US 11,938,128 B2
Small molecule BAX inhibitors and uses thereof
Evripidis Gavathiotis, Roslyn, NY (US); Richard N. Kitsis, New York, NY (US); Thomas P. Garner, Long Island City, NY (US); Dulguun Amgalan, Bronx, NY (US); Lorrie Kirshenbaum, Winnipeg (CA); and Felix Kopp, Brooklyn, NY (US)
Assigned to Albert Einstein College of Medicine, Bronx, NY (US); and The University of Manitoba, Winnipeg (CA)
Appl. No. 16/492,300
Filed by Albert Einstein College of Medicine, Bronx, NY (US); and The University of Manitoba, Winnipeg (CA)
PCT Filed Mar. 9, 2018, PCT No. PCT/US2018/021644
§ 371(c)(1), (2) Date Sep. 9, 2019,
PCT Pub. No. WO2018/165494, PCT Pub. Date Sep. 13, 2018.
Claims priority of provisional application 62/469,551, filed on Mar. 10, 2017.
Prior Publication US 2020/0009132 A1, Jan. 9, 2020
Int. Cl. A61K 31/496 (2006.01); A61K 31/495 (2006.01); C07D 209/86 (2006.01); C07D 209/88 (2006.01); C07D 279/26 (2006.01); C07D 295/13 (2006.01)
CPC A61K 31/496 (2013.01) [A61K 31/495 (2013.01); C07D 209/86 (2013.01); C07D 209/88 (2013.01); C07D 279/26 (2013.01); C07D 295/13 (2013.01)] 22 Claims
 
1. A compound having the structure of formula (VII)

OG Complex Work Unit Chemistry
wherein
A is phenyl;
B is phenyl;
R1 and R2 are independently none, C1-C5 alkyl, F, Cl, Br, I, CN, NO2, NR42, OR4, CF3, COOH, COOR4, NHR4, OCR4, SR4, SOR4, or SO2R4;
X is F, Cl, Br, I, NR42, or OR4; wherein the bond between X and the main scaffold is a single bond;
Q is

OG Complex Work Unit Chemistry
R3 is none, H, C1-C6 alkyl, R4(C═O), or (CH2)pOH;
R4 is H or C1-C3 alkyl;
Y is S, or N;
p is 1-3;
m is 1 and n is 1;
or a pharmaceutically acceptable salt thereof.