Wuhan Ll Science and Technology Development Co., Ltd.

Wuhan Qr Pharmaceuticals Co., Ltd.

Anxiao Zheng

Li Liu

Chaodong Wang

Yongkai Chen

Jun Lou

Penggao Yu

Hongwei Tang

The present disclosure provides a triazole antibacterial derivative and a pharmaceutical composition thereof and a use thereof and in particular relates to a compound represented by the following formula (I), and a racemate, a stereoisomer, a tautomer, an oxynitride or a pharmaceutically acceptable salt thereof:  The compound of the present disclosure has a desirable water solubility and can be formulated into an injection for use without adding a cosolvent having a potential safety risk (such as hydroxypropyl-&#x3b2;-cyclodextrin, sulfobutylether-&#x3b2;-cyclodextrin, and the like), facilitating drug administration for patients, and greatly improving clinical safety. The drug can be used even by patients with moderate or severe renal impairment, thereby expanding the application scope of the drug.

Triazole antimicrobial derivative, pharmaceutical composition and use thereof

The present disclosure provides a posaconazole derivative, a pharmaceutical composition and use thereof, which specifically include a compound represented by the following formula (I), a racemate, stereoisomer, tautomer, oxynitride, or a pharmaceutically acceptable salt thereof:  The compounds of the present disclosure have strong antifungal activity, high safety, and good water solubility, without the need for the addition of a cosolvent (such as hydroxypropyl-&#x3b2;-cyclodextrin, sulfobutyl ether-&#x3b2;-cyclodextrin, and the like) with potential safety risks. Furthermore, the formulation process of the compound could have less difficulty and less cost, and therefore can be used to prepare improved antifungal drugs.

Posaconazole derivative, pharmaceutical composition and use thereof

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Hubei, China

Anxiao Zheng