Pharmaceutical compositions containing geminal diphosphonates

A diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure:

• ##STR7## wherein Z is a pyridine ring;
• n is 0 or 1;
• R.sub.2 is hydrogen, or a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms;
• and R.sub.3 is hydrogen, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted benzyl, hydroxy, halogen, C.sub.1 -C.sub.6 alkoxy, amino, substituted amino, substituted or unsubstituted phenyl, substituted or unsubstituted naphthyl, carbonyl, nitro, amido, or carboxylate;
• and wherein said substituted R.sub.2 and R.sub.3 groups are independently substituted with methyl, ethyl, amino, chloro, nitro, methoxy, hydroxy, acetamido, or acetate.

A diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure:

• ##STR8## wherein Z is a pyridine ring n is 1;
• R.sub.2 is hydrogen, or a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms;
• and R.sub.3 is hydrogen, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted benzyl, hydroxy, halogen, C.sub.1 -C.sub.6 alkoxy, amino, substituted amino, substituted or unsubstituted phenyl, substituted or unsubstituted naphthyl, carbonyl, nitro, amido, or carboxylate;
• and wherein said substituted R.sub.2 and R.sub.3 groups are independently substituted with methyl, ethyl, amino, chloro, nitro, methoxy, hydroxy, acetamido, or acetate.

A pharmaceutical composition comprising:

• (a) a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, at a level providing from 0.001 to 600 mg of phosphorus in said composition, wherein said diphosphonic acid compound is of the formula:
• ##STR9## wherein Z is a pyridine ring;
• m+n is an integer from 0 to 5;
• R.sub.1 is hydrogen, substituted or unsubstituted amino, amido, hydroxy, C.sub.1 -C.sub.6 alkoxy, halogen, carboxylate, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl, except that when n=0, then R.sub.1 is hydrogen, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl;
• R.sub.2 is hydrogen, or a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms;
• R.sub.3 is hydrogen, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted benzyl, hydroxy, halogen, C.sub.1 -C.sub.6 alkoxy, amino, substituted amino, substituted or unsubstituted phenyl, substituted or unsubstituted naphthyl, carbonyl, nitro, amido, or carboxylate;
• and R.sub.4 is hydrogen, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms, or acetyl;
• (b) a pharmaceutically-acceptable carrier.

A pharmaceutical composition comprising:

• (a) a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, at a level providing from 0.001 to 600 mg of phosphorus in said composition, wherein said diphosphonic acid compound is of the formula:
• ##STR10## wherein Z is a pyridine ring;
• m+n is an integer from 0 to 5;
• R.sub.1 is hydrogen, substituted or unsubstituted amino, amido, hydroxy, C.sub.1 -C.sub.6 alkoxy, halogen, carboxylate, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl, except that when n=0, then R.sub.1 is hydrogen, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl;
• R.sub.2 is hydrogen, or a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms:
• and R.sub.3 is hydrogen, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted benzyl, hydroxy, halogen, C.sub.1 -C.sub.6 alkoxy, amino, substituted amino, substituted or unsubstituted phenyl, substituted or unsubstituted naphthyl, carbonyl, nitro, amido, or carboxylate;
• and
• (b) a pharmaceutically-acceptable carrier.

A pharmaceutical composition comprising:

• (a) a geminal diphosphonic acid compound or a pharmaceutically-acceptable salt or ester thereof, at a level providing from 0.001 to 600 milligrams phosphorus in said composition, wherein said compound is of the formula:
• ##STR13## wherein Z is a pyridine ring;
• n is 0 or 1;
• R.sub.1 is hydrogen, substituted or unsubstituted amino, amido, hydroxy, C.sub.1 -C.sub.6 alkoxy, halogen, carboxylate, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl;
• R.sub.2 is hydrogen, or a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms;
• and R.sub.3 is hydrogen, a substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted benzyl, hydroxy, halogen, C.sub.1 -C.sub.6 alkoxy, amino, substituted amino, substituted or unsubstituted phenyl, substituted or unsubstituted naphthyl, carbonyl, nitro, amido, or carboxylate;
• and wherein said substituted R.sub.1, R.sub.2 and R.sub.3 groups are independently substituted with methyl, ethyl, amino, chloro, nitro, methoxy, hydroxy, acetamido, or acetate;
• and
• (b) a pharmaceutically-acceptable carrier.