C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/04 (2006.01) C07F 9/32 (2006.01) C07F 9/40 (2006.01) C07F 9/48 (2006.01) C07F 9/547 (2006.01) C07K 5/02 (2006.01)
Patent
CA 2125080
ABSTRACT Disclosed are compounds of the formula: Image (I) (wherein: n is 0 - 4; Y is Image (in which R2 is hydrogen or deuterium; R3 is OH, OR7, NR7OR8 or NR7R8; R4 is H or lower alkyl; R5 and R6 are H, OH, alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, alkoxy, aroxy, heteroaroxy, aralkoxy, heteroaralkoxy, alkenyl, aralkenyl or heteroaralkenyl; and R7 and R8 are H, alkyl, cycloalkyl, aralkyl, heteroaralkyl, aryl or heteroaryl] AA is: (a) an amino acid residue of the formula: Image (II) [in which R7 and R8 are as defined above; and R9 is (CR6R7)0-6-R10 where R10 has a meaning given for R11 defined below] or (b) a group selected from the group consisting of: (1) Image (2) Image (3) Image (4) Image (5) Image (6) Image (7) Image (8) Image (9) Image (10) Image (11) Image (12) Image (13) Image and (14) Image [in which W and X are independently CH2, O, S or NR7] R1 is R10-CO- or R10-S02- [in which R10 has a meaning given to R11]; and R11 is H, alkyl, alkenyl, aryl, etc.), compositions and methods for inhibiting interleukin - 1.beta. protease activity using the compounds of the formula (I).
Dolle Roland E.
Singh Jasbir
Fetherstonhaugh & Co.
Vertex Pharmaceuticals Incorporated
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