Szegedi Tudomanyegyetem

Magyar Tudományos Akadémia Természettudományi Kutatóközpont

University of Debrecen

István Szatmári

Ferenc Fülöp

Tibor Soós

Gergely Szakács

József Toldi

László Vécsei

Szilárd Tóth

Dóra Türk

Veronika Pape

György Dormán

László Nagy

Roberta Ferenczi-Palkó

András Füredi

Éva Rajnavölgyi

Péter Gogolák

Bence Réthi

The invention relates to C-3 substituted kynurenic acid derivatives with the general formula (I) wherein Ris Calkyl-, RRN&#x2014;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 &#x2014;OH, Calkyl-O&#x2014;, &#x2014;NH, Calkyl-NH&#x2014;, Caryl-Calkyl-NH&#x2014; or &#x2014;NH&#x2014; &#x2014;(CH)&#x2014;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. 

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

The present invention is related to 8-hydroxy-quinoline derivatives having multidrug-resistance reversing activity with improved selectivity and increased cytotoxicity towards multidrug-resistant cancer cells, preparation thereof and use of the same in the treatment of cancer, especially multidrug-resistant variants thereof. 

MDR-reversing 8-hydroxy-quinoline derivatives

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Szeged, Hungary

István Szatmári