US 11,786,498 B2
Sacubitril calcium salts
David Hook, Rheinfelden (CH); Bin Hu, Green Brook, NJ (US); Florian Karl Kleinbeck, Zurich (CH); Ulrich Meier, Riehen (CH); Sibylle Mueller, Frenkendorf (CH); Jean-Paul Mutz, Blotzheim (FR); Jan Schlomach, Basel (CH); Paul Allen Sutton, Getzville, NY (US); Liladhar Murlidhar Waykole, Succasunna, NJ (US); and Bernhard Wietfeld, Efringen-Kirchen (DE)
Assigned to Novartis AG, Basel (CH)
Appl. No. 15/737,985
Filed by Novartis AG, Basel (CH)
PCT Filed Jul. 2, 2015, PCT No. PCT/US2015/039010
§ 371(c)(1), (2) Date Dec. 19, 2017,
PCT Pub. No. WO2017/003483, PCT Pub. Date Jan. 5, 2017.
Prior Publication US 2018/0296519 A1, Oct. 18, 2018
Int. Cl. A61K 31/22 (2006.01); A61P 9/10 (2006.01); A61P 9/06 (2006.01); A61P 25/02 (2006.01); C07C 229/34 (2006.01); A61P 9/12 (2006.01); A61P 25/06 (2006.01); A61K 31/4178 (2006.01); A61K 31/423 (2006.01)
CPC A61K 31/22 (2013.01) [A61P 9/06 (2018.01); A61P 9/10 (2018.01); A61P 9/12 (2018.01); A61P 25/02 (2018.01); A61P 25/06 (2018.01); C07C 229/34 (2013.01); A61K 31/4178 (2013.01); A61K 31/423 (2013.01); A61K 2300/00 (2013.01); C07B 2200/13 (2013.01)] 12 Claims
OG exemplary drawing
 
1. A crystalline form of a calcium salt of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl) -4-amino-(2R)-methyl butanoic acid ethyl ester having the formula (I)

OG Complex Work Unit Chemistry
wherein the crystalline form is Modification B or hydrate form HB, wherein
Modification B is characterized in that said form has an X-ray powder diffraction pattern comprising 2θ values (±0.1°) (CuKα; 45 kV, 40 mA;λ=1.540598 Å) selected from 4.6, 6.0, 12.6, 15.5, 16.6, 19.6 and 22.5 degrees at a temperature of 20 to 25° C., and
Modification HB is characterized in that said form has an X-ray powder diffraction pattern comprising 2θ values (±0.1°) (CuKα; 45 kV, 40 mA;λ=1.540598 Å) selected from 3.6, 6.4, 8.4, 14.6, 15.3, 16.8, 17.8, 19.7 and 20.6 degrees at a temperature of 20 to 25° C.