Novel methylenebisphosphonic acid derivatives

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 9/40 (2006.01) A61K 31/66 (2006.01) C07F 9/547 (2006.01) C07F 9/58 (2006.01)

Patent

CA 2098735

Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R1-R4 independently are C1-C10-alkyl, C3-C10-cycloalkyl, aryl, aralkyl, silyl SiR3 or hydrogen, whereby in formula (I) at least one of the groups R1-R4 is hydrogen and at least one of the groups R1-R4 is different from hydrogen; Q1 is hydrogen, hydroxyl, halogen, ami- no NH2, or OR'1, wherein R'1 is C1-C4-alkyl or acyl; Q2 is the group,(.alpha.) wherein Y is a six-membered heterocyclic group, or a carbocyclic aromatic group, X is a bond, O, S or NR"', wherein R"' is hydrogen, lower alkyl, or acyl, n is the integer 0 to 6, and R' and R" are hydrogen or lower alkyl provided that as a ring atom of the ring Y and/or a chain atom of the group X, there is always at least one heteroatom from the group of O, N and S, including the stereoisomers and the salts of the compounds.

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