IP Library › Granted Patent US 12,065,442
Granted Patent B2
US 12,065,442 · App. 17/269,670 · Granted Aug 20, 2024

Tropomyosin receptor kinase (TRK) degradation compounds and methods of use

Inventors: Jing Liu (Oradell, NJ); Liqun Chen (Shanghai, CN)
Assignee: CULLGEN (SHANGHAI), INC.
C07D487/04C07D405/14C07D417/14C07D471/04
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Quick Facts
Patent No.
US 12,065,442
App. No.
17/269,670
Granted
Aug 20, 2024
Kind
B2
Abstract

Bivalent compounds, compositions comprising one or more of the bivalent compounds, and methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof are provided. Methods for identifying such bivalent compounds are provided, either.

Claims (6)

1. A compound which is N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-[4-[[1-[2-(2,6-dioxo-3-piperidyl)-1,3-dioxo-isoindolin-5-yl]azetidin-3-yl]methyl]piperazin-1-yl]-2-(tetrahydropyran-4-ylamino)benzamide (TR-231), or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

3. A compound which is N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-[4-[[1-[2-(2,6-dioxo-3-piperidyl)-1,3-dioxo-isoindolin-5-yl]azetidin-3-yl]methyl]piperazin-1-yl]-2-(tetrahydropyran-4-ylamino)benzamide (TR-231).

4. A pharmaceutical composition comprising a compound of claim 3 , and a pharmaceutically acceptable excipient.

5. A pharmaceutically acceptable salt of N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-[4-[[1-[2-(2,6-dioxo-3-piperidyl)-1,3-dioxo-isoindolin-5-yl]azetidin-3-yl]methyl]piperazin-1-yl]-2-(tetrahydropyran-4-ylamino)benzamide (TR-231).

6. A pharmaceutical composition comprising a pharmaceutically acceptable salt of claim 5 , and a pharmaceutically acceptable excipient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2021
From: LIU, JING; PLEWE, MICHAEL BRUNO; WANG, JIALIANG; HAN, XIAORAN; CHEN, LIQUN
To: CULLGEN (SHANGHAI), INC.
Reel/Frame 055449/0848 →
Priority Claims (2)
WO PCT/CN2018/101715 · Aug 22, 2018 · international
WO PCT/CN2019/086894 · May 14, 2019 · international
Continuity (1)
Related Publication 20210363146A1 · Nov 25, 2021
Cited By (1)
US 12,410,171