Amine derivatives as protease inhibitors

Details Amine derivatives as protease inhibitors Amine derivatives as protease inhibitors

C - Chemistry, Metallurgy

07

D

C07D 413/12 (2006.01) A61K 31/42 (2006.01) A61K 31/44 (2006.01) A61K 45/06 (2006.01) A61P 9/00 (2006.01) A61P 37/00 (2006.01) C07D 209/08 (2006.01) C07D 209/14 (2006.01) C07D 213/30 (2006.01) C07D 213/40 (2006.01) C07D 263/14 (2006.01) C07D 263/26 (2006.01) C07D 263/32 (2006.01) C07D 263/34 (2006.01) C07D 263/56 (2006.01) C07D 263/60 (2006.01) C07D 307/80 (2006.01) C07D 307/81 (2006.01) C07D 413/04 (2006.01) C07D 413/14 (2006.01) C07F 7/18 (2006.01)

Patent

CA 2367352

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 (I) in which: A comprises a heteromonocyclic ring containing 5 to 6 ring member atoms or a fused heteropolycyclic 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; X1 is =C- or -CH-; X2 is a bond or a divalent group of Formula (a) or (b); R1 - R8 = as in the application.

La présente invention concerne de nouveaux dérivés hétérocycliques substitués par alkanoyle, constituant des inhibiteurs de protéase cystéine; l'invention concernant par ailleurs les sels acceptables sur le plan pharmaceutique et les N-oxydes de ceux-ci; leurs utilisations comme agents thérapeutiques et les procédés de leur préparation. Selon la formule (I), A comprend un noyau hétérocyclique de 5 à 6 atomes de chaînons ou un noyau hétéropolycyclique concentré comprenant de 8 à 14 atomes de chaînons, chaque noyau contenant de 5 à 7 atomes de chaînon; X?1¿ est un atome de carbone de chaînon et chaque atome de chaînon autre que X?1¿ est un atome de carbone ou un hétéroatome, à condition (i) qu'au moins un atome de chaînon soit un hétoréatome et que (ii), lorsque A est un radical hétéromonocyclique contenant 5 atomes de chaînon, pas plus de 2 des atomes de chaînon renfermant A soit des hétéroatomes; n est 0, 1, 2 ou 3; X?1¿ est =C- ou -CH-; X?2¿ est une liaison ou un groupe divalent de formule (a) ou (b) : R?1¿-R?8¿ = comme dans l'application.

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