18-membered nitrobenzyl-substituted and...

A - Human Necessities – 61 – K

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Details

A61K 38/15 (2006.01) A61K 31/395 (2006.01) A61P 33/10 (2006.01) C07D 273/00 (2006.01) C07K 11/02 (2006.01)

Patent

CA 2550344

The invention relates to cyclic depsipeptides, especially 18-membered cyclohexadepsipeptides of general formula (I) and the salts thereof, wherein R1 represents nitrobenzyl or R'R''N-benzyl - wherein R' and R'' independently represent hydrogen, optionally substituted C1-C4-alkyl, formyl, C1-C4-alkoxy- C1-C4-alkyl, C1-C4-alkoxycarbonyl, or hydroxy-C1-C2-alkyl-sulfonyl-C1-C2- alkyl, or, together with the nitrogen atom to which they are bound, R' and R'' form an optionally substituted monocyclic or polycyclic, optionally bridged and/or spirocyclic, saturated or unsaturated heterocycle containing between one and three other heteroatoms from the group of nitrogen, oxygen and sulphur, or R' and R'' together form C3-C5-alkylene monocarbonyl or an optionally susbtituted diacyl radical of a C4-C6-dicarboxylic acid - and R2, R3 and R4 independently represent C1-C4-alkyl. The invention also relates to the optical isomers and racemates of said cyclic depsipeptides, to a method for the production thereof, and to the use of the same for controlling endoparasites.

L'invention concerne des depsipeptides cycliques, notamment des cyclohexadepsipeptides à 18 chaînons, de formule générale (I) et leurs sels. Dans la formule (I), R?1¿ représente nitrobenzyle ou R'R''N-benzyle, R' et R'' représentant indépendamment l'un de l'autre respectivement hydrogène, alkyle C¿1?-C¿4? éventuellement substitué, formyle, alcoxy C¿1?-C¿4?-alkyle C¿1?-C¿4?, alcoxy C¿1?-C¿4?-carbonyle, hydroxy-alkyle C¿1?-C¿2?-sulfonyl-alkyle C¿1?-C¿2?, ou bien R' et R'' formant avec l'atome d'azote auquel ils sont liés un hétérocycle saturé ou insaturé, monocyclique ou polycyclique, éventuellement ponté et/ou spirocyclique, éventuellement substitué, qui contient un à trois autres hétéroatomes du groupe azote, oxygène et soufre ou R' et R'' formant ensemble alkylène C¿3?-C¿5?-monocarbonyle ou un reste diacyle éventuellement substitué d'un acide dicarboxylique C¿4?-C¿6?, et R?2¿, R?3¿ et R?4¿ représentent indépendamment les uns des autres alkyle C¿1?-C¿4?. L'invention concerne également les isomères optiques et les mélanges racémiques de ces depsipeptides, un procédé pour la production de ces depsipeptides, ainsi que leur utilisation pour lutter contre des endoparasites.

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