Novel dicarboxylic acid linked amino acid and peptide...

A - Human Necessities – 61 – K

Patent

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A61K 31/485 (2006.01) A61K 31/55 (2006.01) A61K 47/48 (2006.01) A61P 23/00 (2006.01) C07D 223/04 (2006.01) C07D 489/02 (2006.01)

Patent

CA 2756397

The present invention concerns dicarboxylic acid linked amino acid and peptide prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing pain relief, decreasing the adverse GI side effects of the opioid analgesic and increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are also pro-vided. In one embodiment, prodrugs having the amino acid side chains of valine, leucine, isoleucine and glycine; and mono-, di- and tripeptides thereof are provided.

La présente invention porte sur des promédicaments analgésiques opioïdes à base d'acide aminé et de peptide liés à l'acide dicarboxylique et sur des compositions pharmaceutiques contenant lesdits promédicaments. L'invention porte également sur des procédés destinés à apporter un soulagement de la douleur, à diminuer les effets secondaires gastro-intestinaux néfastes de l'analgésique opioïde et à augmenter la biocompatibilité de l'analgésique opioïde avec les promédicaments mentionnés ci-dessus. Dans un certain mode de réalisation, l'invention porte sur des promédicaments ayant les chaînes latérales d'acide aminé de valine, leucine, isoleucine et glycine ; et des mono-, di- et tripeptides de ceux-ci.

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