US2002151552A1PendingUtilityA1

Novel compounds

Priority: Dec 22, 2000Filed: Dec 17, 2001Published: Oct 17, 2002
Est. expiryDec 22, 2020(expired)· nominal 20-yr term from priority
Inventors:Adnan Badwan
C07D 405/12C07D 295/13A61K 31/495C07D 295/26C07D 239/04C07D 211/96C07D 295/30
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Claims

Abstract

The compounds of the formulas described herein, wherein X, R 0 , R 1 , R 2 , n and m have the meanings given in the specification, are useful as active ingredients in pharmaceutical compositions. The invention relates to the use of said compounds as a medicament and for the manufacture of a medicament for the treatment of erectile dysfunction.

Claims

exact text as granted — not AI-modified
1 . A compound having the general formula (I):  
       
         
           
           
               
               
           
         
       
       wherein 
 X is chosen from N and C;  
 R 0  is chosen from H, a lower alkyl group, a lower O-alkyl group, a lower aldehyde group, a benzyl group, a phenyl group, a phenyl group substituted with halogen or O-alkyl, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl, and a furyl group;  
 R 1  and R 2  are, independently, chosen from H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group and a lower N-alkyl group, or R 1  and R 2  taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are chosen from O, S and N, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N;  
 n is 0,1,2,3 or 4;  
 m is 0 or 1;  
 and pharmaceutically acceptable salts thereof;  
 with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.  
 
     
     
         2 . A compound according to  claim 1 , wherein X is N.  
     
     
         3 . A compound according to  claim 1  or  2 , wherein R 0  is chosen from H, methyl, methoxy and ethoxy.  
     
     
         4 . A compound according to any one of claims  1 - 3 , wherein R 1  and R 2  are, independently, chosen from H, methyl, methoxy and ethoxy, or R 1  and R 2  taken together with the carbon atoms to which they are attached form a five-membered ring, wherein R 1  and R 2  are O.  
     
     
         5 . A compound according to  claim 1 , wherein said compound is:  
       
         
           
           
               
               
           
         
       
     
     
         6 . A compound according to any one of claims  1 - 5 , for use as a medicament.  
     
     
         7 . A pharmaceutical composition comprising a compound according to any one of claims  1 - 5  as active ingredient together with a pharmaceutically acceptable adjuvant, diluent, excepient or carrier.  
     
     
         8 . Use of a compound of the general formula (I)  
       
         
           
           
               
               
           
         
       
       wherein 
 X is chosen from N and C;  
 R 0  is chosen from H, a lower alkyl group, a lower O-alkyl group, a lower aldehyde group, a benzyl group, a phenyl group, a phenyl group substituted with halogen or O-alkyl, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl, and a furyl group;  
 R 1  and R 2  are, independently, chosen from H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group and a lower N-alkyl group, or R 1  and R 2  taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are chosen from O, S and N and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N;  
 n is 0,1,2,3 or 4;  
 m is 0 or 1;  
 and pharmaceutically acceptable salts thereof, as a selective PDES-inhibitor for the manufacture of a medicament for the treatment of erectile dysfunction.  
 
     
     
         9 . A method for treatment of erectile dysfunction, comprising administering a therapeutically effective amount of a compound according to any one of claims  1 - 5  to an animal or human.

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