COMPOUND AS BRAIN-PERMEABLE BTK OR HER2 INHIBITOR, PREPARATION METHOD THEREFOR, AND USE THEREOF

Title:

COMPOUND AS BRAIN-PERMEABLE BTK OR HER2 INHIBITOR, PREPARATION METHOD THEREFOR, AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2022/012509

Kind Code:

A1

Abstract:

A compound as a BTK inhibitor or an HER2 inhibitor, a preparation method therefor, and a use thereof. The compound comprises a structure as shown in formula II or a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer, or a mixture form thereof, and a pharmaceutically acceptable hydrate, a solvate, or salt. The BTK protein kinase inhibitor of the present invention has strong inhibitory activity on wild-type BTK or mutated BTK (C481S), and some of the compounds have high brain permeability; the HER2 inhibitor of the present invention has good HER2 kinase inhibitory activity and high blood-brain barrier transmittance; and the compound of the present invention has good pharmacokinetic properties and a good application prospect.

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Inventors:

YUE CHUNCHAO (CN)
LIU GUANFENG (CN)
LI SHAI (CN)
LI JING (CN)
CHEN GANG (CN)
YUAN CHENGUANG (CN)
LI YINGFU (CN)

Application Number:

PCT/CN2021/105960

Publication Date:

January 20, 2022

Filing Date:

July 13, 2021

Export Citation:

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Assignee:

CHENGDU HYPERWAY PHARMACEUTICALS CO LTD (CN)
SHENZHEN HYPERWAY PHARMACEUTICALS CO LTD (CN)

International Classes:

C07D487/04; A61K31/437; A61K31/4985; A61K31/519; A61P1/00; A61P1/04; A61P7/04; A61P9/00; A61P11/00; A61P11/06; A61P17/00; A61P17/06; A61P19/02; A61P25/28; A61P35/00; A61P35/02; A61P37/06; A61P37/08; C07D471/04; C07D519/00

Domestic Patent References:

WO2016106624A1	2016-07-07
WO2009143051A1	2009-11-26
WO2016106652A1	2016-07-07

Foreign References:

CN106146511A	2016-11-23
CN202010679776A	2020-07-15
CN202011337022A	2020-11-25

Other References:

JOURNAL OF MEDICINAL CHEMISTRY, vol. 63, no. 10, 2020, pages 5102 - 5118
ANGEW. CHEM. INT. ED., vol. 59, 2020, pages 7161 - 7167

Attorney, Agent or Firm:

UNITALEN ATTORNEYS AT LAW (CN)

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