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CN101541779A IKK-β丝氨酸-苏氨酸蛋白激酶抑制剂 无效 - 撤回

IKK-β丝氨酸-苏氨酸蛋白激酶抑制剂
摘要：
式(IA)或(IB)的化合物是IkB激酶(IKK)活性抑制剂，可用于治疗自身免疫性疾病和炎性疾病，式(IA)或(IB)中，R7是H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或环系统；Z是式R1R2CHNH－Y－L1－X1－(CH2)z－的基团，其中：z是0或1；R1是羧酸基(－COOH)，或可被一种或多种胞内羧酸酯酶水解成羧酸基的酯基；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)NR3－、－C(＝S)－NR3、－C(＝NH)NR3或－S(＝O)2NR3－，其中R3是氢或任选取代的C1－C6烷基；L1是式－(Alk1)m(Q)n(Alk2)p－的二价基团，其中m、n、p、Q、Alk1和Alk2如权利要求中所定义。
摘要（英）：

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-L-X-(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(=O)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 -(Alk)m(Q)n(Alk)p- wherein m, n, p, Q, AIk and AIk are as defined in the claims.

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