BERTHEL, STEVEN JOSEPH,柏森 史堤芬 裘瑟夫,柏森 史堤芬 裘瑟夫,BILLEDEAU, ROLAND J.,毕尔杜 罗兰J,畢爾杜 羅蘭J,BROTHERTON-PLEISS, CHRISTINE E.,巴松顿 布列斯 克里斯汀E,巴松頓 布列斯 克里斯汀E,FIROOZNIA, FARIBORZ,菲罗兹尼亚 法罗伯兹,菲羅茲尼亞 法羅伯茲,GABRIEL, STEPHEN
申请号：
TW100128247
公开号：
TW201211039A
申请日:
2011.08.08
申请国别(地区):
TW
年份:
2012
代理人:
摘要：
This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I:wherein, variables X, R, and Y4, 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 inflammatoty and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compouads of Formula I and at least one carrier, diluent or excipient.本申請案揭示根據通式I之6-(2-羥甲基-苯基)-2-甲基-2H-噠嗪-3-酮衍生物:其中變數X、R及Y4如本文所述而定義,該等衍生物抑制Btk。本文所揭示之化合物適用於調節Btk活性及治療與過度Btk活性相關之疾病。該等化合物另外適用於治療與異常B細胞增殖相關之發炎性疾病及自體免疫疾病,諸如類風濕性關節炎。亦揭示含有式I化合物及至少一種載劑、稀釋劑或賦形劑之組合物。
