Tri-substituted heteroaryls and methods of making and using the same

摘要

Disclosed is a compound of formula (I) or an N-oxide or pharmaceutical acceptable salt thereof wherein R1 is aryl, heteroaryl, aralkyl or heteroaralkyl; X is piperidinyl, piperazinyl, pyrrolidinyl, tetrahydrofuran, cyclohexyl, cyclopentyl, bicyclo[2.2.1]heptane, bicyclo[2.2.2]octane, bicyclo[3.2.1]octane, 2-oxa-bicyclo[2.2.2]octane, 2-aza- bicyclo[2.2.2]octane, 3-aza- bicyclo[3.2.1]octane or 1-aza-bicyclo[2.2.2]octane; Each of A1 and A2 are independently O, S, N or NRb provided that at least one of A1 and A2 is N; and the remainder of the substituents are as described in the specification. The compounds described are antagonists of the TGF beta type I receptors Alk5 and Alk4 useful in the treatment of disorder related to the TGF beta signalling pathway.