公开(公告)号：US5646177A

公开(公告)日：1997-07-08

申请号：US432836

申请日：1995-05-02

申请人： Tad H. Koch ,  Giorgio Gaudiano

发明人： Tad H. Koch ,  Giorgio Gaudiano

IPC分类号： A61K38/00 ,  C07H15/252 ,  C07K5/02 ,  C07D319/04 ,  C07D319/08 ,  C07D50/22

CPC分类号： C07H15/252 ,  C07K5/0215 ,  A61K38/00

摘要： Disclosed herein are new anthracyclines which are derived from conjugation with glutathione, for example from conjugation of adriamycin, daunomycin and menogaril with glutathione: compounds 7 I, 7 II, 8 I, 8 II, 9 I and 9II, are obtained by reduction of the anthracycline followed by reaction of the reduced product with glutathione in aqueous (H.sub.2 O or D.sub.2 O) or organic solvent. The invention also provides salts of these glutathione derivatives, particularly salts formed from anthracycline glutathione anions with anthracycline cations. These anthracycline derivatives are useful as antibiotics, as antitumor agents, and in the treatment of AIDS. These derivatives are particularly useful in the treatment of cancer when multiple drug resistance is present.

摘要翻译： 本文公开的是新型蒽环类抗生素，其衍生自与谷胱甘肽的缀合，例如从阿霉素，道诺霉素和menogaril与谷胱甘肽的结合：化合物7 I，7 II，8 I，8 II，9 I和9II通过将 然后将还原产物与谷胱甘肽在水（H 2 O或D 2 O）或有机溶剂中反应。 本发明还提供这些谷胱甘肽衍生物的盐，特别是由蒽环类型的谷胱甘肽阴离子与蒽环类阳离子形成的盐。 这些蒽环类衍生物可用作抗生素，作为抗肿瘤剂和用于治疗AIDS。 当存在多种耐药性时，这些衍生物特别可用于治疗癌症。

公开(公告)号：US4632922A

公开(公告)日：1986-12-30

申请号：US791120

申请日：1985-10-24

申请人： Steven D. Averbuch ,  Nicholas R. Bachur ,  Giorgio Gaudiano ,  Tad H. Koch

发明人： Steven D. Averbuch ,  Nicholas R. Bachur ,  Giorgio Gaudiano ,  Tad H. Koch

IPC分类号： C07D265/32 ,  A61K31/535

CPC分类号： C07D265/32

摘要： The present invention discloses a bi(3,5-dimethyl-5-hydroxymethyl-2-oxomorpholin-3-yl) compound and its efficacy as a rescue agent against anthracycline and mitomycin C induced tissue damage. A method of synthesizing said compound has also been described.

摘要翻译： 本发明公开了一种双（3,5-二甲基-5-羟甲基-2-氧代吗啉-3-基）化合物及其作为抗蒽环霉素和丝裂霉素C诱导的组织损伤的救援剂的功效。 还描述了合成所述化合物的方法。