13-substituted milbemycin 5-oxime derivatives, their preparation

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514183, 514274, 514338, 514321, 514369, 514376, 514422, 514444, 549264, 549 60, 544316, 548187, 548229, 548526, 548952, 546197, 5462817, 5462831, A61K 31335, A61K 3138, A61K 31505, A61K 31425

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active

058614290

ABSTRACT:
Compounds of formula (I): ##STR1## wherein: R.sup.1 is methyl, ethyl, isopropyl or sec-butyl; X is carbonyl or methylene; Z is .dbd.C.dbd.(R.sup.2).sub.2 or .dbd.C.dbd.(CH.sub.2).sub.m, in which R.sup.2 is alkyl, and m is integer of from 2 to 5); n is 0 or 1; R.sup.3 is nitro, amino, alkylamino, dialkylamino, alkoxy, alkoxyalkoxy, or a group (iii), (iv), (v), (vi), (vii), (viii) or (ix): ##STR2## , wherein: R.sup.4 represents: alkyl; substituted alkyl; cycloalkyl having from 3 to 6 carbon atoms; substituted cycloalkyl; alkenyl; alkynyl; carbocyclic aryl; or heterocyclic; R.sup.5 is hydrogen atom or alkyl; R.sup.6 represents: hydrogen; alkyl; or cycloalkyl; R.sup.7 represents: alkyl; cycloalkyl; carbocyclic aryl; or aralkyl; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, are fuised to form heterocyclic ring; Y is oxygen or sulfur; r is 1, 2 or 3; Q is methylene or carbonyl; R.sup.8 is: alkyl or carbocyclic aryl; R.sup.9 is: alkyl; cycloalkyl; carbocyclic aryl; or aralkyl; R.sup.10 is heterocyclic; and R.sup.11 is aLkyl; have valuable acaricidal, insecticidal and anthelmintic activities.

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