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    Synthesis of twelve member diazamonocyclic compounds
    4.
    发明公开
    Synthesis of twelve member diazamonocyclic compounds 失效
    Synthesezwölfgliedrigerdiazamonocyclischer Verbindungen。

    公开(公告)号：EP0321199A2

    公开(公告)日：1989-06-21

    申请号：EP88311810.1

    申请日：1988-12-14

    申请人： Bayer Corporation

    发明人： Czech, Bronislaw P.

    IPC分类号： C07D273/00 ,  C07D291/02

    CPC分类号： C07D273/00 ,  C07D291/02 ,  G01N27/3335

    摘要： Compounds opf formula I
    are made by mixing a solution of a compound of formula II
    with a solution of a compound of formula III
    wherein each A is independently N-R, O, S, CRR′ or P(O)R, and each R and R′ is hydrogen, alkyl, alkylidene, aryl, tosyl, allyl or benzyl; and B is O.
    Compounds of formula I are reduced to form an azacorand of formula IV
    wherein each K and l are N-R, O, S, CRR′, or P(O)R, and R and R′ are hydrogen, alkyl, alkylidene, aryl, tosyl, allyl or benzyl.

    摘要翻译： 通过将式II化合物的溶液与式III化合物的溶液混合而制备化合物，其中每个A独立地是NR，O，S，CRR min或P（ O）R，每个R和R min是氢，烷基，亚烷基，芳基，甲苯磺酰基，烯丙基或苄基; 式I的化合物被还原形成式IV的化学式（CHEM），其中每个K和l是NR，O，S，CRR min或P（O）R，R和R min是氢 ，烷基，亚烷基，芳基，甲苯磺酰基，烯丙基或苄基。

    Cryptophycin derivatives and their use as anti-microtubule agents
    8.
    发明公开
    Cryptophycin derivatives and their use as anti-microtubule agents 失效
    Cryptophycinderivate und ihre Verwendung als antimikrotubuli Mittel

    公开(公告)号：EP0792875A1

    公开(公告)日：1997-09-03

    申请号：EP97301272.7

    申请日：1997-02-26

    申请人： ELI LILLY AND COMPANY ,  UNIVERSITY OF HAWAII ,  Wayne State University

    发明人： Norman, Bryan Hurst ,  Shih, Chuan ,  Kroin, Julian Stanley

    IPC分类号： C07D255/02 ,  C07D257/02 ,  C07D273/02 ,  C07D273/08 ,  C07D273/00 ,  C07D285/00 ,  C07D291/02 ,  C07D413/06 ,  C07D417/06 ,  C07D419/06 ,  A61K31/395

    CPC分类号： C07D273/00 ,  C07D273/02 ,  C07D413/06

    摘要： The invention provides novel cryptophycin compounds which can be useful for disrupting the microtubulin system, as antineoplastic agents, and for the treatment of cancer. The invention further provides a formulation for administering the novel cryptophycin compounds. The compounds are of the formula
    wherein

    Ar is phenyl or any simple unsubstituted or substituted aromatic or heteroaromatic group;
    R 1 is halogen, SH, amino, monoalkylamino, dialkylamino, trialkylammonium, alkylthio, dialkylsulfonium, sulfate, or phosphate;
    R 2 is OH or SH; or
    R 1 and R 2 may be taken together to form an epoxide ring, and aziridine ring, an episulfide ring, a sulfate ring, or monoalkylphosphate ring; or
    R 1 and R 2 may be taken together to form a second bond between C 18 and C 19 ;
    R 3 is a lower alkyl group;
    R 4 is H;
    R 5 is H;
    R 4 and R 5 may be taken together to form a second bond between C 13 and C 14 ;
    R 6 is benzyl, hydroxybenzyl, alkoxybenzyl, halohydroxybenzyl, dihalohydroxybenzyl, haloalkoxybenzyl, or dihaloalkoxybenzyl group;
    R 7 is H or a lower alkyl group;
    R 8 is H or a lower alkyl group; or
    R 7 and R 8 may optionally be taken together to form a cyclopropyl ring;
    R 9 is selected from the group consisting of H, a lower alkyl group, (C 1 -C 3 ) alkylaryl, and aryl;
    R 10 is selected from the group consisting of H, a lower alkyl group, (C 1 -C 3 ) alkylaryl, and aryl;
    R 11 is H; simple alkyl; phenyl, substituted phenyl, benzyl, substituted benzyl;
    X is O, NH or alkylamino;
    Y is C, O, NH, S, SO, SO 2 or alkylamino; and
    a pharmaceutically acceptable salt or solvate thereof.

