Inhibitors of picornavirus proteases

C - Chemistry – Metallurgy – 07 – K

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C07K 7/02 (2006.01) A61K 38/04 (2006.01) A61K 38/55 (2006.01) C07K 5/02 (2006.01) C07K 5/083 (2006.01) C07K 7/06 (2006.01) C07K 14/085 (2006.01) C07K 14/81 (2006.01)

Patent

CA 2111471

2111471 9222570 PCTABS00018 Compounds of formula (I) inhibit the proteolytic activity of picornaviral proteases, and are thus effective antiviral agents. In formula (I) R1 is -OR3 or -NR3R4, where R3 is lower alkyl, hydroxy, lower alkoxy, or aryl-lower alkyl, and R4 is H or lower alkyl; R2 is H or lower acyl; n is an integer from 2 to 40 inclusive; X is an anchor group selected from the group consisting of -CHO, -C=N, -COCH2F, -COCH2Cl, -COCH2N2, -CH=N-NHC(=S)NH2 or -COCOR5 where R5 is lower alkyl, lower alkoxy, lower aryl, aryl-lower alkyl or aryl-lower alkoxy; and aa indicates an amino acid; wherein (aa)n is an amino acid sequence recognized specifically by said selected protease.

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