公开(公告)号：US5789386A

公开(公告)日：1998-08-04

申请号：US709297

申请日：1996-09-09

申请人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yasushi Takagi ,  Hiromi Sohtome

发明人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yasushi Takagi ,  Hiromi Sohtome

IPC分类号： C07H15/252 ,  A61K31/70 ,  C07H15/24

CPC分类号： C07H15/252

摘要： To provide novel fluorine-containing anthracycline derivatives having high antitumor activities and a solubility in water, there have now been synthesized a 7-O-(2,6-dideoxy-2-fluoro-3-O- or -4-O- or -3,4-di-O-aminoalkanoyl-.alpha.-L-talopyranosyl)daunomycinone or -adriamycinone of general formula (I) shown below, as well as a 7-O-(3-O- or -4-O- or -3,4-di-O-aminoalkanoyl-2,6-dideoxy-2,6,6,6-tetrafluoro-.alpha.-L-talopyranosyl- or -2,6-dideoxy-6,6,6-trifluoro-.alpha.-L-lyxo-hexopyranosyl)adriamycinone of general formula (II) shown below: General formula (I) ##STR1## General formula (II) ##STR2## wherein either one or both of A.sup.1 and A.sup.2 is or are an .alpha.-amino acid residue or an .omega.-amino acid residue and T denotes a fluorine or hydrogen atom. The novel fluorine-containing anthracycline derivatives of general formulae (I) and (II) are highly active against tumors and soluble in water, and they are useful as antitumor agents administrable in the form of injectable solution.

摘要翻译： 为了提供具有高抗肿瘤活性和在水中的溶解性的新型含氟蒽环类衍生物，现在已经合成了7-O-（2,6-二脱氧-2-氟-3-O-或-4-O-或 -3,4-二-O-氨基链烷酰-α-L-吡喃葡萄糖基）道诺霉素酮或下列通式（I）的阿霉素酮，以及7-O-（3-O-或-4-O-或 -3,4-二-O-氨基链烷酰基-2,6-二脱氧-2,6,6,6-四氟-α-L-吡喃木糖基或-2,6-二脱氧-6,6,6-三氟-α （II）的通式（Ⅰ）所示的通式（Ⅰ）所示的通式（Ⅰ）的L-赖氨酸 - 六吡喃糖基）的阿霉素酮：通式（Ⅰ） 是α-氨基酸残基或ω-氨基酸残基，T表示氟或氢原子。 通式（I）和（II）的新型含氟蒽环类衍生物对肿瘤具有高度活性并且可溶于水，并且它们可用作以可注射溶液形式施用的抗肿瘤剂。