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COMPOSES DE 2,4-DIAMINOPYRIMIDINE ET PROCEDE DE PREPARATION ET D'UTILISATION DE CES COMPOSES
专利权人:
RIGEL PHARMACEUTICALS; INC.
发明人:
CHEN, YAN,YEN, ROSE,YU, JIAXIN,TAYLOR, VANESSA,SINGH, RAJINDER
申请号:
CA3028997
公开号:
CA3028997A1
申请日:
2017.06.26
申请国别(地区):
CA
年份:
2018
代理人:
摘要:
Compounds within the scope of the present invention have a Formula 1 or a salt or produg thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 µ? to 3.7 µ?; a TAK1 IC50 of from 0.008 µ? to 132 µ?; 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.
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