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    Use of cyclic depsipeptides having 12 ring atoms for combating endoparasites, new cyclic despipeptides having 12 ring atoms, and processes for their preparation
    15.
    发明授权
    Use of cyclic depsipeptides having 12 ring atoms for combating endoparasites, new cyclic despipeptides having 12 ring atoms, and processes for their preparation 失效
    具有12个环原子的环状缩水甘油醚与具有12个环原子的新环状脱磷酸酯的反应的内源寄生虫的使用及其制备方法

    公开(公告)号：US5663140A

    公开(公告)日：1997-09-02

    申请号：US372543

    申请日：1995-01-13

    Applicant: Jurgen Scherkenbeck ,  Peter Jeschke ,  Andrew Plant ,  Achim Harder ,  Norbert Mencke

    Inventor： Jurgen Scherkenbeck ,  Peter Jeschke ,  Andrew Plant ,  Achim Harder ,  Norbert Mencke

    IPC: A61K31/33 ,  A61K31/38 ,  A61K31/41 ,  A61K38/00 ,  A61P33/00 ,  A61P33/10 ,  C07D273/00 ,  C07D273/08 ,  C07D413/06 ,  C07K11/02 ,  A61K35/78

    CPC classification number: C07D273/00 ,  A61K31/33 ,  A61K31/38 ,  C07D413/06

    Abstract: The present invention relates to the use of cyclic depsipeptides having 12 ring atoms of the general formula (I) ##STR1## in which R.sup.1 and R.sup.4 independently of one another represent hydrogen, straight-chain or branched alkyl, cycloalkyl, aralkyl, aryl, heteroaryl or heteroarylalkyl, each of which is optionally substituted,R.sup.2, R.sup.3, R.sup.5 and R.sup.6 independently of one another represent hydrogen, straight-chain or branched alkyl having up to 8 carbon atoms, halogenoalkyl, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carbamoylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, guanidinoalkyl which can optionally be substituted by one or two benzyloxycarbonyl radicals or by one, two, three or four alkyl radicals, alkoxycarbonylaminoalkyl, 9-fluorenylmethoxycarbonyl(Fmoc)aminoalkyl, alkenyl, cycloalkyl, cycloalkylalkyl, and optionally substituted aryl, arylalkyl, heteroaryl and heteroarylalkyl, and their optical isomers and racemates,in medicine and veterinary medicine for combating endoparasites, to new depsipeptides having 12 ring atoms, and to processes for their preparation.

    Abstract translation: 本发明涉及具有通式（I）的12个环原子的环状缩水甘油酯的用途，其中R 1和R 4彼此独立地表示氢，直链或支链烷基，环烷基，芳烷基， 芳基，杂芳基或杂芳基烷基，其各自任选被取代，R 2，R 3，R 5和R 6彼此独立地表示氢，具有至多8个碳原子的直链或支链烷基，卤代烷基，羟烷基，烷酰氧基烷基，烷氧基烷基，芳氧基烷基， 烷基磺酰基烷基，烷基亚磺酰基烷基，烷基磺酰基烷基，羧基烷基，烷氧基羰基烷基，芳基烷氧基羰基烷基，氨基甲酰基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，胍基烷基，其可以任选被一个或两个苄氧基羰基取代或被一个，二个，三个或四个烷基取代，烷氧基羰基氨基烷基， 芴基甲氧基羰基（Fmoc）氨基烷基，烯基，环烷基，环烷基烷基和任选取代的a 芳基烷基，杂芳基和杂芳基烷基，以及它们的光学异构体和外消旋体，在用于抗内寄生物的医药和兽医学中，具有12个环原子的新的缩肽，以及它们的制备方法。

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