Biologically active bistramides; process for producing the...

Details Biologically active bistramides; process for producing the... Biologically active bistramides; process for producing the...

C - Chemistry, Metallurgy

07

D

C07D 493/10 (2006.01) A61K 31/35 (2006.01)

Patent

CA 2157760

Bistramide derivatives with virtually no toxic effects, of formula (I) wherein -R1, X, Y and R2 are a saturated or unsaturated hydrocarbonaceous chain having from 1 to 20 carbon atoms, substituted by at least one -OH group and/or a ketone function, including, if need be, at least one ring (a), the ring including one more unsaturations; -R3, R4 and R5 are the same or different and are selected from hydrogen, alkyl or alkoxy radicals having from 1 to 4 carbon atoms, a group -COOH, -OH, -NH or -NO2, or a halogen atom. The invention also concern bistramide derivatives of formula (I) such as ethers or esters and their isomers, excluding A, B and C bistramides. Said bistramides are useful especially as drugs having a cytostatic effect, in particular as antitumour or anti-parasitic drugs.

L'invention concerne des dérivés de bistramides de toxicité faible, voire inexistante, de formule (I) dans laquelle -R1, X, Y et R2, représentent une chaîne hydrocarbonée de 1 à 20 atomes de carbone, saturée ou insaturée, substituée par au moins un groupe -OH et/ou une fonction cétone, comportant, le cas échéant, au moins un cycle (a), ce cycle pouvant comporter une ou plusieurs insaturations, -R3, R4 et R5, identiques ou différents les uns des autres, sont choisis parmi l'hydrogène, les radicaux alcoyle ou alcoxy de 1 à 4 atomes de carbone, un groupe -COOH, -OH, -NH2 ou -NO2, ou un atome d'halogène, leurs dérives tels qu'éthers ou esters, ainsi que leurs isomères, à l'exclusion des bistramides A, B et C sont utiles notamment comme médicaments à effet cytostatique, en particulier comme médicaments antitumoraux ou anti-parasitaires.

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