Antiparasitic agents

C - Chemistry – Metallurgy – 07 – H

Patent

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167/202, 260/228

C07H 19/01 (2006.01) A01N 43/90 (2006.01) A23K 1/17 (2006.01) A61K 31/70 (2006.01)

Patent

CA 1325208

ABSTRACT "Antiparasitic Avermectin Derivatives" Compounds of the formula: Image (I) wherein the broken line at the 22-23 position represents an optional double bond and wherein either R1 is H or OH and the double bond is absent, or, the double bond is present and R1 is absent; R2 is =CH2 or a group of the formula -(X)-C(R5)=CHR6; R3 is H or CH3: R5 and R6 are both H; R5 is H and R6 is C1-C3 alkyl; or one of R5 and R6 is H and the other is phenyl, heteroaryl, C2-C6 alkoxycarbonyl or substituted phenyl or heteroaryl wherein said substituent is fluorine, chlorine, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, hydroxy(C1-C4)alkyl, cyano, aminosulphonyl, C2-C6 alkanoyl, C2-C6 alkoxycarbonyl, nitro, trifluoromethyl, trifluoromethoxy, amino or mono or di-C1-C4 alkylamino; and X is a direct bond or is an alkylene group having from 2 to 6 carbon atoms which may be straight or branched-chain; with the proviso that R5 and R6 are not both hydrogen when X is -CH(CH3)CH2-, are broad spectrum antiparasitic agents having utility as anthelmintics, ectoparasiticides, insecticides, acaricides and animal growth promotants.

594739

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