C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/01 (2006.01) A01N 43/90 (2006.01) A61K 31/70 (2006.01) C07D 493/22 (2006.01)
Patent
CA 2118491
Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are also disclosed which incorporate two fluorine atoms at position 13 or 23. These difluoro avermectin analogs are derived from corresponding ketones and enones which in turn are prepared by chemical modification of naturally occurring avermectins. These compounds are used as antiparisitic; insecticidal and antihelmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.
L'invention décrit des dérivés d'avermectine comportant deux atomes de fluor à la position 4' de monosaccharide, à la position 4'' de disaccharide ou à la position 23. L'invention décrit également des dérivés d'aglycone d'avermectine comportant deux atomes de fluor à la position 13 ou 23. Ces analogues difluoro d'avermectine sont dérivés de cétones et d'énones correspondants préparés eux-mêmes par modification chimique d'avermectines naturelles. On utilise ces composés en tant qu'agents antiparasites, insecticides et antihelminthiques chez l'homme et l'animal. L'invention décrit également des compositions contenant lesdits composés en tant qu'ingrédient actif.
Fisher Michael H.
Meinke Peter T.
Mrozik Helmut
Merck Sharp & Dohme Corp.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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