发明公开
EP0761678A1 Fluorine-containing anthracycline derivatives having hydroxyl group(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof
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- 专利标题： Fluorine-containing anthracycline derivatives having hydroxyl group(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof
- 专利标题（中）： 荧光e e mit rest mit mit mit rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest
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申请号： EP96420288.1申请日： 1996-09-06
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公开(公告)号： EP0761678A1公开(公告)日： 1997-03-12
- 发明人: Takeuchi, Tomio, New Fuji Mansion 701, 1-11 , Umezawa, Sumio , Tsuchiya, Tsutomu , Takagi, Yasushi , Sohtome, Hiromi
- 申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
- 申请人地址： 14-23, Kami Ohsaki 3-chome Shinagawa-ku Tokyo JP
- 专利权人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
- 当前专利权人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
- 当前专利权人地址： 14-23, Kami Ohsaki 3-chome Shinagawa-ku Tokyo JP
- 代理机构： Guerre, Dominique
- 优先权： JP257152/95 19950908
- 主分类号： C07H15/252
- IPC分类号： C07H15/252 ; A61K31/70
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-α-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-α-L-talopyranosyl- or -2,6-dideoxy-6,6,6-trifluoro-α-L-lyxo-hexopyranosyl)adriamycinone of general formula (II) shown below:-
wherein either one or both of A 1 and A 2 is or are an α-amino acid residue or an ω-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.
wherein either one or both of A 1 and A 2 is or are an α-amino acid residue or an ω-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.
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