US 12,410,171 B2
Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
Jing Liu, Oradell, NJ (US); Jialiang Wang, Nashville, TN (US); Xiaoran Han, Shanghai (CN); Liqun Chen, Shanghai (CN); and Chengwei Zhang, Shanghai (CN)
Assigned to CULLGEN (SHANGHAI), INC., Shanghai (CN)
Appl. No. 17/904,822
Filed by Cullgen (Shanghai), Inc., Shanghai (CN)
PCT Filed Feb. 26, 2021, PCT No. PCT/CN2021/078240
§ 371(c)(1), (2) Date Aug. 23, 2022,
PCT Pub. No. WO2021/170109, PCT Pub. Date Sep. 2, 2021.
Claims priority of application No. PCT/CN2020/076748 (WO), filed on Feb. 26, 2020.
Prior Publication US 2023/0257380 A1, Aug. 17, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 45/06 (2006.01); A61K 31/496 (2006.01); A61K 31/5025 (2006.01); A61K 31/53 (2006.01); A61P 19/00 (2006.01); A61P 25/28 (2006.01); A61P 29/00 (2006.01); A61P 31/00 (2006.01); A61P 35/00 (2006.01); C07D 405/14 (2006.01); C07D 417/14 (2006.01); C07D 471/04 (2006.01); C07D 487/04 (2006.01)
CPC C07D 487/04 (2013.01) [C07D 405/14 (2013.01); C07D 417/14 (2013.01); C07D 471/04 (2013.01)] 12 Claims
 
1. A bivalent compound, selected from the group consisting of:
(S)-N-(5-(3,5-Difluorobenzyl)-1H-indazol-3-yl)-4-(4-((1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)azetidin-3-yl)methyl)piperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino)benzamide (TR-341); and
(R)-N-(5-(3,5-Difluorobenzyl)-1H-indazol-3-yl)-4-(4-((1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)azetidin-3-yl)methyl)piperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino)benzamide (TR-342);
or a pharmaceutically acceptable salt thereof.