Salts of isophosphoramide mustard and analogs thereof as...

Details Salts of isophosphoramide mustard and analogs thereof as... Salts of isophosphoramide mustard and analogs thereof as...

C - Chemistry, Metallurgy

07

F

C07F 9/22 (2006.01) A61K 31/66 (2006.01) A61K 31/675 (2006.01)

Patent

CA 2585125

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.

L'invention se rapporte à des sels et des compositions d'yperite d'isophosphoramide et à des analogues d'yperite d'isophosphoramide. Dans un mode de réalisation, les sels peuvent être représentés par la formule (I) dans laquelle A+ représente une espèce d'ammonium choisie dans les formes protonées (acide conjugué) ou quaternaires d'amines aliphatiques et d'amines aromatiques, y compris des acides aminés basiques, des amines hétérocycliques, des pyridines substitués ou non substitués, des guanidines et des amidines ; et X et Y représentent chacun des nucléofuges. L'invention porte aussi sur des procédés de fabrication de ces composés et de formulations de compositions pharmaceutiques. Elle concerne également des procédés d'administration des composés mentionnés à des sujets, notamment afin de traiter des troubles hyperprolifératifs.

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