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35 条记录 (耗时 0.022 秒)

    GEMCITABINE DERIVATIVES
    13.
    发明申请
    GEMCITABINE DERIVATIVES 有权
    化学药剂衍生物

    公开(公告)号：US20020042391A1

    公开(公告)日：2002-04-11

    申请号：US09355112

    申请日：1999-09-15

    发明人： FINN MYHREN ,  BERNT BORRETZEN ,  ARE DALEN ,  MARIT LILAND SANDVOLD

    IPC分类号： C07H019/00 ,  C07H019/048 ,  C07H019/09 ,  C07H019/073 ,  A61K031/70

    CPC分类号： C07H19/06

    摘要： The invention provides Gemcitabine esters or amides in which the 3null- and/or 5null-OH group and/or the N4-amino group is derivatised with a C18- and/or C20-saturated or mono-unsaturated acyl group, preferably an acyl group selected from oleoyl, elaidoyl, cis-eicosenioyl and trans-eicosenoyl. The Gemcitabine esters and amides are useful as anti-cancer and anti-viral agents.

    摘要翻译： 本发明提供吉西他滨酯或酰胺，其中3'-和/或5'-羟基和/或N 4 - 氨基被C 18 - 和/或C 20饱和或单不饱和酰基衍生，优选为 酰基选自油酰基，反酰基，顺式 - 二十碳烯酰基和反式二十碳烯酰基。 吉西他滨酯和酰胺可用作抗癌和抗病毒剂。

    Pharmaceutically active uridine esters
    14.
    发明申请
    Pharmaceutically active uridine esters 失效
    药学活性尿苷酯

    公开(公告)号：US20040121979A1

    公开(公告)日：2004-06-24

    申请号：US10476287

    申请日：2003-10-29

    发明人： Rudy Susilo

    IPC分类号： A61K031/7072 ,  C07H019/067 ,  C07H019/073

    CPC分类号： C07H19/06 ,  A61K31/20 ,  A61K31/385 ,  A61K31/7072 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to novel uridine esters of the general formula (I) wherein R represents a carboxylic acid residue, preferably a fatty acid residue and Rnull represents hydrogen or a hydroxy group, their use as pharmaceutically active agents against a variety of diseases, methods for the preparation of said uridine esters and pharmaceutical compositions containing at least one uridine ester as active ingredient. The present invention relates also to a drug combination comprising free fatty acids and/or fatty acid esters and uridine, deoxyuridine, uridine monophosphate and/or deoxyuridine monophosphate, and to the use of such a drug combination. 1

    摘要翻译： 本发明涉及通式（I）的新型尿苷酯，其中R代表羧酸残基，优选脂肪酸残基，R'代表氢或羟基，它们作为药物活性剂用于各种疾病， 用于制备所述尿苷酯的方法和含有至少一种尿苷酯作为活性成分的药物组合物。 本发明还涉及包含游离脂肪酸和/或脂肪酸酯和尿苷，脱氧尿苷，单磷酸尿苷和/或脱氧尿苷单磷酸酯的药物组合，以及这种药物组合的用途。

    L-nucleic acid derivative and processes for the synthesis thereof
    15.
    发明申请
    L-nucleic acid derivative and processes for the synthesis thereof 有权
    L-核酸衍生物及其合成方法

    公开(公告)号：US20040063926A1

    公开(公告)日：2004-04-01

    申请号：US10433004

    申请日：2003-05-29

    发明人： Hajime Iizuka ,  Kazuhiko Togashi ,  Tsuneji Suzuki

    IPC分类号： C07H019/073

    CPC分类号： C07D498/04 ,  C07D498/14 ,  C07H9/06 ,  C07H19/06 ,  C07H19/073 ,  C07H19/09

    摘要： A novel method has been found to produce 2,2null-anhydro-1-(null-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2null-anhydro-1-(null-L-arabinofuranosyl)thymine. A novel method has been further found to L-2null-deoxyribose derivatives as a useful synthetic intermediate through L-2,2null-anhydro-5,6-dihydrocyclouridine derivative. According to these methods, synthesis of various L-nucleic acid derivatives, synthesis of which has been difficult till now.

    摘要翻译： 已经发现一种新的方法生产2,2'-脱水-1-（β-L-阿拉伯呋喃糖基）胸腺嘧啶作为新的有用的中间体化合物。 已经进一步发现一种从2,2'-脱水-1-（β-L-阿拉伯呋喃糖基）胸腺嘧啶产生胸苷的新方法。 通过L-2,2'-脱水-5,6-二氢环尿苷衍生物，进一步发现L-2'-脱氧核糖衍生物作为有用的合成中间体的新方法。 根据这些方法，合成各种L-核酸衍生物，其合成迄今难以实现。

    Uridine derivatives as antibiotics
    18.
    发明申请
    Uridine derivatives as antibiotics 有权
    尿苷衍生物作为抗生素

