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.
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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)
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:
Assignee:
SUZHOU YUTAI PHARMACEUTICAL TECH CO LTD (CN)
International Classes:
A61K47/54; A61K31/337; A61K47/60; A61K47/69; A61P35/00; C07D305/14
Foreign References:
CN105884719A | 2016-08-24 | |||
CN112604002A | 2021-04-06 | |||
CN109851593A | 2019-06-07 | |||
CN112494458A | 2021-03-16 | |||
CN110898231A | 2020-03-24 | |||
US20170151339A1 | 2017-06-01 | |||
CN105541762A | 2016-05-04 | |||
CN106432141A | 2017-02-22 |
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
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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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