Patent ID: 6303652
Filing Date: 2001-10-16
Classification: A61K

Abstract:
A method for inhibiting BTK activity, comprising contacting BTK or a cell that expresses BTK with a compound of formula I: ##STR13##where:R.sub.1 is (C.sub.1 -C.sub.3)alkyl, (C.sub.3 -C.sub.6)cycloalkyl, phenyl, or NR.sub.a R.sub.b ;R.sub.2 is hydroxy, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkanoyloxy amino (C.sub.2 -C.sub.5)alkoxy; hydroxy (C.sub.2 -C.sub.5)alkoxy amino (C.sub.2 -C.sub.5)alkanoxy; or hydroxy (C.sub.2 -C.sub.5)alkanoxy;R.sub.3 is cyano or (C.sub.1 -C.sub.3)alkanoyl;R.sub.4 is hydrogen, (C.sub.1 -C.sub.3)alkyl; hydroxy (C.sub.2 -C.sub.5)alkyl; or amino (C.sub.2 -C.sub.5)alkyl;R.sub.5 is phenyl substituted by --S(O).sub.2 R.sub.c, or by halo and at least one other substituent;R.sub.a and R.sub.b are each independently hydrogen, or (C.sub.1 -C.sub.3)alkyl; or R.sub.a and R.sub.b together with the nitrogen to which they are attached are pyrrolidino, piperidino, morpholino, or thiomorpholino;wherein any phenyl of R.sub.1 and R.sub.5 is optionally substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkanoyl, --S(O).sub.2 R.sub.c, or NR.sub.a R.sub.b ; wherein R.sub.c is (C.sub.1 -C.sub.3)alkyl, or arylor a pharmaceutically acceptable salt thereof.