4-(4-pyridinyl)-benzamides and their use as rock activity modulators

Abstract

The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). Rand Rare, independently of each other, hydrogen, hydroxy, cyano, C-C-alkyl, C-C-haloalkyl, C-C-alkoxy or C-C-haloalkoxy; R, R, Rand Rare, independently of each other, hydrogen, hydroxy, halogen, cyano, C-C-alkyl, C-C-haloalkyl, C-C-alkoxy, C-C-haloalkoxy, amino, C-C-alkylamino or di-(C-C-alkyl)-amino; Ris hydrogen, C-C-alkyl, C-C-haloalkyl, aryl or aryl-C-C-alkyl; Ris a group of the formula —X—W, where X is a single bond, C-C-alkylene or C-C-alkylene-O—, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; Ris a group of the formula —Y—Z, where Z is hydrogen, halogen, OR, NRR, S(O)—R, phenyl which may carry 1, 2, 3 or 4 substituents Ror a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched CC-alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.