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公开(公告)号:EP1671980B1
公开(公告)日:2011-05-18
申请号:EP06004047.4
申请日:1990-01-17
申请人: Merial Limited
发明人: Fisher, Michael H. , Mrozik, Helmut
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公开(公告)号:EP1671980A2
公开(公告)日:2006-06-21
申请号:EP06004047.4
申请日:1990-01-17
申请人: Merial Limited
发明人: Fisher, Michael H. , Mrozik, Helmut
摘要: Novel avermectin derivatives are disclosed, wherein the 5-hydroxy group is replaced by an oxime group. The avermectin-5-oximes can further be derivatized at the 4"- or 4'-positions as amino, substituted amino, acylhydrazone, semicarbazone, or substituted semicarbazone analogues. The avermectin-5-oximes are prepared by the oxidation of the 5-hydroxy compounds with manganese dioxide or with pyridinium dichromate to the known 5-oxo analogues, and these are then reacted with a hydroxylamine salt. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
摘要翻译: 公开了新的阿维菌素衍生物,其中5-羟基被肟基替代。 阿维菌素-5-肟可以进一步在4“ - 或4'-位被衍生为氨基,取代的氨基,酰腙,缩氨基脲或取代的缩氨基脲类似物,阿维菌素-5-肟通过氧化5- 羟基化合物与二氧化锰或与重铬酸吡啶鎓转化成已知的5-氧代类似物,然后将它们与羟胺盐反应,新化合物是有效的抗寄生虫剂,特别是该化合物是驱虫剂,杀虫剂和杀螨剂。
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公开(公告)号:EP1671980A3
公开(公告)日:2006-07-05
申请号:EP06004047.4
申请日:1990-01-17
申请人: Merial Limited
发明人: Fisher, Michael H. , Mrozik, Helmut
摘要: Novel avermectin derivatives of formula (I) are disclosed, wherein the 5-hydroxy group is replaced by an oxime group. The avermectin-5-oximes can further be derivatized at the 4"- or 4'-positions as amino, substituted amino, acylhydrazone, semicarbazone, or substituted semicarbazone analogues. The avermectin-5-oximes are prepared by the oxidation of the 5-hydroxy compounds with manganese dioxide or with pyridinium dichromate to the known 5-oxo analogues, and these are then reacted with a hydroxylamine salt. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
摘要翻译: 公开了式(I)的新型除虫菊酯衍生物,其中5-羟基被肟基取代。 阿维菌素-5-肟可以在4“或4”位进一步衍生为氨基,取代的氨基,酰腙,缩氨基脲或取代的缩氨基脲类似物。除虫菊酯-5-肟通过氧化5- 具有二氧化锰或与重铬酸吡啶鎓的羟基化合物与已知的5-氧代类似物反应,然后将其与羟胺盐反应。新化合物是有效的抗寄生虫剂,特别是化合物是驱肠虫,杀虫剂和杀螨剂。
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公开(公告)号:EP0379341B1
公开(公告)日:2006-05-10
申请号:EP90300458.8
申请日:1990-01-17
申请人: Merial Limited
发明人: Fisher, Michael H. , Mrozik, Helmut
IPC分类号: C07H17/08 , C07D493/22 , A61K31/70 , A01N43/90 , C07D313/00 , C07D311/00 , C07D307/00
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