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1. WO2022007168 - BENZO FIVE-MEMBERED NITROGEN HETEROCYCLIC COMPOUND AND APPLICATION THEREOF

Publication Number WO/2022/007168
Publication Date 13.01.2022
International Application No. PCT/CN2020/113949
International Filing Date 08.09.2020
IPC
C07D 277/66 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
277Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
60condensed with carbocyclic rings or ring systems
62Benzothiazoles
64with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
66with aromatic rings or ring systems directly attached in position 2
C07D 235/18 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
235Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02condensed with carbocyclic rings or ring systems
04Benzimidazoles; Hydrogenated benzimidazoles
18with aryl radicals directly attached in position 2
C07D 401/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/4439 2006.1
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
C07D 401/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
A61K 31/4184 2006.1
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
41641,3-Diazoles
4184condensed with carbocyclic rings, e.g. benzimidazoles
Applicants
  • 中国科学院广州生物医药与健康研究院 GUANGZHOU INSTITUTES OF BIOMEDICINE AND HEALTH CHINESE ACADEMY OF SCIENCES [CN]/[CN]
Inventors
  • 许永 XU, Yong
  • 吴锡山 WU, Xishan
  • 张岩 ZHANG, Yan
  • 王蕊 WANG, Rui
  • 沈慧 SHEN, Hui
Agents
  • 北京品源专利代理有限公司 BEYOND ATTORNEYS AT LAW
Priority Data
202010663949.510.07.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) BENZO FIVE-MEMBERED NITROGEN HETEROCYCLIC COMPOUND AND APPLICATION THEREOF
(FR) COMPOSÉ HÉTÉROCYCLIQUE AZOTÉ À CINQ CHAÎNONS BENZO ET UTILISATION ASSOCIÉE
(ZH) 一种苯并五元氮杂环化合物及其应用
Abstract
(EN) The present application relates to a benzo five-membered nitrogen heterocyclic compound and an application thereof. The benzo five-membered nitrogen heterocyclic compound has the structure represented by formula I. The compound can be used as a compound of RORγ receptor inhibitor. The compound can effectively inhibit RORγ proteins and have good selectivity to other nuclear receptor family proteins. The benzo five-membered nitrogen heterocyclic compound or a pharmaceutical composition thereof provided by the present application can be used for preparing a drug for treating, preventing or ameliorating diseases such as inflammations, autoimmune diseases, cell proliferative disorder diseases, sepsis, cancer, neurodegeneration diseases or viral infections, has a good inhibitory effect on the treatment of tumors, especially the treatment of prostate cancer, and also has an amelioration effect on the treatment of other diseases.
(FR) La présente invention concerne un composé hétérocyclique azoté à cinq chaînons benzo et une utilisation associée. Le composé hétérocyclique azoté à cinq chaînons a la structure représentée par la formule I. Le composé peut être utilisé en tant que composé d'inhibiteur du récepteur RORγ. Le composé peut inhiber de manière efficace des protéines RORγ et a une bonne sélectivité vis-à-vis d'autres protéines de la famille des récepteurs nucléaires. Le composé hétérocyclique azoté à cinq chaînons benzo ou une composition pharmaceutique de celui-ci fourni par la présente invention peut être utilisé pour préparer un médicament destiné au traitement, à la prévention ou le soulagement de maladies telles que des inflammations, maladies auto-immunes, maladies des troubles prolifératifs cellulaires, la sepsie, le cancer, les maladies neurodégénératives ou les infections virales, a un bon effet inhibiteur sur le traitement de tumeurs, en particulier le traitement du cancer de la prostate, et a également un effet d'amélioration sur le traitement d'autres maladies.
(ZH) 本申请涉及一种苯并五元氮杂环化合物及其应用,所述苯并五元氮杂环化合物具有式I所示的结构,所述化合物可作为RORγ受体抑制剂的化合物,该类化合物可有效抑制RORγ蛋白,并对其他核受体家族蛋白具有很好的选择性;本申请提供的苯并五元含氮杂环类化合物或其药物组合物可用于制备治疗、预防或改善炎症、自身免疫性疾病、细胞增殖性紊乱疾病、败血病、癌症、神经性衰退性疾病或病毒感染等疾病的药物,对肿瘤的治疗具有良好的抑制作用,特别是对于前列腺癌的疗效尤为突出,对其他疾病的治疗也具有改善作用。
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