Claims
- 1. Compound of the formula: ##STR9## wherein Het is a substituted or unsubtituted heterocyclic ring selected from the group consisting of 1,2,3-triazole, and 1,2,4-triazole, and wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen selected from the group consisting of fluorine, chlorine, bromine, iodine; hydroxyl, carboxyl, an amino group optionally substituted by C.sub.1 -C.sub.4 alkyl or alkanoyl of 1 to 6 carbon atoms; benzyl and benzyl substituted by C.sub.1 -C.sub.4 alkyl, nitro, amino and aminoalkyl with 1 to 4 carbon atoms,
- A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 atoms,
- X is a hydrogen atom, hydroxy optionally substituted by alkanoyl of 1 to 6 carbon atoms or an amino group optionally substituted by an alkyl radical of 1 to 4 carbon atoms or by alkanoyl of from 1 to 6 carbon atoms and R is a hydrogen atom or an alkyl of 1 to 4 carbon atoms or a pharmaceutically acceptable salt thereof.
- 2. Composition useful for treating a calcium metabolism disorder comprising an effective amount of the compound of claim 1 to treat said disorder and at least one pharmaceutically acceptable carrier or adjuvant to a mammal in need of such treatment.
- 3. Compound of claim 1 wherein each said alkyl is individually selected from the group consisting of methyl, ethyl and isopropyl.
- 4. Compound of claim 1 wherein each said alkanoyl is individually selected from the group consisting of formyl, acetyl, propionyl, butyryl, and valeroyl.
- 5. Compound of claim 3 wherein each said alkanoyl is individually selected from the group consisting of formyl, acetyl, propionyl, butyryl, and valeroyl.
- 6. Compound of claim 1 wherein Het is unsubstituted or substituted by methyl, ethyl, or benzyl optionally substituted by methyl, aminomethyl, nitro or amino.
- 7. Compound of claim 1 wherein X is hydroxyl.
- 8. Compound of claim 1 wherein X is amino.
- 9. Compound of claim 1 wherein A is --(CH.sub.2).sub.n -- wherein n is 2 to 5, ##STR10## wherein m is 2 to 5, --CH.dbd.CH--CH.sub.2 --CH.sub.2, --CH.dbd.CH--CH.sub.2 --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--CH.dbd.CH--.
- 10. Compound of claim 1 wherein A is a straight-chained, saturated hydrocarbon chain containing 2 to 4 carbon atoms.
- 11. A pharmaceutical composition according to claim 2 having 1 to 1000 mg of the active ingredient.
- 12. A method according to claim 2 wherein 1 to 1000 mg of the diphosphonate, are administered.
- 13. Compound of claim 1, wherein Het is 1,2,3-triazole or 1,2,4-triazole.
- 14. Compound of claim 1, designated 3-[1-benzyl-4-(1,2,3-triazolyl)]-1-hydroxypropane-1,1-diphosphonic acid.
- 15. Compound of claim 1, designated 5-[1-benzyl-4-(1,2,3-triazolyl)]-1-hydroxypentane-1,1-diphosphonic acid.
- 16. Compound of claim 1, designated 3-[1-(4-aminomethylbenzyl)-1,2,3-triazol-4-yl)]-1-hydroxypropane-1,1-diphosphonic acid.
- 17. A method for the treatment of calcium metabolism disturbances comprising administering to a subject an effective amount of a compound of the formula: ##STR11## wherein Het is a substituted or unsubstituted heterocyclic ring selected from the group consisting of 1,2,3-trizole and 1,2,4-triazole, and wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen selected from the group consisting of fluorine, chlorine, bromine, iodine; hydroxyl, carboxyl, an amino group optionally substituted by C.sub.1 -C.sub.4 alkyl or alkanoyl of 1 to 6 carbon atoms; benzyl and benzyl substituted by C.sub.1 -C.sub.4 alkyl, nitro, amino and aminoalkyl with 1 to 4 carbon atoms,
- A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms,
- X is a hydrogen atom, hydroxy optionally substituted by alkanoyl of 1 to 6 carbon atoms or an amino group optionally substituted by an alkyl radical of 1 to 4 carbon atoms or by alkanoyl of from 1 to 6 carbon atoms and R is a hydrogen atom or an alkyl of 1 to 4 carbon atoms or a pharmaceutically acceptable salt thereof.
Priority Claims (1)
Number |
Date |
Country |
Kind |
3428524 |
Aug 1984 |
DEX |
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Parent Case Info
This is a division of Ser. No. 759,608 filed July 26, 1985.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4503049 |
Bierre et al. |
Mar 1985 |
|
4687767 |
Bosies et al. |
Aug 1987 |
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Divisions (1)
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Number |
Date |
Country |
Parent |
759608 |
Jul 1985 |
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