Pharmaceutical composition promoting defecation

Abstract

The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A 2 receptor antagonism, preferably an adenosine A 2b receptor antagonism, or a salt thereof.

1 . A defecation-promoting agent comprising a compound having an adenosine A 2  receptor antagonism or a salt thereof.  
   
   
       2 . A compound represented by the formula:  
     
       
         
         
             
             
         
       
       wherein  
       A represents a phenyl group, pyridyl group, thienyl group or furyl group which may be substituted with one or two groups selected from a halogen atom, a hydroxyl group, a 
 C 1-6 alkyl group, a C 1-6 alkoxy group and a C 1-6 alkoxy-carbonyl group;  
 
       B may be substituted with one or more groups selected from a halogen atom, hydroxyl group, a C 1-6  alkyl group and amino group;  
       R 1  represents a hydrogen atom, a morpholinyl group or a group represented by the formula —NR 1a R 1b , wherein R 1a  and R 1b  are the same as or different from each other and each represents a hydrogen atom, a C 1-6  alkyl group, a C 1-6  acyl group, a phenyl group or a 
 C 1-6  alkylsulfonyl group; and  
 
       R 2  represents a hydrogen atom or a group represented by the formula —NR 2a R 2b , wherein R 2a  and R 2b  are the same as or different from each other and each represents a hydrogen atom or a C 16  alkyl group,  
       provided that, in the above definition, the cases 
 (i) where, A is a 4-fluorophenyl group; B is a 4-pyridyl group; R 1  is an amino group; and R 2  is a hydrogen atom, and  
 (ii) where, A is a 4-fluorophenyl group; B is a 4-pyridyl group, R 1  is an acetamide group; and R 2  is a hydrogen atom  
 
       are excluded,  
       or a salt thereof.  
     
   
   
       3 . A pharmaceutical composition comprising a pharmacologically effective amount of the compound according to  claim 2 , or a pharmacologically acceptable salt of thereof and a pharmaceutically acceptable carrier.  
   
   
       4 . A method for promotion of defecation, by administering a pharmacologically effective amount of the compound described in  claim 2  or a salt thereof to a patient.  
   
   
       5 . A method for treating or improving constipation, by administering a pharmacologically effective amount of the compound described in  claim 2  or a salt thereof to a patient.  
   
   
       6 . The method according to  claim 3 , wherein the patient is suffering from a disease selected from the group consisting of constipation, functional constipation, spastic constipation, atonic constipation, irritable bowel syndrome, constipation accompanying irritable bowel syndrome, organic constipation, constipation accompanying enteroparalytic ileus, constipation accompanying congenital digestive tract dysfunction and constipation accompanying ileus, or combinations thereof.  
   
   
       7 . The method according to  claim 4 , wherein the patient is suffering from a disease selected from the group consisting of constipation, functional constipation, spastic constipation, atonic constipation, irritable bowel syndrome, constipation accompanying irritable bowel syndrome, organic constipation, constipation accompanying enteroparalytic ileus, constipation accompanying congenital digestive tract dysfunction and constipation accompanying ileus, or combinations thereof.