Dibenzo-oxazepine and -dioxepine derivatives and their use...

C - Chemistry – Metallurgy – 12 – N

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C12N 1/14 (2006.01) A61K 31/335 (2006.01) A61K 31/365 (2006.01) A61K 31/55 (2006.01) C07D 267/20 (2006.01) C07D 321/10 (2006.01) C12P 17/08 (2006.01) C12P 17/14 (2006.01)

Patent

CA 2257422

Compounds of formula (I), wherein R1 and R2 are independently hydrogen, unsubstituted lower alkyl or lower alkyl substituted by lower alkoxy or lower alkyl thio, or acyl which is unsubstituted or substituted by one or more of lower alkyl, lower alkyl substituted by halogen, and lower alkoxy; X is CO or CHOH; Y is CO or CH2; and Z is O or NH, and epimers and enantiomers thereof, or the physiologically usable salts thereof are useful as anti-tumor agents. They can be prepared by fermentation of Aspergillus sp. and, optionally, subsequent modification of functional groups.

Composés de la formule (I), dans laquelle R?1¿ et R?2¿ représentent indépendamment hydrogène, alkyle inférieur non substitué ou alkyle inférieur substitué par alcoxy inférieur ou alkyle thio inférieur, ou acyle non substitué ou substitué par un ou plusieurs éléments choisis parmi alkyle inférieur, alkyle inférieur substitué par halogène et alcoxy inférieur; X représente CO ou CHOH; Y est CO ou CH¿2?; et Z est O ou NH. Ces composés, et leurs épimères et énantiomères ou leurs sels physiologiquement utiles, agissent comme agents antitumoraux. Ils peuvent être préparés par fermentation d'Aspergillus sp. et, éventuellement, par modification ultérieure des groupes fonctionnels.

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