US 11,903,936 B2
Anti-malarial agents
Margaret Phillips, Dallas, TX (US); Michael Palmer, Broadstairs (GB); Susan A. Charman, South Melbourne (AU); Karl Shawn Watts, Portland, OR (US); Aleksey I. Gerasyuto, Flemington, NJ (US); and Goran Krilov, Long Island City, NY (US)
Assigned to THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, Austin, TX (US); and MMV MEDICINES FOR MALARIA VENTURE, Geneva (CH)
Appl. No. 17/787,378
Filed by THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, Austin, TX (US); and MMV MEDICINES FOR MALARIA VENTURE, Geneva (CH)
PCT Filed Dec. 18, 2020, PCT No. PCT/EP2020/087166
§ 371(c)(1), (2) Date Jun. 20, 2022,
PCT Pub. No. WO2021/123266, PCT Pub. Date Jun. 24, 2021.
Claims priority of provisional application 62/951,218, filed on Dec. 20, 2019.
Claims priority of application No. 19219647 (EP), filed on Dec. 24, 2019.
Prior Publication US 2023/0056202 A1, Feb. 23, 2023
Int. Cl. C07D 401/14 (2006.01); A61P 33/06 (2006.01); A61K 31/4439 (2006.01); A61K 31/122 (2006.01); A61K 31/137 (2006.01); A61K 31/155 (2006.01); A61K 31/366 (2006.01); A61K 31/4196 (2006.01); A61K 31/4706 (2006.01); A61K 31/4709 (2006.01); A61K 31/473 (2006.01); A61K 31/4745 (2006.01); A61K 31/65 (2006.01); C07D 403/12 (2006.01)
CPC A61K 31/4439 (2013.01) [A61K 31/122 (2013.01); A61K 31/137 (2013.01); A61K 31/155 (2013.01); A61K 31/366 (2013.01); A61K 31/4196 (2013.01); A61K 31/473 (2013.01); A61K 31/4706 (2013.01); A61K 31/4709 (2013.01); A61K 31/4745 (2013.01); A61K 31/65 (2013.01); A61P 33/06 (2018.01); C07D 401/14 (2013.01); C07D 403/12 (2013.01)] 24 Claims
 
1. A compound according to Formula (I):

OG Complex Work Unit Chemistry
wherein R1 is an optionally substituted 5-membered heterocycle; R2 is H or both R2 are joined to form an optionally substituted cyclopropyl; R3 is selected from an optionally substituted monocyclic aryl and an optionally substituted heteroaryl; pharmaceutically acceptable salts, hydrates, tautomers, racemic mixtures, or optically active forms thereof, wherein the term substituted refers to a group substituted with from 1 to 5 substituents selected from the group consisting of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8-cycloalkyl, heterocycloalkyl, C1-C6 alkyl aryl, C1-C6 alkyl heteroaryl, C1-C6 alkyl C3-C8-cycloalkyl, C1-C6 alkyl heterocycloalkyl, acyl, amino, amide, aminosulfonyl, ammonium, acyl amino, aminocarbonyl, aryl, heteroaryl, sulfinyl, sulfonyl, sulphonamide, alkoxy, alkoxy carbonyl, carbamate, sulfanyl, halogen, trihalomethyl, cyano, hydroxy, mercapto, and nitro.