Carbamate caspase inhibitors and uses thereof

Details Carbamate caspase inhibitors and uses thereof Carbamate caspase inhibitors and uses thereof

C - Chemistry, Metallurgy

07

D

C07D 209/86 (2006.01) A61K 31/395 (2006.01) A61P 43/00 (2006.01) C07D 209/08 (2006.01) C07D 209/88 (2006.01) C07D 221/12 (2006.01) C07D 223/22 (2006.01) C07D 223/26 (2006.01) C07D 223/28 (2006.01) C07D 279/30 (2006.01) C07D 403/12 (2006.01)

Patent

CA 2403959

This invention provides caspase inhibitors of formula (I): wherein Z is oxygen or sulfur; R1 is hydrogen, -CHN2,R, CH2OR, CH2SR, or -CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1.beta. secretion.

L'invention concerne des inhibiteurs de caspase de formule (I): dans laquelle Z représente oxygène ou soufre; R?1¿ est hydrogène, -CHN¿2?,R, CH¿2?OR, CH¿2?SR, ou -CH¿2?Y; Y représente un groupe partant électronégatif; R?2¿ signifie CO¿2?H, CH¿2?CO¿2?H, ou leur esters, amides ou isosthères; R?3¿ représente un groupe capable de s'adapter dans le sous-site S2 d'une enzyme caspase; R?4¿ et R?5¿ sont regroupés avec l'azote intervenant pour former un noyau hétérocyclique et R est comme décrit dans la spécification. Ces composés sont des inhibiteurs efficaces de l'apoptose et de la sécrétion IL-1.beta..

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