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Title:
ヒポクレリンのペリ位及び2−位の両方がアミノ置換された誘導体、その調製方法及びそれを含む光増感薬
Document Type and Number:
Japanese Patent JP6911197
Kind Code:
B2
Abstract:
The present invention discloses a hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino, and a preparation method and use thereof. A general structural formula of the derivative is as represented by formulas I-a to I-d:The hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino prepared in the present invention has a maximum absorption wavelength of 600-650 nm and a molar extinction coefficient reaching about 20000-40000 M-1cm-1. Compared with unmodified hypocrellin or hypocrellin having only a 2-position modified, an absorption spectrum of the derivative is significantly red-shifted and the molar extinction coefficient is greatly improved, and the derivative can efficiently produce reactive oxygen species such as singlet oxygen in a photosensitive condition. In the same condition, the hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino involved in the present invention, when used as a photosensitizer, has a stronger ability to photo-dynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

Inventors:
Peng Fei
Kakatsu Wu
Liu Wei Shun
Chung Shurei
Application Number:
JP2020512571A
Publication Date:
July 28, 2021
Filing Date:
September 05, 2018
Export Citation:
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Assignee:
Institute of Science and Technology, Chinese Academy of Sciences
International Classes:
C07C225/22; A61K31/136; A61K31/77; A61K41/00; A61K47/59; A61P35/00; C07C221/00; C07C227/12; C07C229/18; C07C319/20; C07C323/25; C07D211/26; C07D213/36; C07D241/08; C07D295/13; C07D487/08
Foreign References:
CN105541647A
WO2013020204A1
CN1600780A
Attorney, Agent or Firm:
Goto Patent Office