Pharmaceutical compounds for the inhibition of hepatitis c...

Details Pharmaceutical compounds for the inhibition of hepatitis c... Pharmaceutical compounds for the inhibition of hepatitis c...

C - Chemistry, Metallurgy

07

K

C07K 14/18 (2006.01) A61K 39/29 (2006.01) A61P 31/20 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2352493

Peptidic inhibitors of hepatitis C virus NS3 protease are disclosed which are based on the P and P' regions of the natural substrate. The P' part of the inhibitor is optimised to achieve maximum binding energy through interaction with the S' region of the enzyme. By selecting amino acids such that the inhibitor is substantially not cleavable by the NS3 protease inhibitors having potency in the low nanomolar to sub-nanomolar range can be achieved.

L'invention porte sur des inhibiteurs peptidiques de la protéase NS3 du virus de l'hépatite C basés sur les régions P et P' du substrat naturel. La partie P' de l'inhibiteur est optimisée pour obtenir l'énergie de liaison maximale de par son interaction avec la région S' de l'enzyme. En sélectionnant des acides aminés tels que l'inhibiteur ne puisse pratiquement pas être scindé par les protéases NS3, on obtient des inhibiteurs efficaces dans les plages nanomolaire et subnanomolaire.

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