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:
Sep. 13, 2022

Filed:

Sep. 05, 2018
Applicant:

Technical Institute of Physics and Chemistry of the Chinese Academy of Sciences, Beijing, CN;

Inventors:

Pengfei Wang, Beijing, CN;

Jiasheng Wu, Beijing, CN;

Weimin Liu, Beijing, CN;

Xiuli Zheng, Beijing, CN;

Ying Gu, Beijing, CN;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 47/10 (2017.01); A61K 41/00 (2020.01); C07C 221/00 (2006.01); C07C 225/32 (2006.01); C07C 227/28 (2006.01); C07C 229/16 (2006.01); C07C 229/28 (2006.01); C07C 241/02 (2006.01); C07C 243/20 (2006.01); C07C 323/30 (2006.01); C07C 323/38 (2006.01); C07D 295/13 (2006.01); C07D 295/205 (2006.01); C07D 401/12 (2006.01); C07D 403/12 (2006.01); C07D 519/00 (2006.01);
U.S. Cl.
CPC ...
A61K 41/0057 (2013.01); A61K 47/10 (2013.01); C07C 221/00 (2013.01); C07C 225/32 (2013.01); C07C 227/28 (2013.01); C07C 229/16 (2013.01); C07C 229/28 (2013.01); C07C 241/02 (2013.01); C07C 243/20 (2013.01); C07C 323/30 (2013.01); C07C 323/38 (2013.01); C07D 295/13 (2013.01); C07D 295/205 (2013.01); C07D 401/12 (2013.01); C07D 403/12 (2013.01); C07D 519/00 (2013.01);
Abstract

The present invention discloses a hypocrellin derivative substituted both in a pen-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 Mcm. 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 pen-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.


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