Fused cyclic compound capable of degrading protein and use thereof

Patent metadata

Field	Value
Publication number	US-12466816-B2
Application number	US-202017641759-A
Country	US
Kind code	B2
Filing date	Sep 11, 2020
Priority date	Sep 12, 2019
Publication date	Nov 11, 2025
Grant date	Nov 11, 2025

Abstract

The present disclosure discloses a compound shown in formula (II) and a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising the compound as an active ingredient, and use thereof in the preparation of medicaments for protein degradation.

First claim

The invention claimed is:

1 . A compound of formula (II) or a pharmaceutically acceptable salt thereof,

wherein,
E is selected from CH and N;
R 1 is selected from C 1-4 alkyl, C 2-3 alkenyl,

cyclopropyl and furyl, wherein the C 1-4 alkyl and C 2-3 alkenyl may be optionally substituted with 1, 2, or 3 R a ;
T 1 is selected from C(R 3 ) and N;
R 2 is selected from H, F, Cl, Br, I, CH 3 and CF 3 ;
R 3 is selected from H, F, Cl, Br, I and CH 3 , wherein the CH 3 may be optionally substituted with 1, 2 or 3 halogen;
each R a is selected from halogen, OCH 3 , and NH 2 .

2 . The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R 2 is selected from H, Cl, and CF 3 .

3 . The compound according to claim 2 or a pharmaceutically acceptable salt thereof, wherein R 2 is Cl.

4 . The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R 3 is selected from H, F, Cl, Br, I, and CH 3 , and wherein CH 3 may be optionally substituted with 1, 2, or 3 F.

5 . The compound according to claim 4 or a pharmaceutically acceptable salt thereof, wherein R 3 is selected from H, F, Cl, Br, I, and CH 3 .

6 . The compound according to claim 5 or a pharmaceutically acceptable salt thereof, wherein R 3 is H or CH 3 .

7 . The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from

CH═CH 2 , CH 3 , CH 2 CH 3 , and CH 2 CH 2 CH 3 , and wherein the CH 3 , CH 2 CH 3 , and CH 2 CH 2 CH 3 may be optionally substituted with 1, 2, or 3 R a .

8 . The compound according to claim 7 or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from

—CH═CH 2 , —CH 2 NH 2 , —CH 2 CH 3 , —CH 2 CH 2 OCH 3 , and —CH 2 CH 2 CH 3 .

9 . The compound according to claim 1 or a pharmaceutically acceptable salt thereof, which is selected from

wherein,
m is selected from 1, 2, and 3.

10 . A compound or a pharmaceutically acceptable salt thereof, which is selected from

11 . A pharmaceutical composition comprising the compound according to claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Assignees

• Medshine Discovery Inc
• Univ Shanghai Technology

Inventors

• Luo Yunfu
• Cang Yong
• Peng Bo
• Lei Maoyi
• Xu Yu
• Chen Shuhui

Classifications

• C07D413/04

  directly linked by a ring-member-to-ring-member bond · CPC title

• C07D405/14

  containing three or more hetero rings · CPC title

• C07D307/79

  with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring · CPC title

• C07D261/20

  condensed with carbocyclic rings or ring systems · CPC title

• A61P37/02

  Immunomodulators · CPC title