The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Nov. 14, 2023

Filed:

Dec. 03, 2018
Applicant:

Jiangsu Kanion Pharmaceutical Co., Ltd., Lianyungang, CN;

Inventors:

Yihua Zhang, Nanjing, CN;

Wei Xiao, Lianyungang, CN;

Zhangjian Huang, Nanjing, CN;

Jianbing Wu, Nanjing, CN;

Jiayi Zhu, Nanjing, CN;

Zhenzhong Wang, Lianyungang, CN;

Tuanjie Wang, Lianyungang, CN;

Assignee:
Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07C 69/78 (2006.01); A61P 9/10 (2006.01); A61K 9/00 (2006.01); C07C 227/26 (2006.01); C07C 279/14 (2006.01); C07C 281/16 (2006.01); C07D 233/64 (2006.01);
U.S. Cl.
CPC ...
C07C 69/78 (2013.01); A61K 9/0019 (2013.01); A61P 9/10 (2018.01); C07C 227/26 (2013.01); C07C 279/14 (2013.01); C07C 281/16 (2013.01); C07D 233/64 (2013.01);
Abstract

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).


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