Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6150352
    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 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, Eric E Allen, Matthew J. Wyvratt, Jr., Jinlong Jiang, Richard B. Toupence, Thomas F Walsh, Feroze Ujjainwalla, Jonathan R Young, Robert J. Devita
  • 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
  • Glass vial dryer
    Patent number: 6145216
    Abstract: A dryer for drying articles, such as vials of pharmaceutical bulk product, such as vaccines is disclosed. The dryer circulates ambient air through a plenum to evenly evaporate condensation on vials of pharmaceutical brought from refrigeration for labeling and further handling.
    Type: Grant
    Filed: May 3, 1999
    Date of Patent: November 14, 2000
    Assignee: Merck & Co., Inc.
    Inventor: Timothy J. Bauer
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6147088
    Abstract: There are disclosed compounds of formula (I) and pharmaceutical 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.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: November 14, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Eric E Allen, Matthew J. Wyvratt, Jr., Jinlong Jiang, Roy G. Smith, Thomas F Walsh, Yi Tien Yang, Jonathan R Young, Robert J. Devita
  • Preparation of beta-methyl carbapenem intermediates
    Patent number: 6143885
    Abstract: The instant invention relates to a compound of the formula: ##STR1## wherein R.sub.a and P are: (a) hydrogen,(b) methyl, or(c) a hydroxy protecting groupand an efficient process for its synthesis characterized by combining a ketoester with an acid and a catalyst at a temperature of from about 0.degree. to about 50.degree. C. and from about 0 to 500 psig to produce the above compound.
    Type: Grant
    Filed: July 28, 1998
    Date of Patent: November 7, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Woo-Baeg Choi, Jaemoon Lee, Joseph E. Lynch, Paul J. Reider, Ralph P. Volante
  • Peptides
    Patent number: 6143864
    Abstract: Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 7, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Deborah DeFeo-Jones, Dong-Mei Feng, Victor M. Garsky, Raymond E. Jones, Allen I. Oliff
  • Process for making 1,5-disubstituted imidazoles
    Patent number: 6140508
    Abstract: The present invention is directed to a process for synthesizing 1,5-disubstituted imidazoles, which are useful in the preparation of farnesyl-protein transferase inhibitors.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: October 31, 2000
    Assignee: Merck & Co., inc.
    Inventors: David Askin, Jennifer A. Cowen, Peter E. Maligres, J. Christopher McWilliams, Marjorie S. Waters
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 6140318
    Abstract: Compounds of formula I are disclosed. ##STR1## as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group -A-Q-L-B.The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: October 31, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lovji D. Cama, Robert R. Wilkening, Ronald W. Ratcliffe, Kenneth J. Wildonger, Wanying Sun
  • Antifungal compositions
    Patent number: 6136783
    Abstract: The invention is a pharmaceutical composition for intravenous administration to a patient comprisinga) a pharmaceutically effective amount of a compound having the formula ##STR1## and the pharmaceutically acceptable salts thereof; b) a pharmaceutically acceptable amount of an excipient such as a bulking agent effective to form a lyophilized cake; andc) a pharmaceutically acceptable amount of acetate buffer effective to provide a pH of between about 4 and 7.
    Type: Grant
    Filed: June 15, 1999
    Date of Patent: October 24, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Maneesh J. Neururkar, Michael J. Kaufman, William A. Hunke
  • Peptides
    Patent number: 6130204
    Abstract: Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
    Type: Grant
    Filed: April 6, 1998
    Date of Patent: October 10, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Deborah DeFeo-Jones, Dong-Mei Feng, Victor M. Garsky, Raymond E. Jones, Allen I. Oliff
  • Conjugates useful in the treatment of prostate cancer
    Patent number: 6127333
    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 a diamine linker between the oligopeptide and vinblastine. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
    Type: Grant
    Filed: July 9, 1998
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Stephen F. Brady, Victor M. Garsky, Joseph M. Pawluczyk
  • Inhibitors of prenyl-protein transferase
    Patent number: 6127390
    Abstract: The present invention is directed to compounds which inhibit prenyl-protein transferase (FTase) 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: October 1, 1998
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, William C. Lumma, Jr., Anthony W. Shaw, John T. Sisko, Thomas J. Tucker
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6127366
    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 famesylation of the oncogene protein Ras.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Byeong M. Kim, Anthony W. Shaw, Samuel L. Graham, S. Jane deSolms, Terrence M. Ciccarone
  • Flow control orifice
    Patent number: 6126037
    Abstract: An improved process of creating a uniform puncture in a medication dispenser bottle utilizes a membrane within the tip of the dispenser which is punctured with the hole being of a controlled, uniform size. The size of the hole is controlled by a mechanical stop created by shoulders integral to the base of the puncturing member.
    Type: Grant
    Filed: August 24, 1998
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventor: Arthur L. Lifshey
  • 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
  • Process for cleaning mercury-contaminated soils
    Patent number: 6120579
    Abstract: The present invention relates to a process for cleaning mercury-contaminated soils that is simple, efficient and safe to use. This process can also be used to clean soils contaminated with additional metals, such as zinc, copper and lead, at a lower pH. The invention involves treating contaminated soils with solid hypochlorite in a continuous counter-current process.
    Type: Grant
    Filed: September 14, 1998
    Date of Patent: September 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Youssef El-Shoubary, Subash C. Seth, William F. Lavosky, Ned A. Speizer
  • Tablet dispensing cap
    Patent number: 6112942
    Abstract: A tablet dispensing cap that allows an individual who is elderly, infirm, handicapped or visually impaired to dispense a single, non-liquid form through a single-handed operation.
    Type: Grant
    Filed: February 3, 1998
    Date of Patent: September 5, 2000
    Assignee: Merck & Co., Inc.
    Inventor: Gordon D. Deacon
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6110931
    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: March 25, 1999
    Date of Patent: August 29, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla, Jonathan R. Young
  • Method of treating cancer
    Patent number: 6103487
    Abstract: The instant invention provides for a method of inhibiting prenyl-protein transferases and treating cancer which comprises administering to a mammal a prenyl-protein transferase inhibitor which is efficacious in vivo as an inhibitor of geranylgeranyl-protein transferase type I (GGTase-I). The invention also provides for a method of inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I by administering a compound that is a dual inhibitor of both of those prenyl-protein transferases. The invention also provides for a method of identifying such a compound, the method comprising a modified inhibitory assay that incorporates a modulator anion that alters the in vitro potency of prenyl-protein transferase inhibitors in a way that predicts their potency in vivo, thus providing convenient identification of compounds that possess such in vivo activity.
    Type: Grant
    Filed: August 26, 1998
    Date of Patent: August 15, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Stanley F. Barnett, David C. Heimbrook, Hans E. Huber, Denis R. Patrick