Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Conjugates useful in the treatment of benign prostatic hyperplasia
    Patent number: 6177404
    Abstract: Novel pharmaceutical compositions useful for the treatment of benign prostatic hyperplasia which comprises novel oligopeptides, which are selectively cleaved by enzymatically active PSA, in conjugation with a cytotoxic agent are described. Methods of treating benign prostate hypertrophy are also disclosed.
    Type: Grant
    Filed: August 3, 1998
    Date of Patent: January 23, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Deborah DeFeo-Jones, Raymond E. Jones, Allen I. Oliff, Edward M. Scolnick, Victor M. Garsky
  • Dual compartment solid phase extraction cartridge
    Patent number: 6177008
    Abstract: There is disclosed a dual compartment solid phase extraction cartridge comprising a container divided into a top volume and a bottom volume by a porous filter or frit, the top and bottom volumes having a quantity of sorbent. The cartridge is useful in the separation of components of a liquid and solid mixture.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: January 23, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Laszlo R. Treiber, Ali Shafiee
  • Conjugates useful in the treatment of prostate cancer
    Patent number: 6174858
    Abstract: Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. The conjugates of the invention are characterized by attachment of the cleavable oligopeptide to the oxygen atom at the 4-position on a vinca drug that has be desacetylated. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
    Type: Grant
    Filed: November 17, 1998
    Date of Patent: January 16, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Stephen F. Brady, Dong-Mei Feng, Victor M. Garsky
  • Oxidation process using periodic acid
    Patent number: 6172231
    Abstract: The present invention relates to a periodic acid oxidation which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Zhiguo Song, Mangzu Zhao, David M. Tschaen
  • 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
  • Inhibitors of prenyl-protein transferase
    Patent number: 6172076
    Abstract: The present invention is directed to conformationally constrained compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark W. Embrey, John S. Wai, Debra S. Perlow, Jacob M. Hoffman
  • 6-azaindole compounds as antagonists of gonadotropin releasing hormone
    Patent number: 6172080
    Abstract: There are disclosed compounds of formula (I) 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: March 7, 2000
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Thomas F. Walsh, Feroze Ujjainwalla
  • Tyrosine kinase inhibitors
    Patent number: 6162804
    Abstract: The present invention relates to benzinidazole compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
    Type: Grant
    Filed: March 11, 1999
    Date of Patent: December 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, April M. Cunningham, Randall W. Hungate, Timothy J. Koester
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6162813
    Abstract: There are disclosed compounds of formula (I) 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 conditions in both men and women.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: December 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Robert J. Devita, Matthew J. Wyvratt, Jr., Jonathan R. Young
  • Crystalline imidazole complexes as carbapenem intermediates and synthesis
    Patent number: 6162911
    Abstract: Novel crystalline carbapenem intermediate compounds of formula I: ##STR1## wherein: R.sub.1 represents CH.sub.3 or H and an efficient process for synthesis thereof are described.
    Type: Grant
    Filed: August 13, 1998
    Date of Patent: December 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Richard G. Ball, Nancy N. Tsou, James A. Mc Cauley, Chunhua Yang, Nobuyoshi Yasuda
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6159975
    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: February 10, 1999
    Date of Patent: December 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jonathan R. Young, Thomas F. Walsh, Mark T. Goulet, Michael H. Fisher
  • 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
  • Compounds useful in the treatment of neurofibromatosis
    Patent number: 6160015
    Abstract: The present invention relates to compositions useful in the treatment of benign proliferative disorder neurofibromatosis comprising a farnesyl protein transferase inhibitor. Further contained in this invention are methods of treating benign proliferative disorder neurofibromatosis in a mammal, which methods comprise administering to said mammal, a farnesyl protein transferase inhibitor.
    Type: Grant
    Filed: July 27, 1999
    Date of Patent: December 12, 2000
    Assignee: University of Cincinnati
    Inventor: Nancy Ratner
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6159989
    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 15, 1999
    Date of Patent: December 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
  • Process for the synthesis of substituted piperazinones via Mitsunobu reaction
    Patent number: 6160118
    Abstract: The present invention is directed to a process for synthesizing substituted piperazinones, which are useful intermediates for making farnesyl-protein transferase inhibitors, using a Mitsunobu reaction.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: December 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Stephanie Lewis, Steven A. Weissman
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6156772
    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: May 14, 1999
    Date of Patent: December 5, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr.
  • Method for increasing oxygen tension in the optic nerve and retina
    Patent number: 6156785
    Abstract: There is disclosed a method for increasing retinal and optic nerve head oxygen tension by application of a composition comprising carbonic anhydrase inhibitors to the eye.
    Type: Grant
    Filed: January 19, 1999
    Date of Patent: December 5, 2000
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Einae Stefansson, Jens Dollerup, Kurt Bang
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6156767
    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: May 22, 1998
    Date of Patent: December 5, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Matthew J. Wyvratt, Jr., Peter Lin, Lin Chu, Narindar N. Girotra
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6150522
    Abstract: There are disclosed compounds of formula (I) 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 conditions in both men and women.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: November 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Robert J. DeVita, Matthew J. Wyvratt, Jr., Jonathan R. Young
  • 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