Treatment of brain and central nervous system tumors
The present invention provides methods for treating tumors of the brain by administering the compounds of the Formula A and particularly N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine, or a pharmaceutically acceptable salt thereof, to a subject in need of such treatment. In the methods of the invention, the compounds disclosed herein were surprisingly found to cross the blood brain barrier. The method of the present invention further relates to the treatment of cancers of any type potentially responding to EGFR, HER2, VEGFR2, or Src family kinase inhibitors and that are found in the brain.
1. A method for treating a brain or central nervous system tumor comprising administering to a subject in need of such treatment a therapeutically effective amount of a compound of Formula A:
wherein
each of X 1 , X 2 and X 3 are independently selected from the group consisting of H, F and Cl, wherein at least two of X 1 , X 2 and X 3 are F or Cl;
R 1 is C 1 to C 3 alkyl; and R 2 is C 1 to C 3 alkyl;
or a pharmaceutically acceptable salt thereof.
2. The method according to claim 1 , comprising administering to a subject in need of such treatment a therapeutically effective amount of a compound of Formula I:
or a pharmaceutically acceptable salt thereof.