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: 25.02.2016
• 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 heteroaryl pyridone and aza-pyridone compounds having Bruton's Tyrosine Kinase (Btk) modulating activity.SOLUTION: The present invention provides a compound of the following formula, where Xis CRor N; Xis CRor N; Xis CRor N; one or two of X-Xis N; one of Yand Yis substitutable CH and the other is substitutable CH or substitutable N; R-Rindependently represent H, F, Cl, NH, OH, alkyl or the like; Ris F, Cl, N, CF, hydroxymethyl or the like; Ris a substitutable monocycle or condensed heterocycle, or the like; Ris H, methyl, ethyl, NH, OH or the like; and Rhas 5 membered rings with N and represents a condensed heterocycle comprising N or the like.SELECTED DRAWING: None 【課題】ブルトン型チロシンキナーゼ（Ｂｔｋ）調節活性を有するヘテロアリールピリドン及びアザ−ピリドン化合物の提供。【解決手段】下記式で表される化合物。（Ｘ１はＣＲ１又はＮ；Ｘ２はＣＲ２又はＮ；Ｘ３はＣＲ３又はＮ；Ｘ１〜Ｘ３のうち１又は２個はＮ；Ｙ１及びＹ２は一方が置換可ＣＨ、他方が置換可ＣＨ又は置換可Ｎ；Ｒ１〜Ｒ３は各々独立にＨ、Ｆ、Ｃｌ、ＮＨ２、ＯＨ、アルキル等；Ｒ４はＦ、Ｃｌ、Ｎ、ＣＦ３、ヒドロキシメチル等；Ｒ５は置換可の単環若しくは縮合複素環等；Ｒ６はＨ、メチル、エチル、ＮＨ２、ＯＨ等；Ｒ７はＮを有する５員を有し、Ｎを含む縮合複素環等。）【選択図】なし