Nonapeptide with anti-tumour activity

Abstract

The present invention relates to peptides or peptide like molecules and their uses in therapy, in particular as anti-tumour agents.

1 - 15 . (canceled) 
     
     
         16 . A compound of formula: 
       
         
           
                 
                 
               
                     
                   (I) 
                 
                     
                   (SEQ ID NO: 1) 
                 
                     
                   CCLLCCLLC 
                 
                     
                   or 
                 
                     
                     
                 
                     
                   (III) 
                 
                     
                   (SEQ ID NO: 3) 
                 
                     
                   CLLCCLLCC; 
                 
             
                
                
                
                
                
                
                
                
               
            
           
         
         wherein C represents a cationic amino acid and L represents an amino acid with a lipophilic R group, wherein the R group has at least 7 non-hydrogen atoms and in which one of the amino acids having a lipophilic R group is a non-genetically coded amino acid, or a salt, ester or amide of said compound. 
       
     
     
         17 . A compound as claimed in  claim 16  wherein each lipophilic R group has at least 9 non-hydrogen atoms. 
     
     
         18 . A compound as claimed in  claim 16  wherein each lipophilic R group has at least one cyclic group. 
     
     
         19 . A compound as claimed in  claim 16  in which 1 to 3 of the amino acids with lipophilic R groups are tryptophan. 
     
     
         20 . A compound as claimed in  claim 16  which incorporates a non-genetically coded amino acid selected from the group consisting of:
 2-amino-3-(biphenyl-4-yl)propanoic acid (biphenylalanine), 2-amino-3,3-diphenylpropanoic acid (diphenylalanine), 2-amino-3-(anthracen-9-yl)propanoic acid, 2-amino-3-(naphthalen-2-yl)propanoic acid, 2-amino-3-(naphthalen-1-yl)propanoic acid, 2-amino-3-[1,1′:4′,1″-terphenyl-4-yl]-propionic acid, 2-amino-3-(2,5,7-tri-tert-butyl-1H-indol-3-yl)propanoic acid, 2-amino-3-[1,1′:3′,1″-terphenyl-4-yl]-propionic acid, 2-amino-3-[1,1′:2′,1″-terphenyl-4-yl]-propionic acid, 2-amino-3-(4-naphthalen-2-yl-phenyl)-propionic acid, 2-amino-3-(4′-butylbiphenyl-4-yl)propanoic acid, 2-amino-3-[1,1′:3′,1″-terphenyl-5′-yl]-propionic acid and 2-amino-3-(4-(2,2-diphenylethyl)phenyl)propanoic acid. 
 
     
     
         21 . A compound as claimed  claim 16  having the formula of SEQ ID NO: 23 (LTX-315), or a salt, ester or amide thereof. 
     
     
         22 . A composition comprising a compound as claimed in  claim 16 , in combination with a pharmaceutically acceptable carrier, diluent or excipient. 
     
     
         23 . A composition comprising a compound as claimed in  claim 16  in combination with at least one other therapeutic ingredient. 
     
     
         24 . A method of treatment of a tumour, comprising the step of administering a pharmaceutically effective amount of a compound as claimed in  claim 16  to a patient in need of such treatment.