Title:
ANGIOGENESIS INHIBITOR, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/184958
Kind Code:
A1
Abstract:
The present invention falls within the field of medical technology, and discloses a compound as shown by formula I or a pharmaceutically acceptable salt, cis- or trans-isomer, prodrug, metabolite, isotope derivative and solvate thereof. The compound of the present invention is a cyclobutyl-containing compound used as a tyrosine kinase inhibitor, and can be used for treating tumor diseases related to tyrosine kinase, especially VEGFR. Due to the presence of the cyclobutyl group, the substituents at 1- and 3-position have cis and trans configurations. The rigidity of a branched chain molecule and the directivity of the molecule can be enhanced, and the compound can easily be better bound to a target, so that the dosage of a drug can be reduced, and side effects of the drug is reduced. The present invention also provides a preparation method, the kinase activity, pharmacokinetic data, and pharmacodynamic data of the compound, and the results show that the compound of the present invention has a wide range of application in the treatment of tumor diseases caused by abnormal activity of tyrosine kinases such as VEGFR.
Inventors:
SUN XIAOHUA (CN)
YANG YANG (CN)
CHEN QINGGUANG (CN)
YIN DAWEI (CN)
LIU YANG (CN)
WANG JING (CN)
WANG JINGRAN (CN)
LI YUHUA (CN)
YANG HONGZHEN (CN)
HU HUAIZHONG (CN)
YANG YANG (CN)
CHEN QINGGUANG (CN)
YIN DAWEI (CN)
LIU YANG (CN)
WANG JING (CN)
WANG JINGRAN (CN)
LI YUHUA (CN)
YANG HONGZHEN (CN)
HU HUAIZHONG (CN)
Application Number:
PCT/CN2021/073616
Publication Date:
September 23, 2021
Filing Date:
January 25, 2021
Export Citation:
Assignee:
BEIJING KONRUNS PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D403/12; A61K31/517; A61P35/00
Domestic Patent References:
| WO2018214925A1 | 2018-11-29 |
Foreign References:
| CN101809012A | 2010-08-18 | |||
| CN107235896A | 2017-10-10 |
Other References:
ALI S. ABDELHAMEED ET AL.: "Molecular Interactions of AL3818 (Anlotinib) to Human Serum Albumin as Revealed by Spectroscopic and Molecular Docking Studies", JOURNAL OF MOLECULAR LIQUIDS, vol. 273, 5 October 2018 (2018-10-05), pages 259 - 265, XP085571160, DOI: 10.1016/j.molliq.2018.10.025
Attorney, Agent or Firm:
UNI-INTEL PATENT AND TRADEMARK LAW FIRM (CN)
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