The Activity of Kinase Inhibitors useful in the treatment of disorders mediated by mechanisms of ikk2

摘要

The compounds are inhibitors of this kinase activity, particularly the activity of ikk2.Claim 1: a compound according to formula (1): wherein R1 is - or - so2nr3r4 nr5so2ch3, R2 is chr6r7 Cf3 -, - or - C (CH3) 3; R3 is Hydrogen or Methyl and R4 is Hydrogen, alkyl, optionally substituted with hydroxyl C1 - 6, - (CH2) acicloalquilo C3 6, which is optionally substituted cycloalkyl Mind with hydroxyl or - NH2, - (CH2) bnr8r9 optionally substituted alkyl, piperidinilo C1 - 6Formula (2), R3 and R4 are United to form pirrolidinilo, or optionally substituted with - NH2 piperidinilo; R5 is Hydrogen or Methyl; R6 and R7 is Hydrogen Hydrogen, alkyl C1 - 6, - (CH2) dor10, nr11r12 - alkyl -, CO2 - C1 - 6, - conr13r14 phenyl,Five members or heteroaryl containing from one to four nitrogen Atoms in the heteroaryl is optionally substituted with one or two alkyl substituents selected regardless of C1 - 6 - CO alkyl C1 - 6, - (CH2) efenilo and tienilo, R6 and R7 are each fluor, R6 is met ILO and r7es Methyl and hydroxylOr R6 and R7 are United to form a cycloalkyl, optionally substituted with Methyl C3 - 6; R9 R8 is Hydrogen; C1 is Hydrogen, alkyl or alkyl - 6 - CO2 - C1 - 6; R10 is Hydrogen, phenyl optionally substituted with - (CH2) fco2r15 piridilo, or optionally substituted with one or two substituents SEL Eccionados Rent regardless of chlorine and Hydrogen is C1 - 6; R11 and R12 is Hydrogen,- (CH2) gnr16r17 HNCO, - (CH2) - alkyl C1 - 6, - (CH2) icicloalquilo C3 - 6, - (CH2) jfeniio, - (CH2) kpiridilo, or mheterociclilo - (CH2), in which the heterociclilo is optionally substituted alkyl C1 - 6, R11 is C1 - Rent 6 and R12 is C1 - 6 or - alkyl so2fenilo, R11 and R12 are United to form a Het Erociclilo 6-membered optionally containing one nitrogenIn the heterociclilo is optionally substituted with alkyl - CO2 - C1 - 6 or piperidinilo, R11 and R12 or are United to form formula (3); R13 and R14 is H is H, alkyl C1 - 6, - (CH2) nor18, - (CH2) pnr19r20, - (CH2) qco2r21, - (CH2) rso2nh2 c3-6, cycloalkyl, optionally substituted phenyl or with C Parrot or alkyl - or - C1 - 6, R13 and R14 are each independently alkyl C1 - 6Or R13 and R14 are United to form pirrolidinilo; R15, R17, R16, R18, R19, R20 R21 and are each independently Hydrogen or alkyl of C1 - 6, a, D, e, F, I, J, K and M are each independently selected an integer from 0 to 4; b g, h, N, P, Q and R are each independently You selected an integer from 1 to 4; and C is 0 OR 1; or a Salt thereof.