    公开(公告)号：US20030130227A1

    公开(公告)日：2003-07-10

    申请号：US10258759

    申请日：2002-10-25

    发明人： Jozsef Aszodi ,  Christophe Dini ,  Jean-Claude Guillot ,  Stanislas Didierlaurent ,  Nathalie Drochon ,  Jidong Zhang

    IPC分类号： A61K031/7072 ,  C07H019/06 ,  C07H019/067 ,  C07H019/073

    CPC分类号： C07H15/18 ,  C07H19/06

    摘要： The invention concerns compounds of formula (I) wherein: R2 is hydrogen, halogen, alkyl, alkenyl or alkynyl, a OH, O-alkyl, OCO-alkyl radical, an O-aryl or OCO-aryl radical; R4 is CH2NH2; CH2NHalkyl, CH2N(alkyl1)(alkyl2), CH2-guanidine, CH2-amidine optionally substituted; R5 represents in particular (a) or (b) or (c) or (d), a CH2N3 radical (e); R8 is hydrogen or alkyl; R9 is alkyl, aryl or heteroaryl, R8 and R9 capable of forming a heterocycle, or R5 represents a CH2alkyl, CH2Oalkyl or CO2alkyl, CH2Salkyl radical; R6 is hydrogen or halogen, OH, Oalkyl, OCOalkyl, S-alkyl or S-aryl; R7 is hydrogen or OH. The compounds of formula (I) exhibit antibiotic properties.

    摘要翻译： 本发明涉及式（I）的化合物，其中：R 2是氢，卤素，烷基，烯基或炔基，OH，O-烷基，OCO-烷基，O-芳基或OCO-芳基; R4是CH2NH2; CH2NH烷基，CH2N（烷基）（烷基2），CH2-胍，任选取代的CH2-脒基; R 5特别表示（a）或（b）或（c）或（d），CH 2 N 3基团（e）; R8是氢或烷基; R9是能够形成杂环的烷基，芳基或杂芳基，R 8和R 9，或R 5表示CH 2烷基，CH 2烷基或CO 2烷基，CH 2 S烷基; R 6是氢或卤素，OH，O烷基，OCO烷基，S-烷基或S-芳基; R7是氢或OH。 式（I）化合物具有抗生素特性。

    Drugs for the diagnosis of tissue-reproductive activity or the treatment of proliferative diseases
    19.
    发明申请
    Drugs for the diagnosis of tissue-reproductive activity or the treatment of proliferative diseases 有权
    药物用于诊断组织生殖活性或治疗增殖性疾病

    公开(公告)号：US20030124054A1

    公开(公告)日：2003-07-03

    申请号：US10239355

    申请日：2002-09-23

    发明人： Jun Toyohara ,  Akio Hayashi

    IPC分类号： A61K051/00 ,  C07H019/073 ,  A61K031/7072 ,  A61K031/513 ,  C07D43/04

    CPC分类号： A61K51/0491 ,  C07H19/06

    摘要： An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: 1 wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1-8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

    摘要翻译： 作为活性成分含有由下式表示的放射性标记化合物或其药学上可接受的盐的试剂，其中R1表示氢或具有1-8个碳原子的直链或支链烷基，R2表示 氢，羟基或卤素取代基，R3表示氢或氟取代基，R4表示氧，硫或亚甲基取代基，R5表示放射性卤素取代基。 该试剂在体内是稳定的，并且停留在细胞中或被并入DNA中，从而用于诊断组织增生活性或治疗增殖性疾病。

    Process for the preparation of 2'-halo-beta-L-arabinofuranosyl nucleosides
    20.
    发明申请
    Process for the preparation of 2'-halo-beta-L-arabinofuranosyl nucleosides 有权
    制备2'-卤代-β-L-阿拉伯呋喃糖苷的方法

    公开(公告)号：US20030060622A1

    公开(公告)日：2003-03-27

    申请号：US10112403

    申请日：2002-03-29

    发明人： Marcos Sznaidman

    IPC分类号： C07H019/19 ,  C07H019/06 ,  C07H019/067 ,  C07H019/073 ,  C07H019/09

    CPC分类号： C07H15/04 ,  C07H19/06

    摘要： The present invention is directed to the process for the preparation of 2null-deoxy-2null-halo-null-L-arabinofuranosyl nucleosides, and in particular, 2null-deoxy-2null-fluoro-null-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and less expensive than L-ribose or L-xylose, in ten steps. All of the reagents and starting materials are inexpensive and no special equipment is required to carry out the reactions.

    摘要翻译： 本发明涉及2'-脱氧-2'-卤-β-L-阿拉伯呋喃糖基核苷的制备方法，特别是2'-脱氧-2'-氟-β-L-阿拉伯呋喃糖基胸腺嘧啶 L-FMAU），来自L-阿拉伯糖，其可商购并且比L-核糖或L-木糖便宜，分为十个步骤。 所有的试剂和原料都是廉价的，不需要特殊的设备来进行反应。