Application of trans-adamantanamine derivative or salt thereof

By modifying the structure of ambroxol and developing trans-adamantane ammonia derivatives and its salts, the problem of side effects and poor efficacy of drugs for treating lung injury and chronic cough in the existing technology has been solved, and more effective treatment of lung injury and cough has been achieved. , reducing side effects and significantly increasing sputum production and phenol red excretion.

CN114685292AInactive Publication Date: 2022-07-01CHENGDU SHIBEIKANG BIOLOGICAL MEDICINE TECH CO LTD
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Patent Information

Application Number
CN202110284357.7
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2021-03-17
Publication Date
2022-07-01
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

The existing technology lacks effective drugs for the treatment of lung injury and chronic cough, especially acute lung injury and refractory cough, and existing drugs such as ambroxol have side effects, such as constipation and drowsiness.

Method used

By structurally modifying ambroxol, trans-adamantane ammonia derivatives and their pharmaceutically acceptable salts were developed, prepared by condensation reaction and reduction reaction, and used to prevent or treat respiratory diseases, including lung injury and acute pulmonary disease. Injury, acute respiratory distress syndrome, cough and chronic cough.

Benefits of technology

Trans-amantadine derivatives and their hydrochloride significantly improve the therapeutic effect on lung injury and cough, are superior to existing drugs, reduce side effects, significantly increase sputum production and phenol red excretion, and have better of medicinal efficacy.

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Abstract

The invention belongs to the technical field of medicinal chemistry, and discloses an application of a trans-adamantanamine derivative with a structure shown as a formula I or a pharmaceutically acceptable salt thereof in preparation of medicines for preventing or / and treating respiratory system diseases. Compared with ambroxol hydrochloride and amantadine hydrochloride derivative racemates (isomer mixtures), the trans-amantadine derivative and the salt thereof have better drug effects. A mouse acute lung injury test and an ammonia water induced mouse cough model show that the compound has an excellent effect of treating lung injury and cough, the effect of the compound is superior to that of ambroxol hydrochloride and adamantanamine hydrochloride derivative raceme, and the compound has statistical significance. Compared with ambroxol hydrochloride, the trans-adamantanamine derivative and the hydrochloride of the trans-adamantanamine derivative have the advantages that the sputum excretion amount of rats can be remarkably increased, the phenol red excretion amount of mice can be remarkably increased, and the effect of the trans-adamantanamine derivative and the hydrochloride of the trans-adamantanamine derivative is superior to that of ambroxol hydrochloride and the hydrochloride of the trans-adamantanamine derivative.
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