Nintedanib derivative as well as preparation method and application thereof

By modifying the structure of nintedanib, a long-acting nintedanib derivative was prepared, which solved the problems of low bioavailability and large adverse reactions of nintedanib, and achieved long-acting injection administration, thus improving the therapeutic effect and patient compliance.

CN121930160AActive Publication Date: 2026-04-28ANHUI IPCKE PHARMACEUTICAL TECHNOLOGY DEVELOPMENT CO LTD
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Patent Information

Application Number
CN202610088125.7
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-01-22
Publication Date
2026-04-28
Estimated Expiration
2046-01-22

AI Technical Summary

Technical Problem

Existing nintedanib drugs suffer from low bioavailability and significant adverse reactions, leading to poor patient tolerance. Clinical treatment doses cannot reach the daily doses used in studies, and there is a lack of long-acting injectable administration routes to improve compliance and treatment efficacy.

Method used

By modifying the structure of nintedanib, a long-acting nintedanib derivative was prepared, forming a formulation that can be injected intramuscularly, subcutaneously, or intravenously. The drug forms a reservoir in the body and is slowly released to achieve a long-acting effect.

Benefits of technology

It improves the bioavailability of nintedanib, reduces toxicity, increases patient compliance, and maintains therapeutic levels in vivo for a long time, making it suitable for the treatment of diseases such as systemic sclerosis-related interstitial lung disease and idiopathic pulmonary fibrosis.

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Abstract

The invention relates to a crystal form of a novel nintedanib derivative as shown in a formula (I), a preparation method of the crystal form, and medical application of a medicinal preparation containing the crystal form. The invention further provides application of the compound shown in the formula (I) in preparation of drugs for treating systemic sclerosis related pulmonary interstitial diseases, idiopathic pulmonary fibrosis and non-small cell lung cancer. The compound has the advantages of being remarkable in stability and long-acting.
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