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    Fluorine-containing anthracycline derivatives having hydroxyl groups(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof
    1.
    发明授权
    Fluorine-containing anthracycline derivatives having hydroxyl groups(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof 失效
    在其糖部分中具有单或二氨基烷氧基的羟基的含氟蒽环类衍生物

    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。

    Anthracycline derivatives having 4-amino-2,4,6-trideoxy-2 fluoro-&agr;-L-talopyranosyl group
    5.
    发明授权
    Anthracycline derivatives having 4-amino-2,4,6-trideoxy-2 fluoro-&agr;-L-talopyranosyl group 失效
    具有4-氨基-2,4,6-三脱氧-2氟-α-L-吡喃葡萄糖基的蒽环类衍生物

    公开(公告)号：US06184365B2

    公开(公告)日：2001-02-06

    申请号：US08991436

    申请日：1997-12-16

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

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

    IPC分类号： C07H100

    CPC分类号： C07H15/12 ,  C07H15/252 ,  Y02P20/55

    摘要： 7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-&agr;-L-talopyranosyl)-daunomycinone or -adriamycinone is now synthesized as a novel daunomycinone or adriamycinone derivative having the general formula wherein R is a hydrogen atom or hydroxyl group. These novel compounds according to this invention exhibit excellent antitumor activities and have a high solubility in water, and hence they are useful as an antitumor agent.

    摘要翻译： 7-O-（4-氨基-2,4,6-三脱氧-2-氟-α-L-吡喃葡萄糖基） - 日光霉素酮或阿德米霉素现在被合成为具有通式化合物的新的道诺霉素酮或阿霉素酮衍生物，R是氢 原子或羟基。 根据本发明的这些新化合物表现出优异的抗肿瘤活性，并且在水中的溶解度高，因此它们可用作抗肿瘤剂。

    Anthracycline derivative having a trifluoromethylated sugar
    6.
    发明授权
    Anthracycline derivative having a trifluoromethylated sugar 失效
    具有三氟甲基化糖的蒽环类衍生物

    公开(公告)号：US5801257A

    公开(公告)日：1998-09-01

    申请号：US954519

    申请日：1997-10-20

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

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

    IPC分类号： C07C31/42 ,  C07C43/178 ,  C07H13/04 ,  C07H15/18 ,  C07H15/252 ,  C07D309/10

    CPC分类号： C07H13/04 ,  C07C31/42 ,  C07C43/1786 ,  C07H15/18 ,  C07H15/252

    摘要： Novel anthracycline derivatives have now been produced, which exhibit higher antitumor activities and lower toxicities than those of daunomycin, adriamycin etc. that have been clinically used as anticancer agents. That is, a daunomycinone or adriamycinone derivative represented by the general formula (I): ##STR1## wherein R is a hydrogen atom or a hydroxyl group, and 7-O-(2,6-dideoxy-6,6,6-trifluoro-.alpha.-L-lyxo-hexopyranosyl)adriamycinone derivative which is an adriamycinone derivative represented by formula (II): ##STR2## have now been newly synthesized. The novel anthracycline derivatives having the general formula (I) and formula (II), respectively, show excellent anticancer or antitumor activities and are of low toxicities. These novel compounds are very useful as anticancer or antitumor agents and are expected to be useful for the therapeutic treatments of a variety of cancers and tumors, similarly to daunomycin or adriamycin.

    摘要翻译： 现在已经生产了新的蒽环类衍生物，其具有比已被临床用作抗癌剂的道诺霉素，阿霉素等更高的抗肿瘤活性和更低的毒性。 也就是说，通式（I）表示的道诺霉素酮或阿霉素酮衍生物：其中R是氢原子或羟基，和7-O-（2,6-二脱氧-6,6， 6-三氟-α-L-吡喃半乳糖基）阿霉素酮衍生物，其是由式（II）表示的阿霉素酮衍生物：现在已经新合成。 具有通式（I）和式（II）的新型蒽环类衍生物分别显示出优异的抗癌或抗肿瘤活性，毒性低。 这些新型化合物作为抗癌剂或抗肿瘤剂非常有用，并且预期可用于多种癌症和肿瘤的治疗方法，类似道诺霉素或阿霉素。