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1. WO2022002097 - PYRAZOLO[1,5-A]PYRIDINE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF

Publication Number WO/2022/002097
Publication Date 06.01.2022
International Application No. PCT/CN2021/103358
International Filing Date 30.06.2021
IPC
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 519/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
519Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
A61K 31/437 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
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4995 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
4995Pyrazines or piperazines forming part of bridged ring systems
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 1/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
Applicants
  • 上海艾力斯医药科技股份有限公司 SHANGHAI ALLIST PHARMACEUTICALS CO., LTD. [CN]/[CN]
Inventors
  • 罗会兵 LUO, Huibing
  • 周华勇 ZHOU, Huayong
  • 李庆 LI, Qing
Agents
  • 中国专利代理(香港)有限公司 CHINA PATENT AGENT (H.K.) LTD.
Priority Data
202010625119.301.07.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PYRAZOLO[1,5-A]PYRIDINE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
(FR) COMPOSÉ DE PYRAZOLO[1,5-A]PYRIDINE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 吡唑[1,5-a]吡啶类化合物及其制备方法与应用
Abstract
(EN) The present invention relates to a pyrazolo[1,5-a]pyridine compound as represented by the general formula (I), a preparation method therefor, a pharmaceutical composition, and the use thereof. In the formula, R1, R2, R3, R4, R5, X, Y, and Z are as defined in the description. The pyrazolo[1,5-a]pyridine compound of the present invention can effectively inhibit wild-type RET, mutant RET, specifically G810R mutant RET, and RET fusion, such as KIF5B-RET and CCDC6-RET, same has good safety, and can be used for treating RET-mediated diseases, such as cancers and irritable bowel syndrome.
(FR) La présente invention concerne un composé de pyrazolo[1,5-a]pyridine tel que représenté par la formule générale suivante (I), son procédé de préparation, une composition pharmaceutique et une utilisation associée. Dans la formule, R1, R2, R3, R4, R5, X, Y et Z sont tels que définis dans la description. Le composé pyrazolo[1,5-a]pyridine selon la présente invention peut inhiber de manière efficace la RET de type sauvage, RET mutante, en particulier RET mutante G810R, et fusion RET, telle que KIF5B-RET et CCDC6-RET, qui a une bonne innocuité, et peut être utilisé pour traiter des maladies à médiation par RET, telles que des cancers et le syndrome du côlon irritable.
(ZH) 本发明涉及通式(I)所示的吡唑[1,5-a]吡啶类化合物、其制备方法、药物组合物及应用,式中R1、R2、R3、R4、R5、X、Y、Z如说明书中所定义。本发明所述吡唑[1,5-a]吡啶类化合物能够有效抑制野生型RET、突变型RET特别是G810R突变型RET、以及KIF5B-RET和CCDC6-RET等RET融合,且安全性好,可用于治疗由RET介导的疾病,例如癌症和肠易激综合征。
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