EP1402888A1 — The use of substituted carbocyclic compounds as rotamases inhibitors

USPTO Abstract

The present invention is related to the use of a compound as an inhibitor to a rotamase, whereby the compound has the structure:         A-X-Y     (I) wherein A is cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; X is a spacer and is selected from X 1 or X 2 , wherein X 1 is selected from the group comprising -[(CR a R b ) n -NR c -CO-NR d -(CR a R b ) m ] t -, -[(CR a R b ) n -NR c -CS-NR d -(CR a R b ) m ] t -, -[(CR a R b ) n -NR c -C(N-CN)-NR d -(CR a R b ) m ] t -, -[(CR a R b ) n -NR c -C(N-R e )-NR d -(CR a R b ) m ] t -, -[(CR a R b ) n -CO-NR c -(CR a R b ) m ] t -, -[(CR a R b ) n -NR c -(CR a R b ) m ] t -, -[(CR a R b ) n -NR c -CO-O-(CR a R b ) m ] t -, -[(CR a R b ) n -O-CO-NR c -(CR a R b ) m ] t -, -[(CR a R b ) n -O-(CR a R b ) m ] t -, -[(CR a R b ) n -SR c -(CR a R b ) m ] t -; wherein X 2 is selected from the group comprising - [(CR a R b ) n -CO-(CR a R b ) m ] t -, -[(CR a R b ) n -CS-(CR a R b ) m ] t -, -[(CR a R b ) n -NR c -CO-(CR a R b ) m ] t -, -[(CR a R b ) n -CO-NR c -(CR a R b ) m ] t -, -[(CR a R b ) n -NR c -CS-(CR a R b ) m ] t -, -[(CR a R b ) n -CS-NR c -(CR a R b ) m ] t -, -[(CR a R b ) n -NR c -SO 2 -(CR a R b ) m ] t -, -[(CR a R b ) n -SO 2 -NR c -(CR a R b ) m ] t -, -[(CR a R b ) n -SO-(CR a R b ) m ] t -, -[(CR a R b ) n -SO 2 -(CR a R b ) m ] t -, -[(CR a R b ) n ] t -; wherein n and m are independently selected from each other and are any integer between 0 and 10 provided that if n is 0, m is different from 0, and if m is 0, n is different from 0; wherein t is independently selected from n and/or m and is any integer between 0 and 10; wherein R a , R b , R c , R d and R e are independently from each other selected from the group comprising H, alkyl, cycloalkyl, aryl, heteroaryl and heterocyclyl; and wherein Y is selected from the group comprising alkyl, substituted alkyl, 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, aryl, substituted aryl, heteroaryl and substituted heteroaryl, wherein Y is different from a peptide.