Tri-fused ring compound as well as preparation method and application thereof

By designing and synthesizing tricyclic compounds, the problems of insufficient activity and high toxicity of existing PDE3/4 inhibitors are solved, and the efficient dual inhibition of PDE3 and PDE4 is achieved, providing a safer drug solution.

CN120329299APending Publication Date: 2025-07-18GUANGZHOU JOINCARE RESPIRATORY DRUG ENG TECH CO LTD
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Patent Information

Application Number
CN202510489912.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2024-07-24
Filing Date
2025-04-18
Publication Date
2025-07-18

AI Technical Summary

Technical Problem

The existing PDE3/4 dual-target inhibitors need to be improved in terms of inhibitory activity on PDE4, and there is still room for improvement in the inhibitor activity of PDE3, and there is potential toxicity problem.

Method used

A trigonocyclic compound was developed, and the compound was prepared by chemical synthesis by designing specific structures and used in pharmaceutical compositions to achieve double inhibition of PDE3 and PDE4.

Benefits of technology

The compound showed stronger PDE3/4 inhibitory activity and lower toxicity, significantly better than the existing dual-target inhibitor RPL554, and had better efficacy.

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Abstract

The invention relates to a tricyclic compound as well as a preparation method and application thereof. The structural formula of the tri-fused ring compound is as shown in formula (I): # imgabs0 #, wherein R1, R2, R3, R4, R5, R6, R7, E, X and Y are as described in the specification. The compound can inhibit PDE3 and PDE4 at the same time, and compared with an existing PDE3 and PDE4 double-target inhibitor, the effect is better.
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