Pharmaceutical composition for cancer immunotherapy and/or immunological activation containing diamino heterocyclic carboxamide compound as active ingredient

Abstract

[Means for Solution] The present inventors have conducted intensive studies for the purpose of creating a pharmaceutical composition for cancer immunotherapy and/or a pharmaceutical composition for immunological activation. As a result, the present inventors have found that 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide or a pharmaceutically acceptable salt thereof has an excellent immunological activation effect, and a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof as an active ingredient is expected to be used as a pharmaceutical composition for cancer immunotherapy and/or as a pharmaceutical composition for immunological activation, thereby completing the present invention.

1 - 10 . (canceled) 
     
     
         11 : A method for the treatment of cancer by immunotherapy, comprising administering, to a subject in need thereof, a therapeutically effective amount of 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide or a pharmaceutically acceptable salt thereof in combination with a monoclonal antibody inhibiting binding of PD-1 and PD-L1. 
     
     
         12 : The method according to  claim 11 , wherein said monoclonal antibody inhibiting the binding of PD-1 and PD-L1 is selected from the group consisting of nivolumab, pembrolizumab, atezolizumab, pidilizumab, avelumab, and durvalumab. 
     
     
         13 : The method according to  claim 12 , wherein said 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide or a pharmaceutically acceptable salt thereof is administered simultaneously, separately, continuously, or intermittently with said monoclonal antibody inhibiting the binding of PD-1 and PD-L1. 
     
     
         14 : The method according to  claim 11 , comprising administering 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide hemifumarate. 
     
     
         15 : The method according to  claim 12 , comprising administering 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide hemifumarate. 
     
     
         16 : The method according to  claim 13 , comprising administering 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide hemifumarate.