The present disclosure novel pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.本公開涉及靶向腺苷受體(尤其A1和A2,特別地,A2a)的新穎吡化合物。本公開還涉及包含所述化合物中的一種或多種作為活性成分的藥物組合物,和所述化合物在治療腺苷受體(AR)相關疾病,例如如NSCLC、RCC、前列腺癌和乳腺癌的癌症中的用途。