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1. WO2020140924 - DIHYDRAZONE COMPOUNDS HAVING HIGH AFFINITY TO AΒ PROTEIN AND TAU PROTEIN, DERIVATIVES THEREOF AND USE THEREOF

Publication Number WO/2020/140924
Publication Date 09.07.2020
International Application No. PCT/CN2020/070009
International Filing Date 02.01.2020
IPC
C07C 251/88 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
251Compounds containing nitrogen atoms doubly- bound to a carbon skeleton
72Hydrazones
88having also the other nitrogen atom doubly-bound to a carbon atom, e.g. azines
CPC
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
C07C 249/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
249Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton
16of hydrazones
C07C 251/88
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
251Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
72Hydrazones
88having also the other nitrogen atom doubly-bound to a carbon atom, e.g. azines
C07D 213/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
62Oxygen or sulfur atoms
63One oxygen atom
64attached in position 2 or 6
C07D 213/75
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
Applicants
  • 原子高科股份有限公司 HTA CO., LTD. [CN]/[CN]
  • 北京师范大学 BEIJING NORMAL UNIVERSITY [CN]/[CN]
Inventors
  • 崔孟超 CUI, Mengchao
  • 沈浪涛 SHEN, Langtao
  • 邓雪松 DENG, Xuesong
  • 周凯翔 ZHOU, Kaixiang
Agents
  • 北京路浩知识产权代理有限公司 CN-KNOWHOW INTELLECTUAL PROPERTY AGENT LIMITED
Priority Data
201910007703.X04.01.2019CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) DIHYDRAZONE COMPOUNDS HAVING HIGH AFFINITY TO AΒ PROTEIN AND TAU PROTEIN, DERIVATIVES THEREOF AND USE THEREOF
(FR) COMPOSÉS DE DIHYDRAZONE AYANT UNE AFFINITÉ ÉLEVÉE VIS-À-VIS DE LA PROTÉINE AΒ ET DE LA PROTÉINE TAU, LEURS DÉRIVÉS ET LEUR UTILISATION
(ZH) 与Aβ蛋白和Tau蛋白具有高亲和力的双腙类化合物及其衍生物与应用
Abstract
(EN)
The present invention provides dihydrazone compounds having high affinity to Aβ protein and Tau protein and derivatives thereof. The structure of said compounds is as shown in formula (I): (I). Such compounds can be directly used as fluorescent probes for detecting neurofibrillary tangles in vivo or in a tissue sample, and when used in nuclear medicine imaging, the compounds need to be labelled using a suitable radioactive isotope. Such compounds are particularly useful for diagnosing patients with neurodegenerative diseases, including Alzheimer's disease, having the characteristics of Aβ plaques and neurofibrillary tangles.
(FR)
La présente invention concerne des composés de dihydrazone ayant une affinité élevée vis-à-vis de la protéine Aβ et de la protéine Tau et des dérivés de ceux-ci. La structure desdits composés est telle que représentée par la formule (I) : (I). De tels composés peuvent être utilisés directement en tant que sondes fluorescentes pour détecter des enchevêtrements neurofibrillaires in vivo ou dans un échantillon de tissu, et lorsqu'ils sont utilisés en imagerie médicale nucléaire, les composés doivent être marqués à l'aide d'un isotope radioactif approprié. De tels composés sont particulièrement utiles pour diagnostiquer des patients atteints de maladies neurodégénératives, y compris la maladie d'Alzheimer, ayant des caractéristiques de plaques Aβ et d'enchevêtrements neurofibrillaires.
(ZH)
本发明提供与Aβ蛋白和Tau蛋白具有高亲和力的双腙类化合物及其衍生物,所述化合物的结构如式(I)所示:(I)此类化合物可直接作为检测体内或组织样本中神经纤维缠结的荧光探针,当用于核医学显像时,需用合适的放射性同位素对其进行标记。该类化合物尤其适用于诊断神经退行性疾病,包括阿尔茨海默病在内的具有Aβ斑块和神经纤维缠结特征的患者。
Also published as
GB2105614.8
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