Claims for Patent: 3,683,080

Summary for Patent: 3,683,080

Title:	Compositions for inhibiting anomalous deposition and mobilization of calcium phosphate in animal tissue
Abstract:	Compositions for inhibiting anomalous deposition and mobilization of calcium phosphates in animal tissue, comprising an effective amount of certain polyphosphonates as herein defined, and a pharmaceutical carrier; and a method for treating or preventing conditions involving pathological calcification and hard tissue demineralization in an animal comprising administering to such animal said compositions.
Inventor(s):	Marion D Francis
Assignee:	Procter and Gamble Co
Application Number:	US68029A
Patent Claims:	2. The composition of claim 1 wherein the polyphosphonate is methanehydroxydiphosphonic acid or a pharmaceutically acceptable salt thereof. 3. The composition of claim 1 wherein the polyphosphonate is ethane-1-amino-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 4. The composition of claim 1 wherein the polyphosphonate is methanediphosphonic acid or a pharmaceutically acceptable salt thereof. 5. The composition of claim 1 wherein the polyphosphonate is ethane-1-hydroxy-1,1,2-triphosphonic acid or a pharmaceutically acceptable salt thereof. 6. The composition of claim 1 wherein the polyphosphonate is propane-1,2,3-triphosphonic acid or a pharmaceutically acceptable salt thereof. 7. The composition of claim 1 wherein the polyphosphonate is butane-1,2,3,4-tetraphosphonic acid or a pharmaceutically acceptable salt thereof. 8. The composition of claim 1 wherein the polyphosphonate is hexane-1,2,3,4,5,6-hexaphosphonic acid or a pharmaceutically acceptable salt thereof. 9. The composition of claim 1 wherein the polyphosphonate is methanephenylaminodiphosphonic acid or a pharmaceutically acceptable salt thereof. 10. The composition of claim 1 wherein the dosage unit form is adapted to oral administration. 11. The composition of claim 1 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt thereof. 12. The composition of claim 11 wherein the dosage unit form is adapted to oral administration and comprises from about 100 mg. to about 500 mg. of polyphosphonate. 13. The composition of claim 1 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 14. The composition of claim 13 wherein the dosage unit form is adapted to oral administration and comprises from about 100 mg. to about 500 mg. of polyphosphonate. 15. A method for inhibiting anomalous deposition or mobilization of calcium phosphates in animal tissue which comprises systemically administering to animals an effective but non-toxic amount of a polyphosphonate selected from the group consisting of wherein R1 and R2 are each hydrogen or CH2OH; n is an integer of from 3 to 10; R3 is hydrogen, alkyl containing from one to about 20 carbon atoms, alkenyl containing from two to about 20 carbon atoms, phenyl, naphthyl, phenylethenyl, benzyl, halogen, amino, substituted amino, -CH2COOH, -CH2PO3H2, -CH(PO3H2)(OH), or -CH2CH(PO3H2)2; R4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, -CH2COOH, -CH2PO3H2, or -CH2CH2PO3H2; and the pharmaceutically acceptable salts thereof, and a pharmaceutical carrier. 16. The method of claim 15 wherein the polyphosphonate is methanedichlorodiphosphonic acid. 17. The method of claim 15 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid. 18. The method of claim 15 wherein the polyphosphonate is methanehydroxydiphosphonic acid. 19. The method of claim 15 wherein the polyphosphonate is ethane-1-amino-1,1-diphosphonic acid. 20. The method of claim 15 wherein the polyphosphonate is methanediphosphonic acid. 21. The method of claim 15 wherein the polyphosphonate is ethane-1-hydroxy-1,1,1-triphosphonic acid. 22. The method of claim 15 wherein the polyphosphonate is propane-1,2,3-triphosphonic acid. 23. The method of claim 15 wherein the polyphosphonate is butane-1,2,3,4-tetraphosphonic acid. 24. The method of claim 15 wherein the polyphosphonate is hexane-1,2,3,4,5,6-hexaphosphonic acid. 25. The method of claim 15 wherein the polyphosphonate is methanephenylaminodiphosphonic acid. 26. An animal feed composition comprising (1) a minor proportion of a polyphosphonate selected from the group consisting of wherein R1 and R2 are each hydrogen or CH2OH; n is an integer from 3 to 10; R3 is hydrogen, alkyl containing from one to about 20 carbon atoms, alkenyl containing from two to about 20 carbon atoms, phenyl, naphthyl, phenylethenyl, benzyl, halogen, amino, substituted amino, -CH2COOH, -CH2PO3H2, -CH(PO3H2)(OH), or -CH2CH(PO3H2)2; R4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, -CH2COOH, -CH2PO3H2, or -CH2CH2PO3H2; and the pharmaceutically acceptable salts thereof, and (2) a major proportion of animal foodstuff. 27. The composition of claim 26 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt thereof. 28. The composition of claim 26 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 29. The composition of claim 26 wherein the polyphosphonate is methanehydroxydiphosphonic acid or a pharmaceutically acceptable salt thereof. 