IP Library Granted Patent US 12,428,433
Granted Patent B2
US 12,428,433 · App. 17/781,167 · Granted Sep 30, 2025

Fluorine-containing heterocyclic derivatives with macrocyclic structure and use thereof

Inventors: Anle Yang (Sichuan, CN); Haoxi Huang (Sichuan, CN); Tonghui Chen (Sichuan, CN); Jie Liang (Sichuan, CN); Dewei Zhang (Sichuan, CN); Jingen Deng (Sichuan, CN); Hongbo Li (Sichuan, CN); Junjie Pu (Sichuan, CN)
Assignee: SCINNOHUB PHARMACEUTICAL CO., LTD
C07D498/22C07B2200/07
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Quick Facts
Patent No.
US 12,428,433
App. No.
17/781,167
Granted
Sep 30, 2025
Kind
B2
Abstract

Disclosed are a macrocyclic fluorine-containing heterocyclic derivative of formula (I), a preparation method thereof, and a use thereof in treatment of TRK kinase-mediated diseases.

Claims (4)

1. A compound of formula (I), a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer or a mixture thereof, or a pharmaceutically acceptable salt thereof:

2. The compound of formula (I), the tautomer, the mesomer, the racemate, the enantiomer, the diastereomer or the mixture thereof, or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is in a form of a compound of formula (Ia) or (Ib), a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer or a mixture thereof, or a pharmaceutically acceptable salt thereof:

3. A pharmaceutical composition, comprising the compound, the tautomer, the mesomer, the racemate, the enantiomer, the diastereomer or the mixture thereof, or the pharmaceutically acceptable salt thereof according to claim 1 , and a pharmaceutically acceptable diluent or carrier.

4. A method of inhibiting an activity of a TRK kinase, comprising administrating the compound, the tautomer, the mesomer, the racemate, the enantiomer, the diastereomer or the mixture thereof, or the pharmaceutically acceptable salt thereof according to claim 1 , or the pharmaceutical composition thereof to a subject in need thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 31, 2022
From: YANG, ANLE; HUANG, HAOXI; CHEN, TONGHUI; LIANG, JIE; ZHANG, DEWEI; DENG, JINGEN; LI, HONGBO; PU, JUNJIE
To: SCINNOHUB PHARMACEUTICAL CO., LTD.
Reel/Frame 060055/0896 →
Priority Claims (3)
CN 201911285488.6 · Dec 13, 2019 · national
CN 202010040378.X · Jan 15, 2020 · national
CN 202011200880.9 · Nov 2, 2020 · national
Continuity (1)
Related Publication 20230044722A1 · Feb 9, 2023
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WO WO2019210835 · 2019 [cited by examiner]
Int'l Search Report issued Mar. 10, 2021 in Int'l Application No. PCT/CN2020/135526. [cited by applicant]