New salt of abexinostat, associated crystalline form, a process for their preparation and pharmaceutical compositions containing them

Abstract

Abexinostat tosylate of formula (II): and its crystalline form I characterised by its X-ray powder diffraction diagram, its Raman spectrum and its solid-state 13 C CP/MAS NMR spectrum. Medicinal products containing the same which are useful in the treatment of cancer.

1 . N-hydroxy-4-{2-[3-(N,N-dimethylaminomethyl)benzofuran-2ylcarbonylamino]-ethoxy}benzamide tosylate, or a solvate thereof. 
     
     
         2 . A tosylate salt of abexinostat of formula (I): 
       
         
           
           
               
               
           
         
       
     
     
         3 . A pharmaceutical composition comprising, as active ingredient abexinostat tosylate according to  claim 1 , in combination with one or more pharmaceutically acceptable excipients. 
     
     
         4 . A method of treating cancer in a subject in need thereof, comprising administration of an effective amount of the pharmaceutical composition according to  claim 3 . 
     
     
         5 . The method according to  claim 4 , wherein the cancer is a carcinoma, a tumour, a neoplasm, a lymphoma, a melanoma, a glioma, a sarcoma or a blastoma. 
     
     
         6 . A process for the preparation of crystalline form I of abexinostat tosylate, having an X-ray powder diffraction diagram having the following diffraction lines (Bragg's angle 2 theta, expressed in degrees ±0.2°): 6.50; 9.94; 11.35; 12.33; 14.08; 18.95; 21.08; 27.05, wherein the abexinostat is crystallised in the presence of para-toluenesulphonic acid in a polar medium and wherein the crystallisation is seeded using a very small amount of crystalline form I of abexinostat tosylate.