新穎之經取代吡啶－２－酮及嗒－３－酮农业专利-农业学术服务平台

发明人:: DEWDNEY, NOLAN JAMES,杜尼　诺伦　詹姆士,杜尼　諾倫　詹姆士,KONDRU, RAMA K.,柯德鲁　雷玛Ｋ,柯德魯　雷瑪Ｋ,LOE, BRADLEY E.,洛依　布莱利Ｅ,洛依　布萊利Ｅ,LOU, YAN,娄焱,婁焱,MCINTOSH, JOEL,麦克印托许　裘尔,麥克印托許　裘爾,OWENS, TIMOTHY D.,欧文　堤莫斯Ｄ,歐文　堤莫斯Ｄ,SOTH, MICHAEL,杜尼诺伦詹姆士,杜尼諾倫詹姆士,柯德鲁雷玛K,柯德魯雷瑪K,洛依布莱利E,洛依布萊利E,麦克印托许裘尔,麥克印托許裘爾,欧文堤莫斯D,歐文堤莫斯D

摘要：: This invention discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic FormulaeI-IV:wherein variables R, X, Y1, Y2, Y2', Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of FormulaeI-IVand at least one carrier, diluent or excipient.本發明揭示通式I-IV之5-苯基-1H-吡啶-2-酮及6-苯基-2H-嗒-3-酮衍生物：其中變數R、X、Y1、Y2、Y2'、Y3、Y4、n及m係如本文所述定義，其抑制Btk。本文揭示之化合物可用於調節Btk活性及治療與過度Btk活性有關之疾病。該等化合物進一步可用於治療與異常B細胞增殖有關之炎症及自身免疫疾病，例如類風濕性關節炎。本發明亦揭示包含式I-IV之化合物及至少一種載劑、稀釋劑或賦形劑的組合物。