Avermectin compounds with a 6,5-spiroketal ring system

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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514450, 536 71, 549264, A61K 3170, A61K 31365, C07D31500

Patent

active

051770636

ABSTRACT:
Avermectin analogs are disclosed wherein the 6,6-spiroketal ring system has been reduced in size to a 6,5-spiroketal ring system by the deletion of the 25-position carbon atom and the 25-alkyl substituent. This is accomplished by opening the outer spiroketal ring with the elimination of ring carbon atoms 23, 24 and 25 and the alkyl substituent at the 25-position and incorporation a new component, reclosing the spiroketal to a 5-membered ring with new substituents at the 24-position. The compounds are used as anti-parasitic insecticidal and anti-helmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

REFERENCES:
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patent: 4895837 (1990-01-01), Mrozik et al.
patent: 4906619 (1990-03-01), Eskola et al.
T. L. Shih, et al. Tetra Letters vol. 31, No. 25 pp. 3525-3528.
T. L. Shih, et al. Tetra. Letters vol. 31, No. 25 pp. 3529-3532 (1990).

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