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Title:
LAROTAXEL-FATTY ALCOHOL SMALL MOLECULE PRODRUG AND CONSTRUCTION OF SELF-ASSEMBLING NANOPARTICLE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/227554
Kind Code:
A1
Abstract:
The synthesis of a larotaxel-fatty alcohol small molecule prodrug with a tumor reduction response characteristic and the construction of a self-assembling nanoparticle, and the use thereof in the preparation of a drug delivery system. Provided is a larotaxel-stearyl alcohol small molecule prodrug, which is prepared into a larotaxel-fatty alcohol prodrug nanoparticle. The larotaxel-fatty alcohol prodrug nanoparticle can be a non-PEGylated larotaxel-fatty alcohol prodrug nanoparticle, a PEG-modified larotaxel-fatty alcohol prodrug nanoparticle, a drug-loaded larotaxel-fatty alcohol prodrug nanoparticle, and an active targeting larotaxel-fatty alcohol prodrug nanoparticle. The larotaxel-fatty alcohol prodrug has few synthetic steps, a simple process, reduced synthesis costs, a high yield and easy purification, and the nanoparticle formed by the self-assembly of the larotaxel-fatty alcohol small molecule prodrug has an ultra-small particle size, which reduces the toxicity and side effects while improving the curative effect of larotaxel.

Inventors:
LUO CONG (CN)
WANG YONGJUN (CN)
YANG JINCHENG (CN)
MA HONGDA (CN)
SUN JIN (CN)
HE ZHONGGUI (CN)
FENG YAO (CN)
MA ZHINING (CN)
Application Number:
PCT/CN2021/133825
Publication Date:
November 03, 2022
Filing Date:
November 29, 2021
Export Citation:
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Assignee:
SUZHOU YUTAI PHARMACEUTICAL TECH CO LTD (CN)
International Classes:
A61K47/54; A61K31/337; A61K47/60; A61K47/69; A61P35/00; C07D305/14
Foreign References:
CN105884719A2016-08-24
CN112604002A2021-04-06
CN109851593A2019-06-07
CN112494458A2021-03-16
CN110898231A2020-03-24
US20170151339A12017-06-01
CN105541762A2016-05-04
CN106432141A2017-02-22
Other References:
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, vol. 9, no. 1, 11 January 2017 (2017-01-11), US , pages 211 - 217, XP055981508, ISSN: 1944-8244, DOI: 10.1021/acsami.6b13805
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, vol. 27, no. 5, 18 May 2016 (2016-05-18), US , pages 1360 - 1372, XP055981503, ISSN: 1043-1802, DOI: 10.1021/acs.bioconjchem.6b00155
ZHANG SHENWU, GUAN JIBIN, SUN MENGCHI, ZHANG DONG, ZHANG HAOTIAN, SUN BINGJUN, GUO WEILING, LIN BIN, WANG YONGJUN, HE ZHONGGUI, LU: "Self-delivering prodrug-nanoassemblies fabricated by disulfide bond bridged oleate prodrug of docetaxel for breast cancer therapy", DRUG DELIVERY, vol. 24, no. 1, 1 January 2017 (2017-01-01), US , pages 1460 - 1469, XP055982407, ISSN: 1071-7544, DOI: 10.1080/10717544.2017.1381201
Attorney, Agent or Firm:
SHENYANG FEIYANG LINGRUI INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP) (CN)
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