Boron containing polyphosphonates for the treatment of...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/38 (2006.01) A61K 41/00 (2006.01) A61K 51/04 (2006.01) C07F 9/6596 (2006.01)

Patent

CA 1219595

BORON CONTAINING POLYPHOSPHONATES FOR THE TREATMENT OF CALCIFIC TUMORS James J. Benedict Abstract Boron containing polyphosphonates of the formula Image ; or Image ;or Image ; or Image ; wherein Z is a boron-containing radical; R2 is an alkyl group containing from 1 to about 10 carbon atoms; R3 is a geminal, diphosphonate or a vicinal polyphosphonate containing up to 10 phosphonic acid radicals; R4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, - CH2COOH, - CH2PO3H2, or - CH2CH2PO3H2; and the salts and esters thereof, have high affinity for calcified tissues, in particular calcific tumors. The compounds are useful in boron neutron capture therapy of such tumors.

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