US2016206680A1PendingUtilityA1

Anti-trypanosome compounds and treatments

47
Assignee: LININGTON ROGERPriority: Mar 20, 2009Filed: Mar 16, 2016Published: Jul 21, 2016
Est. expiryMar 20, 2029(~2.7 yrs left)· nominal 20-yr term from priority
A61K 38/08A61P 33/02A61K 31/185C07K 7/06A61K 31/155A61K 38/00A61K 31/555Y02A50/30A61P 33/00
47
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Claims

Abstract

A novel structural class of highly N-methylated linear lipopeptide compounds useful for the treatment of parasitic disease.

Claims

exact text as granted — not AI-modified
1 - 13 . (canceled) 
     
     
         14 . A method for affecting the physiology of a trypanosome, the method comprising exposing the pathogen to an almiramide compound, the almiramide compound comprising a linear lipopeptide having the following structure 
       
         
           
           
               
               
           
         
         but specifically excluding compounds (1), (2) and (3) 
         wherein for (1), R 1  consists of 
       
       
         
           
           
               
               
           
         
       
       R 2  consists of Me, R 3  consists of H, and R 4  consists of NH2;
 and wherein for (2), R 1  consists of 
 
       
         
           
           
               
               
           
         
       
       R 2  consists of Me, R 3  consists of H, and R 4  consists of NH2;
 and wherein for (3), R 1  consists of 
 
       
         
           
           
               
               
           
         
       
       R 2  consists of Me, R 3  consists of H, and R 4  consists of NH2. 
     
     
         15 . The method of  claim 14  wherein R 1  is selected from one of the following moieties: 
       
         
           
           
               
               
           
         
         and wherein R 2  is selected from one of the following moieties: Me or H 
         and wherein R 3  is selected from one of the following moieties: Me or H 
         and wherein R 4  is selected from one of the following moieties: NH 2 , NMe 2 , OH, OMe. 
       
     
     
         16 . The method of  claim 14  wherein the almiramide compound is selected from the group consisting of compounds 2, 3, 11, 12, 13, 14, 15 and 16 as shown below: 
       
         
           
                 
                 
                 
                 
                 
               
                     
                 
                   Compound 
                   R 1   
                   R 2   
                   R 3   
                   R 4   
                 
                     
                 
                    2 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   Me 
                   H 
                   NH 2   
                 
                     
                 
                    3 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   Me 
                   H 
                   NH 2   
                 
                     
                 
                   11 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   Me 
                   Me 
                   NH 2   
                 
                     
                 
                   12 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   Me 
                   Me 
                   NMe 2   
                 
                     
                 
                   13 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   NMe 2   
                 
                     
                 
                   14 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   NMe 2   
                 
                     
                 
                   15 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   NMe 2   
                 
                     
                 
                   16 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   NMe 2   
                 
                     
                 
             
                
                
                
               
               
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         17 - 20 . (canceled) 
     
     
         21 . The method of  claim 14  wherein the almiramide possesses anti-trypanosome properties. 
     
     
         22 . The method of  claim 21  wherein the almiramide possesses anti-pathogenic properties against  Trypanosoma gambiense.    
     
     
         23 . The method of  claim 21  wherein the almiramide possesses anti-pathogenic properties against  Trypanosoma rhodesiense.    
     
     
         24 . The method of  claim 21  wherein the almiramide possesses anti-pathogenic properties against  Trypanosoma brucei.    
     
     
         25 . The method of  claim 21  wherein the almiramide molecule is selected from the group consisting of compound 13, compound 14, and compound 16. 
     
     
         26 . The method of  claim 22  comprising additionally administering pentamidine. 
     
     
         27 . The method of  claim 23  comprising additionally administering suramin. 
     
     
         28 . The method of  claim 24  comprising additionally administering melarsoprol.

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