US 12,391,671 B2
Allosteric EGFR inhibitors and methods of use thereof
David A. Scott, Newton, MA (US); David Heppner, Brookline, MA (US); Thomas Gero, Stow, MA (US); Courtney A. Cullis, Bedford, MA (US); Ciric To, Medford, MA (US); Shih-Chung Huang, Lexington, MA (US); Yongbo Hu, Winchester, MA (US); Steve Stroud, Cambridge, MA (US); Tyler Beyett, Brookline, MA (US); Michael Eck, Brookline, MA (US); and Nathanael S. Gray, Jamaica Plain, MA (US)
Assigned to Dana-Farber Cancer Institute, Inc., Boston, MA (US)
Filed by Dana-Farber Cancer Institute, Inc., Boston, MA (US)
Filed on May 10, 2022, as Appl. No. 17/741,206.
Application 17/741,206 is a continuation of application No. PCT/US2020/060001, filed on Nov. 11, 2020.
Claims priority of provisional application 63/030,655, filed on May 27, 2020.
Claims priority of provisional application 62/933,776, filed on Nov. 11, 2019.
Prior Publication US 2022/0411404 A1, Dec. 29, 2022
Int. Cl. A61K 31/4184 (2006.01); A61K 31/4439 (2006.01); A61K 31/454 (2006.01); A61K 31/4545 (2006.01); A61K 31/4725 (2006.01); A61K 31/506 (2006.01); A61K 31/513 (2006.01); A61K 31/517 (2006.01); A61K 31/519 (2006.01); A61K 31/52 (2006.01); A61K 31/5377 (2006.01); A61K 31/541 (2006.01); A61K 45/06 (2006.01); A61P 35/00 (2006.01); C07D 401/14 (2006.01); C07D 403/06 (2006.01); C07D 403/14 (2006.01); C07D 471/04 (2006.01); C07D 473/00 (2006.01); C07D 487/04 (2006.01); C07D 495/14 (2006.01)
CPC C07D 401/14 (2013.01) [C07D 471/04 (2013.01); C07D 473/00 (2013.01); C07D 495/14 (2013.01)] 29 Claims
 
1. A compound of Formula Ia:

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof;
wherein:
A and A′ are each, independently, CH or N;
W and Z are each, independently, CH or C-halo;
R1 is selected from the group consisting of:

OG Complex Work Unit Chemistry
R3 is phenyl optionally substituted one time with piperidine, wherein piperidine is substituted one time with R7;
R6 is independently, at each occurrence, hydroxy or halo; and
R7 is independently, at each occurrence, C1-C6 alkyl.