Aziridine derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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260/385, 260/337

C07D 203/12 (2006.01) C07D 203/08 (2006.01) C07D 451/14 (2006.01)

Patent

CA 1086321

ABSTRACT OF THE DISCLOSURE Novel aziridine derivatives and their process of preparation are provided of the formula (I):- Image in which R is a nitrile or carbamoyl group and R1 and R2, which can be the same or different, are hydrogen atoms or aliphatic hydrocarbon radicals containing up to 10 carbon atoms, which can be straight-chanined, branched, cyclic, saturated or hydrocarbon and optionally substituted by hydroxyl, alkoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, cyano, 1, 2 or 3 halogens, cycloalkyl, phenyl or phenoxy- or axe nitrile, carboxyl, dialkylamino, or optionally hydrogenated monocyclic heteroaryl or phenyl radicals which a-a optionally substituted by alkyl, alkoxy, hydroxy, alkoxycarbonyl, dialkyl- amino, alkylthio, trifluoromethyl, nitro, carbamoyl, nitrile, sulphonamido, hydroxyalkyl or methylenedioxy groups or by halogen, or R1 and R2 together with the carbon atoms to which they are attached, can form a saturated or unsaturated ring containing up to 8 ring members, which can also be inter- rupted by oxygen, sulphur, SO, SO2, NH, N-alkyl, N-acyl or N-alkoxycarbonylalkyl, said ring being unsubstituted or sub- stituted by alkyl, alkoxy, hydroxyl, alkylenedioxy, alkoxy- carbonyl, hydroxylalkyl, alkoxycarbonylalkyl, dialkylamino. oxo or 2-cyanoaziridino groups, or can be fused to 1 or 2 benzene rings or can be bridged by alkylene radicals contain- ing up to 3 carbon atoms: the novel derivatives exhibit very strong imnune-stimulating and cancerostatic properties.

273107

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