Salts of isophosphoramide mustard and analogs thereof as anti-tumor agents
    106.
    发明授权
    Salts of isophosphoramide mustard and analogs thereof as anti-tumor agents 有权
    异磷酰胺芥酸盐及其类似物作为抗肿瘤剂

    公开(公告)号:US08795659B2

    公开(公告)日:2014-08-05

    申请号:US13541522

    申请日:2012-07-03

    申请人: Lee R. Morgan

    发明人: Lee R. Morgan

    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.

    摘要翻译: 本公开涉及异磷酰胺芥酸和异磷酰胺芥菜类似物的盐和组合物。 在一个实施方案中,盐可以由式I表示:(I)其中A +表示选自质子化(共轭酸)或季形式的脂族胺和芳族胺的铵类,包括碱性氨基酸,杂环胺,取代和 未取代的吡啶,胍和脒; X和Y独立地表示离去基团。 本文还公开了制备这些化合物和配制其药物组合物的方法。 公开了给予受试者,特别是治疗过度增殖性疾病的方法。