Macrocyclic peptides active against the hepatitis c virus

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/08 (2006.01) A61K 38/06 (2006.01) A61P 31/14 (2006.01) C07K 5/083 (2006.01) C07K 5/087 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2474035

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 (C5-6)cycloalkyl and R3 is cyclopentyl; or a pharmaceutically acceptable salt thereof, useful as inhibitors of the HCV NS3 protease.

L'invention concerne des composés de formule générale (I), dans laquelle R?1¿ est hydroxy ou NHSO¿2?R?1A¿, R?1A¿ étant (C¿1-8?)alkyle, (C¿3-7?)cycloalkyle ou {(C¿1-6?)alkyle-(C¿3-7?)cycloalkyle} qui sont tous éventuellement substitués de 1 à 3 fois par halo, cyano, nitro, O(C¿1-6?)alkyle, amido, amino ou phényle, ou R?1A¿ étant C¿6? ou C¿10? aryle éventuellement substitué de 1 à 3 fois par halo, cyano, nitro, (C¿1-6?)alkyle, O(C¿1-6?)alkyle, amido, amino ou phényle; R?2¿ est (C¿5-6?)cycloalkyle et R?3¿ est cyclopentyle; ou un sel pharmaceutiquement acceptable correspondant, utilisés en tant qu'inhibiteurs de la protéase HCV NS3.

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