Pyrimidinyl derivatives as interleukin inhibitors

Details Pyrimidinyl derivatives as interleukin inhibitors Pyrimidinyl derivatives as interleukin inhibitors

C - Chemistry, Metallurgy

07

D

C07D 403/12 (2006.01) A61K 31/505 (2006.01) A61K 31/675 (2006.01) C07D 239/47 (2006.01) C07D 401/14 (2006.01) C07D 405/12 (2006.01) C07D 409/04 (2006.01) C07D 409/14 (2006.01) C07F 9/6512 (2006.01)

Patent

CA 2186511

Disclosed are compounds, compositions and methods for inhibiting interleukin -1.beta. (IL-.beta.) protease activity. The compounds, N- (pyrimidinyl)-aspartic acid .alpha.-substituted methyl ketones and aspartic acid aldehydes, have formula (I) set out herein. These compounds are inhibitors of 1.beta.-converting enzyme and as such are useful whenever such inhibition is desired. For example, they may be used as research tools in pharmaceutical, diagnostic and related studies and in the treatment of diseases in mammals in which IL-.beta. protease activity is implicated.

Composés, compositions et méthodes servant à inhiber l'activité de l'interleukine-1.beta. (1L-.beta.)-protéase. Lesdits composés qui sont des cétones méthyliques à substitution par l'acide N-(pyrimidinyl)-aspartique en .alpha. et des aldéhydes de l'acide aspartique présentent la formule (I). Ce sont des inhibiteurs de l'enzyme de conversion de 1.beta. s'avérant utiles lorsqu'une telle inhibition est requise, p. ex. comme outils de recherche pharmacologique, de diagnostic, ou d'études associées, ou pour le traitement chez le mammifère d'affections liées à l'activité de l'1L-.beta.-protéase.

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