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Document Type and Number:
Japanese Patent JP7264999
Kind Code:
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).

Chang Yi
Xiao Wei
Huang Zhang Jian
Ken Kure
朱 嘉▲イー▼
Wang Zhong
united kingdom
Application Number:
Publication Date:
April 25, 2023
Filing Date:
December 03, 2018
Export Citation:
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Jiangsu Kangyuan Pharmaceutical Co., Ltd.
International Classes:
C07C279/14; A61K31/222; A61P7/02; A61P9/00; A61P9/10; A61P29/00; A61P43/00; C07C67/08; C07C67/14; C07C67/52; C07C69/157; C07C277/06; C07C277/08
Domestic Patent References:
Other References:
One-pot synthesis of 2-(1-acyloxypentyl) benzoic acids,Chinese Chemical Letters,2008年,pp. 915-917
Bioorganic and Medicinal Chemistry Letters,2015年09月01日,Vol. 25, Issue 17,pp. 3535-3540
C.G.WERMUTH編,最新 創薬化学 下巻,p.347-365,株式会社 テクノミック,1999年
小嶌隆史,医薬品開発における結晶性選択の効率化を目指して,薬剤学,2008年09月01日,Vol.68, No.5,p.344-349
Attorney, Agent or Firm:
Kimura Mitsuru
Yasushi Morikawa
Kei Sakurada
Hideki Mie