8-FLUOROPHTHALAZIN-1 (2H)-ONE 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: 03.03.2016
• 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 a compound useful for treating immune disorders such as inflammation mediated by Bruton's Tyrosine Kinase (Btk).SOLUTION: The present invention provides 8-fluorophthalazin-1(2h)-one compounds represented by the following structure, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof. The present invention also provides methods of using the compounds for in vitro, in situ, and in vivo diagnosis and treatment of Btk activity-associated disorders in mammalian cells, or related pathological conditions.SELECTED DRAWING: None 【課題】ブルトン型チロシンキナーゼ（Ｂｔｋ）によって媒介される炎症などの免疫障害を治療するために有用な化合物の提供。【解決手段】下記の構造で表される８−フルオロフタラジン−１（２ｈ）−オン化合物、及びその立体異性体、互変異性体及び薬学的に許容可能な塩を含む化合物。哺乳動物細胞におけるＢＴＫ活性に伴う障害又は関連する病的状態のインビトロ、インサイツ及びインビボ診断及び治療の為に前記化合物を使用する方法。【選択図】なし