新穎之吡啶酮及嗒酮农业专利-农业学术服务平台

发明人:: DEWDNEY, NOLAN JAMES,迪尔尼　诺兰　詹姆士,迪爾尼　諾蘭　詹姆士,KENNEDY-SMITH, JOSHUA,甘乃迪　史密斯　裘夏娃,甘迺迪　史密斯　裘夏娃,KONDRU, RAMA K.,康德鲁　雷玛Ｋ,康德魯　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,迪尔尼诺兰詹姆士,迪爾尼諾蘭詹姆士,甘乃迪史密斯裘夏娃,甘迺迪史密斯裘夏娃,康德鲁雷玛K,康德魯雷瑪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

摘要：: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, 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 autoimmune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.本案揭示抑制Btk之通式I-III之5-苯基-1H-吡啶-2-酮及6-苯基-2H-嗒-3-酮衍生物：其中變量R、X、Y1、Y2、Y3、Y4、n及m係如本文所述定義。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體免疫疾病，例如類風濕性關節炎。本案亦揭示含有式I-III之化合物及至少一種載劑、稀釋劑或賦形劑的組合物。