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Benzamide derivatives for the inhibition of the activity ABL2 ABL1, and BCR - ABL1

机译:苯甲酰胺衍生物用于抑制ABL2和ACR1的活性,以及​​BCR-ABL1

摘要

The present Invention relates to Derivatives of benzamide compounds of formula (i), or pharmaceutically acceptable salts of thereof, wherein: R1 is pirazolilo optionally substituted with 1 to 2 groups R6, R7 R2 is replaced with pirrolidinilo; R3 is H or Halogen; R4 is sedan - CF2 - or - y2 y3 R6; h, Among others; R7 is hydroxyl, hydroxyl, Methyl, among others; and Y1 and Y2 are CF2 is n or CH,;- or or - S (o) 0 - 2; Y3 h, Chlorine, among others. It is a Preferred compound: (R) - N - (4 - (chloro difluoro methoxy) - phenyl) - 6 - (2 - hydroxy - pyrrolidin-1-yl) - 5 - (1h pyrazole - 5 - il) - Nicotinamide, among others. It also relates to a Pharmaceutical composition.These compounds inhibit the Enzymatic activity of the Protein Tyrosine Kinase Abelson, ABL1, ABL2 and chimeric protein BCR - ABL1, being useful in the treatment of cancer
机译:本发明涉及式(i)的苯甲酰胺化合物的衍生物或其药学上可接受的盐,其中:R1是任选被1-2个R6基团取代的吡唑索洛,R7R2被吡咯烷基取代。 R3是H或卤素; R4是轿车-CF2-或-y2 y3 R6; h,除其他外; R 7是羟基,羟基,甲基等。并且Y1和Y2为CF2为n或CH ,;或-或-S(o)0-2; Y3小时,氯,等等。它是优选的化合物:(R)-N-(4--(氯二氟甲氧基)-苯基)-6-(2-羟基-吡咯烷基-1-基)-5-(1h吡唑-5-il)-烟酰胺等等。它还涉及药物组合物。这些化合物抑制蛋白酪氨酸激酶Abelson,ABL1,ABL2和嵌合蛋白B​​CR-ABL1的酶活性,可用于治疗癌症。

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