Abstract: Novel 4-(substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
Abstract: Novel N-(substituted) derivatives of 2-aza-2'-hydroxy-5,6-benzotricyclo[6.3.0.sup.1,8.0.sup.4,11 ] undecane of the formula: ##STR1## are centrally acting analgesics effective in the relief of pain.
Abstract: Compounds of the formula Het--O--CH.sub.2 --CHOR--CH.sub.2 -NHaralkyl where Het is a 10 membered N-containing ring are disclosed. The compounds are useful as pharmaceuticals.
Abstract: Heterocyclic ethanolamines of the formulaHet--CHOH--CH.sub.2 --NH--aralkylwhere het is a 10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals.
Abstract: 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro (or hydroxy) pyrazine with a 5-hydroxymethyl (or sulfonyloxymethyl) oxazolidine followed by acid hydrolysis.
Abstract: Compounds of the formula Het-O-CH.sub.2 -CHOR-CH.sub.2 -NH-aralkyl where Het is ##STR1## are disclosed. The compounds are useful as pharmaceuticals.
Abstract: Novel 3-hydroxymethyldibenzo[b,f]thiepin and derivatives are prepared and employed in the treatment and control of allergic conditions such as allergic asthma.
Abstract: 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro(or hydroxy)pyrazine with a 5-hydroxymethyl(or sulfonyloxymethyl)oxazolidine followed by acid hydrolysis.
Abstract: Novel 2-(4-substituted-1,2,5-thiadiazol-3-yloxy) acetaldehydes are disclosed. These acetaldehydes are useful as intermediates for preparing certain .beta.-adrenergic blocking agents.
Abstract: Novel 2-(4-substituted-1,2,5-thiadiazol-3-yloxy)acetaldehydes are disclosed. These acetaldehydes are useful as intermediates for preparing certain .beta.-adrenergic blocking agents.
Abstract: 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro(or hydroxy)pyrazine with a 5-hydroxy-methyl(or sulfonyloxymethyl)oxazolidine followed by acid hydrolysis.
Type:
Grant
Filed:
June 6, 1975
Date of Patent:
August 16, 1977
Assignee:
Merck Sharp & Dohme (I.A.) Corporation
Inventors:
Burton Kendall Wasson, Leonard M. Weinstock
Abstract: There is described 2-amino-5,7-disubstituted-naphthyridine and 5,7-disubstituted-naphthyridin-2(1H)-one derivatives with bronchodilating and hypotensive properties prepared by the reaction of 2,6-diaminopyridine with an appropriate .beta.-diketone providing the 2-amino products. The 2-oxo analogs are prepared from the 2-amino products by treatment with nitrous acid.
Type:
Grant
Filed:
December 9, 1975
Date of Patent:
June 21, 1977
Assignee:
Merck Sharp & Dohme (I.A.) Corporation
Inventors:
Hayden Windsor Richard Williams, Clarence Stanley Rooney
Abstract: 4-[3-(Substituted amino)-2-acyloxypropoxy]-1,2,5-thiadiazole compounds, optionally substituted in the 3-position of the thiadiazole nucleus which exhibit .beta.-adrenergic blocking properties and thus are useful in the management of angina pectoris are described. The products are prepared by reaction of a 4-[3-(substituted amino)-2-hydroxypropoxy]-1,2,5-thiadiazole with the appropriate anhydride. The reaction is run under acidic conditions when the amino nitrogen is protonated.
Abstract: Deuterated functional group-containing hydrocarbons prepared by treating the non-labelled substrate in the liquid state with deuterium gas in the presence of a Group VII or VIII metal catalyst with heating between ambient to 300.degree. C. The labelled compounds are especially useful in reaction mechanism studies, as tracers in separation process studies, in the investigation of the physical properties of labelled compounds and in other specialized research work.
Abstract: 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro(or hydroxy)pyrazine with a 5-hydroxy-methyl(or sulfonyloxymethyl)oxazolidine followed by acid hydrolysis.
Type:
Grant
Filed:
October 19, 1973
Date of Patent:
March 23, 1976
Assignee:
Merck Sharp & Dohme (I.A.) Corporation
Inventors:
Burton Kendall Wasson, Leonard M. Weinstock