Water-soluble benzoazepine compound and its pharmaceutical composition

Abstract

The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R 1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

1 . A benzoazepine compound represented by general formula (1) 
       
         
           
           
               
               
           
         
       
       or a salt thereof,
 wherein R represents a hydrogen atom, a hydroxy group protected with a protecting group, a mercapto group optionally protected with a protecting group, or an amino group optionally protected with one or two protecting groups; R 1  represents a hydrogen atom or a hydroxy-protecting group; and X represents an oxygen atom or a sulfur atom. 
 
     
     
         2 . A benzoazepine compound according to  claim 1  or a salt thereof, wherein X is an oxygen atom. 
     
     
         3 . A benzoazepine compound according to  claim 1  or  2 , or a salt thereof, wherein R is a hydroxy group protected with a protecting group. 
     
     
         4 . A benzoazepine compound according to  claim 1  or  2 , or a salt thereof, wherein R is a hydrogen atom, a mercapto group optionally protected with a protecting group, or an amino group optionally protected with one or two protecting groups. 
     
     
         5 . A benzoazepine compound according to  claim 1  or  2 , or a salt thereof, wherein R 1  is a hydroxy-protecting group. 
     
     
         6 . A benzoazepine compound according to  claim 1  or  2 , or a salt thereof, wherein R 1  is a hydrogen atom. 
     
     
         7 . A benzoazepine compound according to  claim 1  or a salt thereof, wherein X is a sulfur atom. 
     
     
         8 . (canceled) 
     
     
         9 . A pharmaceutical composition comprising a benzoazepine compound of  claim 1  or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable diluent and/or carrier. 
     
     
         10 . A pharmaceutical composition according to  claim 9 , for use as a vasodilator, hypotensor, aquaretic agent, polycystic kidney disease (PKD) treatment, or platelet aggregation inhibitor. 
     
     
         11 . An aqueous solution composition comprising a benzoazepine compound of  claim 1  or a pharmaceutically acceptable salt thereof. 
     
     
         12 . An aqueous solution composition according to  claim 11 , comprising a benzoazepine compound of  claim 1  or a pharmaceutically acceptable salt thereof, together with a buffer, isotonizing agent and injection solvent, and which is in the form of an injection. 
     
     
         13 . An aqueous solution composition according to  claim 12 , further comprising a pH adjuster.