Antihypertensive phosphate derivatives

A method of treating hypertension in a warm-blooded animal which comprises administering to said animal an effective amount of a compound, including the individual R and S enantiomers and racemic mixture, represented by the formula:

• ##STR18## wherein n is an integer 1 or 2;
• m is an integer 1 or 2, and the sum of n and m must be 3;
• X is selected from n-hexadecyloxy, n-heptadecyloxy, n-octadecyloxy, n-pentadecyloxy, 4-tetradecylphenoxy, 3-tetradecylphenoxy, 2-tetradecylphenoxy, 3-tridecylphenoxy and 3-dodecyloxy-2-methyl phenoxy;
• and T is selected from hydrogen and acetyl.

A method of treating hypertension in a warm-blooded animal which comprises administering to said animal an effective amount of a compound, including the individual R and S enantiomers and racemic mixture, represented by the formula:

• ##STR19## wherein n is an integer 1 or 2;
• m is an integer 1 or 2, and the sum of n and m must be 3;
• X is selected from C.sub.11 -C.sub.19 alkoxy and substituted phenoxy wherein the substituents are selected from one or more of C.sub.1 -C.sub.19 alkyl and C.sub.11 -C.sub.15 alkoxy;
• T is selected from hydrogen and ##STR20## wherein R.sub.1 is selected from hydrogen and C.sub.1 -C.sub.4 alkyl;
• Q is a bivalent radical selected from --(CH.sub.2).sub.p --, wherein p is an integer from 2 to 5, and --(CHR).sub.p --, wherein p is an integer from 2 to 5 and R is methyl or phenyl;
• and Z is selected from ##STR21## wherein R.sub.2 may be the same or different and is selected from hydrogen and C.sub.1 -C.sub.4 alkyl and q is an integer from 4 to 7.

A pharmaceutical composition of matter in dosage unit form comprising a compound, including the individual R and S enantiomers and racemic mixture, represented by the formula:

• ##STR22## wherein n is an integer 1 or 2;
• m is an integer 1 or 2, and the sum of n and m must be 3;
• X is selected from the group consisting of C.sub.1 -C.sub.24 branched or straight chain alkoxy and substituted phenoxy wherein the substituents are selected from one or more of the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, phenyl and substituted phenyl;
• T is selected from the group consisting of hydrogen and ##STR23## wherein R.sub.1 is selected from this group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino;
• Q is a bivalent radical selected from the group consisting of --(CH.sub.2).sub.p -- and --(CHR).sub.p --, where p is an integer from 2 to 12 and the moiety --(CHR).sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups;
• and Z is selected from the group consisting of ##STR24## wherein R.sub.2 may be the same or different and is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 branched or straight chain alkyl and q is an integer from 4 to 7;
• in association with a pharmaceutically acceptable carrier.

A pharmaceutical composition of matter in dosage unit form comprising a compound, including the individual R and S enantiomers and racemic mixture in association with a pharmaceutically acceptable carrier, wherein said compound is represented by the formula:

• ##STR25## wherein n is an integer 1 or 2;
• m is an integer 1 or 2, and the sum of n and m must be 3;
• X is selected from n-hexadecyloxy, n-heptadecyloxy, n-octadecyloxy, n-pentadecyloxy, 4-tetradecylphenoxy, 3-tetradecylphenoxy, 2-tetradecylphenoxy, 3-tridecylphenoxy and 3-dodecyloxy-2-methyl phenoxy;
• and T is selected from hydrogen and acetyl.

A pharmaceutical composition of matter in dosage unit form comprising a compound, including the individual R and S enantiomers and racemic mixture, in association with a pharmaceutically acceptable carrier, wherein said compound is represented by the formula:

• ##STR26## wherein n is an integer 1 or 2;
• m is an integer 1 or 2, and the sum of n and m must be 3;
• X is selected from C.sub.11 -C.sub.19 alkoxy and substituted phenoxy wherein the substituents are selected from one or more of C.sub.1 -C.sub.19 alkyl and C.sub.11 -C.sub.15 alkoxy;
• T is selected from hydrogen and ##STR27## wherein R.sub.1 is selected from hydrogen and C.sub.1 -C.sub.4 alkyl;
• Q is a bivalent radical selected from --(CH.sub.2).sub.p --, wherein p is integer from 2 to 5 and --(CHR).sub.p --, wherein p is an integer from 2 to 5 and R is methyl or phenyl;
• and Z is selected from ##STR28## wherein R.sub.2 may be the same or different and is selected from hydrogen and C.sub.1 -C.sub.4 alkyl and q is an integer from 4 to 7.

Compounds, including the individual R and S enantiomers and the racemic mixtures, represented by the formula:

• ##STR29## wherein n is an integer 1 or 2;
• m is an integer 1 or 2, and the sum of n and m must be 3;
• X is selected from the group consisting of C.sub.1 -C.sub.24 branched or straight chain alkoxy and substituted phenoxy wherein the substituents are selected from one or more of the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, phenyl and substituted phenyl;
• t is selected from the group consisting of hydrogen and ##STR30## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino;
• Q is a bivalent radical selected from the group consisting of --(CH.sub.2).sub.p -- and --(CHR).sub.p --, where p is an integer from 2 to 12 and the moiety --(CHR).sub.p --, represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups;
• and Z is selected from the group consisting of .sub.-.sup.+N(R.sub.2).sub.3 and ##STR31## wherein R.sub.2 may be the same or different and is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 branched or straight chain alkyl and q is an integer from 4 to 7.

Compounds, including the individual R and S enantiomers and the racemic mixture, represented by the formula:

• ##STR35## wherein n is an integer 1 or 2;
• m is an integer 1 or 2, and the sum of n and m must be 3;
• X is selected from n-hexadecyloxy, n-heptadecyloxy, n-octadecyloxy, n-pentadecyloxy, 4-tetradecylphenoxy, 3-tetradecylphenoxy, 2-tetradecylphenoxy, 3-tridecylphenoxy and 3-dodecyloxy-2-methyl phenoxy;
• and T is selected from hydrogen and acetyl.

Compounds, including the individual R and S enantiomers and the racemic mixtures, represented by the formula:

• ##STR36## wherein n is an integer 1 or 2;
• m is an integer 1 or 2, and the sum of n and m must be 3;
• X is selected from C.sub.11 -C.sub.19 alkoxy and substituted phenoxy wherein the substituents are selected from one or more of C.sub.1 -C.sub.19 alkyl and C.sub.11 -C.sub.15 alkoxy;
• T is selected from hydrogen and ##STR37## wherein R.sub.1 is selected from hydrogen and C.sub.1 -C.sub.4 alkyl;
• Q is a bivalent radical selected from --(CH.sub.2).sub.p --, wherein p is an integer from 2 to 5, and --(CHR).sub.p --, wherein p is an integer from 2 to 5 and R is methyl or phenyl;
• and Z is selected from ##STR38## wherein R.sub.2 may be the same or different and is selected from hydrogen and C.sub.1 -C.sub.4 alkyl and q is an integer from 4 to 7.