申请人:CELLCENTRIC LTD
公开号:US10428065B2
公开(公告)日:2019-10-01
A compound which is an isoxazolyl imidazopyridine of formula (I): wherein: R0 and R, which are the same or different, are each H or C alkyl; R9′ and R9″, which are the same or different, are each H or F; X is -(alk)n-, -alk-C(═O)—NR—, -alk-NR—C(═O)— or -alk-C(═O)—; R1 is selected from —S(═O)2R′ and a 4- to 7-membered heterocyclic group which is unsubstituted or substituted; R2 and R2′, which are the same or different, are each H or C1-6 alkyl; or R2 and R2′ form, together with the C atom to which they are attached, a C3-6 cycloalkyl group; R3 and R3′, which are the same or different, are each H, C1-6 alkyl, OH or F; R4 is phenyl or a 5- to 12-membered N-containing heteroaryl group and is unsubstituted or substituted; alk is C1-6 alkylene; R′ is C1-6 alkyl; and n is 0 or 1; or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer.
一种化合物,它是式(I)的异噁唑基咪唑吡啶: 其中:R0和R相同或不同,各自为H或C烷基;R9′和R9″相同或不同,各自为H或F;X为-(alk)n-、-alk-C(═O)-NR-、-alk-NR-C(═O)-或-alk-C(═O)-;R1 选自-S(═O)2R′和未取代或取代的 4 至 7 元杂环基团; R2 和 R2′相同或不同,各自为 H 或 C1-6 烷基;R3和R3′相同或不同,各自为H、C1-6烷基、OH或F;R4为苯基或5-12元含N杂芳基且未取代或取代;alk为C1-6亚烷基;R′为C1-6烷基;n为0或1;或其药学上可接受的盐。该化合物具有调节 p300 和/或 CBP 活性的活性,可用于治疗癌症。