Invention Publication
- Patent Title: THIOPHENE COMPOUND AND APPLICATION THEREOF
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Application No.: US18549188Application Date: 2022-03-04
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Publication No.: US20240199571A1Publication Date: 2024-06-20
- Inventor: Lingyun WU , Zhen ZHAN , Lele ZHAO , Jianjun SUN , Yi QIAN , Shuhui CHEN
- Applicant: MEDSHINE DISCOVERY INC.
- Applicant Address: CN Jiangsu
- Assignee: MEDSHINE DISCOVERY INC.
- Current Assignee: MEDSHINE DISCOVERY INC.
- Current Assignee Address: CN Jiangsu
- Priority: CN 2110268287.6 2021.03.11 CN 2110573989.5 2021.05.25 CN 2111217911.6 2021.10.19 CN 2210172993.5 2022.02.24
- International Application: PCT/CN2022/079277 2022.03.04
- Date entered country: 2023-09-06
- Main IPC: C07D333/22
- IPC: C07D333/22 ; A61K31/381 ; A61K31/407 ; A61K31/438 ; A61K31/439 ; A61K31/495 ; A61K31/551 ; C07D403/04 ; C07D413/04

Abstract:
The present invention relates to a thiophene compound and an application thereof. The present invention specifically relates to a compound represented by formula (II) and a pharmaceutically acceptable salt thereof, wherein L1 is —C(═O)— or —C(═O)—NH—; R1 is R1a or aa; ring A is bb or cc; R1a is C1-3 alkyl substituted with 1, 2 or 3 Ra; and R3 is independently H, halogen or C1-3 alkoxy. The compound represented by formula (II) and the pharmaceutically acceptable salt thereof can better inhibit the activity of LSD1, further shows significant inhibitory activity against NCI-H1417 cell proliferation, and has good pharmacokinetic properties (including good oral bioavailability, oral exposure, half-life, and clearance rate, etc.).
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