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    4-O-(aminoglycosyl)- or 4,6-di-O-(aminoglycosyl)-2,5-dideoxy-5,5-difluorostreptamine derivatives
    2.
    发明授权
    4-O-(aminoglycosyl)- or 4,6-di-O-(aminoglycosyl)-2,5-dideoxy-5,5-difluorostreptamine derivatives 失效
    4-O-（氨基糖基） - 或4,6-二-O-（氨基糖基）-2,5-二脱氧-5,5-二氟色胺衍生物

    公开(公告)号：US5527781A

    公开(公告)日：1996-06-18

    申请号：US39447

    申请日：1993-04-21

    申请人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tetsuo Shitara ,  Shunzo Fukatsu ,  Eijiro Umemura

    发明人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tetsuo Shitara ,  Shunzo Fukatsu ,  Eijiro Umemura

    IPC分类号： A01N43/16 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/224 ,  C07H15/234 ,  C07H15/236 ,  C07H15/22

    CPC分类号： C07H15/224 ,  C07H15/234 ,  C07H15/236 ,  Y02P20/55

    摘要： As new compounds are now synthetized 5-deoxy-5,5-difluoro derivatives of aminoglycosidic antibiotics of neamine, kanamycin A-series, kanamycin B-series, gentamicin-series and seldomycin-series. Further, the 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives are synthetized from 5-deoxy-5,5-difluorokanamycins A and B, as well as their analogues now obtained. The 5-deoxy-5,5-difluoro derivatives of the aminoglycosidic antibiotics now provided according to this invention have such antibacterial activities enhanced much more than or equal to those of the respectively corresponding parent aminoglycosidic antibiotics, while these 5-deoxy-5,5-difluoro derivatives exhibit values of the 50% lethal dosage (LD.sub.50) which are improved remarkably better when they are intravenously administered to mice, so that they have remarkedly reduced toxicities to mammals.

    摘要翻译： PCT No.PCT / JP91 / 01115 Sec。 371日期：1993年4月21日 102（e）日期1993年4月21日PCT 1991年8月22日提交PCT公布。 出版物WO92 / 03460 日期为199年3月3日。作为新化合物，目前合成了新胺，卡那霉素A系列，卡那霉素B系列，庆大霉素系列和青霉素系列氨基糖苷类抗生素的5-脱氧-5,5-二氟衍生物。 此外，1-N-（α-羟基ω-氨基烷酰基）衍生物由5-脱氧-5,5-二氟吗啉霉素A和B以及它们现在获得的类似物合成。 现在根据本发明提供的氨基糖苷类抗生素的5-脱氧-5,5-二氟衍生物具有比分别对应的母体氨基糖苷类抗生素的这些抗菌活性更强或更多的抗菌活性，而这些5-脱氧-5,5 二氟衍生物显示50％致死剂量（LD50）的值，当它们静脉内施用于小鼠时，其显着改善，从而显着降低对哺乳动物的毒性。

    Anthracycline derivatives having 4-amino-2,4,6-trideoxy-2 fluoro-&agr;-L-talopyranosyl group
    6.
    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
    7.
    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。

    Fluorine-containing anthracycline derivatives having hydroxyl groups(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof
    9.
    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。

    Process for the preparation of 2'-deoxy-2'-halocoformycins or steroisomers thereof
    10.
    发明授权
    Process for the preparation of 2'-deoxy-2'-halocoformycins or steroisomers thereof 失效
    制备2'-脱氧-2'-卤代环霉素或其立体异构体的方法

    公开(公告)号：US5831072A

    公开(公告)日：1998-11-03

    申请号：US808033

    申请日：1997-03-04

    申请人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

    发明人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

    IPC分类号： C07D487/04 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7056 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07H19/04 ,  C07H19/052 ,  C07H19/23

    CPC分类号： C07H19/052 ,  C07H19/23

    摘要： An object of this invention is to provide a novel process for the synthesis of a 2'-deoxy-2'-halocoformycin having an inhibitory activity against adenosine deaminase in a practically high yield. Thus, there is provided a process comprising multi-stage reactions with using as the starting intermediate a tert-butyl 1-(3,5-di-O-acyl-2-deoxy-2-halo-.beta.-D-ribofuranosyl or arabinofuranosyl)-5-aminoimidazole-4-carboxylate of formula (II) ##STR1## whereby there are produced a 2'-deoxy-2'-halocoformycin or a 2'-deoxy-2'-epi-2'-halocoformycin of formula (I-a) ##STR2## and also a 2'-deoxy-8-epi-2'-halocoformycin or a 2'-deoxy-8,2'-diepi-2'-halocoformycin of formula (I-b) ##STR3## It is expectable that a 2'-deoxy-2'-halocoformycin and epimers thereof are useful as a drug for lymphocytic leukemias and as drugs for various diseases attributable to the actions of adenosine deaminase.

    摘要翻译： 本发明的目的是提供一种以实际高产率合成具有抑制腺苷脱氨酶活性的2'-脱氧-2'-卤代霉素的新方法。 因此，提供一种包含多级反应的方法，其用作起始中间体是1-（3,5-二-O-酰基-2-脱氧-2-卤代-β-呋喃核糖基或阿拉伯呋喃糖基） ）式（II）的5-氨基咪唑-4-羧酸甲酯（II），由此制备2'-脱氧-2'-卤代霉素或2'-脱氧-2'-表 - 2'-卤代霉素 的式（Ia）化合物（Ia）以及式（Ib）的2'-脱氧-8-表 - 2'-卤代霉素或2'-脱氧-8,2'-二哌啶-2'-卤代霉素， （Ib）预期2'-脱氧-2'-卤代霉素及其差向异构体可用作淋巴细胞性白血病药物和作为可归因于腺苷脱氨酶作用的各种疾病的药物。