NITENIN ANALOGUE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CHRONIC AND ACUTE PAIN

The present disclosure relates to nitenin analogue compounds (of formulas I, II, III and IV) and their use as pharmaceutical agent in the treatment, prevention or reduction of both acute and chronic pain. The mode of action disclosed herein allows nitenin and nitenin analogue compounds to act as ana...

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Hauptverfasser: CLAUDETREMBLEAU, Laurent Alain, LOPES DE SOUSA, Marisa Isabel, PENA LINO, Sílvia Patrícia, GOMES, Rui, PINTO FERREIRA, Luísa Maria, SEGÃO MONDRAGÃO, Miguel Angelo, DA SILVEIRA MÁXIMO, Patrícia Isabel, MAÇO ABREU, Ana Rosa, DE SÉRIO BRANCO, Paula Cristina, HIM TONG, Ming, MONTEIRO SERRÃO, Joana Maria, ROSADO SABINO, Vanessa Alexandra, FERREIRA DA COSTA LOURENÇO, Ana Maria, PINHEIRO BASTOS, André Emanuel, DOS SANTOS BALTAZAR DE LIMA, Pedro Afonso, SOVELA MOURÃO, Henrique, SZWARC DOS SANTOS, Beatriz
Format: Patent
Sprache:eng
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Zusammenfassung:The present disclosure relates to nitenin analogue compounds (of formulas I, II, III and IV) and their use as pharmaceutical agent in the treatment, prevention or reduction of both acute and chronic pain. The mode of action disclosed herein allows nitenin and nitenin analogue compounds to act as analgesic through reduction of K30 currents rather than their potentiation. Related to their high efficacy in the treatment of pain, these compounds are highly selective for slow voltage-activated potassium (K30 ) currents expressed in the small diameter dorsal root neurons (sDRGns), mainly on those mediated by the voltage-dependent potassium channel (KV), KV1.3. Such findings, together with those showing that nitenin and nitenin analogue compounds act as activity dependent blockers also lead to very reduced side-effects. The results disclosed herein show that nitenin and nitenin analogue compounds described herein are a viable alternative to the already existing pharmaceutical compounds used in the treatment of pain.