Patents Represented by Attorney Joseph F. DiPrima

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  • Lipopeptide compounds
    Patent number: 5386010
    Abstract: Antifungal and antiparasital lipopeptide compounds stable in aqueous media are described. Stability in aqueous media render lipopeptides more useful for compositions for therapeutic applications.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: January 31, 1995
    Assignee: Merck & Co., Inc.
    Inventor: James M. Balkovec
  • Substituted pyrazine and its salts, compositions containing them and their use in medicine
    Patent number: 5384408
    Abstract: 3(R)-[2-(6-trifluoromethylpyrazin)yl]-1-azabicyclo[2.2.2]octane and its salts, and pharmaceutical formulations thereof are useful in medicine. In particular, they are useful for the treatment of neurological and mental illnesses whose clinical manifestations are due to cholinergic deficiency, and for lowering intraocular pressure. The compound may be prepared by dehydroxylating or decarboxylating the corresponding 3-hydroxy- or carboxy-quinuclidine analogue.
    Type: Grant
    Filed: March 10, 1993
    Date of Patent: January 24, 1995
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventors: Raymond Baker, Victor J. Lotti, Graham A. Showell
  • Bridged biphenyl carbapenem compounds, compositions containing such compounds and methods of use
    Patent number: 5384317
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: January 24, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. DiNinno
  • (N-pyridiniumphenyl)-carbapenems
    Patent number: 5382575
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: October 7, 1992
    Date of Patent: January 17, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Frank DiNinno, James V. Heck
  • Spirocycles
    Patent number: 5382587
    Abstract: Spirocycles of the general structural formulae: ##STR1## wherein: X is O, CH.sub.2 or SO.sub.m ;R.sup.1 is AlkylSO.sub.2 NH--, AlkylO--, AlkylSO.sub.2 --, AlkylCONH--, or NO.sub.2 --;R.sup.2 is --H, --OAlkyl, or --Alkyl;R.sup.3 is --NHCOCH.sub.2 SO.sub.m Phenyl, --NHCOCH.sub.2 SO.sub.m Alkyl,--NHCOC(CH.sub.3).sub.2 OH, or NHSO.sub.2 Alkyl;R.sup.4 and R.sup.5 are --H, or --Alkyl;R.sup.6 is ##STR2## R.sup.7 is --H, --CN, --NHSO.sub.2 Alkyl, --Br, --OAlkyl, --NH.sub.2, --NO.sub.2, --NHCOAlkyl, or NHCONHAlkyl;R.sub.8 is --H, --OH, --CN, --OAlkyl, --CONHAlkyl, --NHSO.sub.2 Alkyl, --NHCOAlkyl, --SO.sub.m Alkyl, or --CO.sub.2 Alkyl;and m is 0-2; or a pharmaceutically acceptable salt, hydrate or crystal form thereof; which are Class III antiarrhythmic agents.
    Type: Grant
    Filed: June 30, 1993
    Date of Patent: January 17, 1995
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott
  • Stable solvates of avermectin compounds
    Patent number: 5380838
    Abstract: There is disclosed a novel form of avermectin compounds wherein the avermectin compounds are crystallized as alcohol solvates to greatly enhance stability of the avermectin drug during long-term storage. The avermectin compounds have utility as highly potent antiparasitic, insecticidal, and anthelmintic agents and compositions for that use are also disclosed.
    Type: Grant
    Filed: October 8, 1993
    Date of Patent: January 10, 1995
    Assignee: Merck & Co. Inc.
    Inventors: Joseph S. Amato, Raymond Cvetovich
  • Aza cyclohexapeptide compounds
    Patent number: 5378804
    Abstract: Aza cyclohexapeptide compounds are disclosed with a nitrogen attached to the cyclohexapeptide ring at the 5-carbon of the 4-hydroxyornithine component. Such compounds are represented by the formula: ##STR1## The compounds are disclosed as having antifungal, antiprotozoal and anti-Pneumocystis carinii activity.
    Type: Grant
    Filed: March 16, 1993
    Date of Patent: January 3, 1995
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Regina M. Black, Frances A. Bouffard
  • Benzodiazepine cholecystokinin antagonists
    Patent number: 5378838
    Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).
    Type: Grant
    Filed: January 13, 1993
    Date of Patent: January 3, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Jeffrey M. Bergman, Roger M. Freidinger, Mark G. Bock
  • Bridged carbapenem antibacterial compounds
    Patent number: 5374630
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: June 10, 1993
    Date of Patent: December 20, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. DiNinno
  • Six membered ring fused imidazoles substituted with phenoxyphenylacetic acid derivatives used to treat asthma
    Patent number: 5374638
    Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin 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: December 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Daljit S. Dhanoa, Kenneth J. Fitch, Daniel F. Veber, Thomas F. Walsh, David L. Williams, Jr.
  • Benzo-fused lactams promote release of growth hormone
    Patent number: 5374721
    Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: December 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: William R. Schoen, Matthew J. Wyvratt
  • 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
  • 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
  • Substituted cephalosporin sulfones as anti-inflammatory and antidegenerative agents
    Patent number: 5364848
    Abstract: New substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
    Type: Grant
    Filed: May 1, 1992
    Date of Patent: November 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Raymond A. Firestone, Paul E. Finke, William K. Hagmann, Shrenik K. Shah, Kevan R. Thompson
  • Process for the preparation of 4"-amino avermectin compounds
    Patent number: 5362863
    Abstract: A 4"-oxoavermectin intermediate is reductively aminated using hexa- or heptamethyldisilazane and sodium borohydride to produce a 4"-amino (or methylamino)avermectin. The 4"- aminoavermectin is a useful intermediate in the preparation of N-acyl derivatives. The compounds are useful as agricultural and animal health insecticides and parasiticides.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Raymond Cvetovich
  • 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
  • Process for 4"-EPI-acetylamino-4"-deoxy-5-oximinoavermectin-B.sub.1
    Patent number: 5362862
    Abstract: An improved process for formation of a 5-oxime on avermectin derivatives comprises the treatment of the oxo compound with O-(trimethylsilyl)hydroxylamine in the presence of a Lewis acid.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Joseph S. Amato, Raymond Cvetovich
  • Single use fluid dispensing device
    Patent number: 5361947
    Abstract: A flexible fluid dispensing bottle is provided which conveniently meters out its contents in several small controlled doses. The device is designed to specifically provide multiple extended outlets to facilitate access beneath the fur of an animal ("comb effect") and to better spread treatment. In addition, the device uses a combination of bottle geometry, and internal ribs and cores to control capacity as well as volume displaced during individual pump strokes of the squeeze bottle.
    Type: Grant
    Filed: March 8, 1993
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Arthur L. Lifshey
  • Carbostyril oxytocin receptor antagonists
    Patent number: 5356904
    Abstract: A method of inhibiting oxytocin from acting at its receptor site by administering oxytocin receptor antagonist compounds of the formula ##STR1## wherein X is oxygen or sulfur; Y is hydrogen or lower alkyl; R.sup.
    Type: Grant
    Filed: October 7, 1992
    Date of Patent: October 18, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Roger M. Freidinger, Joseph M. Pawluczyk, Douglas J. Pettibone, Peter D. Williams