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
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	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
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Beschreibung
Zusammenfassung:	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