US 11,944,611 B2
Capsid inhibitors for the treatment of HIV
Laura Elizabeth Bauer, Santa Clara, CA (US); Anna Chiu, Burlingame, CA (US); Eric M. Gorman, Hayward, CA (US); Andrew Stephen Mulato, Dublin, CA (US); Martin Sunkwang Rhee, Foster City, CA (US); Charles William Rowe, San Bruno, CA (US); Scott P. Sellers, Hillsborough, CA (US); Dimitrios Stefanidis, Saratoga, CA (US); Winston C. Tse, Redwood City, CA (US); Stephen R. Yant, Boulder Creek, CA (US); and Dana J. Levine, San Leandro, CA (US)
Assigned to Gilead Sciences, Inc., Foster City, CA (US)
Filed by Gilead Sciences, Inc., Foster City, CA (US)
Filed on Jul. 15, 2019, as Appl. No. 16/512,166.
Claims priority of provisional application 62/698,611, filed on Jul. 16, 2018.
Prior Publication US 2020/0038389 A1, Feb. 6, 2020
Int. Cl. A61K 31/4439 (2006.01); A61K 9/00 (2006.01); A61K 9/48 (2006.01); A61K 31/34 (2006.01); A61K 31/4418 (2006.01); A61K 31/536 (2006.01); A61K 31/5365 (2006.01); A61K 31/685 (2006.01); A61P 31/18 (2006.01)
CPC A61K 31/4439 (2013.01) [A61K 9/0019 (2013.01); A61K 9/0053 (2013.01); A61K 9/4825 (2013.01); A61K 31/34 (2013.01); A61K 31/4418 (2013.01); A61K 31/536 (2013.01); A61K 31/5365 (2013.01); A61K 31/685 (2013.01); A61P 31/18 (2018.01)] 34 Claims
 
1. A method of treating human immunodeficiency virus (HIV) infection in a heavily treatment-experienced patient, the method comprising administering to the patient a therapeutically effective amount of a pharmaceutical composition comprising a sodium salt of the compound of Formula (Ia):

OG Complex Work Unit Chemistry
one or more pharmaceutically acceptable excipients, wherein the pharmaceutical composition is in the form of a solution comprising about 10 w/w % to about 40 w/w % water, about 35 w/w % to about 75 w/w % polyethylene glycol 300 (PEG 300), and about 5 w/w % to about 35 w/w % of the sodium salt of the compound of Formula (Ia);
wherein the HIV infection is an HIV-1 infection characterized by HIV-1 mutant resistance to one or more antiretroviral medications.