Thiadiazoline derivative

Abstract

(wherein R 1 and R 4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R 5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R 2 represents —C(═W)R 6 or the like; R 3 represents a hydrogen atom, —C(═W A )R 6A , or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.

1 . A compound of formula  
       
         
           
           
               
               
           
         
       
       wherein 
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —OCH 3  and R 4A  is —H 2 NHSO 2 CH 3 ;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COCH 3  and R 4A  is —CH 2 NHSO 2 CH 2 Cl;  
 R 2A  is —COCH 3 , R 3A  is —COCH 3  and R 4A  is —CH 2 NHSO 2 CH 2 Cl;  
 R 2A  is—COC(CH 3 ) 3 , R 3A  is —COCH 3  and R 4A  is —CH 2 NHSO 2 CH═CH 2 ;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COC(CH 3 ) 3  and R 4A  is —CH 2 NHSO 2 CH═CH 2 ;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COCH 3  and R 4A  is  
                     
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COCH 3  and R 4A  is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COCH 3  and R 4A  is —CH 2 NHSO 2 (CH 2 ) 2 N(CH 3 ) 2 ;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COCH 3  and R 4A  is —CH 2 NHSO 2 (CH 2 ) 2 NH(CH 2 ) 2 0H;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COC(CH 3 ) 3  and R 4A  is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COC(CH 3 ) 3  and R 4A  is —CH 2 NHSO 2 (CH 2 ) 2 N(CH 3 ) 2 ;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COCH(CH 3 ) 2  and R 4A  is —CH 2 ) 2  NHSO 2 CH 3 ;  
 R 2A  is —COCH 2 CH 3 , R 3A  is —COCH 2 CH3 and R 4A  is —CH( 2 ) 2 NHSO 2 CH 3 ; or  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COCH 2 CH 3  and R 4A  is —CH 2 ) 2 NHSO 2 CH 3 ;  
 or a pharmacologically acceptable salt thereof.  
 
     
     
         2 . A compound according to  claim 1  of formula  
       
         
           
           
               
               
           
         
       
       wherein 
 R 2A  is —COC(CH 3 ) 3 , R 3 A is —COCH 3  and R 4A  is —CH 2 NHSO 2 CH═CH 2 ;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COC(CH 3 ) 3  and R 4A  is —CH 2 NHSO 2 CH═CH 2 ;  
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COCH3 and R 4A  is —CH 2 NHSO 2 (CH( 2 ) 2 NHCH 2 CH 3 ; 
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COC(CH 3 ) 3  and R 4A  is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ; or  
 
 R 2A  is —OC(CH 3 ) 3 , R 3A  is —COCH(CH 3 ) 2  and R 4A  is —CH 2 ) 2 NHSO 2 CH 3 ;  
 or a pharmacologically acceptable salt thereof.  
 
     
     
         3 . A compound according to  claim 2  of formula  
       
         
           
           
               
               
           
         
       
       wherein 
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —OC(CH 3 ) 3  and R 4A  is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ;  
 or a pharmacologically acceptable salt thereof.  
 
     
     
         4 . A compound according to  claim 2  of formula  
       
         
           
           
               
               
           
         
       
       wherein 
 R 2A  is —OC(CH 3 ) 3 , R 3A  is —COCH(CH 3 ) 2  and R 4A  is —CH 2 ) 2 NHSO 2 CH 3    
 or a pharmacologically acceptable salt thereof.  
 
     
     
         5 . A pharmaceutical composition comprising a compound of formula  
       
         
           
           
               
               
           
         
       
       wherein 
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COC(CH 3 ) 3  and R 4A  is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ;  
 or a pharmacologically acceptable salt thereof.  
 
     
     
         6 . A pharmaceutical composition comprising a compound of formula  
       
         
           
           
               
               
           
         
       
       wherein 
 R 2A  is —COC(CH 3 ) 3 , R 3A  is —COCH(CH 3 ) 2  and R 4A  is —CH 2 ) 2 NHSO 2 CH 3    
 or a pharmacologically acceptable salt thereof.  
 
     
     
         7 . A method of treating a human malignant tumor in a patient in need thereof comprising administering a compound according to  claim 3 .  
     
     
         8 . A method of treating a human malignant tumor in a patient in need thereof comprising administering a compound according to  claim 4.