30. The composition of claim 26 wherein the polyphosphonate is ethane-1-amino-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 31. The composition of claim 26 wherein the polyphosphonate is methanediphosphonic acid or a pharmaceutically acceptable salt thereof. 32. The composition of claim 26 wherein the polyphosphonate is ethane-1-hydroxy-1,1,2-triphosphonic acid or a pharmaceutically acceptable salt thereof. 33. The composition of claim 26 wherein the polyphosphonate is propane-1,2,3-triphosphonic acid or a pharmaceutically acceptable salt thereof. 34. The composition of claim 26 wherein the polyphosphonate is butane-1,2,3,4-tetraphosphonic acid or a pharmaceutically acceptable salt thereof. 35. The composition of claim 26 wherein the polyphosphonate is hexane-1,2,3,4,5,6-hexaphosphonic acid or a pharmaceutically acceptable salt thereof. 36. The composition of claim 26 wherein the polyphosphonate is methanephenylaminodiphosphonic acid or a pharmaceutically acceptable salt thereof. 37. A method for treating Paget''s disease comprising sYstemically administering to an animal afflicted therewith an effective but non-toxic amount of a polyphosphonate selected from the group consisting of wherein R1 and R2 are each hydrogen or CH2OH; n is an integer of from 3 to 10; R3 is hydrogen, alkyl containing from one to about 20 carbon atoms, alkenyl containing from two to about 20 carbon atoms, phenyl, naphthyl, phenylethenyl, benzyl, halogen, amino, substituted amino, -CH2COOH, -CH2PO3H2, -CH(PO3H2)(OH), or -CH2CH(PO3H2)2; R4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, -CH2COOH, -CH2PO3H2, or -CH2CH2PO3H2; and the pharmaceutically acceptable salts thereof. 38. The method of claim 37 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 39. The method of claim 37 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt thereof. 40. A method for treating osteoporosis comprising administering to an animal afflicted therewith an effective but non-toxic amount of polyphosphonate selected from the group consisting of wherein R1 and R2 are each hydrogen or CH2OH; n is an integer of from 3 to 10; R3 is hydrogen, alkyl containing from one to about 20 carbon atoms, alkenyl containing from two to about 20 carbon atoms, phenyl, naphthyl, phenylethenyl, benzyl, halogen, amino, substituted amino, -CH2COOH, -CH2PO3H2, -CH(PO3H2)(OH), or -CH2CH(PO3H2)2;R4is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, -CH2COOH, -CH2PO3H2, or -CH2CH2PO3H2; and the pharmaceutically acceptable salts thereof. 41. The method of claim 40 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 42. The method of claim 40 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt thereof. 43. A method for treating arthritis comprising administering to an animal afflicted therewith an effective but non-toxic amount of a polyphosphonate selected from the group consisting of wherein R1 and R2 are each hydrogen or CH2OH; n is an integer of from 3 to 10; R3 is hydrogen, alkyl containing from one to about 20 carbon atoms, alkenyl containing from two to about 20 carbon atoms, phenyl, naphthyl, phenylethenyl, benzyl, halogen, amino, substituted amino, -CH2COOH, -CH2PO3H2, -CH(PO3H2)(OH), or -CH2CH(PO3H2)2;R4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, -CH2COOH,-CH2PO3H2, or -CH2CH2PO3H2; and the pharmaceutically acceptable salts thereof. 44. The method of claim 43 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 45. The method of claim 43 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt hereof. 46. A method for treating urolithiasis comprising administering to an animal afflicted therewith an effective but non-toxic amount of a polyphosphonate selected from the group consisting of wherein R1 and R2 are each hydrogen or CH2OH; n is an integer of from 3 to 10; R3 is hydrogen, alkyl Containing from one to about 20 carbon atoms, alkenyl containing from two to about 20 carbon atoms, phenyl, naphthyl, phenylethenyl, benzyl, halogen, amino, substituted amino, -CH2COOH, -CH2PO3H2, -CH(PO3H2)(OH), or -CH2CH(PO3H2)2; R4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, -CH2COOH, -CH2PO3H2, or -CH2CH2PO3H2; and the pharmaceutically acceptable salts thereof. 47. The method of claim 46 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 48. The method of claim 46 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt thereof. 49. A method for treating arteriosclerosis comprising administering to an animal afflicted therewith an effective but non-toxic amount of a polyphosphonate selected from the group consisting of wherein R1 and R2 are each hydrogen or CH2OH; n is an integer of from 3 to 10; R3 is hydrogen, alkyl containing from one to about 20 carbon atoms, alkenyl containing from two to about 20 carbon atoms, phenyl, naphthyl, phenylethenyl, benzyl, halogen, amino, substituted amino, -CH2COOH, -CH2PO3H2, -CH(PO3H2)(OH), or -CH2CH(PO3H2)2; R4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, -CH2COOH, -CH2PO3H2, or -CH2CH2PO3H2; and the pharmaceutically acceptable salts thereof. 50. The method of claim 49 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 51. The method of claim 49 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt thereof.