Novel bisphosphonic acid derivative and application for same
AssigneeNagasaki University
InventorsYoshimasa TANAKA, Kenji MATSUMOTO, Kosuke HAYASHI, Yuki SAKAI, Nagahiro MINATO
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Abstract
The novel bisphosphonic acid ester derivatives represented by the following formula (1): Y—Cy—(NH)m—(CH2)n—C(X)(PO(OR1)(OR2))2 (1) wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.
Claims21
-25. (canceled)
A bisphosphonic acid ester derivative represented by the following formula (1):
- Y—Cy—(NH)m—(CH2)n—C(X)(PO(OR1)(OR2))2 (1)
- wherein Cy is a thiazolyl group, a pyridyl group, a pyrimidyl group, or a 7-azaindolyl group, Y is a hydrogen atom, an alkyl group, a halogen atom, an alkyl halide group, a hydroxyl group, an aryl group optionally substituted by a halogen atom or an alkoxy group, or an aralkyloxy group, X is a hydrogen atom or a hydroxyl group, R1 and R2 are the same or different from each other and each is a hydrogen atom or an alkylcarbonyloxyalkyl group, at least one of R1 and R2 is an alkylcarbonyloxyalkyl group, m is 1, and n is an integer of 1 to 6, excluding when Cy is a 2-pyridyl group, m is 1, n is 1, X is a hydrogen atom, Y is a hydrogen atom, and R1 and R2 are each a pivaloyloxymethyl group.
Dependencies are inferred from the claim text.