一种达罗他胺衍生物及其制备方法与用途

By modifying the structure of dalolactam, a long-acting prodrug was prepared, which solved the problem of low bioavailability of oral dalolactam formulations, achieving high compliance and stable therapeutic effects, and making it suitable for long-acting dosing regimens.

CN121226255BActive Publication Date: 2026-07-17ANHUI IPCKE PHARMACEUTICAL TECHNOLOGY DEVELOPMENT CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ANHUI IPCKE PHARMACEUTICAL TECHNOLOGY DEVELOPMENT CO LTD
Filing Date
2025-09-25
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing oral formulations of darotamid have low bioavailability, require frequent administration of high doses, resulting in significant side effects and poor patient compliance. Furthermore, there are currently no long-acting parenteral formulations to meet the needs of long-term treatment.

Method used

By modifying the structure of dalolactamine, a prodrug with long-acting properties is prepared, forming a formulation that can be injected intramuscularly, subcutaneously, or intravenously. After injection, it forms a drug reservoir in the body, slowly and continuously releasing dalolactamine and prolonging the duration of action.

Benefits of technology

It improves the bioavailability of darotamide, eliminates the food effect, reduces the frequency of administration, maintains stable therapeutic plasma levels, and is suitable for weekly, monthly or even longer dosing, thus improving patient compliance.

✦ Generated by Eureka AI based on patent content.

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Abstract

本发明涉及一种式I化合物或其盐或其溶剂化物,式Ⅰ化合物的制备方法或其药物组合物及其用途。式I化合物可用于制备治疗高危转移风险的非转移性去势抵抗性前列腺癌成年患者药物,具有长效低毒的优点。
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Citation Information

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