Method of producing fr901228

Abstract

Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.

1 . A pharmaceutical composition, comprising:
 type B crystalline form of FR901228:   
       
         
           
           
               
               
           
         
         and 
         a pharmaceutically acceptable carrier. 
       
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the type B crystalline form of FR901228 exhibits a powder X-ray diffraction pattern substantially similar to  FIG. 5 . 
     
     
         3 . The pharmaceutical composition of  claim 1 , wherein the type B crystalline form of FR901228 exhibits one or more of the following peaks in a powder X-ray diffraction pattern: about 7.1, about 11.7, about 11.9, and about 15.1 degrees 2-theta.