Vancoresmycin, a process for its production and its use as a pharmaceutical

Abstract

The present invention relates to a compound named Vancoresmycin which is obtainable by cultivation of the microorganism HIL-006734 (DSM 12216), and to its pharmaceutically acceptable salts. The present invention further relates to a process for the production of Vancoresmycin, to the microorganism HIL-006734 (DSM 12216), to the use of Vancoresmycin and its pharmaceutically acceptable salts as pharmaceuticals, and in particular to their use as antibiotics, and to pharmaceutical compositions comprising Vancoresmycin or a pharmaceutically acceptable salt thereof.

We claim:  
     
         1 . Vancoresmycin, a compound of the formula:  
       
         
           
           
               
               
           
         
         and its pharmaceutically acceptable salts and derivatives, in all their stereoisomeric and tautomeric forms.  
       
     
     
         2 . Vancoresmycin, a compound of the molecular formula C 71 H 126 N 2 O 21 , obtainable by cultivation of the microorganism Amycolatopsis species HIL-006734 (DSM 12216) or one of its variants or mutants under aerobic conditions in a nutrient medium containing sources of carbon and nitrogen, followed by isolation and purification, and its pharmaceutically acceptable salts, and derivatives, in all their stereoisomeric and tautomeric forms.  
     
     
         3 . A process for the production of a compound as claimed in  claim 1  comprising the steps of: 
 cultivating the microorganism Amycolatopsis species HIL-006734 (DSM 12216) or one of its variants or mutants under aerobic conditions in a nutrient medium containing sources of carbon and nitrogen to produce Vancoresmycin,  
 isolating the Vancoresmycin, and  
 purifying the Vancoresmycin.  
 
     
     
         4 . A process for the production of a compound as claimed in  claim 2  comprising the steps of: 
 cultivating the microorganism Amycolatopsis species HIL-006734 (DSM 12216) or one of its variants or mutants under aerobic conditions in a nutrient medium containing sources of carbon and nitrogen to produce Vancoresmycin,  
 isolating the Vancoresmycin, and  
 purifying the Vancoresmycin.  
 
     
     
         5 . A process as claimed in  claim 3 , further comprising the step of reacting the Vancoresmycin with a suitable agent to form a pharmaceutically acceptable salt or derivative.  
     
     
         6 . A process as claimed in  claim 4 , further comprising the step of reacting the Vancoresmycin with a suitable agent to form a pharmaceutically acceptable salt or derivative.  
     
     
         7 . Amycolatopsis species HIL-006734 (DSM 12216) or one of its variants or mutants.  
     
     
         8 . A pharmaceutical composition, comprising an effective amount of Vancoresmycin or a pharmaceutically acceptable salt or derivative thereof as claimed in  claim 1  and a pharmaceutically acceptable carrier.  
     
     
         9 . A pharmaceutical composition, comprising an effective amount of Vancoresmycin or a pharmaceutically acceptable salt or derivative thereof as claimed in  claim 2  and a pharmaceutically acceptable carrier.  
     
     
         10 . A method of treating an infection comprising administering to a patient in need thereof an effective amount of a compound as claimed in  claim 1 .  
     
     
         11 . A method of treating an infection comprising administering to a patient in need thereof an effective amount of a compound as claimed in  claim 2 .  
     
     
         12 . A method of treating a  Staphylococcus aureas  infection comprising administering to a patient in need thereof an effective amount of a compound as claimed in  claim 1 .  
     
     
         13 . A method of treating a  Staphylococcus aureas  infection comprising administering to a patient in need thereof an effective amount of a compound as claimed in  claim 2 .  
     
     
         14 . The method of  claim 12 , wherein the  Staphylococcus aureas  is vancomycin-resistant and/or teicoplanin-resistant.  
     
     
         15 . The method of  claim 13 , wherein the  Staphylococcus aureas  is vancomycin-resistant and/or teicoplanin-resistant.  
     
     
         16 . The method of  claim 10 , wherein the infecting organism is a Staphylococcus.  
     
     
         17 . The method of  claim 11 , wherein the infecting organism is a Staphylococcus.  
     
     
         18 . The method of  claim 10 , wherein the infecting organism is an Enterococcus.  
     
     
         19 . The method of  claim 11 , wherein the infecting organism is an Enterococcus.