US 11,718,591 B2
Crystalline (2S,4R)-5-(5′-chloro-2′-fluoro-[1,1′-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2- methylpentanoic acid and uses thereof
Adam D. Hughes, Half Moon Bay, CA (US); Melissa Fleury, Brisbane, CA (US); Miroslav Rapta, San Carlos, CA (US); Venkat R. Thalladi, Foster City, CA (US); Gene Timothy Fass, San Bruno, CA (US); Michael Simeone, San Francisco, CA (US); R. Michael Baldwin, San Mateo, CA (US); and David L. Bourdet, Millbrae, CA (US)
Assigned to Theravance Biopharma R&D IP, LLC, South San Francisco, CA (US)
Filed by Theravance Biopharma R&D IP, LLC, South San Francisco, CA (US)
Filed on Dec. 14, 2021, as Appl. No. 17/550,564.
Application 16/582,051 is a division of application No. 16/125,991, filed on Sep. 10, 2018, granted, now 10,472,335, issued on Nov. 12, 2019.
Application 16/125,991 is a division of application No. 15/452,333, filed on Mar. 7, 2017, granted, now 10,100,021, issued on Oct. 16, 2018.
Application 17/550,564 is a continuation of application No. 16/928,206, filed on Jul. 14, 2020, granted, now 11,230,536.
Application 16/928,206 is a continuation of application No. 16/582,051, filed on Sep. 25, 2019, granted, now 10,752,599, issued on Aug. 25, 2020.
Claims priority of provisional application 62/346,336, filed on Jun. 6, 2016.
Claims priority of provisional application 62/305,393, filed on Mar. 8, 2016.
Prior Publication US 2022/0242836 A1, Aug. 4, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 261/18 (2006.01); A61K 9/00 (2006.01); A61K 9/48 (2006.01); A61K 31/415 (2006.01); A61K 45/06 (2006.01)
CPC C07D 261/18 (2013.01) [A61K 9/0053 (2013.01); A61K 9/4816 (2013.01); A61K 31/415 (2013.01); A61K 45/06 (2013.01); C07B 2200/13 (2013.01)] 20 Claims
 
1. A method of treating a disease mediated at least in part by neprilysin in a subject in need thereof, comprising administering to the subject an effective amount of a crystalline free acid form of (2S,4R)-5-(5′-chloro-2′-fluoro-[1,1′-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid.