Azaaspartic acid analogs as interleukin-1 beta converting...

Details Azaaspartic acid analogs as interleukin-1 beta converting... Azaaspartic acid analogs as interleukin-1 beta converting...

C - Chemistry, Metallurgy

07

K

C07K 5/062 (2006.01) A61K 31/195 (2006.01) A61K 31/215 (2006.01) A61K 38/05 (2006.01) C07C 243/28 (2006.01) C07C 243/34 (2006.01) C07C 243/38 (2006.01) C07K 5/06 (2006.01) C07K 5/083 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2196183

Disclosed are compounds, compositions and methods for inhibiting interleukin-1 .beta. protease activity. The compounds, .alpha.-substituted acetamides are of formula (A), wherein: R2 = H or alkyl; R3 = halo, O(CO)0-1aryl, OPOR4R5; (a), (b) where R4 and R5 = aryl; R6 = H, aryl or aralkyl; R7 = independently selected from R6, CF3 and CF2CF3; R1 = R6-CO, heteroaryl-CO, heteroaralkyl-CO and amino acid.

L'invention concerne des composés, des compositions et des procédés pour l'inhibition de l'activité de la protéase de l'interleukine-1 .beta.. Les composés, des acétamides .alpha.-substitués, sont représentés par la formule (A) dans laquelle R?2¿= H ou alkyle; R?3¿= halo, O(CO)¿0-1?aryle, OPOR?4¿R?5¿; (a), (b) R?4¿ et R?5¿ = aryle; R?6¿ = H, aryle ou aralkyle; R?7¿ est choisi indépendamment parmi R?6¿, CF¿3? et CF¿2?CF¿3?; R?1¿ = R?6¿-CO, hétéroaryle-CO, hétéroaralkyl-CO et aminoacide.

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