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1. WO2022002241 - ARYLPHOSPHINE OXIDE COMPOUNDS AND USE THEREOF

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Publication Number WO/2022/002241
Publication Date 06.01.2022
International Application No. PCT/CN2021/104219
International Filing Date 02.07.2021
IPC
C07F 9/6558 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6558containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07F 9/6512 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
645having two nitrogen atoms as the only ring hetero atoms
6509Six-membered rings
6512having the nitrogen atoms in positions 1 and 3
A61P 35/02 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/675 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
CPC
A61K 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
C07F 9/6512
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
645having two nitrogen atoms as the only ring hetero atoms
6509Six-membered rings
6512having the nitrogen atoms in positions 1 and 3
C07F 9/6558
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6558containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
Applicants
  • 成都地奥九泓制药厂 CHENGDU DI'AO JIUHONG PHARMACEUTICAL FACTORY [CN]/[CN]
Inventors
  • 何鹏 HE, Peng
  • 董光新 DONG, Guangxin
  • 赵海 ZHAO, Hai
  • 王学超 WANG, Xuechao
  • 陈爽 CHEN, Shuang
  • 黄沛 HUANG, Pei
  • 邓塔 DENG, Ta
  • 张锐 ZHANG, Rui
  • 李海燕 LI, Haiyan
Agents
  • 北京信诺创成知识产权代理有限公司 SINO-CREATIVITY INTELLECTUAL PROPERTY LAW FIRM
Priority Data
202010638649.103.07.2020CN
202011464023.X11.12.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) ARYLPHOSPHINE OXIDE COMPOUNDS AND USE THEREOF
(FR) COMPOSÉS D'OXYDE D'ARYLPHOSPHINE ET LEUR UTILISATION
(ZH) 芳基磷氧类化合物及其用途
Abstract
(EN) The present invention provides arylphosphine oxide compounds with kinase inhibitory activity. The compounds can effectively inhibit the activity of various types of EGFR drug-resistant mutants (e.g., EGFRdel19, EGFRdel19/T790M, EGFRdel19/C797S, EGFRT790M/L858R, EGFRL858R/C797S, EGFRdel19/T790M/C797S, and EGFRL858R/T790M/C797S), and also have significant inhibition of ALK fusion genes and mutants (e.g., L1196M), and thus can be used for treatment, combined therapy or prevention of various types of cancers.
(FR) La présente invention concerne des composés d'oxyde d'arylphosphine ayant une activité inhibitrice de kinase. Les composés peuvent inhiber de manière efficace l'activité de divers types de mutants résistants aux médicaments EGFR (par exemple, EGFRdel19, EGFRdel19/T790M, EGFRdel19/C797S, EGFRT790M/L858R, EGFRL858R/C797S, EGFRdel19/T790M/C797S et EGFRL858R/T790M/C797S), et ont également une inhibition significative des gènes de fusion ALK et des mutants (par exemple L1196M), et peuvent ainsi être utilisés pour le traitement, la thérapie combinée ou la prévention de divers types de cancers.
(ZH) 本发明提供了具有激酶抑制活性的芳基磷氧化合物，该类化合物可以有效抑制各种类型EGFR耐药突变体(如EGFR del19、EGFR del19/T790M、EGFR del19/C797S、EGFR T790M/L858R、EGFR L858R/C797S、EGFR del19/T790M/C797S、EGFR L858R/T790M/C797S)的活性，并对ALK融合基因及突变体(如L1196M)同样具有显著抑制作用，可用于多种癌症的治疗、联合治疗或预防。
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