HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY

• Main Authors: WENDY B YOUNG, WEI BINQING, JAMES JOHN CRAWFORD, DANIEL FRED ORTWINE
• Format: Patent
• Language: English; Japanese
• Published: 24.05.2018
• 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

PROBLEM TO BE SOLVED: To provide compounds that inhibit Bruton's Tyrosine Kinase activity for treating disorders including inflammation, immunological disease, and cancer, and stereoisomers, tautomers, and pharmaceutically acceptable salts thereof.SOLUTION: The present invention provides compounds represented by the formula, or stereoisomers, tautomers, and pharmaceutically acceptable salts thereof (X-Xindependently represent CR or N; R is H, F, Cl, NH, NHCH, OH, alkyl and the like; Ris H, F, Cl, CN, CHOH, CHF, NH, cyclopropyl or the like; Ris substituted aryl, carbocyclyl, heterocyclyl, heteroaryl or the like; Ris H, CH, CHCHOH, CHF, NHor OH; Ris a 3,4,6,7,8,9-hexahydropyrazino[1,2-a]indole-1(2H)-one-2-yl group and the like; Yand Yare CH or N, where both of them are not N at the same time).SELECTED DRAWING: None 【課題】炎症、免疫疾患及び癌を含めた障害の治療の為のブルトン型チロシンキナーゼ活性を阻害する化合物、その立体異性体、互変異性体及び薬学的に許容可能な塩の提供。【解決手段】下式で表される化合物又はその立体異性体、互変異性体又は或いは薬学的に許容可能な塩。（Ｘ１〜Ｘ３は各々独立にＣＲ又はＮ；ＲはＨ、Ｆ、Ｃｌ、ＮＨ２、ＮＨＣＨ３、ＯＨ、アルキル等Ｒ４はＨ、Ｆ、Ｃｌ、ＣＮ、ＣＨ２ＯＨ、ＣＨ２Ｆ、ＮＨ２、シクロプロピル等；Ｒ５は置換のアリール、カルボシクリル、ヘテロシクリル、ヘテロアリール等；Ｒ６はＨ、ＣＨ３、Ｃ２Ｈ５Ｃ２Ｈ４ＯＨ、ＣＨＦ２、ＮＨ２又はＯＨ；Ｒ７は３，４，６，７，８，９−ヘキサヒドロピラジノ［１，２−ａ］インドール−１（２Ｈ）−オン−２−イル基等Ｙ１及びＹ２はＣＨまたはＮ、両方がＮではない）【選択図】なし