Abstract: A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6- membered carbocyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3,4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.

Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependent, neutral endopiptidase.

Abstract: A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.

Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.

Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.

Abstract: 1-(3- or 4-substituted piperidino)phthalazines of the formula ##STR1## wherein R is C.sub.1-6 alkyl; Y is a 3- or 4-position substituent and is --X-(CHR.sup.1).sub.m -Z wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; m is 1 or 2; X is oxygen or a direct link provided that when m is 1, X is a direct link; and Z is --N(R.sup.2)COR.sup.3, --N(R.sup.2)COOR.sup.3, --N(R.sup.2)SO.sub.2 R.sup.3, --N(R.sup.2)SO.sub.2 NR.sup.4 R.sup.5, --N(R.sup.2)SOR.sup.3, --N(R.sup.2)CONR.sup.4 R.sup.5 or --OCONR.sup.4 R.sup.5, wherein R.sup.2 and R.sup.5 are each independently hydrogen or C.sub.1-6 alkyl; R.sup.3 is C.sub.1-6 alkyl, phenethyl, benzyl, C.sub.3-7 cycloalkyl, phenyl or pyridyl; R.sup.4 is hydrogen or R.sup.3 ; provided that when X is a direct link, R.sup.3 or R.sup.4 is C.sub.3-7 cycloalkyl; the pharmaceutically acceptable acid addition salts thereof; processes for their preparation; and their use as cardiac stimulants and phosphodiesterase inhibitors.

Abstract: Derivates of L- and DL-hydroxyphenylglycines of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl, R.sup.1 is hydrogen, amino or alkoxy having from one to six carbon atoms and R.sup.2 is the residue of certain .alpha.-amino acids are useful in treating diseases and conditions which are characterized by reduced blood flow, oxygen availability or carbohydrate metabolism in the cardiovascular system. Derivatives of D-hydroxyphenylglycine of formula (II) are substantially inactive in treating such diseases and conditions.

Abstract: A series of 1-piperidinophthalazine derivatives as phosphodiesterase inhibitors and cardiac stimulants.

Abstract: Regulators of the cardiovascular system and, in particular, in the treatment of hypertension having the formula ##STR1## wherein R is lower alkyl;X, is a 3- or 4-position substituent and is --(CH.sub.2).sub.n CONR.sup.1 R.sup.2, --O(CH.sub.2).sub.n CONR.sup.1 R.sup.2 or ##STR2## wherein n is 0, 1 or 2;R.sup.1 is hydrogen or lower alkyl, andR.sup.2 is lower alkyl; lower alkenyl, lower alkynyl, phenyl, substituted phenyl, C.sub.3 -C.sub.7 cycloalkyl; lower alkyl substituted by phenyl, substituted phenyl, C.sub.3 -C.sub.7 cycloalkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, lower alkoxycarbonyl, phenoxy, substituted phenoxy or --NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl, lower alkanoyl or lower alkylsulfonyl; with the proviso that any O, N or halogen atom in R.sup.2 is separated by at least 2 carbon atoms from the nitrogen atom to which R.sup.2 is attached; orR.sup.1 and R.sup.

Abstract: The use of phenylglyoxylic acids and derivatives thereof in the treatment of ischemic heart disease and the hyperglycemia of diabetes.

Abstract: Regulators of the cardiovascular system and, in particular, in the treatment of hypertension having the formula ##STR1## pharmaceutically-acceptable bioprecursors thereof, and the pharmaceutically-acceptable acid addition salts thereof; wherein each of R.sup.1 and R.sup.2 is C.sub.1-4 alkyl or --CH.sub.2 CF.sub.3 ; alk is ethylene, monophenyl substituted ethylene, mono- and dimethyl substituted ethylene or monophenylmonomethyl substituted ethylene; and R.sup.3 is hydrogen, C.sub.1-4 alkyl, C.sub.3 -C.sub.6 cycloalkyl; phenyl or substituted phenyl; and methods for their preparation.

Abstract: The use of phenylglyoxylic acids and derivatives thereof in the treatment of ischemic heart disease and the hyperglycemia of diabetes.

Abstract: L- and DL-isomers of compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl; R.sup.1 is alkynyl, alkenyl or cycloalkyl, each having from three to seven carbon atoms or alkyl having from one to six carbon atoms which may optionally be substituted by one or more groups selected from hydroxy, alkoxy, carboxy, amino, monoalkylamino, dialkylamino, phenyl and phenoxy, any such phenyl or phenoxy being optionally substituted with one or more hydroxy, alkyl or alkoxy groups, said alkyl and alkoxy optional substituents having from one to six carbon atoms; provided that R.sup.1 is other than 4-hydroxy-.alpha.-carboxybenzyl or 4-methoxy-.alpha.-carboxybenzyl. Said compounds are useful in treating diseases and conditions characterized by reduced blood flow, oxygen availability or carbohydrate metabolism in the cardiovascular system. The D-isomers of the compounds of formula (II) are substantially inactive in treating such diseases and conditions.

Abstract: 6,7-Dialkoxy-4-[4-(substituted)piperidino]quinazolines wherein the 4-substituent is -(CHR.sup.1).sub.m -Z wherein R.sup.1 is hydrogen or lower alkyl; m is 1 or 2, with the proviso that when m is 2, each R.sup.1 can be the same or different; Z is -N(R.sup.2)COR.sup.3, -OCONR.sup.4 R.sup.5, N(R.sup.2)SO.sub.2 R.sup.3 or -N(R.sup.2)CONR.sup.4 R.sup.5 wherein R.sup.2 is hydrogen or lower alkyl; R.sup.3 is lower alkyl, benzyl or phenyl; and each of R.sup.4 and R.sup.5 is hydrogen or is selected from group R.sup.3 ; and methods for their preparation. The compounds are phosphodiesterase inhibitors and cardiac stimulants.

Abstract: L- and DL- Phenylglycines of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl and R.sup.1 is NH.sub.2, OH or completes a carboxylic ester group, useful in treating certain cardiovascular diseases, diabetes and obesity.

Abstract: L- and DL- Phenylglycines of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl and R.sup.1 is NH.sub.2, OH or completes a carboxylic ester group, useful in treating certain cardiovascular diseases, diabetes and obesity.

Abstract: L- and DL- Phenylglycines of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl and R.sup.1 is NH.sub.2, OH or completes a carboxylic ester group, useful in treating certain cardiovascular diseases, diabetes and obesity.

Abstract: L- and DL-Phenylglycines of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl and R.sup.1 is NH.sub.2, OH or completes a carboxylic ester group, useful in treating certain cardiovascular diseases, diabetes and obesity.

Abstract: L- and DL-Phenylglycines of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl and R.sup.1 is NH.sub.2, OH or completes a carboxylic ester group, useful in treating certain cardiovascular diseases, diabetes and obesity.

Abstract: L- and DL- Phenylglycines of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl and R.sup.1 is NH.sub.2, OH or completes a carboxylic ester group, useful in treating certain cardiovascular diseases, diabetes and obesity.