Substituted pyrimidines useful as EGFR-T790M kinase inhibitors
The present invention is directed to novel pyrimidines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases and/or mutants mediated diseases and conditions.
1. A compound according to Formula I:
or a pharmaceutically acceptable salt, solvate, stereoisomer or tautomer thereof, wherein
R 1 is hydrogen, C 1 -C 6 alkoxy, F, Cl, or CF 3 ;
R 2 is C 1 -C 6 alkyl or C(O)R 3 ; and
R 3 is C 1 -C 6 alkyl;
with the proviso that when R 1 is C 1 -C 6 alkoxy, R 2 is not C(O)R 3 .
2. The compound as claimed in claim 1 , wherein R′ is selected from the group consisting of hydrogen and C 1 -C 6 alkoxy.
3. The compound as claimed in claim 1 , wherein R 1 is hydrogen.
4. The compound as claimed in claim 1 , wherein R 1 is hydrogen and R 2 is C 1 -C 6 alkyl.
5. The compound as claimed in claim 1 , wherein R 1 is C 1 -C 6 alkoxy and R 2 is C 1 -C 6 alkyl.
6. A compound or its pharmaceutically acceptable salt, solvate, stereoisomer or tautomer thereof selected from the group consisting of:
7. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
8. A method for treating neoplasia in an individual, comprising: administering to the individual a therapeutically effective amount of a pharmaceutical composition, the pharmaceutical composition comprising a compound of claim 1 or a pharmaceutical acceptable salt thereof and a pharmaceutically acceptable carrier, and wherein the neoplasia is non-small cell lung cancer.