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New antiparasitic agent derivatives of milbemycin and avermectin

机译:米尔贝霉素和阿维菌素的新型抗寄生虫药衍生物

摘要

Antiparasitic compounds of formula (I) wherein the broken line at the 22-23 position represents an optional bond and either this bond is present and R1 is absent or this bond is absent and R1 is H, OH, oxo or oximino optionally substituted by C1-C8 alkyl group, R2 is C1-C8 alkyl, C2-C8 alkenyl or C3-C8 cycloalkyl group, or a 3- to 6- membered heterocyclic ring containing a sulphur or oxygen atom, said ring being saturated or fully or partially unsaturated and optionally substituted by one or more C1-C4 alkyl groups or halogen atoms, R3 is H or OH, and R4 is H or a group capable of being hydrolyzed in vivo to yield a compound in which R4 is H, R5 is OH, optionally substituted with a group capable of being hydrolyzed in vivo to yield a compound in which R5 is OH, and R6 is H or C1-C4 alkyl or R6 is H and R5 is amino, optionally substituted with at least one group selected from C1-C8 alkyl and acyl groups.
机译:式(I)的抗寄生虫化合物,其中在22-23位的虚线表示任选的键,并且该键存在且R 1不存在或该键不存在且R 1为H,OH,氧代其中R 2是C 1 -C 8烷基,C 2 -C 8烯基或C 3 -C 8环烷基,或含有硫或氧原子的3至6元杂环,或任选被C 1 -C 8烷基取代的肟基。环是饱和的或完全或部分不饱和的,并且任选地被一个或多个C 1 -C 4烷基或卤素原子取代,R 3是H或OH,并且R 4是H或能够在体内水解成氢的基团产生其中R 4为H,R 5为OH的化合物,任选地被能够在体内水解的基团取代以产生其中R 5为OH且R 6为H的化合物或C 1 -C 4烷基或R 6为H且R 5为氨基,任选地被选自C 1 -C 8烷基和酰基中的至少一个取代。

著录项

  • 公开/公告号DE10075003I1

    专利类型

  • 公开/公告日2000-06-29

    原文格式PDF

  • 申请/专利权人 PFIZER US;

    申请/专利号DE2000175003C

  • 申请日1994-01-12

  • 分类号C07H19/01;

  • 国家 DE

  • 入库时间 2022-08-22 01:41:55

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