	US 12,227,536 B2
	Crystalline forms of an NRTTI compound
Daniel Skomski, East Brunswick, NJ (US); Yongchao Su, Chalfont, PA (US); Wei Xu, North Wales, NJ (US); Marko Cubrovic, Ridgewood, NJ (US); and Stephanie Elizabeth Barrett, Cranford, NJ (US)
Assigned to Merck Sharp & Dohme LLC, Rahway, NJ (US)
Appl. No. 17/415,570
Filed by Merck Sharp & Dohme LLC, Rahway, NJ (US)
PCT Filed Dec. 16, 2019, PCT No. PCT/US2019/066436 § 371(c)(1), (2) Date Jun. 17, 2021, PCT Pub. No. WO2020/131649, PCT Pub. Date Jun. 25, 2020.
Claims priority of provisional application 62/782,549, filed on Dec. 20, 2018.
Prior Publication US 2022/0056067 A1, Feb. 24, 2022
Int. Cl. C07H 19/173 (2006.01)

CPC C07H 19/173 (2013.01) [C07B 2200/13 (2013.01)]

18 Claims

1. Crystalline anhydrous Form 1 of 2′ deoxy-4′-C-ethynyl-2-fluoroadenosine (EFdA) characterized by:

(1) a powder x-ray diffraction pattern with peaks at diffraction angles degrees 2 theta (+/−) 0.2° of 4.48, 11.79, 14.70 and 25.81 in a powder x-ray diffraction obtained using Cu K alpha radiation, and/or

(2) a solid state ¹⁹F NMR spectrum comprising any two of the following peaks: −114.75, −117.09 and −118.92 ppm.