Phenol derivatives and their use as rotamase inhibitors

C - Chemistry – Metallurgy – 07 – C

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C07C 275/34 (2006.01) A61K 31/135 (2006.01) A61K 31/155 (2006.01) A61K 31/165 (2006.01) A61K 31/17 (2006.01) A61K 31/18 (2006.01) C07C 335/18 (2006.01)

Patent

CA 2498662

The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)-, -C(S)-, -C(O)-NR10-, -C(S)-NR11-, - C(N-CN)-NR12-, -S(O)-, -S(O2)-, -S(O)-NR13-, and S(O2)-NR14-, -O-, -S- or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-Ll-K-L2-M2-, wherein Y. is selected from the group comprising alkyl, substituted alkyl, straight alkyl, substituted straight alkyl, branched alkyl, substituted branched alkyl, straight alkenyl, substituted straight alkenyl, branched alkenyl , substituted branched alkenyl, straight alkynyl, substituted straight alkynyl, branched alkynyl, substituted branched alkynyl, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, heterocyclyl, substituted heterocyclyl, mono- unsaturated heterocyclyl, poly-unsaturated heterocyclyl, mono-substituted poly- unsaturated heterocyclyl, poly-substituted poly-unsaturated heterocyclyl, mono- substituted mono-unsaturated heterocyclyl, poly-substituted mono-unsaturated heterocyclyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl, wherein Y is different from a peptide or is absent.

L'invention concerne un composé représenté par les formules (I), (II), (III), (IV), (V): dans lesquelles Z¿1?, Z¿2?, Z¿3? et Z¿4? sont sélectionnés chacun séparément dans le groupe comprenant C(O)-, -C(S)-, -C(O)-NR¿10?-, -C(S)-NR¿11?-, -C(N-CN)-NR¿12?-, -S(O)-, -S(O¿2?)-, -S(O)-NR¿13?-, et S(O¿2?)-NR¿14?-, -O-, -S- ou peuvent être chacun individuellement absents; X représente un espaceur sélectionné indépendamment dans le groupe comprenant -M1-Ll-K-L2-M2-, (fig. B, C, D, E, F, G, H, I). Y est sélectionné dans le groupe comprenant alkyle, alkyle substitué, alkyle linéaire, alkyle linéaire substitué, alkyle ramifié, alkyle ramifié substitué, alcényle linéaire, alcényle linéaire substitué, alcényle ramifié, alcényle ramifié substitué, alcynyle linéaire, alcynyle linéaire substitué, alcynyle ramifié, alcynyle ramifié substitué, cycloalkyle, cycloalkyle substitué, cycloalcényle, cycloalcényle substitué, hétérocyclyle, hétérocyclyle substitué, hétérocyclyle monoinsaturé, hétérocyclyle polyinsaturé, hétérocyclylepolyinsaturé monosubstitué, hétérocyclyle polyinsaturé polysubstitué, hétérocyclyle monoinsaturé monosubstitué, hétérocyclyle monoinsaturé polysubstitué, aryle, aryle substitué, hétéroaryle et hétéroaryle substitué, Y étant différent d'un peptide ou absent.

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