Nodulisporic acid derivative spot-on formulations for...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 491/052 (2006.01) A01N 43/90 (2006.01) A61K 9/00 (2006.01) A61K 31/407 (2006.01) A61K 31/475 (2006.01) C07D 405/06 (2006.01) C07D 491/14 (2006.01)

Patent

CA 2500822

This invention provides for, inter alia, spot-on compositions for the treatment or prophylaxis of parasite infestations in mammals or birds which comprise: (1) at least one nodulisporic acid derivative; (2) an acceptable liquid carrier vehicle; and (3) optionally, a crystallization inhibitor. The invention also provides for a method of treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprise topically applying to said mammal or bird an effective amount of a composition according to the present invention. Further, this invention relates to an amidation process to prepare amide derivatives of nodulisporic acid and to intermediate formed in this process.

L'invention concerne, entre autres, des compositions pour un traitement cutané localisé ou pour la prophylaxie d'infestations parasitaires, chez des mammifères ou chez des oiseaux. Ces compositions comprennent: (1) au moins un dérivé d'acide nodulisporique; (2) un excipient liquide acceptable; et (3) éventuellement, un inhibiteur de cristallisation. L'invention concerne également une méthode de traitement d'infestations parasitaires ou de prophylaxie d'infestations parasitaires chez des mammifères ou chez des animaux. Cette méthode comprend l'application topique auxdits mammifères ou auxdits oiseaux, d'une dose efficace d'une composition selon l'invention. En outre, l'invention concerne un procédé d'amidation permettant de préparer des dérivés amide d'acide nodulisporique, ainsi qu'un intermédiaire formé par le biais de ce procédé.

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