You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 28, 2024

Claims for Patent: 3,683,080


✉ Email this page to a colleague

« Back to Dashboard


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. 51 Claims, No Drawings
Inventor(s): Marion D. Francis, Springfield Township (Hamilton County), OH (N/A)
Assignee: The Procter & Gamble Company, Cincinnati, OH (N/A)
Application Number:05/068,029
Patent Claims: 1. A composition in dosage unit form for inhibiting deposition and mobilization of calcium phosphate in animal tissue comprising (1) an effective but non-toxic amount, within the range from about 15 mg. to about 1,000 mg., of a polyphosphonate selected from the group consisting of wherein R.sub.1 and R.sub.2 are each hydrogen or CH.sub.2 OH; n is an integer of from 3 to 10; R.sub.3 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, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, --CH(PO.sub.3 H.sub.2)(OH), or --CH.sub.2 CH(PO.sub.3 H.sub.2).sub.2 ; R.sub.4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, or --CH.sub.2 CH.sub.2 PO.sub.3 H.sub.2 ; and the pharmaceutically acceptable salts thereof, and (2) a pharmaceutical carrier, said composition being adapted to systemic

2. The composition of claim 1 wherein the polyphosphonate is methanehydroxydiphosphonic acid or a pharmaceutically acceptable salt

3. The composition of claim 1 wherein the polyphosphonate is ethane-1-amino-1,1-diphosphonic acid or a pharmaceutically acceptable salt

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

6. The composition of claim 1 wherein the polyphosphonate is propane-1,2,3-triphosphonic acid or a pharmaceutically acceptable salt

7. The composition of claim 1 wherein the polyphosphonate is butane-1,2,3,4-tetraphosphonic acid or a pharmaceutically acceptable salt

8. The composition of claim 1 wherein the polyphosphonate is hexane-1,2,3,4,5,6-hexaphosphonic acid or a pharmaceutically acceptable

9. The composition of claim 1 wherein the polyphosphonate is methanephenylaminodiphosphonic acid or a pharmaceutically acceptable salt

10. The composition of claim 1 wherein the dosage unit form is adapted to

11. The composition of claim 1 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt

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

13. The composition of claim 1 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable

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

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 R.sub.1 and R.sub.2 are each hydrogen or CH.sub.2 OH; n is an integer of from 3 to 10; R.sub.3 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, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, --CH(PO.sub.3 H.sub.2)(OH), or --CH.sub.2 CH(PO.sub.3 H.sub.2).sub.2 ; R.sub.4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, or --CH.sub.2 CH.sub.2 PO.sub.3 H.sub.2 ; and the pharmaceutically acceptable salts thereof, and

16. The method of claim 15 wherein the polyphosphonate is

17. The method of claim 15 wherein the polyphosphonate is

18. The method of claim 15 wherein the polyphosphonate is

19. The method of claim 15 wherein the polyphosphonate is

20. The method of claim 15 wherein the polyphosphonate is

21. The method of claim 15 wherein the polyphosphonate is

22. The method of claim 15 wherein the polyphosphonate is

23. The method of claim 15 wherein the polyphosphonate is

24. The method of claim 15 wherein the polyphosphonate is

25. The method of claim 15 wherein the polyphosphonate is

26. An animal feed composition comprising (1) a minor proportion of a polyphosphonate selected from the group consisting of wherein R.sub.1 and R.sub.2 are each hydrogen or CH.sub.2 OH; n is an integer from 3 to 10; R.sub.3 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, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, --CH(PO.sub.3 H.sub.2)(OH), or --CH.sub.2 CH(PO.sub.3 H.sub.2).sub.2 ; R.sub.4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, or --CH.sub.2 CH.sub.2 PO.sub.3 H.sub.2 ; and the pharmaceutically acceptable salts thereof, and

27. The composition of claim 26 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt

28. The composition of claim 26 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable

29. The composition of claim 26 wherein the polyphosphonate is methanehydroxydiphosphonic acid or a pharmaceutically acceptable salt

30. The composition of claim 26 wherein the polyphosphonate is ethane-1-amino-1,1-diphosphonic acid or a pharmaceutically acceptable salt

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

33. The composition of claim 26 wherein the polyphosphonate is propane-1,2,3-triphosphonic acid or a pharmaceutically acceptable salt

34. The composition of claim 26 wherein the polyphosphonate is butane-1,2,3,4-tetraphosphonic acid or a pharmaceutically acceptable salt

35. The composition of claim 26 wherein the polyphosphonate is hexane-1,2,3,4,5,6-hexaphosphonic acid or a pharmaceutically acceptable

36. The composition of claim 26 wherein the polyphosphonate is methanephenylaminodiphosphonic acid or a pharmaceutically acceptable salt

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 R.sub.1 and R.sub.2 are each hydrogen or CH.sub.2 OH; n is an integer of from 3 to 10; R.sub.3 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, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, --CH(PO.sub.3 H.sub.2)(OH), or --CH.sub.2 CH(PO.sub.3 H.sub.2).sub.2 ; R.sub.4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, or --CH.sub.2 CH.sub.2

38. The method of claim 37 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable

39. The method of claim 37 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt

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 R.sub.1 and R.sub.2 are each hydrogen or CH.sub.2 OH; n is an integer of from 3 to 10; R.sub.3 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, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, --CH(PO.sub.3 H.sub.2)(OH), or --CH.sub.2 CH(PO.sub.3 H.sub.2).sub.2 ;R.sub.4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, or --CH.sub.2 CH.sub.2

41. The method of claim 40 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable

42. The method of claim 40 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt

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 R.sub.1 and R.sub.2 are each hydrogen or CH.sub.2 OH; n is an integer of from 3 to 10; R.sub.3 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, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, --CH(PO.sub.3 H.sub.2)(OH), or --CH.sub.2 CH(PO.sub.3 H.sub.2).sub.2 ;R.sub.4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH.sub.2 COOH,--CH.sub.2 PO.sub.3 H.sub.2, or --CH.sub.2 CH.sub.2

44. The method of claim 43 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable

45. The method of claim 43 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt

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 R.sub.1 and R.sub.2 are each hydrogen or CH.sub.2 OH; n is an integer of from 3 to 10; R.sub.3 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, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, --CH(PO.sub.3 H.sub.2)(OH), or --CH.sub.2 CH(PO.sub.3 H.sub.2).sub.2 ; R.sub.4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, or --CH.sub.2 CH.sub.2

47. The method of claim 46 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable

48. The method of claim 46 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt

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 R.sub.1 and R.sub.2 are each hydrogen or CH.sub.2 OH; n is an integer of from 3 to 10; R.sub.3 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, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, --CH(PO.sub.3 H.sub.2)(OH), or --CH.sub.2 CH(PO.sub.3 H.sub.2).sub.2 ; R.sub.4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, or --CH.sub.2 CH.sub.2

50. The method of claim 49 wherein the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable

51. The method of claim 49 wherein the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt thereof.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.