APPLICATION OF PYRIMIDINE DERIVATIVES FOR TREATMENT OF EGFR-DEPENDENT DISEASES OR DISEASES WITH ACQUIRED RESISTANCE TO AGENTS AIMED AGAINST MEMBERS OF EGFR FAMILY

摘要

1. The use of the compounds of formula I! ! or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein W is CRw or N, wherein Rw is selected from the group consisting of! (1) hydrogen,! (2) cyano group,! (3) halogen,! (4) methyl,! (5) trifluoromethyl,! (6) sulfonamido group,! R1 is selected from the group including! (1) hydrogen,! (2) cyano group,! (3) nitro group,! (4) halogen,! (5) substituted and unsubstituted alkyl,! (6) substituted and unsubstituted alkenyl,! (7) substituted or unsubstituted alkynyl,! (8) substituted or unsubstituted aryl,! (9) substituted or unsubstituted heteroaryl,! (10) substituted or unsubstituted heterocyclyl,! (11) substituted or unsubstituted cycloalkyl,! (12) -COR1a,! (13) -CO2R1a,! (14) -CONR1aR1b,! (15) -NR1aR1b,! (16) -NR1aCOR1b,! (17) -NR1aSO2R1b,! (18) -OCOR1a,! (19) -OR1a,! (20) -SR1a,! (21) -SOR1a,! (22) -SO2R1a and! (23) -SO2NR1aR1b,! wherein R1a and R1b are independently selected from the group consisting of! (a) hydrogen,! (b) substituted and unsubstituted alkyl,! (c) substituted and unsubstituted aryl,! (d) substituted and unsubstituted heteroaryl,! (e) substituted and unsubstituted heterocyclyl and! (e) substituted and unsubstituted cycloalkyl,! R2 is selected from the group consisting of! (1) hydrogen,! (2) cyano group,! (3) nitro group,! (4) halogen,! (5) hydroxy group,! (6) amino group,! (7) substituted and unsubstituted alkyl,! (8) -COR2a and! (9) -NR2aCOR2b,! wherein R2a and R2b are independently selected from the group consisting of! (a) hydrogen and! (b) substituted and unsubstituted alkyl,! R3 is selected from the group including! (1) hydrogen,! (2) cyano group,! (3) nitro group,! (4) halogen,! (5) substituted and unsubstituted alkyl,! (6) substituted and unsubstituted alkenyl,! (7) substituted and unsubstituted alkynyl,! (8) substituted and unsubstituted aryl,! (9) substituted and unsubstituted heteroaryl,! (10) is substituted