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1. WO2020134022 - USE OF AXITINIB AND ANALOGS THEREOF IN PREPARING BLOOD-BRAIN BARRIER PERMEABILITY REGULATOR

Publication Number WO/2020/134022
Publication Date 02.07.2020
International Application No. PCT/CN2019/095242
International Filing Date 09.07.2019
IPC
A61K 31/4439 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 25/28 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
CPC
A61K 31/4439
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Applicants
  • 浙江大学 ZHEJIANG UNIVERSITY [CN]/[CN]
Inventors
  • 胡富强 HU, Fuqiang
  • 温丽娟 WEN, Lijuan
  • 袁弘 YUAN, Hong
  • 王凯 WANG, Kai
  • 孟廷廷 MENG, Tingting
Agents
  • 北京尚诚知识产权代理有限公司 SHANGCHENG & PARTNERS
Priority Data
201811610364.627.12.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) USE OF AXITINIB AND ANALOGS THEREOF IN PREPARING BLOOD-BRAIN BARRIER PERMEABILITY REGULATOR
(FR) UTILISATION D'AXITINIB ET D'ANALOGUES DE CELUI-CI DANS LA PRÉPARATION D'UN RÉGULATEUR DE PERMÉABILITÉ DE LA BARRIÈRE HÉMATO-ENCÉPHALIQUE
(ZH) 阿西替尼及其类似物在制备血脑屏障渗透性调控剂中的应用
Abstract
(EN)
The present invention relates to the use of axitinib and analogs thereof in preparing a blood-brain barrier permeability regulator. The blood-brain barrier permeability regulator can reduce the permeability of the blood-brain barrier, and can promote the recovery of the blood-brain barrier function from a pathologically destroyed state to a state close to that of the physiological barrier. The axitinib and analogs thereof reduce the degree of down-regulation of a pathological blood-brain barrier tight junction protein Claudin-5/Occludin by inhibiting the vascular endothelial cell growth factor-phosphatidylinositol kinase-protein kinase B signaling pathway, thereby reducing the permeability of the blood-brain barrier. The blood-brain barrier permeability regulator can be used in the treatment of related diseases that cause changes in the permeability of the blood-brain barrier.
(FR)
La présente invention concerne l'utilisation de l'axitinib et d'analogues de celui-ci dans la préparation d'un régulateur de perméabilité de la barrière hémato-encéphalique. Le régulateur de perméabilité de barrière hémato-encéphalique peut réduire la perméabilité de la barrière hémato-encéphalique, et peut favoriser la récupération de la fonction de barrière hémato-encéphalique d'un état pathologique détruit à un état proche de celui de la barrière physiologique. L'axitinib et les analogues de celui-ci réduisent le degré de régulation à la baisse d'une protéine de jonction étanche Claudine-5/Occludine de la barrière hémato-encéphalique pathologique par l'inhibition de la voie de signalisation facteur de croissance des cellules endothéliales vasculaires - phosphatidylinositol kinase - protéine kinase B, ce qui permet de réduire la perméabilité de la barrière hémato-encéphalique. Le régulateur de perméabilité de la barrière hémato-encéphalique peut être utilisé dans le traitement de maladies associées qui provoquent des changements de la perméabilité de la barrière hémato-encéphalique.
(ZH)
本发明涉及阿西替尼及其类似物在制备血脑屏障渗透性调控剂中的应用。所述血脑屏障渗透性调控剂能够降低血脑屏障渗透性,促进血脑屏障功能由病理性破坏状态恢复至接近生理性屏障状态。阿西替尼及其类似物通过抑制血管内皮细胞生长因子-磷脂酰肌醇激酶-蛋白激酶B信号通路,减少病理性血脑屏障紧密连接蛋白Claudin-5/Occludin下调的程度,降低血脑屏障渗透性。所述血脑屏障渗透性调控剂能够用于引起血脑屏障渗透性改变的相关疾病的治疗。
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