This invention relates to a novel class of acidic amino acid/dicarboxylic acid derivatives (sulfonic acid/sulfate derivatives of naturally occurring amino acids and their amides) useful as inhibitors of osteoclastogenesis. The invention also provides methods of using the novel class of acidic amino acid/dicarboxylic acid derivatives of the general formula ZOC--(CRR).sub.m--COOH, wherein: m=2, 3 or 4; Z is OH or NH.sub.2; one R in the compound is from the group consisting of SO.sub.3H, OSO.sub.3H, CH.sub.2--SO.sub.3H, CH.sub.2--OSO.sub.3H, and NHSO.sub.3H, and the remaining Rs are H or NH.sub.2, for inhibition of osteoclastogenesis.