Title:
CABAZITAXEL PRODRUG ANTI-TUMOR PREPARATION
Document Type and Number:
WIPO Patent Application WO/2023/109563
Kind Code:
A1
Abstract:
The present invention relates to a cabazitaxel prodrug anti-tumor preparation, designs and synthesizes a cabazitaxel-fatty alcohol small molecule prodrug containing different fatty alcohol side chains and different connecting chains of general formulas (I), (II) and (III), and prepares a self-assembly nanoparticle. A result shows that the cabazitaxel-fatty alcohol small molecule prodrug self-assembly nanoparticle can effectively improve a curative effect of cabazitaxel and reduce toxic and side effects thereof. The length of a side chain of a branched chain fatty alcohol, the structure of the side chain of the fatty alcohol, the composition of a connecting chain element and the length of a connecting chain can significantly affect the pharmaceutical property and the anti-tumor activity of the cabazitaxel prodrug self-assembly nanoparticle. The prodrug self-assembly nanoparticle has higher anti-tumor activity and lower toxicity than a cabazitaxel-linear fatty alcohol small molecule prodrug self-assembly nanoparticle.
Inventors:
SUN JIN (CN)
SUN BINGJUN (CN)
HE ZHONGGUI (CN)
ZHANG YU (CN)
WANG DANPING (CN)
LUO CONG (CN)
ZUO SHIYI (CN)
LI LINGXIAO (CN)
DU CHAOYING (CN)
SUN BINGJUN (CN)
HE ZHONGGUI (CN)
ZHANG YU (CN)
WANG DANPING (CN)
LUO CONG (CN)
ZUO SHIYI (CN)
LI LINGXIAO (CN)
DU CHAOYING (CN)
Application Number:
PCT/CN2022/136743
Publication Date:
June 22, 2023
Filing Date:
December 06, 2022
Export Citation:
Assignee:
UNIV SHENYANG PHARMACEUTICAL (CN)
International Classes:
A61K9/51; C07D305/14; A61K31/337; A61K45/06; A61K47/10; A61K47/54; A61K47/60; A61K47/69; A61K49/00; A61P35/00
Foreign References:
| CN105884719A | 2016-08-24 | |||
| CN115252805A | 2022-11-01 | |||
| CN113398277A | 2021-09-17 | |||
| CN109350748A | 2019-02-19 | |||
| CN111116521A | 2020-05-08 | |||
| CN108478803A | 2018-09-04 |
Other References:
XUE PENG, LIU DAN, WANG JING, ZHANG NA, ZHOU JIAHUA, LI LIN, GUO WEILING, SUN MENGCHI, HAN XIANGFEI, WANG YONGJUN: "Redox-Sensitive Citronellol–Cabazitaxel Conjugate: Maintained in Vitro Cytotoxicity and Self-Assembled as Multifunctional Nanomedicine", BIOCONJUGATE CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 27, no. 5, 18 May 2016 (2016-05-18), US , pages 1360 - 1372, XP055981503, ISSN: 1043-1802, DOI: 10.1021/acs.bioconjchem.6b00155
JIANG YAN, WANG XIUZHEN, LIU XIN, LV WEI, ZHANG HONGJUAN, ZHANG MINGWAN, LI XINRUI, XIN HONGLIANG, XU QUNWEI: "Enhanced Antiglioma Efficacy of Ultrahigh Loading Capacity Paclitaxel Prodrug Conjugate Self-Assembled Targeted Nanoparticles", APPLIED MATERIALS & INTERFACES, AMERICAN CHEMICAL SOCIETY, US, vol. 9, no. 1, 11 January 2017 (2017-01-11), US , pages 211 - 217, XP055981508, ISSN: 1944-8244, DOI: 10.1021/acsami.6b13805
JIANG YAN, WANG XIUZHEN, LIU XIN, LV WEI, ZHANG HONGJUAN, ZHANG MINGWAN, LI XINRUI, XIN HONGLIANG, XU QUNWEI: "Enhanced Antiglioma Efficacy of Ultrahigh Loading Capacity Paclitaxel Prodrug Conjugate Self-Assembled Targeted Nanoparticles", APPLIED MATERIALS & INTERFACES, AMERICAN CHEMICAL SOCIETY, US, vol. 9, no. 1, 11 January 2017 (2017-01-11), US , pages 211 - 217, XP055981508, ISSN: 1944-8244, DOI: 10.1021/acsami.6b13805
Attorney, Agent or Firm:
SHENYANG DONGDA INTELLECTUAL PROPERTY AGENCY CO., LTD (CN)
Download PDF: