Amine derivatives as protease inhibitors

C - Chemistry – Metallurgy – 07 – D

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C07D 413/12 (2006.01) A61K 31/5377 (2006.01)

Patent

CA 2475069

<SEE FORMULA (I)> <SEE FORMULA (a) <SEE FORMULA (b) The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making; according to Formula (1) in which: A comprises a heteromonocyctic ring containing 5 to 6 ring member atoms or a fused heteropolyeyclic ring system containing 8 to 14 ring member atoms, wherein each ring contains 5 to 7 ring member atoms, X1 is a ring member carbon atom and each ring member atom other than X1 is a carbon atom or a heteroatom, with the proviso that (i) at least one ring member atom is a heteroatom and (ii) when A is a heteromonocyclic radical containing 5 ring member atoms, no more than two of the ring member atoms comprising A are heteroatoms; n is 0, 1, 2 or 3. X2 is -C- or -CH-; X2 is a bond or a divalent group of Formula (a) or (b); R1 - R8 = as in the application.

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