Tegorasan monoethyl fumarate, preparation method thereof, pharmaceutical composition and application of tegorasan monoethyl fumarate

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By preparing ticoraxan monoethyl fumarate salt, the problems of ticoraxan solubility and stability were solved, and the bioavailability was improved, making it suitable for industrial production.

CN120923480APending Publication Date: 2025-11-11SHANGHAI NEO-LEADING PHARMATECH CO LTD

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Patent Information

Application Number: CN202510603656.0
Authority / Receiving Office: CN · China
Patent Type: Applications(China)
Current Assignee / Owner
Priority Date: 2024-05-10
Filing Date: 2025-05-09
Publication Date: 2025-11-11

Application Information

Patent Timeline

10 May 2024

Priority

09 May 2025

Application

CN202510603656.0

11 Nov 2025

Publication

CN120923480A

IPC: C07D405/12; C07C69/60; C07C67/30; A61K31/404; A61P1/00; A61P1/04; A61P1/14; A61P11/06; A61P11/00; A61P1/08; A61P29/00

CPC: C07D405/12; C07C69/60; A61P1/00; A61P1/04; A61P1/14; A61P11/06; A61P11/00; A61P1/08

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Application Domain

Organic active ingredients Organic compound preparation

Technology Topics

Pharmacy medicine Pharmaceutical drug

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AI Technical Summary

Technical Problem

The existing ticoraxan free base has poor solubility, which affects bioavailability, and it is unstable under acidic conditions, posing production difficulties and safety risks.

Method used

Tigorafenib monoethyl fumarate was prepared by forming a salt with monoethyl fumarate, which improved its solubility and bioavailability, making it suitable for industrial production.

Benefits of technology

Tigorafenib monoethyl fumarate has good solubility and stability, which improves the bioavailability of the drug, making it suitable for industrial production and with a promising market prospect.

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Abstract

The invention provides tegorasan monoethyl fumarate as well as a preparation method, a pharmaceutical composition and an application of the tegorasan monoethyl fumarate. The tegorac monoethyl fumarate provided by the invention is relatively good in solubility and good in stability, the bioavailability of a medicine is increased by improving the solubility of the medicine, and the tegorac monoethyl fumarate is suitable for industrial production and has a good market prospect.

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