Title:
ALBUMIN-BOUND ANTITUMOR DRUG-MALEIMIDE MOLECULAR PRODRUG
Document Type and Number:
WIPO Patent Application WO/2019/137018
Kind Code:
A1
Abstract:
The present application relates to a series of redox-sensitive albumin-bound prodrugs specifically responsive to tumor tissue, and in particular, to three small-molecule docetaxel-maleimide prodrugs. A maleimide ring in the prodrug structure is used as a target for binding a free thiol group at position 34 of a plasma albumin in the body, such that the drug rapidly and specifically binds to the albumin after intravenous injection into the body and forms an albumin-drug complex, thereby enhancing drug stability and significantly prolonging the circulation time of the drug in the body. Furthermore, the EPR effect is leveraged to achieve drug accumulation in tumor tissue.
Inventors:
SUN JIN (CN)
HE ZHONG GUI (CN)
WEI WEI (CN)
HE ZHONG GUI (CN)
WEI WEI (CN)
Application Number:
PCT/CN2018/102715
Publication Date:
July 18, 2019
Filing Date:
August 28, 2018
Export Citation:
Assignee:
UNIV SHENYANG PHARMACEUTICAL (CN)
International Classes:
A61K47/64; A61K31/337; A61K45/00; A61K47/54; A61P35/00; C07D405/12
Foreign References:
| CN108164512A | 2018-06-15 | |||
| CN108187063A | 2018-06-22 | |||
| CN106083769A | 2016-11-09 | |||
| CN102939109A | 2013-02-20 | |||
| CN101138634A | 2008-03-12 |
Attorney, Agent or Firm:
SHENYANG JACK INTELLECTUAL PROPERTY AGENT LTD. (CN)
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