Substituted alkanediphosphonic acids and pharmaceutical use

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

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514 92, 514 93, 548112, 548119, A61K 31675, C07F 965

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active

049391305

ABSTRACT:
Alkanediphosphonic acids, in particular heteroarylalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is a 5-membered heteroaryl radical which may be fused with benzene or cyclohexene nuclei and which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen, and R.sub.2 is hydrogen, hydroxy, amino, lower alkylthio or halogen, and salts thereof, have regulatory action on calcium metabolism and can be used as medicaments for the treatment of diseases associated with impairment of calcium metabolism. The compounds are obtained for example by converting, in a compound of formula ##STR2## wherein X.sub.1 is a functionally modified phosphono group and X.sub.2 is a free or functionally modified phosphono group, X.sub.1 and, if appropriate X.sub.2, into the free phosphono group.

REFERENCES:
patent: 4503049 (1985-03-01), Biere et al.
patent: 4687767 (1987-08-01), Bosies et al.
patent: 4777163 (1988-10-01), Bosies et al.
CA 105:134140r (1986).

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