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    Therapeutic agent for liver disease and piperazine derivatives
    42.
    发明公开
    Therapeutic agent for liver disease and piperazine derivatives 失效
    ArzneimittelfürLeberkrankheiten und Piperazin-Derivate。

    公开(公告)号：EP0326379A2

    公开(公告)日：1989-08-02

    申请号：EP89300743.5

    申请日：1989-01-26

    申请人： NIPPON CHEMIPHAR CO., LTD.

    发明人： Masaki, Mitsuo ,  Yamakawa, Tomio ,  Satoh, Masaru ,  Takeda, Hiromitsu ,  Yoshino, Yasushi ,  Matsukura, Hitoshi

    IPC分类号： C07D295/20 ,  C07D311/16 ,  C07H17/075 ,  A61K31/495 ,  A61K31/70

    CPC分类号： C07D295/21 ,  C07D317/60 ,  C07H15/26

    摘要： A therapeutic agent for liver disease contain­ing as an active ingredient a piperazine derivative having the formula:
    wherein, A represents a phenyl, p-benzoquinonyl or cumarinyl group which may have at least one substituent selected from the group consisting of halogen, alkyl, fluoroalkyl, formyl, alkoxycarbonyl, acyl, hydroxy, alkoxy, acyloxy, glycosyloxy, amino, alkylamino, mercapto, alkylthio and nitro; B represents a single bond or a straight chain alkylene group containing 1-4 carbon atoms which may have at least one substituent selected from the group consisting of alkyl, aryl, aralkyl, hydroxy and oxo; R represents an atom or a group selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, alkyl, cycloalkyl, aralkyl and aryl; and n is 2 or 3, or its pharmaceutically acceptable salt is diclosed.

    摘要翻译： 含有下式的哌嗪衍生物作为活性成分的肝病治疗剂：其中，A表示可具有选自卤素，烷基，芳基， 氟烷基，甲酰基，烷氧基羰基，酰基，羟基，烷氧基，酰氧基，糖氧基，氨基，烷基氨基，巯基，烷硫基和硝基; B表示单键或含有1-4个碳原子的直链亚烷基，其可以具有至少一个选自烷基，芳基，芳烷基，羟基和氧代的取代基; R表示选自氢，碱金属，碱土金属，烷基，环烷基，芳烷基和芳基的原子或基团; 并且n为2或3，或其药学上可接受的盐被包围。

    PROCESS FOR THE ATTACHMENT OF A GALNAC MOIETY COMPRISING A (HETERO)ARYL GROUP TO A GLCNAC MOIETY, AND PRODUCT OBTAINED THEREBY
    48.
    发明公开
    PROCESS FOR THE ATTACHMENT OF A GALNAC MOIETY COMPRISING A (HETERO)ARYL GROUP TO A GLCNAC MOIETY, AND PRODUCT OBTAINED THEREBY 审中-公开
    方法用于结合的GalNAc COMPONENT A（杂）芳基AT A的GalNAc COMPONENT从而GOT PRODUCT

    公开(公告)号：EP3097200A1

    公开(公告)日：2016-11-30

    申请号：EP15704105.4

    申请日：2015-01-26

    申请人： SynAffix B.V.

    发明人： VAN DELFT, Floris Louis ,  VAN GEEL, Remon ,  WIJDEVEN, Maria Antonia ,  HEESBEEN, Ryan

    IPC分类号： C12P19/18 ,  C07H17/075 ,  C07H19/10 ,  C07K16/00 ,  C07K19/00

    CPC分类号： C12P19/18 ,  C07H17/075 ,  C07H19/06 ,  C07H19/10 ,  C07K16/22 ,  C07K16/241 ,  C07K16/2863 ,  C07K16/30 ,  C07K16/32 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/41 ,  C07K2317/76 ,  C12N9/1051 ,  C12P19/305 ,  C12P21/005 ,  C12Y204/01

    摘要： The present invention relates to a process for attaching an N-acetylgalactosamine- (hetero)arylmoiety to an N-acetylglucosaminemoiety, the process comprising the step of contacting the N-acetylgalactosamine-(hetero)arylmoiety with the N- acetylglucosaminemoiety in the presence of a mutant galactosyltransferase, wherein the N-acetylglucosaminemoiety is according to Formula (1)the N- acetylgalactosamine-(hetero)arylmoiety is according to Formula (2): In a particularly preferred embodiment of the process according to the invention, the N-acetylgalactosamine-(hetero)arylmoiety comprises a 1,3-dipole functional group, and the N-acetylglucosaminemoiety is a terminal GlcNAc moiety of a glycoprotein glycan. The invention further relates to a productobtainable by the process according to the invention, in particular to glycoproteins. Also, the invention relates to several compounds comprising an N-acetylgalactosamine-(hetero)arylmoiety.

    摘要翻译： 本发明涉及一种用于附连到N-acetylgalactosamine-（杂）arylmoiety到N-acetylglucosaminemoiety，该方法包括使与N- acetylglucosaminemoiety的N acetylgalactosamine-（杂）arylmoiety中的存在的步骤 突变体半乳糖转移酶，worin的N acetylglucosaminemoiety是雅丁式（1）的N个acetylgalactosamine-（杂）arylmoiety是雅丁到式（2）：在这个过程中雅丁到本发明的一个特别优选的实施方式中，N-acetylgalactosamine- （杂）arylmoiety包括1.3偶极官能团，并且N acetylglucosaminemoiety是糖蛋白的聚糖的末端GlcNAc部分。 本发明还涉及到一个productobtainable由过程gemäß所述的发明，特别是糖蛋白。 所以，（杂）arylmoiety本发明涉及的几种化合物包含N- acetylgalactosamine-的。