Novel compounds

Abstract

Compounds of general formula (I), wherein R 1 is selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl and triazolyl; where each R 1 phenyl ring and R 1 heteroaromatic ring optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C 1 -C 6 alkyl, NO 2 , CF 3 , C 1 -C 6 alkoxy, chloro, fluoro, bromo, and iodo.

1 . A compound according to formula I  
       
         
           
           
               
               
           
         
       
       wherein 
 R 1  is selected from  
 (i) phenyl;  
 (ii) pyrdinyl  
                     
 (iii) thiophenyl  
                     
 (iv) furanyl  
                     
 (v) imidazolyl  
                     
 (vi) triazolyl  
                     
 where each R 1  phenyl ring and R 1  heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C 1 -C 6  alkyl, NO 2 , CF 3 , C 1 -C 6  alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems;  
 as well as pharmaceutically acceptable salts and isomers thereof.  
 
     
     
         2 . A compound according to  claim 1 , wherein the optional substituent(s) on the aromatic or the heteroaromatic ring(s) is selected from anyone of NO 2 , iso-butyl, CF 3 , methoxy, methyl, or chloro.  
     
     
         3 . A compound according to  claim 1  or  2 , selected from any one of 
 4-[(4-benzyl-1-piperazinyl)(2,2-dimethyl-2,3-dihydro-1-benzofuran-7-yl)methyl]-N,N-diethylbenzamide dihydrochloride (compound 6);  
 4-{(2,2-dimethyl-2,3-dihydro-1-benzofuran-7-yl)[4-(4-iodobenzyl)-1-piperazinyl]methyl}-N,N-diethylbenzamide dihydrochloride (compound 7);  
 4-{(2,2-dimethyl-2,3-dihydro-1-benzofuran-7-yl)[4-(3-pyridinylmethyl)-1-piperazinyl]methyl}-N,N-diethylbenzamide dihydrochloride (compound 8); and  
 4-{(2,2-dimethyl-2,3-dihydro-1-benzofuran-7-yl)[4-(2-pyridinylmethyl)-1-piperazinyl]methyl}-N,N-diethylbenzamide ditrifuroacetae (compound 9).  
 
     
     
         4 . A compound according to any one of claims  1 - 3 , which compound is present as the (+)-enantiomer.  
     
     
         5 . A compound according to anyone of claims  1 - 3 , which compound is present as the (−)-enantiomer.  
     
     
         6 . A compound according to any of the preceding claims, in form of its hydrochloride, sulfate, tartrate or citrate salts.  
     
     
         7 . A compound according to any of claims  1 - 6  for use in therapy.  
     
     
         8 . A compound according to  claim 7 , wherein the therapy is pain management.  
     
     
         9 . A compound according to  claim 7 , wherein the therapy is directed towards gastrointestinal disorders.  
     
     
         10 . A compound according to  claim 7 , wherein the therapy is directed towards spinal injuries.  
     
     
         11 . A compound according to  claim 7 , wherein the therapy is directed to disorders of the sympathetic nervous system.  
     
     
         12 . Use of a compound according to formula I of  claim 1  for the manufacture of a medicament for use in the treatment of pain.  
     
     
         13 . Use of a compound according to formula I of  claim 1  for the manufacture of a medicament for use in the treatment of gastrointestinal disorders.  
     
     
         14 . Use of a compound according to formula I of  claim 1  for the manufacture of a medicament for use in the treatment of spinal injuries.  
     
     
         15 . A pharmaceutical composition comprising a compound of the formula I according to  claim 1  as an active ingredient, together with a pharmacologically and pharmaceutically acceptable carrier.  
     
     
         16 . A method for the treatment of pain, whereby an effective amount of a compound of the formula I according to  claim 1  is administered to a subject in need of pain management.  
     
     
         17 . A method for the treatment of gastrointestinal disorders, whereby an effective amount of a compound of the formula I according to  claim 1 , is administered to a subject suffering from said gastrointestinal disorder.  
     
     
         18 . A method for the treatment of spinal injuries, whereby an effective amount of a compound of the formula I according to  claim 1 , is administered to a subject suffering from said spinal injury.