Antiparasitic pyrrolobenzoxazine compounds

C - Chemistry – Metallurgy – 12 – P

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C12P 17/18 (2006.01) A61K 31/535 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2181168

This invention provides compounds of chemi- cal formula (I) or their pharmaceutically acceptable salts, wherein R is hydrogen or chloro. Also, the present invention provides a process for the produc- tion of the compound of formula (I), which comprises cultivating a microorganism having the identifying characteristics of Aspergillus fischeri var. thermomu- tatus ATCC 18618 or the like, and then isolating the compound of formula (I) from the fermentation broth. The pyrrolobenzoxazine compounds of formula (I) of this invention have broad antiparasitic activity, and thus are useful as antiparasitic agents, especially as anthelmintics.

Composés de formule chimique (I) ou leurs sels pharmaceutiquement acceptables dans laquelle R représente hydrogène ou chloro. L'invention porte également sur un procédé de production desdits composés de formule (I) consistant à mettre en culture un micro-organisme présentant les caractères d'identification de l'Aspergillus fischeri var. thermomutatus ATCC 18618 ou analogue, puis à isoler ledit composé de formule (I) du bouillon de fermentation. Les composés à base de pyrrolobenzoxazine de formule (I) de cette invention présentent une activité antiparasitaire étendue et sont de ce fait utiles comme agents antiparasitaires et plus particulièrement comme anthelmintiques.

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