Heterocyclic compound and use thereof

Abstract

Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.

1 . A compound represented by the formula (I): 
       
         
           
           
               
               
           
         
       
       wherein
 R 1  is a C 1-6  alkyl group; 
 R 2  is a group represented by the formula: —CO—NR′R″ wherein R′ and R″ form, to ether with the nitrogen atom bonded thereto, a nitrogen-containing heterocycle; 
 X is a C 1-6  alkyl group optionally substituted by 1 to 3 substituents selected from the group consisting of
 (a) C 1-6  alkoxy group optionally having a C 1-6  alkoxy group, and 
 (b) an aryloxy group; and 
 
 ring A is
 (1) triazole optionally further having substituent(s) selected from a C 6-10  aryl group optionally having halogen atom(s), 
 (2) imidazo[1,2-a]pyridine, or 
 (3) benzimidazole further having substituent(s) selected from the group consisting of a halogen atom and a C 1-6  alkoxy group, 
 
 
       or a salt thereof. 
     
     
         2 . A compound represented by the formula (II): 
       
         
           
           
               
               
           
         
       
       wherein
 R 1  is a C 1-6  alkyl group; 
 R 3  is a C 1-6  alkoxy group optionally substituted by a C 1-6  alkoxy group; 
 X is a C 1-6  alkylene group; 
 ring A 1  is
 (1) triazole optionally further having substituent(s) selected from a C 6-10  aryl group optionally having halogen atom(s), 
 (2) imidazo[1,2-a]pyridine, or 
 (3) benzimidazole further having substituent(s) selected from the group consisting of a halogen atom and a C 1-6  alkoxy group; and 
 
 the group represented by the formula: 
 
       
         
           
           
               
               
           
         
       
       is a group represented by the formula: 
       
         
           
           
               
               
           
         
       
       wherein R 4  is a group represented by the formula: —CO—NR′R″ wherein R′ and R″ from, together with the nitrogen atom bonded thereto, a nitrogen-containing heterocycle, or a salt thereof. 
     
     
         3 - 4 . (canceled) 
     
     
         5 . The compound of  claim 1 , wherein ring A is a ring represented by the formula: 
       
         
           
           
               
               
           
         
       
       wherein R a  and R b  are each independently a hydrogen atom, a halogen atom, or a C 1-6  alkoxy group, and at least one of R a  and R b  is not a hydrogen atom; and
 Y 1  is N, and Y 2  is CH. 
 
     
     
         6 . The compound of  claim 2 , wherein ring A 1  is a ring represented by the formula: 
       
         
           
           
               
               
           
         
       
       wherein R a  and R b  are each independently a hydrogen atom, a halogen atom, or a C 1-6  alkoxy group, and at least one of R a  and R b  is not a hydrogen atom; and
 Y is N, and Y 2  is CH. 
 
     
     
         7 . (canceled) 
     
     
         8 . The compound of  claim 2 , wherein the group represented by the formula: 
       
         
           
           
               
               
           
         
       
       is a group represented by the formula: 
       
         
           
           
               
               
           
         
       
       wherein R 4  is a group represented by the formula: —CO—NR′R″ wherein R′ and R″ form, together with the nitrogen atom bonded thereto, a nitrogen-containing heterocycle. 
     
     
         9 - 20 . (canceled) 
     
     
         21 . 1-(2-Fluorophenyl)-5-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-1,2,3-triazole-4-carboxamide or a salt thereof. 
     
     
         22 - 31 . (canceled)