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    1-N-(4-Amino-3-fluoro-2-hydroxybutyryl)-kanamycins
    11.
    发明公开
    1-N-(4-Amino-3-fluoro-2-hydroxybutyryl)-kanamycins 失效
    1-N-（4-氨基-3-氟-2-羟基丁基）卡那霉素。

    公开(公告)号：EP0285526A2

    公开(公告)日：1988-10-05

    申请号：EP88420066.8

    申请日：1988-02-24

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

    发明人： Umezawa, Sumio ,  Tsuchiya, Tsutomu ,  Takeuchi, Tomio ,  Umezawa, Kazuo ,  Takahashi, Yoshiaki ,  Shitara, Tetsuo ,  Kobayashi, Yoshihiko ,  Takagi, Yasushi

    IPC分类号： C07H15/234 ,  A61K31/70

    CPC分类号： C07H15/234

    摘要： As new compound are now provided ten compounds, namely 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-kanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybuty- ryl}-2',3'-dideoxykanamycin A; 1-N-{(2R,3R)-4-amino-fluoro-2-hydorxybutyryl}-2',3'-dideoxy-2'-fluorokanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin A; 1-N-((2R,3R)-4-amino-fluoro-2-hydrox- ybutyryl}-kanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hy- droxybutyryl}-3'-deoxykanamycin B; 1-N-((2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-3',4'-dideoxykanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydrox- ybutyryl}-5,3'-dideoxy-5-fluorokanamycin B; and 1-N{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5,3',4'-tride- oxy-5-fluorokanamycin B, which are all useful as antibacterial agent in the therapeutic treatment of bacterial infections.

    摘要翻译： 现在提供了新的化合物十个化合物，即1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} - 卡那霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -2'，3'-二脱氧卡那霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -2'，3'-二脱氧-2'-感染甲卡霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5-脱氧-5-氟霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} - 卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -3'-脱氧卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -3'，4'-二脱氧卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5-脱氧-5-氟霉素B; 在B中的1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5,3'-二脱氧-5-氟代烟酰胺; 和1-N（（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5,3'，4'-三脱氧-5-氟卡那霉素B，它们都可用作治疗剂中的抗菌剂 治疗细菌感染。

    5-Deoxy-5-fluorokanamycin B derivatives and processes for the production thereof
    13.
    发明公开
    5-Deoxy-5-fluorokanamycin B derivatives and processes for the production thereof 失效
    5-Deoxy-5-fluorokanamycin-B-Derivate und Verfahren zu ihrer Herstellung。

    公开(公告)号：EP0259014A2

    公开(公告)日：1988-03-09

    申请号：EP87306904.1

    申请日：1987-08-04

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

    发明人： Umezawa, Hamao ,  Umezawa, Sumio ,  Tsuchiya, Tsutomu ,  Shitara, Tetsuo ,  Kobayashi, Yoshihiko

    IPC分类号： C07H15/236 ,  A61K31/70

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： As new compounds are now provided 5-deoxy-5-fluorokanamycin B, 5,3'-dideoxy-5-fluorokanamycin B, 5,4'- dideoxy-5-fluorokanamycin B and 5,3',4'-trideoxy-5-fluorokanamycin B as well as 1-N-(3-amino-2-hydrox- ypropionyl)-or 1-N-(4-amino-2-hydroxybutyryl)-derivatives thereof which are all useful as antibacterial agents and exhibit improved antibacterial activities. These new compounds may be produced by synthetic processes starting from an appropriately N,O-protected 5-epi-kanamycin B, 3'-deoxy-5-epi-kanamycin B, 4'-deoxy-5-epi-kanamycin B or 3',4'-dideoxy-5-epi-kanamycin B derivative which is now prepared by a combination of reaction steps.

    摘要翻译： 由于新化合物现在提供5-脱氧-5-氟乙酰霉素B，5,3'-二脱氧-5-氟沙卡他霉素B，5,4'-二脱氧-5-氟沙卡他霉素B和5,3'，4'-三脱氧-5 - 氟卡那霉素B以及1-N-（3-氨基-2-羟基丙酰基） - 或1-N-（4-氨基-2-羟基丁酰基）衍生物，它们都可用作抗菌剂并表现出改善的抗菌活性。 这些新化合物可以通过合适的方法从合适的N，O-保护的5-表卡那霉素B，3'-脱氧-5-表卡那霉素B，4'-脱氧-5-表卡那霉素B或3 '，4'-双脱氧-5-表卡那霉素B衍生物，其现在通过反应步骤的组合制备。

    1-N-(4-Amino-3-fluoro-2-hydroxybutyryl)-kanamycins
    16.
    发明公开
    1-N-(4-Amino-3-fluoro-2-hydroxybutyryl)-kanamycins 失效
    1-N-（4-氨基-3-氟-2-羟）-kanamycins

