Rigel Pharmaceuticals, Inc.
2,4-DIAMINO-PYRIMIDINE COMPOUNDS AND METHOD FOR MAKING AND USING THE COMPOUNDS

Abstract:

Compounds within the scope of the present invention have a Formula 1 ##STR00001## or a salt or produg thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R.sup.1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R.sup.2 and R.sup.3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC.sub.50 of from 0.003 .mu.M to 3.7 M; a TAK1 IC.sub.50 of from 0.008 .mu.M to 132 M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.