Use of organophosphorus compounds for the therapeutic and prophylactic treatment of infections

Abstract

Use of organophosphorus compounds of general Formula (I) for the therapeutic and prophylactic treatment of infections in humans and animals caused by viruses, fungi and parasites.

1 - 11 . (canceled) 
     
     
         12 . A method of treating malaria in an individual comprising:
 administering to said individual a therapeutically effective amount of a compound or a tautomer, ester or amide of the compound, or a pharmaceutically acceptable salt of the compound, tautomer, ester or aide, wherein the compound corresponds in structure to Formula I:   
       
         
           
           
               
               
           
         
          wherein: 
         R 1  and R 2  are independently selected from the group consisting of hydrogen, substituted and unsubstituted alkyl, substituted and unsubstituted hydroxyalkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted alkinyl, substituted and unsubstituted aryl, substituted and unsubstituted acyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted aralkyl, substituted and unsubstituted heterocyclic radical, halogen, OX 1  and OX 2 ; 
         X 1  and X 2  being independently selected from the group consisting of hydrogen, substituted and unsubstituted alkyl, substituted and unsubstituted hydroxyalkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted alkinyl, substituted and unsubstituted aryl, substituted and unsubstituted acyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted aralkyl, substituted and unsubstituted heterocyclic radical; 
         A is a 3-9 carbon moiety selected from the group consisting of alkylene radical, alkenylene radical, and hydroxyalkylene radical, wherein A includes a straight chain of at least two carbon atoms between the nitrogen atom and the phosphorus atom of general formula (I); and 
         R 3  and R 4  are independently selected from the group consisting of hydrogen, substituted and unsubstituted C 1-26 -alkyl, substituted and unsubstituted hydroxy-C 1-26 -alkyl, substituted and unsubstituted aryl, substituted and unsubstituted acyl, substituted and unsubstituted aralkyl, substituted and unsubstituted C 1-26 -alkenyl, substituted and unsubstituted C 1-26 -alkinyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocyclic radical, halogen, OX 3  and OX 4 ; 
         X 3  and X 4  being independently selected from the group consisting of hydrogen, substituted and unsubstituted C 1-26 -alkyl, substituted and unsubstituted hydroxyl-C 1-26 -alkyl, substituted and unsubstituted aryl, substituted and unsubstituted acyl, substituted and unsubstituted aralkyl, substituted and unsubstituted C 1-26 -alkenyl, substituted and unsubstituted C 1-26 -alkinyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocyclic radical, silyl, a metal of the first, second or third main group of the periodic table, ammonium, substituted ammonium, ammonium salt of ethylene diamine and ammonium salt of an amino acid. 
       
     
     
         13 . A method of treating malaria according to  claim 12 , wherein:
 the infectious agent has the potential to produce a malarial infection in a human subject.   
     
     
         14 . A method of treating malaria in an individual comprising:
 administering to said individual a therapeutically effective amount of a compound or a tautomer, ester or amide of the compound, or a pharmaceutically acceptable salt of the compound, tautomer, ester or aide, wherein the compound corresponds in structure to Formula I:   
       
         
           
           
               
               
           
         
          wherein: 
         R 1  is OX 1 ; 
         R 2  is independently selected from the group consisting of hydrogen, substituted and unsubstituted alkyl, substituted and unsubstituted hydroxyalkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted alkinyl, substituted and unsubstituted aryl, substituted and unsubstituted acyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted aralkyl, substituted and unsubstituted heterocyclic radical, halogen, and OX 1  and OX 2 ; 
         X 1  and X 2  being independently selected from the group consisting of hydrogen, substituted and unsubstituted acyl, substituted and unsubstituted alkyl, substituted and unsubstituted aryl, substituted and unsubstituted aralkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocylic radical; 
         A is a 2-9 carbon moiety selected from the group consisting of alkylene radical, alkenylene radical, and hydroxyalkylene radical, and includes a straight chain of at least two carbon atoms between the nitrogen atom and the phosphorous atom of Formula (I); 
         R 3  and R 4  are independently selected from the group consisting of hydrogen, substituted and unsubstituted C 1-26 -alkyl, substituted and unsubstituted hydroxy-C 1-26 -alkyl, substituted and unsubstituted aryl, substituted and unsubstituted acyl, substituted and unsubstituted aralkyl, substituted and unsubstituted C 1-26 -alkenyl, substituted and unsubstituted C 1-26 -alkinyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocyclic radical, halogen, OX 3  and OX 4 ; 
         X 3  and X 4  being independently selected from the group consisting of hydrogen, substituted and unsubstituted C 1-26 -alkyl, substituted and unsubstituted hydroxyl-C 1-26 -alkyl, substituted and unsubstituted aryl, substituted and unsubstituted acyl, substituted and unsubstituted aralkyl, substituted and unsubstituted C 1-26 -alkenyl, substituted and unsubstituted C 1-26 -alkinyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocyclic radical, silyl, a metal of the first, second or third main group of the periodic table, ammonium, substituted ammonium, ammonium salt of ethylene diamine and ammonium salt of an amino acid. 
       
     
     
         15 . The method of treating malaria according to  claim 14 , wherein:
 R2 is a substituted or unsubstituted acyl;   R3 is selected from a group consisting of hydrogen, methyl and ethyl;   R4 is selected from a group consisting of hydrogen, methyl, ethyl and OX 4 ;   X 4  being selected from hydrogen, sodium, potassium, methyl and ethyl; and   A is a 3 carbon moiety selected from the group consisting of alkylene radical, alkenylene radical, and hydroxyalkylene radical.   
     
     
         16 . The method of treating malaria according to  claim 15 , wherein:
 X 1  is hydrogen;   R 2  is selected from formyl and acetyl; and   A is selected from propenylene and hydroxypropylene.