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1. WO2020221236 - TRK KINASE INHIBITOR AND USE THEREOF

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Publication Number WO/2020/221236
Publication Date 05.11.2020
International Application No. PCT/CN2020/087411
International Filing Date 28.04.2020
IPC
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
CPC
A61K 31/519
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
519ortho- or peri-condensed with heterocyclic rings
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
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
  • 江苏柯菲平医药股份有限公司 JIANGSU CAREPHAR PHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 秦引林 QIN, Yinlin
  • 苏梅 SU, Mei
Agents
  • 南京天华专利代理有限责任公司 NANJING TIANHUA PATENT AGENT CO., LTD.
Priority Data
201910362213.130.04.2019CN
202010337981.426.04.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) TRK KINASE INHIBITOR AND USE THEREOF
(FR) INHIBITEUR DE KINASE TRK ET SON UTILISATION
(ZH) TRK激酶抑制剂及其用途
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Abstract
(EN) Disclosed are a TRK kinase inhibitor and use thereof. The TRK kinase inhibitor of the present invention is as shown in formula (I). Also provided are a preparation method for a compound, as well as a pharmaceutical composition containing a kinase inhibitor and use thereof in the prevention and treatment of cancers. The new compound shown in formula I disclosed in the present invention exhibits a good TRK inhibitory activity, and provides a new option for clinical treatment of diseases related to abnormal TRK activity.
(FR) L'invention concerne un inhibiteur de kinase TRK et son utilisation. L'inhibiteur de kinase TRK selon la présente invention est tel que représenté dans la formule (I). L'invention concerne également un procédé de préparation d'un composé, ainsi qu'une composition pharmaceutique contenant un inhibiteur de kinase et son utilisation dans la prévention et le traitement de cancers. Le nouveau composé représenté par la formule (I) selon la présente invention a une bonne activité inhibitrice de TRK, et fournit une nouvelle option pour le traitement clinique de maladies associées à une activité anormale de TRK. (I)
(ZH) 本发明公开一种TRK激酶抑制剂及其用途，本发明所述的TRK激酶抑制剂如式(I)所示，还提供了所述化合物的制备方法、包含有这些激酶抑制剂的药物组合物及其在预防与治疗癌症中的用途；本发明公开的式I所示的新化合物，表现出了良好的TRK抑制活性，为临床治疗与TRK活性异常相关的疾病提供了一种新的选择。
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