Melanocortin receptor antagonist compounds, process for preparing them and use thereof in human medicine and cosmetics

Abstract

The present invention relates to novel melanocortin receptor antagonist compounds corresponding to the general formula (I) below: to compositions containing them, to the process for preparing them and to their use in pharmaceutical or cosmetic compositions.

1 . A compound of formula (I): 
       
         
           
           
               
               
           
         
         in which: 
         R1 represents a hydrogen atom, an aryl, a substituted aryl, an alkyl, a cycloalkyl or a cycloalkylalkyl, 
         R2 represents a hydrogen atom, a hydroxyl or a lower alkyl, a substituted lower alkyl, a higher alkyl, a substituted higher alkyl, a cycloalkyl, a cycloalkylalkyl, a lower alkoxy, a substituted lower alkoxy, a higher alkoxy, a substituted higher alkoxy, a cycloalkylalkoxy, an acyloxy, an acyl, an alkoxycarbonyl, a carboxamide, a carboxylic acid, a cyano or an amino disubstituted with an acyl and an aryl or alkyl, 
         R3 represents an aralkyl or a substituted aralkyl, 
         R4 represents a heteroaralkyl or a substituted heteroaralkyl, 
         R5 represents a hydrogen atom or an alkyl, 
         X represents an oxygen atom or a sulfur atom, 
         n, m may be equal to 1 or 2; 
         or a corresponding salt or enantiomer, having antagonist activity with respect to the MC4R receptor. 
       
     
     
         2 .- 4 . (canceled) 
     
     
         5 . A method for treating a patient in need thereof for a pathology selected from the group consisting of:
 a weight regulation (homeostasis) and disorder related to weight loss (including involuntary weight loss) or weight gain, such as anorexia, obesity, cachexia and related indications, for instance sarcopenia, catabolic diseases, cachexia related to cancer, chronic pulmonary diseases (COPD), cardiac insufficiency, hepatic insufficiency, renal insufficiency, an infectious disease or an autoimmune disease,   a regulating food intake and eating disorder, and   a bone pathology the method comprising administering to the patient in need thereof an effective amount of any compound according to  claim 1 .   
     
     
         6 .- 7 . (canceled)