Patents Assigned to Merck & Co.
  • Hypocholesteremic fermentation products
    Patent number: 4342767
    Abstract: Substances isolated after cultivation of a microorganism belonging to the genus Aspergillus in a culture medium comprise compounds which have structures: ##STR1## Together with salts and esters of the carboxylic acid, these compounds form a class of highly active hypocholesteremic and hypolipemic medicaments.
    Type: Grant
    Filed: June 16, 1980
    Date of Patent: August 3, 1982
    Assignee: Merck & Co., Inc.
    Inventors: George Albers-Schonberg, Richard L. Monaghan, Alfred W. Alberts, Carl H. Hoffman
  • Allylsulfoxide enzyme inhibitors
    Patent number: 4342758
    Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.
    Type: Grant
    Filed: May 7, 1980
    Date of Patent: August 3, 1982
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • 6-, 2- and 1,1-Disubstituted-1-carbadethiapen-2-em-3-carboxylic acid S-oxides
    Patent number: 4341791
    Abstract: Disclosed are S-oxides of 6-, 2- and 1,1-disubstituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; and R.sup.1, R.sup.2, R.sup.6, R.sup.7 and R.sup.8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
    Type: Grant
    Filed: October 10, 1980
    Date of Patent: July 27, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, David H. Shih
  • Derivatives of 2-hydroxy-6,9-methano-11-amino-5,6,7,8,9,10-hexahydro-benzocyclooctene
    Patent number: 4341904
    Abstract: Novel amino derivatives of 2-hydroxy-6,9-methano-11-amino-5,6,7,8,9,10-hexahydro-benzocyclooctenes, methods for their preparation, and their use as effective analgesic agents is described.
    Type: Grant
    Filed: February 19, 1980
    Date of Patent: July 27, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Robert N. Young
  • Process for the preparation of carbapenem antibiotics
    Patent number: 4341706
    Abstract: Disclosed is a process for the synthesis of carbapenem antibiotics I and their pharmaceutically acceptable salts and esters from 1: ##STR1## wherein: R.sup.7, R.sup.6, R.sup.1, R.sup.2 and R.sup.8 are selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, spirocycloalkyl, cycloalkylalkyl, alkylcycloalkyl, aryl, aralkyl, aralkenyl, aralkynyl, heteroalkyl, heteroaralkyl, heterocyclyl and heterocyclyalkyl.
    Type: Grant
    Filed: October 10, 1980
    Date of Patent: July 27, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, David H. Shih
  • Thienamycin derivatives
    Patent number: 4341705
    Abstract: Disclosed is a process for the total synthesis of thienamycin from descysteaminylthinamycin 1 ##STR1## via thienamycin sulfoxide 4: ##STR2## R.sup.3, R.degree., R' are blocking groups.
    Type: Grant
    Filed: October 10, 1980
    Date of Patent: July 27, 1982
    Assignee: Merck & Co., Inc.
    Inventor: David H. Shih
  • Polyamine compounds as antibacterial agents
    Patent number: 4340756
    Abstract: Novel halophenyl and loweralkyl substituted halophenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like.
    Type: Grant
    Filed: February 4, 1981
    Date of Patent: July 20, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
  • Process of producing modified glucans as anti-caries agent
    Patent number: 4340673
    Abstract: Certain glucans modify the biosynthetic route of extracellular polysaccharides involved in dental plaque development causing critical loss of adhesiveness. They interfere with the biosynthesis of cell-bound polysaccharides reducing and preventing agglutination of cells. They thus aid in the prevention of dental plaque formation or concomitant dental caries and periodontal disease.
    Type: Grant
    Filed: November 7, 1980
    Date of Patent: July 20, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Thomas H. Stoudt, Karl H. Nollstadt
  • Antimicrobial aminopyrimidinium salts
    Patent number: 4339453
    Abstract: 4-Amino- and 2,4-diaminopyrimidines with a quaternized ring nitrogen and an oxygen bearing substituent such as hydroxyalkyl, alkoxyalkyl, or alkanoyl on one of the exo- or endocyclic nitrogens and a C.sub.6-18 alkyl on another, are highly active antimicrobial agents with a relatively low acute mammalian toxicity.
    Type: Grant
    Filed: July 23, 1979
    Date of Patent: July 13, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Elbert E. Harris, Henry Joshua, Arthur A. Patchett, Bruce E. Witzel, Richard A. Dybas
  • Use of heteropolysaccharide S-119 as an antimigrant
    Patent number: 4339239
    Abstract: S-119 is used for the control of migration during pad dyeing of fabrics.
    Type: Grant
    Filed: June 20, 1980
    Date of Patent: July 13, 1982
    Assignee: Merck & Co., Inc.
    Inventor: Joseph S. Racciato
  • Vaccine stabilizer containing L-glutamic acid and L-arginine
    Patent number: 4338335
    Abstract: An improved stabilized liquid live viral vaccine contains a live virus, partially hydrolyzed gelatin, a monosaccharide or disaccharide, a cell culture medium, L-glutamic acid, L-arginine and sufficient physiologically acceptable acidic buffer to maintain the pH at from about 6.0 to about 6.5.
    Type: Grant
    Filed: July 30, 1980
    Date of Patent: July 6, 1982
    Assignee: Merck & Co., Inc.
