Use of B-Aminoalcohols in the Treatment of Inflammatory Disorders and Pain

Abstract

A compound for therapeutic use, of the formula wherein R 1 is aryl or heteroaryl optionally substituted with R 5 ; R 2 is H, alkyl or CH 2 OH or forms part of a ring with R 4 ; R 3 is H, alkyl or CH 2 OH or forms part of a ring with R 4 ; R 4 is H, alkyl or (when forming part of a ring with R 2 or R 3 ) CH 2 ; and R 5 is alkyl, CF 3 , OH, Oalkyl, OCOalkyl, CONH 2 , CN, halogen, NH 2 , NO 2 , NHCHO, NHCONH 2 , NHSO 2 Me, CONH 2 , or SOMe; or a salt thereof.

1 . A compound of formula (I) 
       
         
           
           
               
               
           
         
         wherein R 1  is aryl or heteroaryl optionally substituted with R 5 ; 
         R 2  is H, alkyl or CH 2 OH or forms part of a ring with R 4 ; 
         R 3  is H, alkyl or CH 2 OH or forms part of a ring with R 4 ; 
         R 4  is H, alkyl or (when forming part of a ring with R 2  or R 3 ) CH 2 ; and 
         R 5  is alkyl, CF 3 , OH, Oalkyl, OCOalkyl, CONH 2 , CN, halogen, NH 2 , NO 2 , NHCHO, NHCONH 2 , NHSO 2 Me, CONH 2  or SOMe; 
         or a salt thereof. 
       
     
     
         2 . The compound according to  claim 1 , which is α-[(1,1-dimethyl-2-hydroxyethyl)amino]-4-amino-3,5-dichloroacetophenone. 
     
     
         3 . A pharmaceutical composition comprising a compound according to  claim 1  and a carrier or diluent. 
     
     
         4 . A method of treating an inflammatory condition or a pain condition, the method comprising the step of administering to an individual in need thereof a pharmaceutical composition as defined in  claim 3 . 
     
     
         5 . The method according to  claim 4 , wherein the inflammatory condition is a chronic degenerative disease. 
     
     
         6 . The method according to  claim 4 , wherein the inflammatory condition is a chronic demyelinating disease. 
     
     
         7 . The method according to  claim 4 , wherein the inflammatory condition is a respiratory disease. 
     
     
         8 . The method according to  claim 4 , wherein the inflammatory condition is an inflammatory bowel disease (IBD). 
     
     
         9 . The method according to  claim 4 , wherein the inflammatory condition is a dermatological condition. 
     
     
         10 . The method according to  claim 4 , wherein the inflammatory condition is a dental disease such as periodontal disease or gingivitis. 
     
     
         11 . The method according to  claim 4 , wherein the inflammatory condition is diabetic nephropathy, lupus nephritis, IgA nephropathy, or glomerulonephritis. 
     
     
         12 . The method according to  claim 4 , wherein the inflammatory condition is systemic lupus erythematosus. 
     
     
         13 . The method according to  claim 4 , wherein the inflammatory condition is graft vs host disease. 
     
     
         14 . The method according to  claim 4 , wherein the condition is an ophthalmic condition. 
     
     
         15 . The method according to  claim 4 , wherein the pain condition is a chronic pain or an acute pain. 
     
     
         16 . The method according to  claim 4 , wherein the pain condition is neuropathic pain. 
     
     
         17 . The method according to  claim 4 , wherein the individual is also administered another therapeutic agent selected from 
     
     
         18 . The method according to  claim 4 , wherein the individual is also administered an additional therapeutic agent, the additional therapeutic agent includes a corticosteroid, a cytotoxic, an antibiotic, an immunosupressant, a non-steroidal anti-inflammatory drug, a narcotic analgesic, a local anaesthetic, an NMDA antagonist, a neuroleptic, an anti-convulsant, an anti-spasmodic, an anti-depressant, or a muscle relaxant. 
     
     
         19 . The method according to  claim 18 , wherein the compound and the additional therapeutic agent are provided in combination.