Types of c-3 substituted kynurenic acid derivatives with improved neuroprotective activity

Abstract

The invention relates to C-3 substituted kynurenic acid derivatives with the general formula (I) wherein Ris Calkyl-, RRN—Calkyl-, Caryl-Calkyl group; Ris H or Calkyl group; or Rand Rwith the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; Ris —OH, Calkyl-O—, —NH, Calkyl-NH—, Caryl-Calkyl-NH— or —NH— —(CH)—NRRgroup wherein n is an integer from 1 to 3; Ris H, Calkyl-, Caryl group or a halogen atom; Ris H or Caryl group; R6 is Calkyl group; Ris Calkyl group; or Rand Rwith the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; Ris Calkyl group; Ris Calkyl group; Rand Rwith the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; and stereoisomers, tautomers and salts thereof. The invention relates to the pharmaceutical preparations comprising the compounds and stereoisomers, tautomers and pharmaceutically acceptable salts. The compounds of the invention have neuroprotective activity, may be used for the prevention and treatment of neurodegeneration, and for slowing down the development of the conditions and diseases associated with a decline in cognitive abilities.