Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1989-02-13
1990-01-30
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
536 71, 549209, A61K 3171, C07H 1708
Patent
active
048973831
ABSTRACT:
There are disclosed novel avermectin derivatives wherein the 3"- or 3'-methoxy group and/or the 4"- or 4'-hydroxyl group are replaced by hydrogen. The 3"- or 3'-desmethoxy-avermectins can further be derivatized at the 4"- or 4'-positions as the amino, semicarbazone or oxime analogs. The 3"- or 3'-desmethoxy-avermectins are prepared by the reaction of Samarium iodide on the corresponding 4"- or 4'-oxo-avermectins. The 4"- or 4'-deoxo-avermectins are prepared by radical deoxygenation of the corresponding hydroxy-avermectins. Di-deoxygenated avermectin derivatives are obtained by combination of these two methods or by treating avermectin aglycone or avermectin monosaccharide with a dihydropyran. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
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Merck & Co. , Inc.
Pfeiffer Hesna J.
Raymond Richard L.
Rose David L.
Russell Mark W.
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