Mutant-selective EGFR inhibitors and uses thereof
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
1. A method of treating a proliferative disorder comprising administering to a patient in need thereof a compound of formula I:
or a pharmaceutically acceptable salt thereof, wherein:
R 1 is —CF 3 or —Cl;
W is —O— or —NH—;
R 2 is —R or
R 3 is —R, —C(O)R, or —C(O)OR; and
each R is independently C 1-4 alkyl or C 1-4 fluoroalkyl; and wherein the proliferative disorder is a cancer.
2. The method according to claim 1 , wherein R 1 is —CF 3 .
3. The method according to claim 1 , wherein R 1 is —Cl.
4. The method according to claim 1 , wherein R 2 is
5. A method of treating a proliferative disorder comprising administering to a patient in need thereof a compound of formula II:
or a pharmaceutically acceptable salt thereof, wherein:
R 3 is —R, —C(O)R, or —C(O)OR; and
each R is independently C 1-4 alkyl or C 1-4 fluoroalkyl; and
wherein the proliferative disorder is a cancer.
6. The method according to claim 1 , wherein the compound is selected from:
or a pharmaceutically acceptable salt thereof.
7. The method of claim 1 , wherein the cancer is selected from breast cancer, glioblastoma, lung cancer, cancer of the head and neck, colorectal cancer, and bladder cancer.
8. The method of claim 7 , wherein the cancer is a lung cancer.
9. The method of claim 8 , wherein the lung cancer is non-small cell lung cancer.
10. The method of claim 5 , wherein the cancer is selected from breast cancer, glioblastoma, lung cancer, cancer of the head and neck, colorectal cancer, and bladder cancer.
11. The method of claim 10 , wherein the cancer is a lung cancer.
12. The method of claim 11 , wherein the lung cancer is non-small cell lung cancer.
13. The method according to claim 6 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
14. The method of claim 6 , wherein the cancer is selected from breast cancer, glioblastoma, lung cancer, cancer of the head and neck, colorectal cancer, and bladder cancer.
15. The method of claim 14 , wherein the cancer is a lung cancer.
16. The method of claim 15 , wherein the lung cancer is non-small cell lung cancer.