Molecular design synthesis for inhibiting kallikrein activity

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By synthesizing fluoroallyl carboxylic acid esters, the shortcomings of existing technologies in inhibiting kallikrein activity have been overcome, enabling potential applications in the treatment of various diseases and in cancer diagnosis and treatment.

CN116178148BActive Publication Date: 2026-06-23CHUZHOU UNIV

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Patent Information

Application Number: CN202310140369.1
Authority / Receiving Office: CN · China
Patent Type: Patents(China)
Current Assignee / Owner
Filing Date: 2023-02-16
Publication Date: 2026-06-23
Estimated Expiration: 2043-02-16

Application Information

Patent Timeline

16 Feb 2023

Application

CN202310140369.1

23 Jun 2026

Publication

CN116178148B

IPC: C07C67/08; C07C69/757; C07C69/65; C07C69/157; C07C69/73; C07C29/34; C07C33/48; C07C253/30; C07C255/36; C07C67/343; C07C255/38; A61P3/10; A61P27/02; A61P7/12; A61P35/00; A61K49/00

CPC: C07C67/08; C07C29/34; C07C253/30; C07C67/343; A61P3/10; A61P27/02; A61P7/12; A61P35/00

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Application Domain

Senses disorder Metabolism disorder

Technology Topics

Disease Kinin

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AI Technical Summary

Technical Problem

Existing technologies are insufficient to effectively inhibit the activity of kallikrein, leading to deficiencies in the diagnosis and treatment of various diseases and cancer.

Method used

A class of fluoroallyl carboxylic acid esters was designed and synthesized, and compounds with inhibitory kallikrein activity were prepared by reacting them with specific catalysts and solvent systems.

Benefits of technology

It achieves effective inhibition of kallikrein, and has the potential to treat diabetic complications, eye diseases and edema-related diseases, and shows potential value in the diagnosis and treatment of cancer.

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Abstract

The present application relates to the preparation of new physiological and pharmaceutically active molecules, and belongs to the field of pharmaceutical synthesis chemistry, and relates to the design and preparation of a class of molecules capable of inhibiting the activity of human kallikrein. Firstly, fluoroacrylic acid and alcohol compounds are used as raw materials to obtain a class of fluoroallyl alcohol compounds; then the fluoroallyl alcohol is condensed with carboxylic acid compounds to obtain fluoroallyl carboxylic acid ester compounds with general formula (I) capable of inhibiting the activity of human kallikrein. The compounds are considered to be useful for treating diabetic complications, eye diseases and edema-related diseases. In addition, they have potential applications in the diagnosis and treatment of some cancers.

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