POLYMORPHIC FORM OF 6-11 BICYCLIC KETOLIDE DERIVATIVE

摘要

PROBLEM TO BE SOLVED: To meet the requirement for the control of a synthesis process in such a manner as to control at least the percentage of each of various polymorphic forms (if any) within batches to coincide the percentages and satisfy the stock medicine/preparation specification approved by FDA in view of extremely important latent effect of various polymorphic forms of single stock medicine on the safety and efficacy of each preparation. SOLUTION: The present invention includes EP-13420 polymorphic crystalline forms: Form I, Form II, Form Ia, and monohydrate and amorphous EP-13420 having different physical properties. In another embodiment of the present invention, there are provided methods of producing the various polymorphic forms in pure form or in combination with one another. The present invention also provides pharmaceutical compositions and preparations containing the polymorphic and amorphous forms and methods of treating bacterial infections by administering the pharmaceutical compositions to a subject in need of such treatment. COPYRIGHT: (C)2008,JPO&INPIT