Methane diphosphonic acid derivative, its production process...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/547 (2006.01) A61K 31/67 (2006.01) C07F 9/6553 (2006.01)

Patent

CA 2127115

The present invention discloses a methane diphosphonate derivative, a process for producing said derivative and its pharmaceutical applications, said methane diphosphonate derivative indicated with general formula (1): (see fig.I) (wherein, R1, R2, R3 and R4 are independently a pharmacologically acceptable cation, a hydrogen atom or a straight chain or branched alkyl group having 1-4 carbon atoms, R5 is a hydrogen atom or a trialkylsilyl group, m is an integer of 0 to 3, n is an integer of 1 to 3, R6 and R7 are independently a hydrogen atom or an alkyl group, and X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylthio group). The compounds of the present invention are useful as an anti-inflammatory, antipyretic, analgesic, antirheumatic drug, antiarthritic or anti-osteoporosis drug as a result of having anti-inflammatory action, antipyretic and an algesic action, or action which improves bone metabolic disorders caused by rheumatism, arthritis, osteoporosis and so forth.

Dérivé de méthanediphosphonate; méthode pour préparer ce dérivé et son emploi en pharmacie; il répond à la formule générale (1) : (voir fig. I) (où R1, R2, R3 et R4 sont chacun indépendamment l'un de l'autre un cation acceptable en pharmacie, un atome d'hydrogène ou un alkyle de 1 à 4 atomes de carbone à chaîne droite ou ramifiée, R5 est un atome d'hydrogène ou un trialkylsilyle, m est un entier de 0 à 3, n est un entier de 1 à 3, R6 et R7 sont chacun indépendamment l'un de l'autre un atome d'hydrogène ou un alkyle, X représente un atome d'hydrogène, d'halogène, un alkyle, un alcoxy ou un alkylthio). Les composés de la présente invention sont utiles comme anti-inflammatoires, antipyrétiques, analgésiques, et comme médicaments contre les rhumatismes, l'arthrite ou l'ostéoporose du fait de leurs propriétés anti-inflammatoires, antipyrétiques et analgésiques; ils agissent de façon générale sur les troubles métaboliques causés par les les rhumatismes, l'arthrite, l'ostéoporose, etc.

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