US 12,403,198 B2
Benzimidazole thiophene derivative compounds inducing selective degradation of PLK1
Si Woo Choi, Incheon (KR); Soo Hee Ryu, Incheon (KR); Ji Hoon Ryu, Seoul (KR); San Ha Son, Incheon (KR); Hwa Jin Lee, Incheon (KR); Seong Hoon Kim, Incheon (KR); Boas Nam, Incheon (KR); Im Suk Min, Gyeonggi-do (KR); Hye Guk Ryu, Incheon (KR); and Keum Young Kang, Incheon (KR)
Assigned to UPPTHERA, Incheon (KR)
Appl. No. 17/914,565
Filed by UPPTHERA, Incheon (KR)
PCT Filed Mar. 27, 2021, PCT No. PCT/KR2021/003810
§ 371(c)(1), (2) Date Sep. 26, 2022,
PCT Pub. No. WO2021/194321, PCT Pub. Date Sep. 30, 2021.
Claims priority of application No. 10-2020-0037875 (KR), filed on Mar. 27, 2020.
Prior Publication US 2023/0159515 A1, May 25, 2023
Int. Cl. A61K 47/55 (2017.01); A61K 47/54 (2017.01); C07D 401/14 (2006.01); C07D 409/14 (2006.01); C07D 417/14 (2006.01)
CPC A61K 47/55 (2017.08) [A61K 47/545 (2017.08); C07D 401/14 (2013.01); C07D 409/14 (2013.01); C07D 417/14 (2013.01)] 7 Claims
 
1. A compound represented by the following Formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof:
ULM-Linker-PTM  [Formula I]
wherein in the Formula I above,
ULM is E3 ubiquitin ligase binding moiety represented by the following Formula A or B:

OG Complex Work Unit Chemistry
wherein X1 is —CH2— or —CO—;

OG Complex Work Unit Chemistry
wherein

OG Complex Work Unit Chemistry
 is a 5-membered heteroaryl; and Y1 is hydrogen or C1-3 alkyl;
PTM is PLK1 binding moiety represented by the following Formula II:

OG Complex Work Unit Chemistry
 and
Linker is a chemical group that links ULM and PTM.