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Title:
PH-SENSITIVE AXIALLY-SUBSTITUTED SILICON PHTHALOCYANINE COMPLEX, PREPARATION METHOD THEREFOR, AND MEDICAL APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/086242
Kind Code:
A1
Abstract:
The present invention relates to a pH-sensitive ketal-linked cholesterol-silicon phthalocyanine complex, a preparation method therefor and medical application thereof, and in particular, to a silicon phthalocyanine complex represented by a general formula (I), a preparation method therefor, a pharmaceutical composition containing the complex, and use thereof as a photosensitizer, especially use in treating cancers, wherein substituents in the general formula (I) have the same definitions as those in the description. Due to the presence of cholesterol groups, the series of complexes are hardly taken by tumor cells and normal cells; however, in a tumor tissue cell external subacid environment, ketal linkage undergoes hydrolysis reaction, and hydrolysis derivatives of silicon phthalocyanine can be easily taken by cancer cells, show extremely high photosensitivity, and can be prepared into tumor cell external subacid environment targeted photosensitive drug.

Inventors:
JIANG XIONGJIE (CN)
HUANG HUAJING (CN)
Application Number:
PCT/CN2017/070298
Publication Date:
May 17, 2018
Filing Date:
January 05, 2017
Export Citation:
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Assignee:
SHENZHEN SONO PHOTODYNAMIC BIO MED TECH LTD (CN)
International Classes:
C07F7/02; A61K41/00; A61P35/00; C07F5/06
Foreign References:
CN105669735A2016-06-15
CN104844645A2015-08-19
CN103435639A2013-12-11
CN1583762A2005-02-23
CN103864833A2014-06-18
CN102231952A2011-11-02
Other References:
JIANG, XIONGJIE ET AL.: "pH-and Thiol-Responsive BODIPY-based Photosensitizers for Targeted Photodynamic Therapy", CHEMISTRY A EUROPEAN JOURNAL, vol. 22, no. 24, 3 May 2016 (2016-05-03), XP055474100
BARGE, J. ET AL.: "Killing Efficacy of a New Silicon Phthalocyanine in Human Melanoma Cells Treated with Photodynamic Therapy by Early Activation of Mitochondrion-mediated Apoptosis", EXPERIMENTAL DERMATOLOGY, vol. 13, 31 December 2004 (2004-12-31), XP055486070
DECREAU, R. ET AL.: "Synthesis of Silicon Phthalocyanines Bearing Two Cholesterol Moieties", SYNLETT, vol. 4, 30 April 1998 (1998-04-30), XP055486071
Attorney, Agent or Firm:
SHENZHEN KAIDA PARTNERS INTELLECTUAL PROPERTY LAW FIRM (CN)
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