Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Glycosidation route to 4"-epi-methylamino-4"-deoxyavermectin B.sub.1
    Patent number: 5399717
    Abstract: A stereocontrolled glycosidation with thiophenyl 4-(N-allyloxycarbonyl)-epi-methylamino-4-deoxyoleandrose and 5-O-allyloxycarbonyl avermectin B.sub.1 monosaccharide using N-iodosuccinimide produces exclusively the .alpha.-anomer of a precursor of 4"-epi-methylamino-4"-deoxyavermectin B.sub.1 in 90% yield. Deprotection and crystallization as the benzoic acid salt yields 4"-epi-methylamino-4"-deoxyavermectin B.sub.1 (emamectin benzoate), a potent insecticide.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: March 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Raymond Cvetovich, Mallory F. Loewe
  • Antibiotic peptides bearing aminoalkylthioether moieties
    Patent number: 5399552
    Abstract: Certain aminoalkyl thioethers represented by the formula ##STR1## their acid addition salts and quaternary ammonium salts are described. The compounds have useful antimicrobial properties.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: March 21, 1995
    Assignee: Merck & Co, Inc
    Inventor: Frances A. Bouffard
  • Process of synthesizing binaphthyl derivatives
    Patent number: 5399771
    Abstract: A process of synthesizing a compound of the formula 1: ##STR1## is disclosed, which comprises reacting a compound of the formula 2: ##STR2## with diphenylphosphine in the presence of an amine base and a nickel catalyst to produce a compound of formula 1.
    Type: Grant
    Filed: June 1, 1994
    Date of Patent: March 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Dongwei Cai, Joseph F. Payack, Thomas R. Verhoeven
  • 6-amido-1-methyl-2-(substituted-thio)carbapenems
    Patent number: 5395931
    Abstract: New antibacterial 6-amido-1-methyl-2-(substituted-thio)-carbapenems and process for their synthesis involving new azetidinone intermediates.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: March 7, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Frank P. DiNinno, Thomas N. Salzmann
  • Fluid dispensing device with gravity-fill continuously variable dosage selection
    Patent number: 5392966
    Abstract: A device is provided for controlled dispensing of a variable measured quantity of fluid from a container. The device has a dosage cup chamber adapted to hold a measured quantity of fluid when the container is inverted and righted. This fluid is then dispensed from the chamber through a valved conduit.
    Type: Grant
    Filed: January 18, 1994
    Date of Patent: February 28, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Leonid Bunin
  • Packaging vial for a liquid product in particular medicinal or cosmetic
    Patent number: 5390822
    Abstract: Packaging vial for a liquid product in particular medicinal or cosmetic, manufacturing process and device for use of this vial. The vial includes a flexible casing (1), coupled to a rigid support (2), the casing (1) consisting of a pocket (10) with thin and distortable walls, containing the product and free from air, as well as a tubular nozzle (11) for dispensing the product, to which is coupled the pocket (10), the vial including furthermore a pump for dosing and delivering the product, said pump containing a fixed body inserted into the nozzle (11) and a moveable actuating member which is located inside the casing, but Which can be moved from the outside of the latter thanks to the distortable character of its wall which, proximate the actuating member, has the shape of a bellows.
    Type: Grant
    Filed: July 26, 1993
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Gilbert Lataix
  • Benzimidazolinones substituted with phenoxyphenylacetic acid derivatives
    Patent number: 5391566
    Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Elizabeth M. Naylor, James R. Tata, Thomas F. Walsh
  • Lipopeptide derivatives
    Patent number: 5386009
    Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: January 31, 1995
    Assignee: Merck & Co. Inc.
    Inventors: Milton L. Hammond, Robert E. Schwartz, James M. Balkovec
  • Lipopeptide derivatives
    Patent number: 5385884
    Abstract: There are disclosed lipopeptide derviatives of the general formula: ##STR1## where the substituents are defined herein which have antifungal and antiprotozoal activity. There are also disclosed pharmaceutical compositions containing these compounds.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: January 31, 1995
    Assignee: Merck & Co. Inc.
    Inventors: Milton L. Hammond, Robert E. Schwartz, James M. Balkovec
  • Disubstituted 6-aminoquinazolinones
    Patent number: 5385894
    Abstract: Novel disubstituted 6-aminoquinazolinones of the Formula (I), are useful as angiotensin II antagonists: ##STR1##
    Type: Grant
    Filed: April 4, 1994
    Date of Patent: January 31, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Stephen E. de Laszlo, Tomasz W. Glinka, William J. Greenlee, Prasun K. Chakravarty, Arthur A. Patchett
  • 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
  • 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
  • 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
  • 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
  • High speed process for preparing orifices in pharmaceutical dosage forms
    Patent number: 5376771
    Abstract: A laser drilling process capable of producing a plurality of holes in a pharmaceutical dosage form, at high speed, is presented. The process utilizes a digital laser marking system (DigiMark.TM. variable marking system) to produce an unlimited number of holes through the surface or coating of a dosage form, at rates up to 100,000 units or more per hour.
    Type: Grant
    Filed: July 7, 1992
    Date of Patent: December 27, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Stephen Roy
  • 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.