Sensitizing agents for use in boron neutron capture therapy
OwnerRaymond F. Schinazi, Dennis C. Liottainventors
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Abstract
Compounds of formula I and II ##STR1## in which B contains a carboranyl group and one of R.sub.3 and R.sub.4 is a carboranyl group or a boronic acid or ester are useful sensitizing agents for boron neutron capture therapy.
Claims7
A compound having the formula II ##STR15## R.sub.3 and R.sub.4 are each, independently, --H, --B(OH).sub.2, --B(OR.sub.6).sub.2 (wherein R.sub.6 is a C.sub.1-4 alkyl), or a carboranyl group --B.sub.10 H.sub.10 C.sub.2 R.sub.8, wherein R.sub.8 is --H, --OH, --CH.sub.2 OH, --CH.sub.2 X (wherein X is F, Cl, Br, or I) or --B.sub.9 C.sub.2 H.sub.12.sup.- (nidocarborane anion), provided that one of R.sub.3 and R.sub.4 is --H and the other of R.sub.3 and R.sub.4 is not --H, and pharmaceutically acceptable salts thereof.
A pharmaceutical composition for boron neutron capture therapy, comprising an effective amount of a compound having formula II ##STR17## R.sub.3 and R.sub.4 are each, independently, --H, --B(OH).sub.2, --B(OR.sub.6).sub.2 (wherein R.sub.6 is a C.sub.1-4 alkyl), or a carboranyl group --B.sub.10 H.sub.10 C.sub.2 R.sub.8, wherein R.sub.8 is --H, --OH, --CH.sub.2 OH, --CH.sub.2 X (wherein X is F, Cl, Br, or I) or --B.sub.9 C.sub.2 H.sub.12.sup.- (nidocarborane anion), provided that one of R.sub.3 and R.sub.4 is --H and the other of R.sub.3 and R.sub.4 is not --H, and pharmaceutically acceptable salts thereof.
A method of boron neutron capture therapy, comprising:
- administering to a patient in need thereof an effective amount of a sensitizing agent which has the formula II, ##STR18## R.sub.3 and R.sub.4 are each, independently, --H, --B(OH).sub.2, --B(OR.sub.6).sub.2 (wherein R.sub.6 is a C.sub.1-4 alkyl), or a carboranyl group --B.sub.10 H.sub.10 C.sub.2 R.sub.8, wherein R.sub.8 is --H, --OH, --CH.sub.2 OH, --CH.sub.2 X (wherein X is F, Cl, Br, or I) or --B.sub.9 C.sub.2 H.sub.12.sup.- (nidocarborane anion), provided that one of R.sub.3 and R.sub.4 is --H and the other of R.sub.3 and R.sub.4 is not --H, and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.