US2015191451A1PendingUtilityA1

4-(azacycloalkyl)benzene-1,3-diol compounds as tyrosinase inhibitors, process for the preparation thereof and use thereof in human medicine and in cosmetics

Assignee: GALDERMA RES & DEVPriority: Dec 2, 2008Filed: Mar 17, 2015Published: Jul 9, 2015
Est. expiryDec 2, 2028(~2.3 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 37/08C07D 211/60C07D 207/16C07D 211/22C07D 207/08C07D 205/04A61P 17/02C07D 401/12A61K 9/06C07D 211/26A61K 31/397A61P 17/00
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Claims

Abstract

4-(Azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical or cosmetic composition comprising a compound of formula (I) below: 
       
         
           
           
               
               
           
         
         in which: 
         R1 represents:
 a C 1 -C 5  alkyl radical, 
 a C 3 -C 6  cycloalkyl radical, 
 an aryl radical, 
 a substituted aryl radical, 
 an aralkyl radical, 
 a C 1 -C 5  alkoxy radical, 
 an amino radical corresponding to structure (a): 
 
       
       
         
           
           
               
               
           
         
         
           
             in which R2 represents:
 a hydrogen, 
 a C 1 -C 5  alkyl radical, 
 a C 3 -C 6  cycloalkyl radical, 
 an aryl radical, 
 a substituted aryl radical, 
 a pyridyl radical, 
 an aralkyl radical, 
 a radical corresponding to structure (b): 
 
           
         
       
       
         
           
           
               
               
           
         
         
           
             in which p can have the value 1 or 2, 
             a radical corresponding to structure (c): 
           
         
       
       
         
           
           
               
               
           
         
         
           
             in which R4 represents:
 a carboxymethyl —COOCH 3  or carboxyethyl —COOEt radical, 
 a C 1 -C 3  alkyl radical, 
 a hydrogen, 
 
             and R5 represents:
 a substituted or unsubstituted aryl radical, 
 a C 3 -C 6  cycloalkyl radical, 
 a pyridyl, 
 
           
           and R3 represents:
 a hydrogen, 
 a C 1 -C 5  alkyl radical; 
 
         
         or R1 may also represent a radical corresponding to formula (d): 
       
       
         
           
           
               
               
           
         
         
           in which R6 represents:
 a hydrogen, 
 a C 1 -C 5  alkyl radical, 
 a C 3 -C 6  cycloalkyl radical, 
 an aryl radical, 
 a substituted aryl radical, 
 a pyridyl radical, 
 an aralkyl radical, 
 
           R7 represents:
 a hydrogen, 
 a C 1 -C 5  alkyl radical, 
 
           and R8 represents:
 a hydrogen, 
 a hydroxyl, 
 an amino radical, 
 a C 1 -C 3  alkoxy radical; 
 
         
         Y represents a hydrogen or a fluorine, and 
         m and n can have the value 0, 1 or 2, 
         or a salt of a compound of formula (I), or an enantiomer form thereof; 
         and a pharmaceutically acceptable or cosmetically acceptable carrier. 
       
     
     
         2 .- 23 . (canceled)

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