Substituted caprolactam derivatives as antihypertensives

Claim 2

A compound of the formula: ##STR8## wherein: R 1 is hydrogen, loweralkyl, unsubstituted cycloalkyl having 3 to 10 carbon atoms, amino loweralkyl, alkylamino loweralkyl, hydroxyalkyl, dialkylamino loweralkyl, arloweralkyl, aryl, substituted aryl wherein the substituent is halo, alkyl, aminoalkyl, or alkoxy; R 2 is hydrogen or loweralkyl; R 3 is hydroxyl, loweralkoxy, or aralkyloxy; R 4 is hydrogen or loweralkanoyl; and, the pharmaceutically acceptable salts thereof: wherein in said R 1 , R 2 , R 3 and R 4 groups, said alkyl groups have 1 to 12 carbon atoms; said loweralkyl groups have 1 to 8 carbon atoms; said aryl and said ar prefix denote unsubstituted aromatic ring(s) having 6 to 12 carbon atoms.

Claim 3

A compound of claim 1 in which R 1 is hydrogen, loweralkyl, aminoloweralkyl, or aryl; R 2 is hydrogen or loweralkyl; R 3 is hydroxyl, or loweralkoxy; and, R 4 is hydrogen or loweralkanoyl.

Claim 4

A compound of claim 2 which is 1-carboxymethyl-3-mercaptomethylperhydroazepin-2-one.

Claim 5

The compound of claim 2 which is 1-carboxymethyl-3-acetylmercaptomethylperhydroazepin-2-one.

Claim 6

A process for preparing compounds of the formula: ##STR9## wherein R 1 is hydrogen, loweralkyl, unsubstituted cycloalkyl having 3 to 10 carbon atoms, amino loweralkyl, alkylamino loweralkyl, hydroxyalkyl, dialkylamino loweralkyl, arloweralkyl, aryl, substituted aryl wherein the substituent is halo, alkyl, aminoalkyl, or alkoxy; R 2 is hydrogen or loweralkyl; R 3 is hydroxyl, loweralkoxy, or aralkyloxy; R 4 is hydrogen or loweralkanoyl, wherein in said R 1 , R 2 , R 3 and R 4 groups, said alkyl groups have 1 to 12 carbon atoms; said loweralkyl groups have 1 to 8 carbon atoms; said aryl and said ar prefix denote unsubstituted aromatic ring(s) having 6 to 12 carbon atoms which process comprises treating a compound having the structure: ##STR10## wherein R 1 , R 2 and R 3 are as defined above and R 4 is loweralkanoyl, followed by removal of protecting groups, if necessary, to yield the desired product and, if desired, isolating the biologically more active isomer by chromatography, fractional crystallization, or by resolution with an appropriate, optically active base and, if desired, preparing a salt of the desired product by conventional means.

Claim 7

A process for preparing compounds of the formula: ##STR9## wherein R 1 is hydrogen, loweralkyl, unsubstituted cycloalkyl having 3 to 10 carbon atoms, amino loweralkyl, alkylamino loweralkyl, hydroxyalkyl, dialkylamino loweralkyl, arloweralkyl, aryl, substituted aryl wherein the substituent is halo, alkyl, aminoalkyl, or alkoxy; R 2 is hydrogen or loweralkyl; R 3 is hydroxyl, loweralkoxy, or aralkyloxy; R 4 is hydrogen or loweralkanoyl, wherein in said R 1 , R 2 , R 3 and R 4 groups, said alkyl groups have 1 to 12 carbon atoms; said loweralkyl groups have 1 to 8 carbon atoms; said aryl and said ar prefix denote unsubstituted aromatic ring(s) having 6 to 12 carbon atoms which process comprises treating a compound having the structure: ##STR10## wherein R 1 , R 2 and R 3 are as defined above and R 4 is loweralkanoyl, followed by removal of protecting groups, if necessary, to yield the desired product and, if desired, isolating the biologically more active isomer by chromatography, fractional crystallization, or by resolution with an appropriate, optically active base and, if desired, preparing a salt of the desired product by conventional means.

Claim 8

The process of claim 5 wherein in the formula I compounds R 1 is hydrogen, loweralkyl, aminoloweralkyl, or aryl; R 2 is hydrogen or loweralkyl; R 3 is hydroxyl or loweralkoxy; and, R 4 is hydrogen or lower alkanoyl.

Claim 9

The compound: ##STR11## wherein R 1 , R 2 and R 3 are as defined in claim 1.

Claim 10

The compound: ##STR12## and the corresponding carboxylic acid thereof.

Claim 11

The compound: ##STR12## and the corresponding carboxylic acid thereof.