Processing

Please wait...

Settings

Settings

Goto Application

1. WO2020113816 - 4-AROMATIC HETEROCYCLIC SUBSTITUTED INDAZOLE AND USE THEREOF AS IDO/TDO DUAL INHIBITOR

Publication Number WO/2020/113816
Publication Date 11.06.2020
International Application No. PCT/CN2019/074333
International Filing Date 01.02.2019
IPC
A61K 31/416 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4151,2-Diazoles
416condensed with carbocyclic ring systems, e.g. indazole
C07D 231/56 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
54condensed with carbocyclic rings or ring systems
56Benzopyrazoles; Hydrogenated benzopyrazoles
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
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
A61P 25/24 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
24Antidepressants
A61P 37/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
Applicants
  • 西华大学 XIHUA UNIVERSITY [CN]/[CN]
Inventors
  • 王周玉 WANG, Zhouyu
  • 钱珊 QIAN, Shan
  • 曹治兴 CAO, Zhixing
  • 李玉芝 LI, Yuzhi
  • 曹仁旭 CAO, Renxu
  • 王桂 WANG, Gui
  • 袁欣 YUAN, Xin
  • 马兴梅 MA, Xingmei
Agents
  • 成都高远知识产权代理事务所(普通合伙) GAOYUNG INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP)
Priority Data
201811497767.407.12.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) 4-AROMATIC HETEROCYCLIC SUBSTITUTED INDAZOLE AND USE THEREOF AS IDO/TDO DUAL INHIBITOR
(FR) INDAZOLE HÉTÉROCYCLIQUE 4-AROMATIQUE SUBSTITUÉ ET SON UTILISATION EN TANT QU'INHIBITEUR DOUBLE D'IDO/TDO
(ZH) 4位芳杂环取代的吲唑类化合物及其作为IDO/TDO双重抑制剂的用途
Abstract
(EN)
Disclosed is an 4-aromatic heterocyclic substituted indazole represented by formula (I) and the use thereof as an IDO/TDO dual inhibitor. The compounds of the present invention have excellent inhibitory effects on both IDO/TDO enzymes and IDO/TDO cells and significant in vivo antitumor activity, and can be used to prevent and/or treat a variety of diseases, such as tumors, neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, depression, infection associated with cellular immune activation, or abnormal tryptophan metabolism.
(FR)
L'invention concerne un indazole hétérocyclique 4-aromatique substitué représenté par la formule (I) et son utilisation en tant qu'inhibiteur double d'IDO/TDO. Les composés de la présente invention présentent d'excellents effets inhibiteurs sur les enzymes IDO/TDO et les cellules IDO/TDO et une activité antitumorale significative in vivo, et peuvent être utilisés pour prévenir et/ou traiter une variété de maladies, telles que les tumeurs, les maladies neurodégénératives, la maladie d'Alzheimer, la maladie de Parkinson, la dépression, l'infection associée à l'activation immunitaire cellulaire, ou le métabolisme anormal du tryptophane. (I)
(ZH)
本发明公开了一种式(I)所示的4位芳杂环取代的吲唑类化合物作为IDO/TDO双重抑制剂的用途。本发明化合物对IDO/TDO酶和IDO/TDO细胞均具有优异的抑制作用,而且体内具有显著抗肿瘤活性,可以用于预防和/或治疗多种疾病,如肿瘤、神经退行性疾病、阿尔茨海默病、帕金森病、抑郁症、细胞免疫激活相关的感染、或色氨酸代谢异常等。
Latest bibliographic data on file with the International Bureau