PYRIMIDINES FOR DEGRADING BRUTON'S TYROSINE KINASE

To provide compounds that induce proteolysis of Btk via a ubiquitin proteolysis pathway.SOLUTION: The present invention provides compounds of formula (I), where R1, R2, R3, R4A, R4b and R5 are as defined herein, and pharmaceutically acceptable salts thereof, which are useful as agents in treatment o...

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Hauptverfasser: BERENGER BIANNIC, ELIZABETH L NOEY, JOSHUA N PAYETTE, OKANO AKINORI, SHAHAB MORTEZAEI, BIAN ZHIGUO, JASON P BURKE, ASHLEY M ADAMS, VENKAT REDDY MALI, ALEXEY A RIVKIN, ZHAO XIANRUI, MATTHEW H KATCHER, VIOLETA L MARIN, JIANG XINGYU, JIA ZHAOZHONG J, KEVIN R WOLLER, SPENCER O SHOLZ, JEFFERY A ZABLOCKI
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creator BERENGER BIANNIC
ELIZABETH L NOEY
JOSHUA N PAYETTE
OKANO AKINORI
SHAHAB MORTEZAEI
BIAN ZHIGUO
JASON P BURKE
ASHLEY M ADAMS
VENKAT REDDY MALI
ALEXEY A RIVKIN
ZHAO XIANRUI
MATTHEW H KATCHER
VIOLETA L MARIN
JIANG XINGYU
JIA ZHAOZHONG J
KEVIN R WOLLER
SPENCER O SHOLZ
JEFFERY A ZABLOCKI
description To provide compounds that induce proteolysis of Btk via a ubiquitin proteolysis pathway.SOLUTION: The present invention provides compounds of formula (I), where R1, R2, R3, R4A, R4b and R5 are as defined herein, and pharmaceutically acceptable salts thereof, which are useful as agents in treatment of CLL.SELECTED DRAWING: Figure 1 【課題】ユビキチンタンパク質分解経路を介してBtkのタンパク質分解を誘導する化合物を提供すること。【解決手段】本発明は、CLLの治療において薬剤として有用である、式(I)の化合物TIFF2023140319000023.tif78168[式中、R1、R2、R3、R4A、R4b及びR5は、本明細書中に定義される通りである]及び薬学的に許容されるそれらの塩を提供する。【選択図】図1
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title PYRIMIDINES FOR DEGRADING BRUTON'S TYROSINE KINASE
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