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1. WO2020192302 - PYRIMIDINE-CONTAINING TRI-SUBSTITUTED IMIDAZOLE COMPOUND AND APPLICATION THEREOF

Publication Number WO/2020/192302
Publication Date 01.10.2020
International Application No. PCT/CN2020/075475
International Filing Date 17.02.2020
IPC
C07D 403/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
C07D 403/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14containing three or more hetero rings
C07D 405/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
C07D 409/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14containing three or more hetero rings
C07D 401/14 2006.01
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
14containing three or more hetero rings
C07D 413/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
Applicants
  • 广州必贝特医药技术有限公司 GUANGZHOU BEBETTER MEDICINE TECH CO LTD [CN]/[CN]
Inventors
  • 蔡雄 CAI, Xiong
  • 翁运幄 WENG, Yunwo
  • 卿远辉 QING, Yuanhui
  • 林明生 LIN, Mingsheng
  • 刘斌 LIU, Bing
  • 范福顺 FAN, Fushun
  • 封巧 FENG, Qiao
  • 刘怡婷 LIU, Yiting
  • 钱长庚 QIAN, Changgeng
Agents
  • 广州广典知识产权代理事务所(普通合伙) GUANGZHOU GUANGDIAN INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP)
Priority Data
201910238323.727.03.2019CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PYRIMIDINE-CONTAINING TRI-SUBSTITUTED IMIDAZOLE COMPOUND AND APPLICATION THEREOF
(FR) COMPOSÉ D'IMIDAZOLE TRI-SUBSTITUÉ CONTENANT DE LA PYRIMIDINE ET UTILISATION ASSOCIÉE
(ZH) 含嘧啶的三取代咪唑类化合物及其应用
Abstract
(EN)
Disclosed are a pyrimidine-containing tri-substituted imidazole compound having the structure shown in formula (I) and an application thereof. The compound can effectively inhibit EGFR C797S mutations including EGFR ex19del/T790M/C797S and L858R/T790M/C797S, at the same time, it also has higher inhibitory activity against single point mutations L858R, ex19del and double-point mutations such as L858R/T790M and ex19del/T790M, moreover, the compound has a weak inhibitory effect on wild-type EGFR, that is, it has good selectivity. The compound has the potential to be used as a drug for treating malignant tumor carrying EGFR C797S mutations, especially non-small cell lung cancer (NSCLC), and has a greater application value.
(FR)
L'invention concerne un composé d'imidazole tri-substitué contenant de la pyrimidine ayant la structure représentée dans la formule (I) et une utilisation associée. Le composé peut inhiber de manière efficace des mutations EGFR C797S comprenant l'EGFR ex19del/T790M/C797S et L858R/T790M/C797S, en même temps, ledit composé a également une activité inhibitrice supérieure vis-à-vis de mutations ponctuelles uniques L858R, ex19del et des mutations à point double telles que L858R/T790M et ex19del/T790M, en outre, le composé a un effet inhibiteur faible sur EGFR de type sauvage, présentant ainsi une bonne sélectivité. Le composé a le potentiel d'être utilisé en tant que médicament pour traiter une tumeur maligne portant des mutations EGFR C797S, en particulier le cancer du poumon non à petites cellules (NSCLC), et présente une grande valeur d'application.
(ZH)
公开了一种具有式(I)所示结构的含嘧啶的三取代咪唑类化合物及其应用。该类化合物可以有效抑制包括EGFR ex19del/T790M/C797S和L858R/T790M/C797S在内的EGFR C797S突变,同时对包括单点突变L858R、ex19del和双点突变如L858R/T790M,ex19del/T790M等也有较高抑制活性,并且,这类化合物对野生型EGFR抑制作用弱,即具有很好的选择性。该类化合物有潜力成为用作携带EGFR C797S突变的恶性肿瘤,尤其是非小细胞肺癌(NSCLC)治疗的药物,有较大的应用价值。
Also published as
CN202080000490.9
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