Abstract: There are disclosed processes for preparing carboxyalkyl dipeptide derivatives and related compounds which are useful as angiotension converting enzyme (ACE) inhibitors and as antihypertensives and pharmaceutical compositions containing these carboxyalkyl dipeptide compounds in combination with another antihypertensive and/or diuretic compound.
Type:
Grant
Filed:
September 27, 1982
Date of Patent:
September 18, 1984
Assignee:
Merck & Co., Inc.
Inventors:
Elbert E. Harris, Arthur A. Patchett, Edward W. Tristram, Matthew J. Wyvratt
Abstract: A pharmaceutical composition is disclosed which comprises the combination of interphenylene 9-thia-11-oxo-12-aza prostanoic acid derivatives and carboxyalkyl dipeptide derivatives.
Abstract: Antihypertensive compound 176 is a natural product amino acid produced by cultivation of a Streptomyces species under controlled aerobic fermentation conditions. The product is also shown to inhibit angiotensin converting enzyme.
Abstract: Compounds of the formula Het--O--CH.sub.2 --CHOR--CH.sub.2 --NH-aralkyl where Het is a 10 membered N-containing ring are disclosed. The compounds are useful as pharmaceuticals.
Type:
Grant
Filed:
February 22, 1982
Date of Patent:
April 10, 1984
Assignee:
Merck & Co., Inc.
Inventors:
Joseph G. Atkinson, John J. Baldwin, David E. McClure
Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; or loweralkyl;R.sup.2 is hydroxyloweralkyl; (CH.sub.2).sub.n COOR.sup.a, where R.sup.a is hydrogen, loweralkyl, or benzyl; and n is 1 to 3;R.sup.1 and R.sup.2 are taken together with an oxygen or nitrogen atom to form morpholino, piperazinyl, or piperazinyl which is N-loweralkyl substituted; andR.sup.3 is hydrogen; straight or branched C.sub.1-8 alkyl, provided that when R.sup.3 is hydrogen or C.sub.
Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; or loweralkyl;R.sup.2 is (CH.sub.2).sub.n COOR.sup.3, where R.sup.3 is hydrogen, loweralkyl, or benzyl; and n is 1 to 3; andR.sup.1 and R.sup.2 are taken together with an oxygen or nitrogen atom to form morpholino, piperazinyl, or piperazinyl which is N-loweralkyl substituted; are useful in various agricultural and industrial areas.
Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; or loweralkyl;R.sup.2 is (CH.sub.2).sub.n COOR.sup.a, where R.sup.a is hydrogen, loweralkyl, or benzyl; and n is 1 to 3;R.sup.1 andR.sup.2 are taken together with an oxygen or nitrogen atom or form morpholino, piperazinyl, or piperazinyl which is N-loweralkyl substituted;R.sup.3 is hydrogen; straight or branched C.sub.1-8 alkyl; aryl; aryl substituted with up to two members selected from the group consisting of C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halo, and mono- or di-C.sub.
Abstract: Novel substituted imidazoles of the formula ##STR1## and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.
Abstract: There are disclosed novel substituted pyridopyrimidine compounds and processes for preparing such compounds. These compounds are useful as gastric secretion inhibitors in mammals.
Type:
Grant
Filed:
August 24, 1981
Date of Patent:
December 13, 1983
Assignee:
Merck & Co., Inc.
Inventors:
William A. Bolhofer, Edward J. Cragoe, Jacob M. Hoffman, Jr
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: There are disclosed substituted derivatives of amino alkane diols and related compounds as well as processes for the preparation of such compounds. These compounds are useful for the suppression of gastric acid secretions in mammals and compositions for such uses are also disclosed.
Abstract: Novel imidazopyridines, -pyrazines, -pyrimidines and -pyridazines having a 3-amino-2-OR-propoxy substituent, are disclosed. The compounds have .beta.-adrenergic blocking activity.