Abstract: Novel derivatives of glycolic and glyoxylic acid are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate urolithiasis (calcium oxalate kidney and bladder stone disease).
Type:
Grant
Filed:
May 3, 1979
Date of Patent:
November 11, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Haydn W. R. Williams, Edward J. Cragoe, Jr., Clarence S. Rooney
Abstract: Substances isolated after cultivation of a microorganism belonging to the genus Aspergillus in a culture medium comprise a compound designated MSD803 which has the lactone structure: ##STR1## as well as its free hydroxy acid form. Together with salts and esters of the free acid form, these compounds form a class of highly active hypocholesteremic and hypolipemic medicaments.
Type:
Grant
Filed:
June 15, 1979
Date of Patent:
November 4, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Richard L. Monaghan, Alfred W. Alberts, Carl H. Hoffman, George Albers-Schonberg
Abstract: The invention relates to the hydrohalide salts of L-.alpha. -methyl-3,4-dihydroxyphenylalanine (methydopa). The method of preparing these and related compounds in the absence of water or other polar solvents is also shown.
Abstract: Organic chemical compounds based upon the naphthyridine molecule are disclosed which have potent gastric secretion inhibitory properties. The naphthyridinone is substituted with a substituted amino alkyl group at the 1-position, and variously substituted at the remaining positions. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
Type:
Grant
Filed:
October 23, 1978
Date of Patent:
October 21, 1980
Assignee:
Merck & Co., Inc.
Inventors:
William A. Bolhofer, Edward J. Cragoe, Jr., Jacob M. Hoffman, Jr.
Abstract: The invention disclosed herein relates to novel 1-deoxy-glycopyranosides, preferably 1-deoxy-D-mannopyranosides, having in the 1-position of the pyranoside ring an .omega.-aminoalkylthio, .omega.-aminoalkyloxy or .omega.-aminoalkanoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxy-glycopyranosides starting with the corresponding tetra-O-acetyl-glycopyranosyl bromide or amine. These .omega.-amino(alkylthio, alkyloxy or alkanoylamino)-1-deoxy-glycopyranosides, and in particular 1-[(6'-aminohexyl)thio or oxy]-1-deoxy-D-mannopyranosides, possess insulin-like activity.
Type:
Grant
Filed:
July 10, 1978
Date of Patent:
October 14, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Mitree M. Ponpipom, Robert L. Bugianesi, Philippe L. Durette, Howard M. Katzen, Tsung-Ying Shen
Abstract: Heterocyclic carbamates are disclosed which have potent gastric secretion inhibitory properties. The heterocyclic substituent is a pyridyl group or a 6-membered heterocycle with two nitrogen heteroatoms, which may be optionally substituted. Further substituents on the carbamate nitrogen and oxygen atoms are also disclosed. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
Abstract: The case involves novel pyrazinecarboxamide compounds and processes for preparing same. The pyrazinecarboxamides are eukalemic agents possessing diuretic and natriuretic properties.
Type:
Grant
Filed:
March 27, 1979
Date of Patent:
September 23, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Otto W. Woltersdorf, Jr., Susan J. deSolms
Abstract: There are disclosed novel compounds described as imidazole cyanoguanidines in which the imidazole moiety is connected to the cyanoguanidine moiety through a cyclic group which may optionally contain one or two alkylene linkages. The cyclic groups may be phenyl, cyclohexyl, thienyl and the like. Processes for the preparation of such compounds are also disclosed. The compounds are useful for the suppression of gastric acid secretion in mammals, and compositions for such uses are also disclosed.
Type:
Grant
Filed:
June 4, 1979
Date of Patent:
September 2, 1980
Assignee:
Merck & Co., Inc.
Inventors:
William A. Bolhofer, Edward J. Cragoe, Jr., Jacob M. Hoffman, Jr.
Abstract: Mercaptoalkylpyridines carrying an ethenyl or ethynyl substituent are prepared from known pyridine compounds, principally pyridoxine, by known chemical procedures, and are useful in the treatment of rheumatoid arthritis and related inflammatory diseases.
Type:
Grant
Filed:
February 7, 1979
Date of Patent:
August 12, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Tsung-Ying Shen, Howard Jones, Conrad P. Dorn
Abstract: Novel polymers having a linear backbone which is free from both branching and cross-linking, comprising quaternized nitrogen atoms linked to each other through trimethylene groups. By the term "linear backbone" is meant that the polymer has only acyclic groups, i.e. trimethylene, linking the nitrogen atoms in a single continuous chain; the polymer is free from "branching" when it has no repeating monomer units extending from the polymer backbone; and it is free from "cross-linking" when there is no joining of two linear backbones. These polymers are useful as antimicrobials, flocculating agents, antistatic agents, electroconductive agents for coating paper, chelating agents and bile acid binding agents, as well as in similar applications where their high charge to weight ratio and fully accessible nitrogen atoms can be employed. The polymers are obtained by the polymerization of dihydro-oxazine, reductive alkylation of the resulting polymer, followed by quaternization.
Type:
Grant
Filed:
April 11, 1979
Date of Patent:
August 12, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Arthur F. Wagner, Nathaniel Grier, Tsung-Ying Shen
Abstract: Adenine is prepared by heating hydrogen chloride and hydrogen cyanide in a mixture of phosphorus oxychloride and dichlorophosphoric acid as solvent in a sealed vessel or by heating N-dichloromethylformamidine hydrochloride or triazine hydrochloride in a mixture of phosphorus oxychloride and dichlorophorphoric acid.
Abstract: A process for preparing .alpha.-fluoromethyl amino acids from corresponding .alpha.-hydroxymethyl amino acids is disclosed. The process utilizes SF.sub.4 and BF.sub.3 or AlCl.sub.3 in HF to effect the fluorination.
Abstract: A method of treating hypertension by administration, to hypertensive patients, of an anti-hypertensive amount of certain tripeptides, is disclosed.
Abstract: Mercaptoalkylpyridines and various derivatives thereof have utility in the treatment of rheumatoid arthritis. The compounds useful in the method of treatment are generally prepared from known pyridine derivatives and, principally, from pyridoxine and related compounds.
Type:
Grant
Filed:
September 20, 1977
Date of Patent:
July 15, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Tsung-Ying Shen, Howard Jones, Dennis M. Mulvey, Conrad P. Dorn
Abstract: Symmetrically substituted pyromellic diimides are disclosed wherein the compounds are substituted with a variety of substituent groups. The symmetrically substituted compounds are useful for administration to ruminant animals to increase feed efficiency, shift volatile fatty acid production in the ruminant from acetate with an increase in the more energetically efficient propionate and butyrate and to suppress methane formation in the rumen. Compositions and methods of treatment utilizing said compounds as the active ingredient thereof are also disclosed.
Type:
Grant
Filed:
October 23, 1978
Date of Patent:
July 15, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Michael H. Fisher, Peter Kulsa, Bruce O. Linn
Abstract: The case involves novel N-pyrazinecarbonyl-N'-alkoxycarbonyl and N',N"-bis(alkoxycarbonyl)guanidines and processes for preparing same. The compounds are excellent eukalemic agents possessing diuretic and natriuretic properties.
Type:
Grant
Filed:
December 4, 1978
Date of Patent:
June 17, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Abstract: Novel derivatives of glycolic and glyoxylic acid are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate urolithiasis (calcium oxalate kidney and bladder stone disease).
Type:
Grant
Filed:
October 11, 1978
Date of Patent:
June 10, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Haydn W. R. Williams, Edward J. Cragoe, Jr., Clarence S. Rooney