Claims
- 1. A diphosphonic acid derivative of the formula: ##STR13## wherein Het is a piperidine ring wherein the nitrogen is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl,
- B is C-H,
- R.sub.1 and R.sub.2 are each hydrogen,
- Y is a group of the formula: ##STR14## wherein R.sub.3 is hydrogen or a C.sub.1 -C.sub.4 alkyl, alk is a straight-chain or branched C.sub.1 -C.sub.6 alkylene chain except that the chain cannot link with a heteroatom, X is hydrogen or a hydroxyl or amino group, G is hydrogen, m is 1 and r is 0, ; and the stereo-, cis- or trans-isomers and the pharmacologically acceptable salt thereof.
- 2. The compound of formula I of claim 1, wherein Het is a piperidine ring, B is C-H, R.sub.1 and R.sub.2 are hydrogen, Y is a group of the formula: ##STR15## wherein R.sub.3 is hydrogen or a C.sub.1 -C.sub.4 -alkyl, alk is a C.sub.1 -C.sub.2 -alkylene chain, X is hydroxyl, G is a hydrogen, r is 0 and m is 1.
- 3. The compound of claim 1 or 2 wherein the C.sub.1 -C.sub.4 alkyl is methyl, ethyl or isopropyl.
- 4. The compound of claim 1 or 2 wherein when alk is an alkylene chain it is methylene, ethylene or propylene.
- 5. The compound of claim 1 designated 1-hydroxy-3-(piperidine-2-yl)-propane-1,1-diphosphonic acid and the physiologically active salt.
- 6. The compound of claim 1 designated 1-hydroxy-2-(piperidine-2-yl)-ethane-1,1-diphosphonic acid the physiologically active salt.
- 7. A pharmaceutical composition for the treatment or prophylaxis of calcium metabolism disturbance or disease wherein said composition contains a pharmaceutically effective amount of at least one compound of claim 1 or 2 in a pharmaceutically acceptable carrier.
- 8. A pharmaceutical composition for the treatment or prophylaxis of calcium disturbance or disease consisting of a pharmaceutically effective amount of at least one compound selected from the group consisting of 1-hydroxy-2-(1-methylpiperidine-2-yl)ethane-1,1-diphosphonic acid, 1-hydroxy-2-(piperidine-2-yl)-ethane-1,1-diphosphonic acid and 1-hydroxy-3-piperidine-2-yl)-propane-1,1-disphosphonic acid.
- 9. A method for the treatment of prophylaxis of calcium metabolism disturbance or disease comprising administering an effective amount of at least one of a pharmaceutically acceptable compound of claim 1 or 2.
- 10. The method of claim 7 wherein the daily dose is 1-1000 mg. in a human.
- 11. The method of claim 9 wherein the daily dose is 10-200 mg. in a human.
- 12. A method for the treatment or prophylaxis of calcium metabolism disturbance or disease comprising administering an effective amount of at least one of a pharmaceutically acceptable compound selected from the group consisting of 1-hydroxy-2-(1-methyl-piperidine-2-yl)-ethane-1, 1-diphosphonic acid, 1-hydroxy-2-(piperidine-2-yl)-ethane-1,1-diphosphonic acid, and 1-hydroxy-3-(piperidine-2-yl)-propane-1,1-diphosphonic acid.
- 13. The method of claim 12 wherein the daily dose is 1-1000 mg. in a human.
- 14. The method of claim 12 wherein the daily dose is 10-200 mg. in a human.
Priority Claims (1)
Number |
Date |
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Kind |
3640938 |
Nov 1986 |
DEX |
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Parent Case Info
This application is a continuation of application Ser. No. 125,537, filed Nov. 25, 1987, now abandoned.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
3988443 |
Ploger et al. |
Oct 1976 |
|
4761406 |
Flora et al. |
Aug 1988 |
|
Foreign Referenced Citations (9)
Number |
Date |
Country |
0001584 |
May 1979 |
EPX |
0170228 |
Feb 1986 |
EPX |
0186405 |
Jul 1986 |
EPX |
0258618 |
Mar 1988 |
EPX |
0272208 |
Jun 1988 |
EPX |
0274158 |
Jul 1988 |
EPX |
0275821 |
Jul 1988 |
EPX |
1958123 |
May 1971 |
DEX |
0059674 |
May 1978 |
JPX |
Non-Patent Literature Citations (2)
Entry |
Chemical Abstracts, 74-Radiation Chem., Photochem., vol. 96, 1982, p. 591. 774832. |
Chemical Abstracts, 1-Pharmacology, vol. 99, 1983, p. 640. |
Continuations (1)
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Number |
Date |
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Parent |
125537 |
Nov 1987 |
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