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US 5,077,278 AGranted
Non-natural demethylavermectins compositions and method of use
AssigneePfizer Inc.
InventorsEdmund W. Hafner, Kelvin S. Holdom, S. Edward Lee
Life of this patent
Estimating the term…
Abstract
Non-natural demethylavermectins useful as parasiticides and process therefor.
Claims14
A compound of the formula ##STR3## wherein X is a single bond or a double bond;
- R.sup.1 is H or OH;
- provided that when X is a single bond, R.sup.1 is H or OH, and when X is a double bond R.sup.1 is absent;
- R is an alpha-branched C.sub.3 -C.sub.8 alkynyl, alkoxyalkyl or alkylthioalkyl group;
- a C.sub.5 -C.sub.8 cycloalkylalkyl group wherein the alkyl group is an alpha-branched C.sub.2 -C.sub.5 alkyl group;
- a C.sub.3 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkenyl group, either of which may be substituted by methylene or one or more C.sub.1 -C.sub.4 alkyl groups or halo atoms;
- or a 3 to 6 membered oxygen or sulfur containing heterocyclic ring which may be saturated, or fully or partially unsaturated and which may be substituted by one or more C.sub.1 -C.sub.4 alkyl groups or halo atoms;
- with the proviso that when R is alkyl, it is not isopropyl or sec-butyl;
- R.sup.2 is a disaccharide moiety of the formula ##STR4## where each of R.sup.4 and R.sup.5 is hydrogen or methyl, with the proviso that at least one of R.sup.4 and R.sup.5 is hydrogen;
- and
- R.sup.3 is hydrogen or methyl.
7 more elements
A compound of the formula ##STR5## wherein X is a single bond or a double bond;
- R.sup.1 is H or OH;
- provided that when X is a single bond, R.sup.1 is H or OH, and when X is a double bond R.sup.1 is absent;
- R is C.sub.3-8 cycloalkyl;
- R.sup.2 is a disaccharide moiety of the formula ##STR6## wherein each of R.sup.4 and R.sup.5 is hydrogen or methyl, with the proviso that at least one of R.sup.4 and R.sup.5 is hydrogen;
- and
- R.sup.3 is hydrogen or methyl.
3 more elements
A compound of the formula ##STR7## wherein X is a single bond or a double bond;
- R.sup.1 is H or OH;
- provided that when X is a single bond, R.sup.1 is H or OH, and when X is a double bond R.sup.1 is absent;
- R is a 3 to 6 membered oxygen or sulfur containing heterocyclic ring which may be saturated, or fully or partially unsaturated and which may be substituted by one or more C.sub.1 -C.sub.4 alkyl groups or halo atoms;
- R.sup.2 is a disaccharide moiety of the formula ##STR8## where each of R.sup.4 and R.sup.5 is hydrogen or methyl, with the proviso that at least one of R.sup.4 and R.sup.5 is hydrogen;
- and
- R.sup.3 is hydrogen or methyl.
3 more elements
A compound of the formula ##STR9## wherein X is a double bond;
- R is 1-methylthioethyl;
- R.sup.3 is methyl;
- R.sup.2 is a disaccharide moiety of the formula ##STR10## wherein each of R.sup.4 and R.sup.5 is hydrogen.
Dependencies are inferred from the claim text.