Jonathon Gareth Williams;Stuart Thomas Onions;Stephen John Davies;Michael Hugh Charlton;Simon Christopher Hirst;David Charles Festus Moffat
发明人:
David Charles Festus Moffat,Stephen John Davies,Michael Hugh Charlton,Simon Christopher Hirst,Stuart Thomas Onions,Jonathon Gareth Williams
申请号:
US12447271
公开号:
US08106091B2
申请日:
2007.10.29
申请国别(地区):
US
年份:
2012
代理人:
摘要:
Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases:wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y)R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; Y1 is a bond, —(C═O)—, —S(O2)—, —C(═O)O—, —OC(═O)—, —(C═O)NR3—, —NR3(C═O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C═O)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims.