Substituted heteroaromatic amines and uses thereof
The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic protein.
1 . A compound of Formula:
or a pharmaceutically acceptable salt or solvate thereof, wherein:
R 2 is selected from
R 3 is independently selected at each occurrence from C 1-6 alkyl, C 2-6 alkenyl, and C 2-6 alkynyl, each of which is optionally substituted with one, two, or three substituents independently selected from halogen and —CN;
R 6 is selected from hydrogen, halogen, and C 1-3 haloalkyl;
m is 0, 1, 2, or 3; and
n is 1 or 2.
2 . The compound, salt, or solvate of claim 1 , wherein R 2 is selected from
3 . The compound, salt, or solvate of claim 1 , wherein m is 0 or 1.
4 . The compound, salt, or solvate of claim 1 , wherein R 6 is chlorine.
5 . The compound, salt, or solvate of claim 1 , wherein n is 1.
6 . The compound of claim 1 having the formula
or a salt or solvate thereof.
7 . The compound of claim 1 , wherein the compound is selected from
or a salt or solvate thereof.
8 . A compound having the formula
or a salt or solvate thereof.
9 . A compound having the formula
or a salt or solvate thereof.
10 . The compound of claim 7 having the formula
or a salt or solvate thereof.
11 . The compound of claim 7 having the formula
or a salt or solvate thereof.
12 . The compound of claim 7 having the formula
or a salt or solvate thereof.
13 . The compound of claim 7 having the formula
or a salt or solvate thereof.
14 . A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable excipient.
15 . A pharmaceutical composition comprising a compound of claim 7 , or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable excipient.
16 . A method of treating cancer having amplified wildtype Ras or a Ras mutant protein in a subject, the method comprising: inhibiting amplified wildtype Ras or the Ras mutant protein by administering to said subject an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof.