abstract |
IKK-betaserine-threonine protein kinase inhibitorn n n n n n n n Compounds of formula (1A) or (1B) are inhibitors of IKB kinase (IKK) activity and are useful for treating autoimmune and inflammatory diseases: In formulas (A) and (B), R 7 is hydrogen or optionally substituted ( C 1 -C 6 ) alkyl; Ring A is an optionally substituted aryl or hetero aryl ring having 5-13 ring atoms; Z is a group of the formula R (a) R 1 R 2 CHNH-YL 1 -X 1- (CH 2 ) z- , where Z is 0 or 1; R 1 is a carboxylic acid group (-COOH), or an ester group that can be hydrolyzed to a carboxylic acid group by one or more intracellular esterase enzymes; R 2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, -C (= NH) -NR 3 Or -S (= 0) 2 NR 3- , where R 3 is a divalent linker group of the formula-(AlK 1 ) m (Q) n (AlK 2 ) p -and m, n, P, Q in the transplant , AlK 1 and AlK 2 are as defined in the claims. |