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1. WO2022116995 - 2,3-DIHYDRO-1H-PYRROLO[3,2-B]PYRIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF

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Publication Number WO/2022/116995
Publication Date 09.06.2022
International Application No. PCT/CN2021/134790
International Filing Date 01.12.2021
IPC
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
C07D 471/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 487/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 403/04 2006.1
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
A61K 31/506 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 31/506
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 401/04
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
C07D 403/04
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 C07D401/00
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • 上海和誉生物医药科技有限公司 ABBISKO THERAPEUTICS CO., LTD [CN]/[CN]
Inventors
  • 赵保卫 ZHAO, Baowei
  • 张鸣鸣 ZHANG, Mingming
  • 喻红平 YU, Hongping
  • 陈椎 CHEN, Zhui
  • 徐耀昌 XU, Yaochang
Agents
  • 北京戈程知识产权代理有限公司 GE CHENG & CO., LTD
Priority Data
202011400431.902.12.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) 2,3-DIHYDRO-1H-PYRROLO[3,2-B]PYRIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
(FR) DÉRIVÉ DE 2,3-DIHYDRO-1H-PYRROLO[3,2-B]PYRIDINE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 2,3-二氢-1H-吡咯并[3,2-b]吡啶衍生物、其制备方法和应用
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Abstract
(EN) The present invention relates to a 2,3-dihydro-1H-pyrrolo[3,2-b]pyridine derivative, a preparation method therefor, and an application thereof, and in particular to an EGFR inhibitor having the structure of formula (I), a preparation method therefor, a pharmaceutical composition containing same, a use of same as an EGFR inhibitor, and a use of same in the treatment and/or prevention of cancers, tumors, or metastatic diseases at least partially related to EGFR exon 20 insertion or deletion mutations, especially a use in the treatment of hyperproliferative diseases and induced cell death disorders. The definition of each substituent in formula (I) is the same as that in the description.
(FR) La présente invention concerne un dérivé de 2,3-dihydro-1H-pyrrolo[3,2-b]pyridine, son procédé de préparation, et son utilisation, et en particulier un inhibiteur d'EGFR ayant la structure de formule (I), son procédé de préparation, une composition pharmaceutique le contenant, son utilisation en tant qu'inhibiteur d'EGFR, et son utilisation dans le traitement et/ou la prévention de cancers, de tumeurs ou de maladies métastatiques au moins partiellement associées à des mutations d'insertion ou de délétion de l'exon 20 de l'EGFR, en particulier une utilisation dans le traitement de maladies hyperprolifératives et de troubles de la mort cellulaire induite. La définition de chaque substituant dans la formule (I) est identique à celle donnée dans la description.
(ZH) 涉及了2,3-二氢-1H-吡咯并[3,2-b]吡啶衍生物、其制备方法和应用。特别地涉及一种具有式(I)结构的EGFR抑制剂及其制备方法、含有其的药物组合物，以及其作为EGFR抑制剂的用途和其在治疗和/或预防至少部分由与EGFR外显子20插入或缺失突变相关的癌症、肿瘤或转移性疾病中的用途，特别是在治疗过度增殖性疾病和诱导细胞死亡障碍疾病中的用途。其中式(I)的各取代基与说明书中的定义相同。
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