Compounds for treatment of pain

Abstract

The aspects of the disclosed embodiments are directed to novel compounds, formulations containing said compounds or pharmaceutically acceptable salts thereof which are suitable for administration to a patient.

1 . A compound of the formula 
       
         
           
           
               
               
           
         
       
       wherein R 1  is CHR 4 O(C═O)OR 5 , CHR 4 O(C═O)R 6 , CHR 4 O(C═O)NR 6 R 7 , CHR 4 O(C═O)CHR 8 NR 6 R 7 , CHR 4 O(C═O)CHR 8 NH(COCHR 8 NH) n H, CHR 4 R 9 , CHR 4 O(C═O)CR 5 R 6 OR 7 , CHR 4 O(C═O)O(CH 2 ) n NR 5 R 6 , CHR 4 O(C═O)O(CH 2 ) n CO 2 R 5 , CHR 4 O(C═O)(CH 2 ) n NR 5 R 6 , CHR 4 O(C═O)(CH 2 ) n CO 2 R 5 , 
       
         
           
           
               
               
           
         
         R 2  is H; 
         R 3  is H, CH 3 , or (C═O)CH 3 ; 
         R 4  is H or optionally substituted alkyl; wherein said substituents are independently selected from the group OR 3  and (C═O)OR 5 ; 
         R 5  is optionally substituted alkyl, cycloalkyl, phenylalkyl, heteroalkyl, heterocycloalkyl, aryl, or heteroaryl; wherein said substituents are independently (CH 2 ) n CO 2 alkyl; 
         R 6  is H or R 5 ; 
         R 7  is H or R 5 ; 
         R 8  is H or R 5 ; 
         R 9  is 4-isoxazoyl; 
         wherein each n is independently an integer from 1-12; and 
         A is an anion selected from the group consisting of: Br − , Cl − , I − , R 7 CO 2   − , H 2 PO 4   − , NO 3   − , Etodolate, Mefenamate, Urosodeoxycholate and R 6 SO 3 . 
       
     
     
         2 . A compound according to  claim 1  wherein R 1  is CHR 4 O(C═O)OR 5 . 
     
     
         3 . A compound according to  claim 1  wherein R 1  is CHR 4 O(C═O)R 6 . 
     
     
         4 - 16 . (canceled) 
     
     
         17 . A compound according to  claim 1  wherein R 3  is H. 
     
     
         18 . A compound according to  claim 1  wherein R 3  is Methyl. 
     
     
         19 . (canceled) 
     
     
         20 . A compound according to  claim 1  wherein R 4  is H. 
     
     
         21 . (canceled) 
     
     
         22 . (canceled) 
     
     
         23 . A compound according to  claim 1  wherein R 5  is alkyl selected from methyl, ethyl, isopropyl, n-butyl, or n-pentyl. 
     
     
         24 . (canceled) 
     
     
         25 . A compound according to  claim 1  wherein R 5  is cyclohexyl. 
     
     
         26 . (canceled) 
     
     
         27 . A compound according to  claim 1  wherein R 6  is H. 
     
     
         28 . A compound according to  claim 1  wherein R 6  is methyl. 
     
     
         29 . A compound according to  claim 1  wherein R 6  is cyclohexyl. 
     
     
         30 . A compound according to  claim 1  wherein R 6  is t-butyl. 
     
     
         31 . A compound according to  claim 1  wherein R 6  is i-propyl. 
     
     
         32 . (canceled) 
     
     
         33 . (canceled) 
     
     
         34 . (canceled) 
     
     
         35 . A compound according to  claim 1  wherein A is Br − . 
     
     
         36 . A compound according to  claim 1  wherein A is Cl − . 
     
     
         37 . A compound according to  claim 1  wherein A is I − . 
     
     
         38 - 45 . (canceled) 
     
     
         46 . A composition according to  claim 1  wherein said composition is in tablet, capsule, oral solution, or oral suspension dosage form. 
     
     
         47 - 52 . (canceled)