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: 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
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:
June 3, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Arthur F. Wagner, Nathaniel Grier, Tsung-Ying Shen
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:
May 27, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Arthur F. Wagner, Nathaniel Grier, Tsung-Ting Shen
Abstract: Triazoles substituted at the 3 and 5 positions having an optional substituent in the 1 position are provided. Methods of preparing the novel substituted triazoles are described. The substituted triazoles are useful as anti-gout and anti-hyperuricemic agents. Compositions useful in the treatment of gout and hyperuricemia containing a substituted triazole as the active ingredient are also provided.
Abstract: Certain novel acyl saccharins and acyl 3-oxo-1,2-benzisothiazolines, their preparation, pharmaceutical compositions and novel methods of inhibiting elatase and treating emphysema are disclosed.
Type:
Grant
Filed:
August 20, 1975
Date of Patent:
March 25, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Dennis Mulvey, Howard Jones, Morris Zimmerman
Abstract: Bicyclic somatostatin analogs and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by a combination of the solid phase method and the solution method. These analogs have the property of inhibiting the release of insulin, glucagon and growth hormone in humans and animals. The compounds are particularly useful in the treatment of diabetes. Due to the bicyclic structure, these analogs are resistant to enzymatic metabolism and have a longer duration of activity.
Abstract: A novel salt of amiloride particularly amiloride citrate has been discovered. Because of its inherent insolubility and less bitter taste, it would lend itself to be more easily formulated into oral liquids, sustained release formulations and chewable tablets than would amiloride hydrochloride.
Abstract: 2,3-Dihydro-6,7-disubstituted-5-thienylmethyl or furylmethyl benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
Type:
Grant
Filed:
February 16, 1978
Date of Patent:
February 19, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., William F. Hoffman, Otto W. Woltersdorf, Jr.
Abstract: N-Alkyl and N-cycloalkyloxamic acid derivatives are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate urolithiasis (kidney and bladder stone disease).
Type:
Grant
Filed:
October 11, 1978
Date of Patent:
February 5, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Frederick C. Novello, Walfred S. Saari
Abstract: The invention disclosed herein relates to novel non-adhesive, free-flowing, pharmacologically acceptable compositions comprising ionene quaternary polymers effective as bile acid sequestrants, such as poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], adsorbed on a pulverulent, solid aggregate of large surface to mass ratio, such as fumed silicas and silica aerogels. It also relates to the novel process for preparing such adsorbate compositions which comprises forming a substantially, uniform suspension of the finely-divided solid aggregate in an aqueous solution of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], evaporatively removing the water from the suspension, and drying the adsorbate thus produced.
Abstract: Compositions containing substituted 1,2,5 thiadiazole .beta.-blocking agent and pyrazine and/or thiazide diuretic, and a method of treating hypertensive animals are disclosed.
Abstract: 2-Hydroxy-3-butynoic acid is disclosed which inhibits glycolic acid oxidase and thus is useful in the treatment and prevention of calcium oxalate urolithiasis (calcium oxylate kidney and bladder stone disease).
Type:
Grant
Filed:
October 11, 1978
Date of Patent:
December 11, 1979
Assignee:
Merck & Co., Inc.
Inventors:
Haydn W. R. Williams, Edward J. Cragoe, Jr., Clarence S. Rooney