首页> 外国专利> 3-AMINO-PYRAZIN-2-YL CARBOXAMIDE AND 2-AMINO-PYRIDIN-3-YL CARBOXAMIDE DERIVATIVES AS POLO-LIKE KINASE 1 (PLK-1) INHIBITORS FOR THE TREATMENT OF CANCER

3-AMINO-PYRAZIN-2-YL CARBOXAMIDE AND 2-AMINO-PYRIDIN-3-YL CARBOXAMIDE DERIVATIVES AS POLO-LIKE KINASE 1 (PLK-1) INHIBITORS FOR THE TREATMENT OF CANCER

机译:3-氨基吡嗪-2-基羧酰胺和2-氨基吡啶-3-基羧酰胺衍生物作为多聚激酶1(PLK-1)抑制剂,可用于治疗癌症。

摘要

The present invention concerns 2-amino-pyridin-3-yl carboxamide and 3-amino-pyrazin-2-yl carboxamide derivatives of formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein: • A is N or C-H, • Y is 0, S or one of the following groups : sulfoxide (-S(O)-), sulfone (- S(0)2-) or N (R3) with R3being H, or an optionally substituted alkyl, acyl, alkenyl, alkynyl, cycloalkyl, aralkyl, aryl or heteroaryl, • R1 is H or an optionally substituted alkyl, acyl, alkenyl, alkynyl, cycloalkyl, aralkyl, aryl or heteroaryl, or when Y is NR3, R1 and R3 are together included into an optionally substituted 4 to 7-membered heterocycle or 8 to 10-membered heterobicycle, and • R2 is any of the optionally substituted following groups: alkyl, acyl, alkenyl, alkynyl, cycloalkyl, aralkyl, aryl, heteroaryl-alkyl or heteroaryl; for use as polo-like kinase 2 inhibitors for the treatment of cancer; as well as pharmaceutical compositions containing such a compound and processes to prepare such a compound.
机译:本发明涉及式(I)的2-氨基-吡啶-3-基羧酰胺和3-氨基-吡嗪-2-基羧酰胺衍生物:(I)或其药学上可接受的盐,其中:•A是N或CH ,•Y为0,S或以下基团之一:亚砜(-S(O)-),砜(-S(0) 2 -)或N(R 3 < / Sub>),其中R 3 为H,或可选取代的烷基,酰基,烯基,炔基,环烷基,芳烷基,芳基或杂芳基,•R 1 为H或可选取代的烷基,酰基,烯基,炔基,环烷基,芳烷基,芳基或杂芳基,或者当Y为NR 3 ,R 1 和R 3 一起包含在一个可选取代的4至7元杂环或8至10个杂环中,并且•R 2 是任意可选取代的以下基团:烷基,酰基,烯基,炔基,环烷基,芳烷基,芳基,杂芳基-烷基或杂芳基;用作polo样激酶2抑制剂来治疗癌症;以及含有这种化合物的药物组合物和制备这种化合物的方法。

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