Methods and compositions comprising nitric oxide donors and...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 489/04 (2006.01) A61K 31/00 (2006.01) A61K 31/135 (2006.01) A61K 31/198 (2006.01) A61K 31/4468 (2006.01) A61K 31/4535 (2006.01) A61K 31/454 (2006.01) A61K 31/485 (2006.01) A61P 25/04 (2006.01) C07D 489/08 (2006.01)

Patent

CA 2479098

Compositions and methods that induce, promote or otherwise facilitate pain relief are disclosed. These compositions and methods comprise a nitric oxide donor which either directly or indirectly prevents, attenuates or reverses the development of reduced opioid sensitivity, together with a compound which activates the opioid receptor that is the subject of the reduced opioid sensitivity. The compositions and methods prevent or alleviate pain, especially in neuropathic conditions and even more especially in peripheral neuropathic conditions such as painful diabetic neuropathy (PDN). The preferred nitric oxide donor is L-arginine whilst the preferred compounds which activate the opioid receptor are morphine and oxycodone. Conjugate compounds comprising the nitric oxide donor and an opioid analgesic are also disclosed.

L'invention concerne des compositions et des procédés induisant, favorisant ou encore facilitant le soulagement de la douleur. Ces compositions et procédés comprennent un donneur d'oxyde nitrique qui prévient, atténue ou inverse directement ou indirectement le développement de la sensibilité réduire aux opioïdes, avec un composé activant le récepteur opioïde constituant le sujet de la sensibilité réduite aux opioïdes. Les compositions et procédés préviennent ou soulagent la douleur, en particulier dans des états neuropathiques et plus spécifiquement dans des états neuropathiques périphériques tels que la neuropathie diabétique (PDN). Le donneur d'oxyde nitrique préféré est L-arginine tandis que les composés préférés activant le récepteur opioïde sont la morphine et l'oxycodone. L'invention concerne également des composés conjugués contenant le donneur d'oxyde nitrique et un analgésique opioïde.

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