	US 12,187,707 B2
	Pharmaceutical formulations of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylaminde and salts thereof
Michael Nicholas Greco, Lansdale, PA (US); Michael John Costanzo, Bonney Lake, WA (US); Michael Alan Green, Easton, PA (US); Jirong Peng, Mequon, WI (US); Victoria Lynn Wilde, Montclair, NJ (US); and Don Zhang, Princeton, NJ (US)
Assigned to BETA PHARMA, INC., Wilmington, DE (US)
Filed by Beta Pharma, Inc., Wilmington, DE (US)
Filed on Nov. 12, 2021, as Appl. No. 17/524,866.
Application 17/524,866 is a division of application No. 16/622,119, granted, now 11,180,478, previously published as PCT/US2018/037744, filed on Jun. 15, 2018.
Claims priority of provisional application 62/521,007, filed on Jun. 16, 2017.
Prior Publication US 2022/0153726 A1, May 19, 2022
Int. Cl. A61K 31/506 (2006.01); C07D 403/04 (2006.01); A61K 47/02 (2006.01); A61K 47/10 (2017.01); A61K 47/38 (2006.01)

CPC C07D 403/04 (2013.01) [A61K 31/506 (2013.01); A61K 47/02 (2013.01); A61K 47/10 (2013.01); A61K 47/38 (2013.01); C07B 2200/13 (2013.01)]

13 Claims

1. A method of treating a disease or disorder associated with one or more mutants of EGFR selected from the group consisting of L858R activating mutants L858R; delE746-A750; G719S; the Exon 19 deletion activating mutant; and the T790M resistance mutant, comprising administration of a therapeutically effective amount of a pharmaceutical formulation comprising a methanesulfonic acid salt of the compound of

and one or more pharmaceutically acceptable excipients,

wherein

the methanesulfonic acid salt is in crystalline Form 2A having an X-ray powder diffraction pattern comprising the following 20 values measured using CuKα radiation: 1.6°±0.2°, 15.5°±0.2°, 17.9°±0.2°, 22.1°±0.2°, and 25.2°±0.2°, or

the methanesulfonic acid salt is in crystalline Form 2B having an X-ray powder diffraction pattern comprising the following 20 values measured using CuKα radiation: 1.8°±0.2°, 15.7°±0.2°, 18.2°±0.2°, 20.3°±0.2°.