talento
  • 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use
    Patent number: 5837719
    Abstract: The present invention addresses 2, 5-substituted aryl pyrroles of the formula: ##STR1## or a pharmaceutically acceptable salts thereof, as well as compositions containing such compounds and methods of treatment. The compounds are useful for treating Cytokine mediated diseases, which 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 in immunoregulation and other physiological conditions, such as inflammation. The compounds also have glucagon antagonist activity.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: November 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Stephen E. de Laszlo, Nigel J. Liverton, Gerald S. Ponticello, Harold G. Selnick, Nathan B. Mantlo