Title:
ALBUMIN CONJUNCTION-TYPE GEMCITABINE PRODRUG AND SYNTHETIC METHOD AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/169837
Kind Code:
A1
Abstract:
The invention relates to an albumin conjunction-type maleimide functionalized gemcitabine prodrug as well as application thereof in transferring an antitumor prodrug. The albumin conjunction-type maleimide functionalized gemcitabine prodrug is a compound consisting of gemcitabine and maleimide connected by virtue of an amido bond, a carbonate bond or an amino formate bond, and a maleimide group is used as an albumin 34-site cysteine free mercapto group jointed target. The prodrug compound can be rapidly specifically bonded with albumin in blood to form an albumin prodrug compound, thereby lowering the drug metabolism speed, significantly prolonging a half-life period of the drug, and realizing the long cycling effect. In addition, under the EPR effect and the albumin receptor mediation, the tumor targeting can be realized, and the antitumor effect can be improved. The gemcitabine precursor drug is used for intravenous injection and larger in market application prospect.
Inventors:
SUN JIN (CN)
HE ZHONGGUI (CN)
ZHANG HUICONG (CN)
HE ZHONGGUI (CN)
ZHANG HUICONG (CN)
Application Number:
PCT/CN2018/102717
Publication Date:
September 12, 2019
Filing Date:
August 28, 2018
Export Citation:
Assignee:
UNIV SHENYANG PHARMACEUTICAL (CN)
International Classes:
C07H19/073; A61K31/7068; A61P35/00; C07H1/00
Foreign References:
| CN108329371A | 2018-07-27 | |||
| CN106632272A | 2017-05-10 |
Other References:
ZHANG, HUICONG: "Multifunctional Tumor-Targeting Cathepsin B-Sensitive Gemcitabine Prodrug Covalently Targets Albumin in Situ and Improves Cancer Therapy", BIOCONJUGATE CHEM, vol. 29, no. 6, 18 May 2018 (2018-05-18), pages 2 - 3, ISSN: 1043-1802
LI, XINGHAI: "Encapsulating a Hydrophilic Chemotherapeutic into Rod-Like Nanoparticles of a Genetically Encoded Asymmetric Triblock Polypeptide Improves Its Efficacy", ADVANCED FUNCTIONAL MATERIALS, vol. 27, no. 12, 31 December 2017 (2017-12-31), XP055628878, ISSN: 1616-301X
LI, XINGHAI: "Encapsulating a Hydrophilic Chemotherapeutic into Rod-Like Nanoparticles of a Genetically Encoded Asymmetric Triblock Polypeptide Improves Its Efficacy", ADVANCED FUNCTIONAL MATERIALS, vol. 27, no. 12, 31 December 2017 (2017-12-31), XP055628878, ISSN: 1616-301X
Attorney, Agent or Firm:
SHENYANG JACK INTELLECTUAL PROPERTY AGENT LTD. (CN)
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