Benzoxazole compound as well as preparation method, pharmaceutical composition and application thereof

The invention discloses a benzoxazole compound as well as a preparation method, a pharmaceutical composition and application thereof. The structure of the compound is as shown in formula (I), and the compound comprises pharmaceutically acceptable salts thereof. The benzoxazole compound and the pharm...

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Bibliographic Details
Main Authors HU QINGHUA, LI HUANQIU, ZHOU MENGZE, LENG HAIFENG
Format Patent
LanguageChinese
English
Published 13.05.2022
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The invention discloses a benzoxazole compound as well as a preparation method, a pharmaceutical composition and application thereof. The structure of the compound is as shown in formula (I), and the compound comprises pharmaceutically acceptable salts thereof. The benzoxazole compound and the pharmaceutical composition thereof can effectively antagonize a P2Y6 receptor, the optimal in-vitro antagonism rate reaches 100%, and the optimal IC50 value reaches the picomolar concentration level; in-vivo inhibition of mouse colon length shortening, body weight reduction and DAI score increase can be realized. The compound can be used for preparing drugs for treating inflammatory diseases related to P2Y6 receptors, the prepared drugs can exert drug effects at the cellular level and the animal level, the application is wide, and the synthesis method of the compound is simple and easy to implement. 本发明公开了一类苯并恶唑类化合物及其制备方法、药物组合物和应用。该化合物结构如式(I)，其包含其药学上可接受的盐。该类苯并恶唑类化合物及其药物组合物可有效拮抗P2Y6受体，体外拮抗率最优达到100％，IC50值最优达到皮摩尔浓度水平；体内可抑制
Bibliography:Application Number: CN202210174326