Boron containing polyphosphonates for the treatment of calcific

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128783, 2605024P, 424 1, A61K 4900, A61N 506

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043998178

ABSTRACT:
Boron containing polyphosphonates of the formula ##STR1## wherein Z is a boron-containing radical; R.sub.2 is an alkyl group containing from 1 to about 10 carbon atoms; R.sub.3 is a geminal diphosphonate or a vicinal polyphosphonate containing up to 10 phosphonic acid radicals; R.sub.4 is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH.sub.2 COOH, --CH.sub.2 PO.sub.3 H.sub.2, or --CH.sub.2 CH.sub.2 PO.sub.3 H.sub.2 ; 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.

REFERENCES:
patent: 3965254 (1976-01-01), Tofe et al.
patent: 4361544 (1982-11-01), Goldenberg
Zamenhof, et al., "Boron Neutron Capture Therapy for the Treatment of Cerebral Gliomas. I: Theoretical Evaluation of the Efficacy of Various Neutron Beams*", Medical Physics 2 (1975), 47-59.
Escher, et al., "L-Carboranylalanine Substituted TMV, a Highly Boron Labelled Virus as a Model for Slow Neutron Therapy of Tumors", J. Labelled Comp. Radiopharm., vol. XIV (1978), 487-496.
Wong, et al., "Boron Hydride Derivatives for Neutron Capture Therapy Antibody Approach", J. Med. Chem. 17 (1974), 785-791.
Sneath, et al., "Protein-Binding Polyhedral Broanes. 1", J. Med Chem. 17 (1974), 796-799.
Zakharkin, et al., "Synthesis of o-Carboranyl-Substituted Phosphonous Acids", Izv. Akad. Nauk. SSSR, 9 (1969), 2056-2057.
Zakharkin, et al., "Synthesis of o-Carboranylphosphonic Acids", Zh. Obsch. Khim., 41 (1971), 588-592.

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