Substituted azetidin-2-ones as cysteine protease inhibitors

Details Substituted azetidin-2-ones as cysteine protease inhibitors Substituted azetidin-2-ones as cysteine protease inhibitors

C - Chemistry, Metallurgy

07

D

C07D 205/085 (2006.01) A61K 31/395 (2006.01) A61K 31/397 (2006.01) A61K 31/44 (2006.01) A61K 31/505 (2006.01) A61P 9/00 (2006.01) A61P 19/00 (2006.01) A61P 21/00 (2006.01) A61P 35/00 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2369446

This invention relates to substituted azetidin-2-ones and to pharmaceutical compositions containing such compounds. Their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins is also described. The invention includes a compound of formula (I), Y represents -C(O)- or -S(O2)- ; R represents an allyl (ie CH2=CHCH2-) group or a radical. R1 represents - OCOR5, -OR5, -SR5, -S(O)R5, or -S(O)2R5; R2 represents a radical. R3 represents -OR5 or R5; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

La présente invention concerne des azétidine-2-ones et des compositions pharmaceutiques contenant de tels composés. L'invention concerne également leur utilisation en médecine en tant qu'inhibiteurs de la cystéine protéase, notamment des cathepsines. L'invention comporte un composé de formule (I), où Y représente -C(O)- ou -S(O¿2?)-; R représente un groupe allyle (i.e. CH¿2? = CHCH¿2?) ou un radical; R¿1? représente -OCOR¿5?, -OR¿5?, -SR¿5?, ou -S(O)¿2?R¿5?; R¿2? représente un radical; R¿3? représente -OR¿5? ou R¿5?; ou leur sel, hydrate ou solvate pharmaceutiquement acceptables.

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