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 optionally 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 optionally 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 any one of  claims 1 ,  2 ,  3  and  4 , or a salt thereof, wherein R 1  is a hydroxy-protecting group. 
   
   
       6 . A benzoazepine compound according to any one of  claims 1 ,  2 ,  3  and  4 , 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 . A benzoazepine compound according to  claim 1  or a salt thereof, wherein X is an oxygen atom, R is a hydroxy group, and R 1  is a hydrogen atom. 
   
   
       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, PKD, 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.