Macrolide compounds, their preparation and their use

C - Chemistry – Metallurgy – 12 – P

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C12P 17/18 (2006.01) A01N 43/90 (2006.01) A01N 49/00 (2006.01) C07H 19/01 (2006.01) C12N 1/20 (2006.01)

Patent

CA 1338050

Compounds with acaricidal, insecticidal and anthelmintic activities have the formula: Image (I) wherein: -X-Y- is selected from the group consisting of -CH2-CH2-, -CH2-CHOH-, -CH=CH-, and -CH2-C(=O)-; R1 is selected from the group consisting of a methyl group, an ethyl group, an isopropyl group, a sec-butyl group and groups of formula -C(CH3)=CHR5 in which R5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group; R2 represents a group of formula -(CH2)n-C(R6)=C(R7)(R8) in which n is 0, 1 or 2, R6 and R7 each is selected from the group consisting of a hydrogen atom and a methyl group and R8 is selected from the group consisting of a hydrogen atom, a C1-4 alkyl group, a phenyl group and a phenyl group substituted with at least one substituent selected from the group consisting of halogen, methyl and nitro substituents; R4 is selected from the group consisting of a hydrogen atom, a methyl group, a hydroxy-protecting group, an ester-forming carboxylic acid residue, and an ester-forming carbonic acid residue; and R4 is selected from the group consisting of a hydrogen atom and an .alpha.-L-oleandrosyl-.alpha.-L- oleandrosyloxy group, with the proviso that R4 represents a hydrogen atom when the group R1 is selected from the group consisting of a methyl group, an ethyl group, and groups of formula -C(CH3)=CHR5 in which R5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group.

554084

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