Process for the preparation of methylenediphosphonic acid...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/38 (2006.01) A61K 31/66 (2006.01) C07D 213/70 (2006.01) C07F 9/58 (2006.01) C07F 9/59 (2006.01)

Patent

CA 1263397

29 ABSTRACT OF THE DISCLOSURE New methylenediphosphonic acid derivatives useful in the treatment of rheumatic manifestations have the general formula: (I) Image in which : R1 represents: - a C1-C6 alkyl group, - a C5-C7 cycloalkyl group, - a phenyl group optionally monosubstituted or polysubstituted by a halogen, a C1-C6 alkyl group or a trifluoromethyl group, or - a 5-membered or 6-membered heterocycle con- taining 1 or 2 heteroatoms chosen from nitrogen and sulfur, . Alk denotes a linear or branched C1-C6 alkylene group, . R2 represents hydrogen, a C1-C6 alkyl group or a -CONH2 group, . R3 represents hydrogen, a C1-C6 alkyl group, a benzyl group or a phenyl group optionally substituted by chlorine or methyl groups ; or alternatively . R2 and R3, taken together, represent a (CH2)m group, in which m = 4 or 5, and finally . n represents 0 or the integer 1 or 2. Processes for the preparation of the compounds (I) are described.

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