Jiangsu Kanion Pharmaceutical Co., Ltd.

China Pharmaceutical University

Yihua Zhang

Wei Xiao

Zhenzhong Wang

Zhangjian Huang

Jianbing Wu

Jiayi Zhu

Tuanjie Wang

The present disclosure discloses salts formed by 2-(1-acyloxy-n-pentyl)benzoic acid and basic amino acid or aminoguanidine, a preparation method thereof, pharmaceutical preparations containing these salts, and application thereof in preparation of drugs for preventing or treating ischemic cardiovascular and cerebrovascular diseases, resisting thrombosis and improving cardio-cerebral circulation disorders. The compound of the present disclosure has excellent water solubility, aqueous solution stability and pharmacokinetic properties, also has significant anti-platelet aggregation, anti-thrombosis, anti-cerebral ischemia and neuroprotective activity. The compound of the present disclosure has significantly better effects than those of (S)-butylphthalide and potassium (R/S)-2-(1-hydroxy-n-pentyl) benzoate (PHPB), has significantly lower acute toxicity to mice by intravenous injection than that of butylphthalide and PHPB, has a lower inhibition rate of the hERG potassium channel in CHO-hERG cells than that of (S)-butylphthalide, and has a negative result in Bacterial Reverse Mutation Test (Ames test).

Salts formed by 2-(1-acyloxy-n-pentyl) benzoic acid and basic amino acid or aminoguanidine, and preparation method and application thereof

Growing community of inventors

Nanjing, China

Yihua Zhang