    公开(公告)号：EP0285526A3

    公开(公告)日：1991-04-10

    申请号：EP88420066.8

    申请日：1988-02-24

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

    发明人： Umezawa, Sumio ,  Tsuchiya, Tsutomu ,  Takeuchi, Tomio ,  Umezawa, Kazuo ,  Takahashi, Yoshiaki ,  Shitara, Tetsuo ,  Kobayashi, Yoshihiko ,  Takagi, Yasushi

    IPC分类号： C07H15/234 ,  A61K31/70

    CPC分类号： C07H15/234

    摘要： As new compound are now provided ten compounds, namely 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-kanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybuty- ryl}-2',3'-dideoxykanamycin A; 1-N-{(2R,3R)-4-amino-fluoro-2-hydorxybutyryl}-2',3'-dideoxy-2'-fluorokanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin A; 1-N-((2R,3R)-4-amino-fluoro-2-hydrox- ybutyryl}-kanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hy- droxybutyryl}-3'-deoxykanamycin B; 1-N-((2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-3',4'-dideoxykanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydrox- ybutyryl}-5,3'-dideoxy-5-fluorokanamycin B; and 1-N{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5,3',4'-tride- oxy-5-fluorokanamycin B, which are all useful as antibacterial agent in the therapeutic treatment of bacterial infections.

    摘要翻译： 现在提供10种化合物，即1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} - 卡那霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁基} -2'，3'-双脱氧卡那霉素A; 1-N - {（2R，3R）-4-氨基 - 氟-2-羟基丁酰基} -2'，3'-二脱氧-2'-氟尿嘧啶A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5-脱氧-5-氟沙霉素A; 1 -N - （（2R，3R）-4-氨基 - 氟-2-羟基丁酰基} - 卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2- （2R，3R）-4-氨基-3-氟-2-羟丁酰基} -3'，4'-双脱氧卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟丁酰基} 3R）-4-氨基-3-氟-2-羟基丁酰基} -5-脱氧-5-氟沙霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5,3'-二脱氧-5-氟沙霉素B;和1-N {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5,3'，4'-三氧代-5 氟隆霉素B，它们都可用作细菌感染治疗的抗菌剂。

    New anthracycline derivatives, uses thereof as antitumor agent and production thereof
    19.
    发明公开
    New anthracycline derivatives, uses thereof as antitumor agent and production thereof 失效
    Anthracyclinderivate，ihre Verwendung als Antitumorsubstanzen und ihre Herstellung。

    公开(公告)号：EP0230013A1

    公开(公告)日：1987-07-29

    申请号：EP86117662.6

    申请日：1986-12-18

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

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

    IPC分类号： C07H15/252 ,  A61K31/70

    CPC分类号： C07H15/252 ,  Y02P20/55

    摘要： As new anthracycline derivatives are now provided 7-0-(2,6-dideoxy-2-fluoro-a-L-talopyranosyl)-daunomycinone and 7-0-(2,6-dideoxy-2-fluoro-a-L-talopyranosyl)adriamycinone which are useful as antitumor agent and also as antibacterial agent. Briefly, these new compounds may be produced by condensing a 2,6- dideoxy-2-fluoro-a-L-talopyranosyl halide with the 7-hydroxyl group of daunomycinone or adriamycinone.

    摘要翻译： 现在提供新的蒽环类衍生物7-O-（2,6-二脱氧-2-氟-α-L-吡喃葡萄糖基）道诺霉素酮和7-O-（2,6-二脱氧-2-氟-α-L-吡喃葡萄糖基 ）阿霉素，其可用作抗肿瘤剂，也可用作抗菌剂。 简言之，这些新化合物可以通过将2,6-二脱氧-2-氟-α-L-吡喃葡萄糖基卤化物与道诺霉素酮或阿霉素酮的7-羟基缩合来制备。

    Fluorine-containing anthracycline derivatives having hydroxyl group(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof
    20.
    发明公开
    Fluorine-containing anthracycline derivatives having hydroxyl group(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof 失效
    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

    公开(公告)号：EP0761678A1

    公开(公告)日：1997-03-12

    申请号：EP96420288.1

    申请日：1996-09-06

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

    发明人： Takeuchi, Tomio, New Fuji Mansion 701, 1-11 ,  Umezawa, Sumio ,  Tsuchiya, Tsutomu ,  Takagi, Yasushi ,  Sohtome, Hiromi

    IPC分类号： C07H15/252 ,  A61K31/70

    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-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.

    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- -3,4-二-O-氨基烷酰基-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 -L-赖肟基 - 六吡喃糖基）阿霉素酮，其如下所示： - CHEM>其中A 1和A 2中的任一个或两者是或是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和水溶性高度有活性，可用作以可注射溶液形式给药的抗肿瘤剂。