    摘要翻译： 本发明提供了可用于破坏微管蛋白系统作为抗肿瘤药物和用于治疗癌症的新颖的cryptophycin化合物。 本发明还提供了一种用于施用新型cryptophycin化合物的制剂。 所述化合物具有式CHEM，其中Ar是苯基或任何简单的未取代或取代的芳族或杂芳基; R 1是卤素，SH，氨基，一烷基氨基，二烷基氨基，三烷基铵，烷硫基，二烷基锍，硫酸盐或磷酸盐; R 2是OH或SH; 或R 1和R 2可以一起形成环氧化物环，氮丙啶环，环硫醚环，硫酸酯环或磷酸单烷基酯环; 或R 1和R 2可以一起形成C 18和C 19之间的第二个键; R 3是低级烷基; R 4为H; R 5为H; R 4和R 5可以一起形成C13和C14之间的第二键; R 6是苄基，羟基苄基，烷氧基苄基，卤代羟基苄基，二卤代羟基苄基，卤代烷氧基苄基或二卤代烷氧基苄基; R 7是H或低级烷基; R 8是H或低级烷基; 或R 7和R 8可以任选地一起形成环丙基环; R 9选自H，低级烷基，（C 1 -C 3）烷基芳基和芳基; R 10选自H，低级烷基，（C 1 -C 3）烷基芳基和芳基; R 11是H; 简单烷基; 苯基，取代的苯基，苄基，取代的苄基; X是O，NH或烷基氨基; Y是C，O，NH，S，SO，SO 2或烷基氨基; 及其药学上可接受的盐或溶剂合物。

    Synthesis of twelve member diazamonocyclic compounds
    9.
    发明公开
    Synthesis of twelve member diazamonocyclic compounds 失效
    双组份二氮杂环化合物的合成

    公开(公告)号：EP0321199A3

    公开(公告)日：1990-05-02

    申请号：EP88311810.1

    申请日：1988-12-14

    申请人： Bayer Corporation

    发明人： Czech, Bronislaw P.

    IPC分类号： C07D273/00 ,  C07D291/02

    CPC分类号： C07D273/00 ,  C07D291/02 ,  G01N27/3335

    摘要： Compounds opf formula I
    are made by mixing a solution of a compound of formula II
    with a solution of a compound of formula III
    wherein each A is independently N-R, O, S, CRR′ or P(O)R, and each R and R′ is hydrogen, alkyl, alkylidene, aryl, tosyl, allyl or benzyl; and B is O. Compounds of formula I are reduced to form an azacorand of formula IV
    wherein each K and l are N-R, O, S, CRR′, or P(O)R, and R and R′ are hydrogen, alkyl, alkylidene, aryl, tosyl, allyl or benzyl.

    Composition comprising a macrocyclic compound and an organic acid and its use in metal extraction
    10.
    发明公开
    Composition comprising a macrocyclic compound and an organic acid and its use in metal extraction 失效
    含有大环化合物和有机酸，以及它们用于金属的回收利用混合物。

    公开(公告)号：EP0355045A2

    公开(公告)日：1990-02-21

    申请号：EP89306913.8

    申请日：1989-07-07

    申请人： ZENECA LIMITED

    发明人： Lindoy, Leonard Francis ,  Baldwin, Darren Sylvester ,  Tasker, Peter Anthony

    IPC分类号： C07D273/00 ,  C07D285/00 ,  C07D291/02 ,  C22B3/00

    CPC分类号： C07D273/00 ,  C01G3/003 ,  C01G5/003 ,  C07D285/00 ,  C07D291/02 ,  C22B3/0008 ,  Y02P10/234

    摘要： A composition comprising a chelating compound which is a macrocyclic compound containing at least two coordinating centres in the ring, at least one of which is a neutral base moiety, and an organic acid containing at least one akyl or alkenyl group containing 8 or more carbon atoms. The macrocyclic compound contains at least 10 ring atoms and especially at least 12 ring atoms. The neutral base moitey is typically a nitrogen moiety. Preferably there are at least four coordinating centres at least two of which are neutral base moieties. The acid can be an alkyl or alkenyl substituted acid for example a long chain carboxylic acid. The composition can be used as an extractant system for the selective extraction of metals from an aqueous phase into an organic phase.

    摘要翻译： 包含螯合化合物的所有这是在环中含有至少两个配位中心，包含含有8个或更多碳原子的至少一个akyl或链烯基，所有这些是中性碱基部分的至少一种，和有机酸的大环化合物的组合物 ， 所述大环化合物包含至少10原子环和爱尤其是至少12原子环。 中性基moitey通常是氮部分。 优选地，存在至少四个协调中心，其中至少两个是中性碱基部分。 所述酸可以是烷基或链烯基酸substituiertem例如长链羧酸。 该组合物可被用作到萃取剂体系，用于从wässrige相金属的选择性萃取到有机相中。