Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
    Patent number: 6063930
    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: October 2, 1998
    Date of Patent: May 16, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J Dinsmore, Neville J. Anthony, Gerald E. Stokker, Robert P. Gomez
  • Process for synthesizing carbapenem side chain intermediates
    Patent number: 6063931
    Abstract: A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula 4: ##STR3## Compound 4 is then reacted with a group II metal sulfide source in water to produce a compound of formula 1.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: May 16, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Karel M. J. Brands, John M. Williams, Ulf H. Dolling, Ronald B. Jobson, Antony J. Davies, Ian F. Cottrell, Mark Cameron, Michael S. Ashwood
  • Radiolabeled farnesyl-protein transferase inhibitors
    Patent number: 6060038
    Abstract: The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.
    Type: Grant
    Filed: May 7, 1998
    Date of Patent: May 9, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Hugh D. Burns, Wai-Si Eng, Raymond E. Gibson
  • Process for synthesizing carbapenem side chain intermediates
    Patent number: 6060607
    Abstract: A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula 4: ##STR3## Compound 4 is then reacted with a group II metal sulfide source in water to produce a compound of formula 1.
    Type: Grant
    Filed: June 16, 1999
    Date of Patent: May 9, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Karel M. J. Brands, John M. Williams, Ulf H. Dolling, Ronald B. Jobson, Antony J. Davies, Ian F. Cottrell, Mark Cameron, Michael S. Ashwood
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6054466
    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: November 18, 1998
    Date of Patent: April 25, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Terrence M. Ciccarone, S. Jane deSolms
  • Immunosuppressant tricyclic compounds
    Patent number: 6051590
    Abstract: The compounds of Formula I are useful as immunosuppressive agents.
    Type: Grant
    Filed: May 13, 1999
    Date of Patent: April 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jianming Bao, Frank Kayser, Robert K. Baker, Shouwu Miao, William H. Parsons, Kathleen M. Rupprecht
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6051574
    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: February 10, 1999
    Date of Patent: April 18, 2000
    Assignee: Merck & Co., Inc.
    Inventor: Neville J. Anthony
  • Process for the synthesis of carbapenem intermediates, and compounds produced
    Patent number: 6048978
    Abstract: A process of synthesizing a carbapenem compound of formula 6: ##STR1## is disclosed using a compound of formula 4': ##STR2## The intermediate compounds that are described herein are also included in the present invention.
    Type: Grant
    Filed: September 23, 1998
    Date of Patent: April 11, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark S. Jensen, Chunhua Yang, Nobuyoshi Yasuda
  • Phosphate-mediated cyclization
    Patent number: 6046327
    Abstract: This invention relates to a cyclization process useful in the preparation of a key intermediate in the preparation of an endothelin antagonist of the general formula shown below: ##STR1##
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: April 4, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Richard D. Tillyer, David M. Tschaen, Zhiguo Song, Mangzu Zhao
  • Mur D inhibiting compounds, compositions containing such compounds and methods of use
    Patent number: 6030996
    Abstract: The present invention addresses compounds which inhibit Mur D. The compounds are represented by structural formula 1: ##STR1## wherein: X represents OH, OC.sub.1-6 alkyl, O-aryl, O-Har, uridinyl, 5-iodouridinyl or O--Y.sup.+, wherein Y.sup.+ represents a charge balancing group; R.sup.1 and R.sup.2 independently represent H or C.sub.1-6 alkyl, or R.sup.1 and R.sup.2 taken together represent C.sub.1-6 alkylene unsubstituted or substituted with from 1-2 aryl or Har groups; W represents H, aryl, C.sub.1-6 alkyl or a charge balancing group; each M independently represents a member selected from the group consisting of: H, a charge balancing group and a protecting group.Salts and hydrates thereof are included.Also included are pharmaceutical compositions and methods of treatment.
    Type: Grant
    Filed: March 11, 1998
    Date of Patent: February 29, 2000
    Assignee: Merch & Co., Inc.
    Inventor: Laura D. Gegnas
  • Cyclohexapeptidyl bisamine compounds
    Patent number: 6030944
    Abstract: Certain bisamine compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: February 29, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Frances Aileen Bouffard, James F. Dropinski, Robert A. Zambias
  • Oxidation process using tempo
    Patent number: 6031101
    Abstract: The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid ##STR1##
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: February 29, 2000
    Assignees: Merck & Co., Inc., Banyu Pharmaceuticals Co., Ltd
    Inventors: Paul N. Devine, Eiichi Mano, Zhiguo Song, David M. Tschaen, Mangzu Zhao
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6028201
    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: February 25, 1998
    Date of Patent: February 22, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, George D. Hartman
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6025366
    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: February 15, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla, Jonathan R. Young
  • Stereoselective process for enalapril
    Patent number: 6025500
    Abstract: The invention relates to an improved stereoselective heterogenous catalytic reductive amination between ethyl 2-oxo-4-phenylbutyrate and alanylproline using hydrogen, a catalyst and one or more additives to produce the ACE inhibitor, enalapril.
    Type: Grant
    Filed: September 17, 1999
    Date of Patent: February 15, 2000
    Assignee: Merck & Co., Ltd.
    Inventors: Mark A. Huffman, Paul J. Reider, Carl Leblond, Yongkui Sun
  • Immunosuppressant tetracyclic triterpenes
    Patent number: 6022890
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: February 8, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jianming Bao, Robert K. Baker, Frank Kayser, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht, Peter J. Sinclair
  • Pyridine propanoic acid derivatives
    Patent number: 6022972
    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: July 14, 1998
    Date of Patent: February 8, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Paul N. Devine, Richard D. Tillyer, Richard M. Heid, Jr., David M. Tschaen
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6017944
    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: October 26, 1998
    Date of Patent: January 25, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lin Chu, Thomas F. Walsh, Mark Goulet, Matthew J. Wyvratt, Stephanie L. Witkin
  • Efficient enantioselective addition reaction using an organozinc reagent
    Patent number: 6015926
    Abstract: An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.
    Type: Grant
    Filed: May 11, 1998
    Date of Patent: January 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Cheng Yi Chen, Lushi Tan, Richard D. Tillyer
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6015817
    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: December 4, 1997
    Date of Patent: January 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Wasyl Halczenko, Craig A. Stump