Title:
DERIVATIVES OF HYPOCRELLIN WITH PERI-POSITION AND 2-POSITION SIMULTANEOUSLY SUBSTITUTED BY AMINO GROUPS
Document Type and Number:
WIPO Patent Application WO/2019/047846
Kind Code:
A1
Abstract:
Derivatives of hypocrellin with peri-position and 2-position simultaneously substituted by amino groups and a preparation method and application thereof are disclosed. The structural formula of the derivatives is as shown in the formulae I-a to I-d. The prepared derivatives of hypocrellin with peri-position and 2-position simultaneously substituted by amino groups have a maximum absorption wavelength of 600-650nm, and a molar extinction coefficient of about 20000-40000M -1cm -1. Compared with unmodified hypocrellin or hypocrellin only modified at 2-position, the prepared derivatives of hypocrellin have a significantly red-shifted absorption spectrum and a greatly enhanced molar extinction coefficient, and can efficiently produce reactive oxygen species such as singlet oxygen under a photosensitive condition. Under the same condition, the derivatives of hypocrellin with peri-position and 2-position simultaneously substituted by amino groups act as photosensitizers, and have higher photodynamic inactivation of tumor cells than the first and second generations of commercial photosensitizers.
Inventors:
WANG PENGFEI (CN)
WU JIASHENG (CN)
LIU WEIMIN (CN)
ZHENG XIULI (CN)
GU YING (CN)
WU JIASHENG (CN)
LIU WEIMIN (CN)
ZHENG XIULI (CN)
GU YING (CN)
Application Number:
PCT/CN2018/104124
Publication Date:
March 14, 2019
Filing Date:
September 05, 2018
Export Citation:
Assignee:
TECHNICAL INST OF PHYSICS AND CHEMISTRY OF THE CHINESE ACADEMY OF SCIENCES (CN)
International Classes:
C07C221/00; A61K41/00; A61P35/00; C07C225/32; C07C249/02; C07C251/24
Domestic Patent References:
| WO2013020204A1 | 2013-02-14 |
Foreign References:
| CN105541647A | 2016-05-04 | |||
| CN1600780A | 2005-03-30 |
Other References:
"Research and Progress on Novel Photodynamic Drugs-Hypocrellin Derivatives", CHINESE SCIENCE BULLETIN, vol. 48, 2003, pages 1005 - 1015
PHOTOCHEM. PHOTOBIOL., vol. 78, 2003, pages 411 - 415
ZHAO KAIHONG, ORGANIC CHEMISTRY, vol. 9, 1989, pages 252 - 254
See also references of EP 3680230A4
PHOTOCHEM. PHOTOBIOL., vol. 78, 2003, pages 411 - 415
ZHAO KAIHONG, ORGANIC CHEMISTRY, vol. 9, 1989, pages 252 - 254
See also references of EP 3680230A4
Attorney, Agent or Firm:
BEIJING JANLEA PATENT AGENCY CO., LTD. (CN)
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