Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein Junkinases

摘要

The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble under physiological conditions. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. <CHEM> The compounds of formula I according to the present invention being suitable pharmaceutical agents are those wherein Ar<1> and Ar<2> are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R<1> is hydrogen or a C1-C6-alkyl group, or R<1> forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar<1>; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula I is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl which is substituted with at least one ionisable moiety to which a lipophilic chain is attached and which is containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula I thus providing a sulfonamide.ring is forming a bond with the sulfonyl group of formula I thus providing a sulfonamide.