Compounds of formula (I) and salts thereof: wherein R1, R2, R3, a, X1, X2, X3, X4, and X5 are as defined hereinbefore. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain containing proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.
化合物的
化学式(I)及其盐:其中R1、R2、R3、a、X1、X2、X3、X4和X5的定义如前所述。已发现化合物的
化学式(I)及其盐能够抑制BET家族
溴结构域蛋白与例如乙酰化赖
氨酸残基的结合,因此可能在治疗中发挥作用,例如在治疗自身免疫和炎症性疾病(如类风湿性关节炎)和癌症方面。