    Inventors: William J. McAleer, Henry Z. Markus
  • Cephalosporin antibiotics
    Patent number: 4338437
    Abstract: Process and intermediate products useful in the preparation of cephalosporin compounds having a substituent at the 7-position in place of hydrogen are provided. The new cephalosporin compounds are active against various gram-negative and gram-positive organisms.
    Type: Grant
    Filed: April 30, 1980
    Date of Patent: July 6, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Sandor Karady, Lovji D. Cama, Meyer Sletzinger
  • Novel process and intermediates useful in the preparation of sympathomimetic amines
    Patent number: 4338455
    Abstract: The invention relates to a novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protected aromatic amine; and removing the N-protecting group therefrom.
    Type: Grant
    Filed: February 11, 1981
    Date of Patent: July 6, 1982
    Assignee: Merck & Co., Inc.
    Inventor: Jacob A. Zupan
  • Cephalosporin antibiotics
    Patent number: 4338438
    Abstract: Process and intermediate products useful in the preparation of cephalosporin compounds having a substituent at the 7-position in place of hydrogen are provided. The new cephalosporin compounds are active against various gram-negative and gram-positive organisms.
    Type: Grant
    Filed: April 30, 1980
    Date of Patent: July 6, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Sandor Karady, Lovji D. Cama, Meyer Sletzinger
  • 1-[4-(4-Sulfanilyl)phenyl] urea and derivatives in compositions and methods of treating rheumatoid arthritis and immune complex diseases
    Patent number: 4338334
    Abstract: The invention relates to 1-[4-(4-sulfanilyl)phenyl] urea and derivatives thereof in pharmaceutical compositions and in methods of treating rheumatoid arthritis and immune complex diseases such as dermatitis herpetiformis.
    Type: Grant
    Filed: February 29, 1980
    Date of Patent: July 6, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Norman P. Jensen, David P. Jacobus, Howard Jones
  • Vaccine stabilizer containing L-glutamic acid and L-arginine
    Patent number: 4337242
    Abstract: An improved stabilized liquid live viral vaccine contains a live virus, partially hydrolyzed gelatin, a monosaccharide or disaccharide, a cell culture medium, L-glutamic acid, L-arginine and sufficient physiologically acceptable acidic buffer to maintain the pH at from about 6.0 to about 6.5.
    Type: Grant
    Filed: March 10, 1981
    Date of Patent: June 29, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Henry Z. Markus, William J. McAleer
  • Process for preparing methylvanillyl ketone from isoeugenol
    Patent number: 4337360
    Abstract: Methylvanillyl ketone is prepared from a "through process" involving oxidation of isoeugenol followed by subsequent acidic hydrolysis.
    Type: Grant
    Filed: September 28, 1979
    Date of Patent: June 29, 1982
    Assignee: Merck & Co., Inc.
    Inventor: Meyer Sletzinger
  • [(5,6,9a-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkano ic and cycloalkanoic acids, their analogs, esters, salts, and derivatives
    Patent number: 4337354
    Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acid and their analogs, esters, salts and derivatives. 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 in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
    Type: Grant
    Filed: February 19, 1981
    Date of Patent: June 29, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
  • 2,4-Dioxo-4-substituted-1-butanoic acid derivatives useful in treating urinary tract calcium oxalate lithiasis
    Patent number: 4337258
    Abstract: 2,4-Dioxo-4-substituted-1-butanoic acid derivatives of the formula: ##STR1## where R is hydrogen or C.sub.1-4 alkyl; andL is a lipophilic group consisting essentially of(1) ##STR2## where R' is (a) hydrogen; (b) C.sub.1-3 alkyl; (c) benzyl; (d) pyridyl C.sub.1-3 alkyl; or (e) (3,4-dihydro-3-hydroxy-2H-1,5-benzodioxepin-3-yl) methyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted; or(2) ##STR3## where R' has the same meaning as above; or a pharmaceutically acceptable salt thereof; useful in treating urinary tract, especially renal calcium oxalate lithiasis.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: June 29, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Clarence S. Rooney, Haydn W. R. Williams, Edward J. Cragoe, Jr., Arthur A. Patchett
  • 2,4-Dioxo-4-substituted-1-butanoic acid derivatives useful in treating urinary tract calcium oxalate lithiasis
    Patent number: 4336397
    Abstract: 2,4-Dioxo-4-substituted-1-butanoic acid derivatives of the formula: ##STR1## where R is hydrogen or C.sub.1-4 alkyl; andL is a lipophilic group consisting essentially of: ##STR2## where R.sup.1 and R.sup.2 are each independently selected from the group consisting of (a) hydrogen; (b) C.sub.4-12 straight or branched chain alkyl; (c) C.sub.4-7 cycloalkyl; and (d) tetrahydronaphthyl; provided that R.sup.1 and R.sup.2 may not both be hydrogen; and when one of R.sup.1 or R.sup.2 is tetrahydronaphthyl, the other must be some other substituent; and that positions 2 and 6 of the substituted phenyl moiety may not be substituted; and ##STR3## where R.sup.1, and R.sup.2 have the same meaning as above except tetrahydronaphthyl;R.sup.3 is bromine, chlorine, or fluorine;m is 0 to 3;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: June 22, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Arthur A. Patchett, Clarence S. Rooney, Haydn W. R. Williams