Title:
２－（１－アシルオキシ－Ｎ－ペンチル）安息香酸と塩基性アミノ酸またはアミノグアニジンによって形成される塩と、その製造方法及び用途
Document Type and Number:
Japanese Patent JP7264999
Kind Code:
B2
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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Inventors:
Chang Yi
Xiao Wei
Huang Zhang Jian
Ken Kure
朱 嘉▲イー▼
Wang Zhong
united kingdom
Xiao Wei
Huang Zhang Jian
Ken Kure
朱 嘉▲イー▼
Wang Zhong
united kingdom
Application Number:
JP2021517584A
Publication Date:
April 25, 2023
Filing Date:
December 03, 2018
Export Citation:
Assignee:
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:
| JP11509540A |
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
社団法人日本化学会編,第4版実験化学講座1基本操作I,第184-189頁,丸善株式会社発行,1996年04月05日
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
社団法人日本化学会編,第4版実験化学講座1基本操作I,第184-189頁,丸善株式会社発行,1996年04月05日
Attorney, Agent or Firm:
Kimura Mitsuru
Yasushi Morikawa
Kei Sakurada
Hideki Mie
Yasushi Morikawa
Kei Sakurada
Hideki Mie