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Claims for Patent: 5,583,122

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Claims for Patent: 5,583,122

Title: Pharmaceutical compositions containing geminal diphosphonates
Abstract:Pharmaceutical compositions, useful for treating abnormal calcium and phosphate metabolism, which contain geminal-diphosphonic acid compounds; and a method of treating diseases characterized by abnormal calcium and phosphate metabolism utilizing these pharmaceutical compositions.
Inventor(s): Benedict; James J. (Norwich, NY), Perkins; Christopher M. (Cincinnati, OH)
Assignee: The Procter & Gamble Company (Cincinnati, OH)
Application Number:06/806,155
Patent Claims: 1. A diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure: ##STR6## wherein Z is a pyridine ring; R.sub.1 is hydrogen substituted or unsubstituted amino, amido, hydroxy, C.sub.1 -C.sub.6 alkoxy, halogen, carboxylate, a substituted or unsubstituted, a 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; and wherein said substituted R.sub.1, R.sub.2, R.sub.3 and R.sub.4 groups are independently substituted with methyl, ethyl, amino, chloro, nitro, methoxy, hydroxy, acetamido, or acetate.

2. 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.

3. 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.

4. A diphosphonic and acid compound, or pharmaceutically-acceptable salt or ester thereof, which is 2-(3-pyridyl)-1-hydroxyethane diphosphonic acid.

5. 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.

6. 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.

7. A pharmaceutical composition according to claim 5, wherein m+n=0.

8. A pharmaceutical composition according to claim 6, wherein m+n=0.

9. A pharmaceutical composition according to claim 7, wherein said diphosphonic acid compound is of the formula: ##STR11## wherein R.sub.1 is hydrogen; R.sub.3 is hydrogen, methyl, amino, chloro, methoxy, nitro, or hydroxy; and R.sub.4 is hydrogen, methyl, or ethyl.

10. A pharmaceutical composition according to claim 8, wherein said diphosphonic acid compound is of the formula: ##STR12## wherein R.sub.1 is hydrogen, and R.sub.3 is hydrogen, methyl, amino, chloro, methoxy, nitro, or hydroxy.

11. 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.

12. A pharmaceutical composition according to claim 11, wherein n=1.

13. A pharmaceutical composition according to claim 11, wherein said diphosphonic acid compound is of the formula: ##STR14## wherein n=0 or 1; R.sub.1 is hydrogen, chloro, amino, or hydroxy; and R.sub.3 is hydrogen, methyl, amino, chloro, methoxy, hydroxy, or nitro.

14. A pharmaceutical composition according to claim 12, wherein said diphosphonic acid compound is selected from the group consisting of 2-(2-pyridyl)-ethane-1,1-diphosphonic acid; 2-(3-pyridyl)-ethane-1,1-diphosphonic acid; 2-(4-pyridyl)-ethane-1,1-diphosphonic acid; 2-(2-pyridyl)-hydroxyethane-1,1-diphosphonic acid; 2-(3-pyridyl)-hydroxyethane-1,1-diphosphonic acid; and 2-(4-pyridyl)-hydroxyethane-1,1-diphosphonic acid.

15. A pharmaceutical composition according to claim 14, wherein said diphosphonic acid compound is 2-(2-pyridyl)-ethane-1,1-diphosphonic acid.

16. A pharmaceutical composition according to claim 14, wherein said diphosphonic acid compound is 2-(3-pyridyl)-hydroxyethane diphosphonic acid.

17. A method of treating diseases associated with abnormal calcium and phosphate metabolism, comprising administering to a person in need of such treatment a safe and effective amount of a composition of claim 5.

18. A method of treating diseases associated with abnormal calcium and phosphate metabolism, comprising administering to a person in need of such treatment a safe and effective amount of a composition of claim 6.

19. A method of treating diseases associated with abnormal calcium and phosphate metabolism, comprising administering to a person in need of such treatment a safe and effective amount of a composition of claim 7.

20. A method of treating diseases associated with abnormal calcium and phosphate metabolism, comprising administering to a person in need of such treatment a safe and effective amount of a composition of claim 12.

21. A method of treating diseases associated with abnormal calcium and phosphate metabolism, comprising administering to a person in need of such treatment a safe and effective amount of a composition of claim 14.

22. A method of treating diseases associated with abnormal calcium and phosphate metabolism, comprising administering to a person in need of such treatment a safe and effective amount of a composition of claim 15.

23. A method of treating diseases associated with abnormal calcium and phosphate metabolism, comprising administering to a person in need of such treatment a safe and effective amount of a composition of claim 16.
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