Tripeptides having a hydroxyproline ether of a substituted...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/08 (2006.01) A61P 31/14 (2006.01) C07K 5/083 (2006.01) C07K 5/087 (2006.01)

Patent

CA 2474156

Disclosed herein are compounds of formula (I), wherein R1 is hydroxy or NHSO2R1A wherein R1A is (C1-8)alkyl, (C3-7)cycloalkyl or {(C1-6)alkyl-(C3- 7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O-(C1-6)alkyl, amido, amino or phenyl, or R1A is C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O-(C1 6)alkyl, amido, amino or phenyl; R2 is (C4- 6)cycloalkyl; R3 is t-btuyl or (C5-6)cycloalkyl and R4 is (C4-6)cycloalkyl; or a pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of Hepatitis C.

L'invention concerne des composés de la formule (I) ou un sel pharmaceutiquement acceptable desdits composés. Dans ladite formule, R?1¿ est hydroxy ou NHSO¿2?R?1A¿ (R?1A¿ étant alkyle (C¿1-8?), cycloalkyle (C¿3-7?) ou {alkyle (C¿1-6?)-cycloalkyle (C¿3-7?)}, tous éventuellement substitués 1 à 3 fois par halo, cyano, nitro, O-alkyle ( C¿1-6?), amido, amino ou phényle; ou bien R?1A¿ est aryle C¿6? ou C¿10? éventuellement substitué 1 à 3 fois par halo, cyano, nitro, alkyle (C¿1-6?), O-alkyle ( C¿1-6?), amido, amino ou phényle); R?2¿ est cycloalkyle (C¿4-6?); R?3¿ est t-btuyle ou cycloalkyle (C¿5-6?); et R?4¿ est cycloalkyle (C¿4-6?). Les composés de l'invention sont utiles comme inhibiteurs de la protéase NS3 du VHC destinés au traitement de l'hépatite C.

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