US2008200465A1PendingUtilityA1

Antipathogenic benzamide compounds

66
Assignee: GENESOFT PHARMACEUTICALS INCPriority: Jun 13, 2001Filed: Jan 25, 2008Published: Aug 21, 2008
Est. expiryJun 13, 2021(expired)· nominal 20-yr term from priority
C07D 401/12C07D 401/14C07D 403/14A61P 31/04C07D 403/04C07D 413/14C07D 207/42C07D 409/04A61P 33/02C07D 409/14C07D 417/14A61P 31/12C07D 217/26C07D 417/04
66
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Claims

Abstract

The present invention is related to methods of treating viral and protozoan infections in mammals using antipathogenic benzamide compounds having the formula wherein at least one of the R 1 groups is F, Cl, CN or CF 3 and R 2 , R 3 , Y, Z, m, and n are as defined herein.

Claims

exact text as granted — not AI-modified
1 - 28 . (canceled) 
     
     
         29 . A method of treating a viral infection in a mammal, comprising administering to a patient in need of such treatment an effective amount of a compound having the formula 
       
         
           
           
               
               
           
         
         wherein i is 3; 
         one of X 1 , X 2 , and X 3  is a ring vertex selected from the group consisting of —O—, —S—, and —NR 2 —, and the other two of X 1 , X 2 , and X 3  are ring vertices selected from the group consisting of ═N— and ═CR 4 —, wherein each moiety 
       
       
         
           
           
               
               
           
         
          is the same or different and at least one moiety is other than 
       
       
         
           
           
               
               
           
         
         each R 1  is independently H, F, Cl, CN, CF 3 , OH, N(R 2 ) 2 , OR 2  or a substituted or unsubstituted (C 1 -C 12 )alkyl group, with the proviso that at least one R 1  is F, Cl, CN or CF 3 ; 
         each R 2  and R 3  is independently H or a substituted or unsubstituted (C 1 -C 12 )alkyl group; 
         each R 4  is independently H, F, Cl, Br, I, CN, OH, NO 2 , NH 2 , or a substituted or unsubstituted (C 1 -C 12 )alkyl group; 
         Z(R 2 ) n  is 
       
       
         
           
           
               
               
           
         
         r is an integer ranging from 2 to 8, inclusive; 
         each R 25  is independently selected from the group consisting of H, CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , or CH(CH 3 ) 2 ; 
         said compound having at least one basic group having a pK b  of 12 or less or a quaternized nitrogen group. 
       
     
     
         30 . A method according to  claim 29 , wherein 
       
         
           
           
               
               
           
         
       
       is selected from the group consisting of 
       
         
           
           
               
               
           
         
       
     
     
         31 . A method according to  claim 29 , wherein the moiety 
       
         
           
           
               
               
           
         
       
       which is other than 
       
         
           
           
               
               
           
         
       
       is selected from the group consisting of 
       
         
           
           
               
               
           
         
       
     
     
         32 . A method according to  claim 29 , wherein each R 1  is independently H, F or Cl;
 i is 3;   two of said moiety   
       
         
           
           
               
               
           
         
       
     
     
         33 . A method according to  claim 29 , wherein the compound has the formula: 
       
         
           
           
               
               
           
         
       
     
     
         34 . A method of treating a protozoan infection in a mammal, comprising administering to a patient in need of such treatment an effective amount of a compound having the formula 
       
         
           
           
               
               
           
         
         wherein i is 3; 
         one of X 1 , X 2 , and X 3  is a ring vertex selected from the group consisting of —O—, —S—, and —NR 2 —, and the other two of X 1 , X 2 , and X 3  are ring vertices selected from the group consisting of ═N— and ═CR 4 —, wherein each moiety 
       
       
         
           
           
               
               
           
         
          is the same or different and at least one moiety is other than 
       
       
         
           
           
               
               
           
         
         each R 1  is independently H, F, Cl, CN, CF 3 , OH, N(R 2 ) 2 , OR 2  or a substituted or unsubstituted (C 1 -C 12 )alkyl group, with the proviso that at least one R 1  is F, Cl, CN or CF 3 ; 
         each R 2  and R 3  is independently H or a substituted or unsubstituted (C 1 -C 12 )alkyl group; 
         each R 4  is independently H, F, Cl, Br, I, CN, OH, NO 2 , NH 2 , or a substituted or unsubstituted (C 1 -C 12 )alkyl group; 
         Z(R 2 ) n  is 
       
       
         
           
           
               
               
           
         
         r is an integer ranging from 2 to 8, inclusive; 
         each R 25  is independently selected from the group consisting of H, CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , or CH(CH 3 ) 2 ; 
       
       said compound having at least one basic group having a pK b  of 12 or less or a quaternized nitrogen group. 
     
     
         35 . A method according to  claim 34 , wherein 
       
         
           
           
               
               
           
         
       
       is selected from the group consisting of 
       
         
           
           
               
               
           
         
       
     
     
         36 . A method according to  claim 34 , wherein the moiety 
       
         
           
           
               
               
           
         
       
       which is other than 
       
         
           
           
               
               
           
         
         is selected from the group consisting of 
       
       
         
           
           
               
               
           
         
       
     
     
         37 . A method according to  claim 34 , wherein each R 1  is independently H, F or Cl;
 i is 3;   two of said moiety   
       
         
           
           
               
               
           
         
       
     
     
         38 . A method according to  claim 34 , wherein the compound has the formula:

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