US 11,685,725 B2
YAP1 inhibitors that target the interaction of YAP1 with OCT4
Srikumar Chellappan, Tampa, FL (US); Nicholas J. Lawrence, Tampa, FL (US); and Sujeewa Ranatunga Mahanthe Mudiyanselage, Tampa, FL (US)
Assigned to H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC., Tampa, FL (US)
Appl. No. 16/980,538
Filed by H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC., Tampa, FL (US)
PCT Filed Mar. 14, 2019, PCT No. PCT/US2019/022337
§ 371(c)(1), (2) Date Sep. 14, 2020,
PCT Pub. No. WO2019/178401, PCT Pub. Date Sep. 19, 2019.
Claims priority of provisional application 62/643,032, filed on Mar. 14, 2018.
Prior Publication US 2021/0363128 A1, Nov. 25, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 401/06 (2006.01); A61K 45/06 (2006.01); C07D 211/34 (2006.01); C07D 401/10 (2006.01); C07D 401/12 (2006.01)
CPC C07D 401/06 (2013.01) [A61K 45/06 (2013.01); C07D 211/34 (2013.01); C07D 401/10 (2013.01); C07D 401/12 (2013.01)] 29 Claims
 
1. A compound of Formula I,

OG Complex Work Unit Chemistry
wherein,
the dash line is a bond that is present or absent;
n is 0, 1, or 2;
Ar is phenyl, pyridinyl, pyrimidinyl, or pyrazinyl;
R1 is C1-C8 alkyl, C3-C6 cycloalkyl, or C6 aryl, and of which is optionally substituted with one or more groups chosen from halo, hydroxyl, cyano, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxyl, C1-C6 haloalkoxyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, C6 aryl, heteroaryl, OCH2-C6 aryl, or O—CH2-heteroaryl;
R2 is halo, OH, C1-C8 alkyl, C1-C8 alkoxyl, C6 aryl, O—C6 aryl, heteroaryl, O-heteroaryl, O—CH2-C6 aryl, or O—CH2-heteroaryl; and
R3 is CH2OH, CO2H, CO2-C1-C6 alkyl, CO2-C3-C6 cycloalkyl, or CO2-C1-C6 heteroalkyl,
or a pharmaceutically acceptable salt thereof.