Diphosphonic acid derivatives

C - Chemistry – Metallurgy – 07 – F

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167/236, 167/237

C07F 9/58 (2006.01) A61K 31/66 (2006.01) C07F 9/38 (2006.01) C07F 9/6506 (2006.01) C07F 9/6518 (2006.01) C07F 9/653 (2006.01)

Patent

CA 1264326

ABSTRACT The present invention provides diphosphonates of the general formula:- Image (I) wherein Het is an imidazole, oxazole, isoxazole, thiazole, pyridine, 1,2,3,-triazole, 1,2,4-triazole or benzimidazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carb- oxyl, an amino group optionally substituted by alkyl or acyl rad- icals or a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, hydroxyl optionally substituted by acyl, or an amino group optionally substituted by alkyl or acyl radicals and R is a hydrogen atom or an alkyl radical; and the pharma- cologically compatible, pharmaceutically acceptable salts thereof; processes for the preparation of these diphosphonates and pharma- ceutical compositions containing them are also provided; the diphosphonates are suitable for the treatment of diseases of the skeletal system, for example osteoporosis, Paget's disease and Bechterew's disease.

487443

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