Novel methylenebisphosphonic acid derivatives

C - Chemistry – Metallurgy – 07 – F

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C07F 9/40 (2006.01) A61K 31/66 (2006.01) C07F 9/547 (2006.01) C07F 9/553 (2006.01)

Patent

CA 2098732

Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R1, R2, R3 and R4 independently are straight or branched, optionally unsaturated C1-C10-alkyl, optionally unsaturated C3-C10-cycloalkyl, aryl, aralkyl, silyl SiR3 or hydrogen; whereby in formula (I) at least one of the groups R1, R2, R3 and R4 is hydrogen and at least one of the groups is different from hydrogen, Q1 is hydrogen, hydroxyl, halogen, amine NH2, or OR', wherein R' is C1-C4-lower alkyl or acyl, Q2 is straight or branched, optionally unsaturated C1-C10-alkyl, - hydroxyalkyl or -aminoalkyl, whereby the oxygen may, as a substituent, contain one group or the nitrogen as a substituent may contain one or two groups, which are C1-C4-lower alkyl or aryl, or the two substituents of the nitrogen form together with the nitrogen atom a saturated, partly saturated or an aromatic heterocyclic ring; or Q2 is optionally substituted and optionally unsaturated C3-C10-cycloalkyl, which optionally is bound to the molecule over a straight or branched alkylene group containing 1-4 C-atoms, including the stereoisomers, such as the geometrical isomers and the optically active isomers, of the compounds, as well as the pharmaco- logically acceptable salts of these compounds.

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