Patents Represented by Attorney H. J. Pfeiffer
  • Patent number: 4940520
    Abstract: The 4-acyloxyazetidin-2-ones, which are intermediates in the production of carbapenems and penems, are produced from 4-furanylazetidin-2-ones by singlet oxygen oxidation.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: July 10, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Joseph E. Lynch, William L. Laswell, Ralph P. Volante, Ichiro Shinkai
  • Patent number: 4772622
    Abstract: Novel diamino oxadiazoles, wherein one of the amine functions is connected to a basicly-substituted heterocyclic group through a linear or cyclic connecting group, which are useful for the suppression of gastric acid secretions in mammals. Compositions employing these compounds and processes for the preparation of such compounds from known N-cyano-S-methylisothiourea precursors by treatment with hydroxylamine and for alkylation of amine groups are also disclosed.
    Type: Grant
    Filed: June 16, 1986
    Date of Patent: September 20, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Susan F. Britcher, William C. Lumma, Jr.
  • Patent number: 4755508
    Abstract: Benzodiazepines of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: July 5, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger
  • Patent number: 4731369
    Abstract: Amides and esters of 2-[N-(hydroxypiperidinoalkyl) and (hydroxypyrrolidinoalkyl) aminosulfonyl]-6-nitrobenzoic acids are disclosed to have activity in increasing the sensitivity of hypoxic tumor cells to therapeutic radiation. Also disclosed are methods of preparing such compounds, pharmaceutical compositions including such compounds and methods of treating patients in need of therapeutic radiation with effective amounts of such compounds.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: March 15, 1988
    Assignee: Merck & Co. Inc.
    Inventors: Edward L. Engelhardt, Walfred S. Saari
  • Patent number: 4663307
    Abstract: Novel 6H-dibenz[b,e][1,4]oxathiepin derivatives of the Formulae I and IA are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: October 1, 1984
    Date of Patent: May 5, 1987
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Joshua Rokach, Pierre Hamel
  • Patent number: 4634717
    Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.
    Type: Grant
    Filed: May 1, 1984
    Date of Patent: January 6, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • Patent number: 4622403
    Abstract: Novel dibenz[b,f]thiepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: October 11, 1983
    Date of Patent: November 11, 1986
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Haydn Williams, Joshua Rokach
  • Patent number: 4536507
    Abstract: Prostaglandin antagonists are disclosed which are 7- and 8-substituted-dizenzo[b,f]thiepins of the structural formula: ##STR1##
    Type: Grant
    Filed: July 8, 1982
    Date of Patent: August 20, 1985
    Assignees: Merck & Co., Inc., Merck Frosst Canada, Inc.
    Inventors: Joshua Rokach, Clarence S. Rooney, Edward J. Cragoe, Jr.
  • Patent number: 4424355
    Abstract: The present invention is concerned with an improved process for the production of highly active optical isomers of (-) 7 or 8 fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide having the structural formula ##STR1## in which the fluoro substituent replaces a hydrogen in the 7 or 8 position. The two active isomers represented by formula II are S(-)7-fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide and R(-)8-fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide. It is especially concerned with the resolution of the racemic 7 or 8 fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide by first forming and separating diastereomers of said racemic carboxylic acids by salt formation with brucine or ephedrine followed by crystallization and regeneration of the desired (-) isomers and recycling of the (+) isomer by racemization of the regenerated isomer.
    Type: Grant
    Filed: February 24, 1982
    Date of Patent: January 3, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Haydn W. R. Williams, Joshua Rokach
  • Patent number: 4376774
    Abstract: This invention relates to a new class of thienamycins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter referred to as R'): ##STR2## attached to the amino nitrogen group of thienamycin represents a mono- or polycyclic N-containing heterocyclic group; R is, inter alia, hydrogen, substituted and unsubstituted: alkyl, aryl, alkenyl, heterocyclylalkenyl, aralkenyl, heterocyclylalkyl, aralkyl, --NR.sub.2, COOR, CONR.sub.2, --OR, or CN.
    Type: Grant
    Filed: May 29, 1979
    Date of Patent: March 15, 1983
    Assignee: Merck & Co., Inc.
    Inventor: John Hannah