A steroidal FXR agonist containing an oxadiazole structure on the side chain, and its preparation method and application

By developing the steroid FXR agonist compound A6 with side chain oxadiazole structure, the adverse side effects of existing FXR agonists in the treatment of hepatobiliary diseases, especially itching, achieved efficient FXR agonism activity and low side effects.

CN118620018BActive Publication Date: 2025-03-28SOUTH CHINA UNIV OF TECH
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Patent Information

Application Number
CN202410695899.7
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-05-31
Publication Date
2025-03-28
Estimated Expiration
2044-05-31

AI Technical Summary

Technical Problem

Existing FXR agonists have adverse side effects such as itching in the treatment of hepatobiliary diseases, and it is difficult to effectively reduce these side effects.

Method used

A steroid FXR agonist with side chain oxadiazole structure was developed, compound A6, and at the same time, it has low agonism activity against MRGPRX4, aiming to reduce side effects such as itching.

Benefits of technology

Compound A6 significantly improved the agonistic activity against FXR, while also reduced the agonistic activity against MRGPRX4, reduced side effects such as itching, and demonstrated excellent pharmacokinetic properties.

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Abstract

The present invention belongs to the field of medicine, and discloses a steroidal FXR agonist containing an oxadiazole structure in the side chain, and a preparation method and application thereof. The FXR agonist is a compound of formula I or an isomer thereof, or a pharmaceutically acceptable salt thereof or a solvent compound of the salt, or a mixture of any two or more of the foregoing. The steroidal derivative containing an oxadiazole structure in the side chain of the present invention has high FXR agonist activity and good pharmacokinetic advantages, and can be used in the preparation of drugs for preventing and / or treating FXR-mediated and / or FXR-mediated related hepatobiliary diseases.
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