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    • 78. 发明授权
    • Salts of isophosphoramide mustard and analogs thereof as anti-tumor agents
    • 异磷酰胺芥酸盐及其类似物作为抗肿瘤剂
    • US07964583B2
    • 2011-06-21
    • US11709319
    • 2007-02-20
    • Robert Peter Gale
    • Robert Peter Gale
    • A61K31/675A61K31/66A61K31/415
    • A61K31/66A61K31/14A61K45/06A61K2300/00
    • 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 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.
    • 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,盐可以由下式表示: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物质,包括碱性氨基酸,杂环胺,取代和未取代的吡啶,胍和胍 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。