Compounds with nootropic action, their preparation, pharmaceutical compositions containing them, and use thereof

Abstract

Described herein are new bicyclic arylimidazolones having nootropic action (i.e., protecting and stimulating cerebral functions), analgesic action and anti hyperalgesic action; also described is the process for their preparation and pharmaceutical compositions comprising them, useful for the treatment of cognitive deficits, and of various types of pain.

1 .- 36 . (canceled) 
   
   
       37 . A method for the treatment of diseases requiring nootropic and/or neuroprotective, analgesic and/or antihyperanalgesic, and anti-emetic action, characterized by administering, to a patient in need thereof, an effective amount of a compound of general formula (I) 
     
       
         
         
             
             
         
       
     
     wherein:
 A is selected from the group consisting of carbocyclic aromatic groups, heterocyclic aromatic groups, and arylC 1-4 alkyl; 
 R 1  is selected from the group consisting of:
 hydrogen, 
 arylC 1-7 alkyl, optionally substituted on the aryl moiety with one or more groups chosen among hydroxy, C 1-4 alkoxy, halogen, haloC 1-4 alkyl; 
 heterocyclylC 1-7 alkyl, optionally substituted on the heterocyclyl moiety with one or more groups chosen among C 1-4 alkyl and hydroxy; and 
 C 1-7  alkyl, optionally interrupted by an oxygen or sulphur atom or optionally substituted at any position by one or more groups chosen among hydroxy, thio, amino, carboxyl, aminocarbonyl, guanidinyl. 
 
 R 2  is selected from the group consisting of hydrogen, C 1-4 alkyl, arylC 1-4 alkyl and phenyl; or else R 1  and R 2 , taken together, form a saturated carbocyclic ring containing from 3 to 8 carbon atoms; 
 R 3  is selected from the group consisting of hydrogen, C 1-4 alkyl, arylC 1-4 alkyl, CONH 2  and COOR 5  in which R 5  is selected from the group consisting of hydrogen and C 1-4 alkyl; 
 R 4  is selected from the group consisting of hydrogen, C 1-4 alkyl, aryl, arylC 1-4 alkyl and heterocyclyl; 
 n is 2, 3 or 4; 
 in the form of a racemic mixture or in the form of enantiomers, and pharmaceutically acceptable salts. 
 
   
   
       38 . The method according to  claim 37  for the treatment of learning and memory deficits, Alzheimer's disease, dementia, senile dementia, post stroke vascular type dementia, epilepsy, cerebral ischaemia, mood disorders, depression, for the treatment of conditions of chronic paid, inflammatory pain, neuropathic pain, visceral pain, and for the treatment of emesis. 
   
   
       39 . The method according to  claim 37 , wherein said compound of formula (I) is administered in association, concurrently or sequentially, with one or more other active principles.