Farnesyl transferase inhibiting 1,2-annelated quinoline enantiomer

Abstract

(−)-5-(3-Chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)tetrazolo-[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts, and the use of such compounds in medicine especially for the treatment of cancer

1 . (−)-5-(3-Chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)tetrazolo[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts.  
     
     
         2 . (−)-5-(3-Chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)-tetrazolo[1,5-a]quinazoline-7-methanamine.  
     
     
         3 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier, and as active ingredient a therapeutically effective amount of a compound as claimed in  claim 1 .  
     
     
         4 . A pharmaceutical composition as claimed in  claim 3  in which the active ingredient is the compound as claimed in  claim 2 .  
     
     
         5 . A pharmaceutical composition as claimed in  claim 3  or  claim 4  in a dosage unit form.  
     
     
         6 . A pharmaceutical composition as claimed in  claim 5  containing 50 to 300 mg of active ingredient in each unit dosage form.  
     
     
         7 . A pharmaceutical composition as claimed in  claim 5  or  claim 6  in the form of a tablet.  
     
     
         8 . A process for preparing a pharmaceutical composition as claimed in any of  claims 3  to  7  wherein a therapeutically effective amount of the active ingredient is intimately mixed with a pharmaceutically acceptable carrier.  
     
     
         9 . A compound as claimed in  claim 1  or  claim 2  for use in medicine.  
     
     
         10 . Use of a compound as claimed in  claim 1  or  claim 2  in the manufacture of a medicament for inhibiting tumor growth.  
     
     
         11 . A method for inhibiting tumor growth in a subject which comprises administering an effective amount of compound as claimed in  claim 1  or  claim 2  to the subject.  
     
     
         12 . A method as claimed in  claim 11  in which the compound is administered in a daily dose of 10 to 600 mg.  
     
     
         13 . A method as claimed in  claim 12  in which the compound is administered in a daily dose of 50 to 500 mg.  
     
     
         14 . A process for the preparation of a compound as claimed in  claim 1  or  claim 2  which comprises treating (±)-5-(3-chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H -imidazol-5-yl)tetrazolo[1,5-a]quinazoline-7-methanamine or a pharmaceutically acceptable acid addition salt thereof to separate the constituent (+) and (−) enantiomers and isolating the (−) enantiomer or a pharmaceutically acceptable acid addition salt thereof.