Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Bridged carbapenem compounds, compositions containing such compounds and methods of use
    Patent number: 5372993
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents. Compositions containing such compounds and methods of use are also disclosed.
    Type: Grant
    Filed: June 10, 1993
    Date of Patent: December 13, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. DiNinno
  • Lipopeptide derivatives
    Patent number: 5369093
    Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides having the formula. ##STR1## wherein R is H or OH and R' is a phosphono, sulfo or acyl radical possessing a charged group at neutral pH.The derivatives are esters but having a charged group, have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
    Type: Grant
    Filed: March 15, 1991
    Date of Patent: November 29, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Milton L. Hammond, James M. Balkovec, David J. Mathre
  • Controlled release drug dispersion delivery device
    Patent number: 5366738
    Abstract: A device for the controlled delivery of a beneficial agent as a gelatinous dispersion consisting of (i) a core which contains a beneficial agent, a polymer which forms gelatinous microscopic particles upon hydration and if desired an agent to modulate the hydration of the polymer; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of a dispersion comprising gelatinous microscopic particles.
    Type: Grant
    Filed: September 8, 1993
    Date of Patent: November 22, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Gerald S. Rork, James D. Pipkin
  • Antibiotic agent
    Patent number: 5366880
    Abstract: A new antibiotic cyclic lipopeptide having the formula ##STR1## wherein R is H or OH and a method of producing is described. The agent has very high activity against human pathogens and is of very low mammalian toxicity.
    Type: Grant
    Filed: May 21, 1993
    Date of Patent: November 22, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Schwartz, Prakash S. Masurekar, David F. Sesin, Jerrold M. Liesch, Thomas C. Hallada, Otto D. Hensens
  • Farnesyl pyrophosphate analogs
    Patent number: 5362906
    Abstract: The present invention is directed to farnesyl pyrophosphate analogs 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: June 18, 1993
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Ta-Jyh Lee, Robert L. Smith, Gerald E. Stokker
  • 2-(heterocyclylheteroaryliumalkyl) phenyl carbapenem antibacterial agents
    Patent number: 5362723
    Abstract: Carbapenems having the formula: ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Thomas N. Salzmann, David A. Muthard
  • 2-(9-fluorenonyl)-carbapenem intermediates
    Patent number: 5356889
    Abstract: Disclosed are carbapenems of the formula ##STR1## which are 2-(9-fluorenonyl)-carbapenems useful as antibacterial agents. Intermediates for preparation of these compounds is also disclosed.
    Type: Grant
    Filed: October 26, 1992
    Date of Patent: October 18, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Frank P. DiNinno, Lovji D. Cama, James V. Heck
  • Process for the production of a novel endothelin antagonist
    Patent number: 5352800
    Abstract: Fermentation processes for the production of a compound of the Structural Formula I ##STR1## The compound of Structural Formula I has been shown to have endothelin antagonist activity and is therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure vasospasm, cerebral and cardia ischemia, myocardial infarction inflammatory diseases, Raynaud's disease, endotoxin shock and asthma.
    Type: Grant
    Filed: March 11, 1993
    Date of Patent: October 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Gerard F. Bills, Michael A. Goetz, Robert A. Giacobbe, Lucia Herranz, E. Tracy Turner Jones, Fernando Pelaez, Yu L. Kong, Sheo B. Singh, Siobhan Stevens-Miles
  • Inhibitors of farnesyl protein transferase
    Patent number: 5352705
    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: June 26, 1992
    Date of Patent: October 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
  • Triazolyl and tetrazolyl phenyl substituted carbapenems, compositions containing such compounds and methods of use
    Patent number: 5350746
    Abstract: Triazolyl and tetrazolyl phenyl substituted carbapenems of the formula I are disclosed. ##STR1## One or two of the variables X, Y and Z represent nitrogen atoms. The heteroaryl ting may be charged or uncharged.Pharmaceutical compositions and methods of treatment are also disclosed.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, James V. Heck
  • Spheronization process using charged resins
    Patent number: 5350584
    Abstract: The invention comprises a novel process for the spheronization of charged resins. Spherical multiparticlates are produced which range in size from 0.3 mm to 3 mm in diameter. The spherical particle product is microcrystalline-free. The process consists of the steps of mixing followed by wet granulation, spheronization and drying.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Gregory A. McClelland, Gaylen M. Zentner
  • Inhibitors of farnesyl protein transferase
    Patent number: 5350867
    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: June 9, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Sheo B. Singh
  • 2-biphenyl-carbapenems
    Patent number: 5350846
    Abstract: Carbapenems of the formula: ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: January 25, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Thomas N. Salzmann
  • N,N-diacylpiperazines
    Patent number: 5348955
    Abstract: Diacylpiperazines of general structural formula: ##STR1## are: angiotensin II (A-II) antagonists with affinity for both AT.sub.1 and AT.sub.2 receptors useful in the treatment of hypertension, congestive heat failure, cerebrovascular, cognitive, and CNS disorders.
    Type: Grant
    Filed: June 22, 1993
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Mu T. Wu
  • Cationic-2-heteroarylphenyl-carbapenem antibacterial agents
    Patent number: 5342933
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: August 30, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Susan M. Schmitt, Ravindra N. Guthikonda
  • Inhibitors of farnesyl protein transferase
    Patent number: 5340828
    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: September 30, 1991
    Date of Patent: August 23, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, S. Jane deSolms
  • Boron containing intermediates useful in the preparation of carbapenems
    Patent number: 5338875
    Abstract: The present invention is directed to intermediates of the following formula which are useful in the preparation of Carbapenem-antibiotics ##STR1##
    Type: Grant
    Filed: November 19, 1992
    Date of Patent: August 16, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ann DeCamp, Ulf H. Dolling, Yulan Li, Dale L. Rieger, Nobuyoshi Yasuda, Lyndon C. Xavier
  • Process for crystalline cyclic lipopeptides
    Patent number: 5336756
    Abstract: A process for obtaining a compound of the formula ##STR1## in crystalline form by solubilizing the compound in warm aqueous n-propanol and then allowing the solution to stand at ambient temperature until crystal formation is substantially complete is described. The crystalline compound obtained thereby is also described.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: August 9, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Schwartz, August J. Kempf, David J. Mathre
  • Six-membered ring fused imidazoles substituted with phenoxyphenylacetic acid derivatives
    Patent number: 5334598
    Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I have endothelin ##STR1## antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: August 2, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Scott W. Bagley, Prasun K. Chakravarty, Anna Chen, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Elizabeth M. Naylor, Thomas F. Walsh, David L. Williams, Jr.
  • MRSA active 2-phenyl-carbapenems
    Patent number: 5334590
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: August 2, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Ravindra N. Guthikonda