C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/06 (2006.01) A61K 31/27 (2006.01) A61K 31/33 (2006.01) C07C 271/22 (2006.01) C07D 307/60 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01) C07K 5/08 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2123055
ABSTRACT Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: Image (I) wherein R1 is (CR5R6)n, (CR5R6)n-aryl, (CR5R6)n-heteroaryl, X- (CR5R6)n, X-(CR5R6)n-aryl or X-(CR5R6)n-heteroaryl wherein aryl and heteroaryl may be optionally substituted; X is O or NR5; R5 and R6 are independently H or lower alkyl; R2 is H, halo, lower alkyl or (CR5R6)n-aryl; R3 and R4 are independently H or alkyl; A is a D or L isomer of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, proline, phenylalanine, glycine, tyrosine, methionine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, histidine and .beta.-thienylalanine; Z is CH2 or O; and n is 0-4; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta. protease activity in a mammal utilizing the compounds and compositions.
Dolle Roland E.
Graybill Todd L.
Prouty Catherine P.
Schmidt Stanley J.
Speier Gary J.
Fetherstonhaugh & Co.
Vertex Pharmaceuticals Incorporated
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