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发明授权
US08003695B2 IKK-beta serine-threonine protein kinase inhibitors 失效
IKK-β丝氨酸 - 苏氨酸蛋白激酶抑制剂

IKK-beta serine-threonine protein kinase inhibitors
摘要：
Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— wherein: z is 0 or 1; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(═O)—, —S(═P)2-, —C(═O)O—, —C(═O)NR3-, —C(═S)—NR3, —C(═NH)—NR3 or —S(═O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent linker radical of formula -(Alk1)m(Q)(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.
摘要（中）：

式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：式（A）和（B）其中R 7为氢或任选取代的（C1- C6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是（a）式R1R2CHNH-Y-L1-X1-（CH2）z-的基团，其中：z为0或1; R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R2是天然或非天然α氨基酸的侧链; Y是键，-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）NR 3 - ， - C（= NH）-NR 3或-S（= O）2 NR 3 - ，其中R 3是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）（Alk2）p的二价连接基团，其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

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