US 12,077,508 B2
Inhibitors of the Notch transcriptional activation complex kinase (“NACK”) and methods for use of the same
Anthony J. Capobianco, Miami Beach, FL (US); Stephan C. Schürer, Coral Gables, FL (US); Xiaoxia Zhu, Palmetto Bay, FL (US); and Tanya T. Kelley, Miami, FL (US)
Assigned to University of Miami, Miami, FL (US)
Filed by UNIVERSITY OF MIAMI, Miami, FL (US)
Filed on Sep. 6, 2022, as Appl. No. 17/929,957.
Application 17/929,957 is a continuation of application No. 16/967,652, granted, now 11,649,214, previously published as PCT/US2019/016868, filed on Feb. 6, 2019.
Claims priority of provisional application 62/626,870, filed on Feb. 6, 2018.
Prior Publication US 2023/0113546 A1, Apr. 13, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 231/54 (2006.01)
CPC C07D 231/54 (2013.01) [C12Y 207/00 (2013.01); C12Y 306/01003 (2013.01)] 19 Claims
 
1. An oral pharmaceutical composition comprising a therapeutically effective amount of a compound according to Formula (Ia):

OG Complex Work Unit Chemistry
or pharmaceutically acceptable salt thereof, wherein:
A is C1-4alkyl or

OG Complex Work Unit Chemistry
X is CH or N;
Y is CH2 or N, and when X is N, then Y is CH2;
m is 0 or 1, and when m is 1 then Y is CH2;
n is 0 or 1;
R1 is H, C1-6alkyl, C0-6alkyleneC(═O)R6, halo, cyano, aryloxy, amino, C0-3alkylene-amido, carbamyl, S-thiocarbamyl, or ureido;
R2 is H, halo, C1-6alkyl, C3-8cycloalkyl, or heteroaryl;
each R3 and R4 independently is H, C1-6 alkyl, or C1-3aralkyl, or R3 and R4 and the nitrogen to which they are attached join together to form a 3-6 membered ring optionally comprising 1 to 3 additional heteroatoms selected from N, O, and S;
R5 is H, or R1 and R5 together with the atoms to which they are attached form a 5- or 6-membered heterocyclic ring comprising 1 to 3 ring heteroatoms selected from N, O, and S;
R6 is OH, C1-6alkyl, or OC1-6alkyl; and
R7 is H, halo or amino; and
a pharmaceutically acceptable carrier.