US 12,325,708 B2
Adenosine 2 receptor antagonists
Neel K. Anand, San Mateo, CA (US); Natalia Aurrecoechea, Oakland, CA (US); Anthony James Brockway, Oakland, CA (US); Haiying Cai, Cupertino, CA (US); Lin Cheng, Sunnyvale, CA (US); Bo-Liang Deng, San Ramon, CA (US); Donogh John Roger O'Mahony, San Mateo, CA (US); Zhongxu Ren, Foster City, CA (US); and Wen Zhang, Palo Alto, CA (US)
Assigned to Nektar Therapeutics, San Francisco, CA (US)
Appl. No. 17/608,582
Filed by Nektar Therapeutics, San Francisco, CA (US)
PCT Filed May 1, 2020, PCT No. PCT/US2020/031185
§ 371(c)(1), (2) Date Nov. 3, 2021,
PCT Pub. No. WO2020/227156, PCT Pub. Date Nov. 12, 2020.
Claims priority of provisional application 62/863,377, filed on Jun. 19, 2019.
Claims priority of provisional application 62/843,194, filed on May 3, 2019.
Prior Publication US 2022/0235056 A1, Jul. 28, 2022
Int. Cl. C07D 487/04 (2006.01); C07D 519/00 (2006.01)
CPC C07D 487/04 (2013.01) [C07D 519/00 (2013.01); C07B 2200/05 (2013.01)] 17 Claims
 
1. A compound having a formula:

OG Complex Work Unit Chemistry
wherein R, in each instance, is independently selected from H and D;
R1 is selected from —CH3 and —CD3;
R2 is selected from the group consisting of H, F, Cl, —CF3, —OCH3, and —OCD3;
R3 is selected from hydrogen, —CH3, —CD3, and —CF3;
R4 and R5 are each selected from H, D, or combine with the intervening atoms to form a 5-membered ring;
X1, X2 and X3 are independently selected from —N— and —CH—; and
Y is selected from —CH— and —N—
wherein the compound is an adenosine A2A receptor (A2AR) selective antagonist.