Bisphosphonic acid derivatives, their intermediates and bone...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/59 (2006.01) A61K 31/675 (2006.01) C07F 9/572 (2006.01) C07F 9/576 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2060790

ABSTRACT A bisphosphonic acid derivative of the formula (I) or a pharmaceutically acceptable salt thereof: (I) Image wherein A is Image , , , or Image wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a halogen atom, a C1-6 alkyl group or a single bond, each of j, k and e is 0 or a positive integer, provided that (j+k+?) is from 2 to 6, each of R3 and R4, which may be the same or different, is (i) a hydrogen atom, (ii) a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 alkyl-carbonyl group, a C2-6 alkenyl-carbonyl group, a C2-6 alkynyl- carbonyl group (these groups may be substituted by at least one member selected from the group consisting of a substituted amino group, a halogen atom and a carboxyl group), or (iii) a halogen atom, each of R5 and R6, which may be the same or different, is a hydrogen atom, a hydroxyl group, a halogen atom, a cyano group, a carbamoyl group, an aralkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted amino group, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group or a heterocyclic group having a nitrogen atom as the hetero atom, provided that when either one of R5 and R6 is a hydrogen atom, the other is other than a hydrogen atom or a C1-6 alkyl group; each of m and n is 0 or a positive integer, provided that (m+n) is from 2 to 5; and R is a hydrogen atom, a C1-8 alkyl group or a C7-15 aralkyl group.

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