Salts of isophosphoramide mustard and analogs thereof as anti-tumor agents

摘要

The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I:;
(I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.

主权项

1. A compound of the formulawherein
A+ represents a conjugate acid of an amine selected from the group consisting of acyclic aliphatic amine substituted by one or more hydroxy groups, di-acyclicalkyl amine substituted by one or more hydroxy groups, tri-acyclicalkyl amine substituted by one or more hydroxy groups, di-cyclicalkyl amine, tri-cyclicalkyl amine; and X and Y independently represent leaving groups.