US2007270451A1PendingUtilityA1

Methods of preparing pimecrolimus

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Assignee: GYOLLAI VIKTORPriority: Dec 1, 2004Filed: Jul 24, 2007Published: Nov 22, 2007
Est. expiryDec 1, 2024(expired)· nominal 20-yr term from priority
Inventors:Viktor GyollaiCsaba Szabo
A61P 37/08A61P 37/02A61P 37/06A61P 37/00A61P 31/04A61P 31/00A61P 29/00C07H 19/01A61K 9/145C07D 498/18A61P 17/00A61K 31/4745C07D 491/14A61K 9/1688
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Claims

Abstract

The present invention provides a process for the preparation of pimecrolimus from ascomycin in which ascomycin is reacted with a conversion reagent that converts ascomycin to its activated derivative at C-32. The activated ascomycin is then reacted with chloride ion. The process of the invention requires fewer process steps than prior art processes, and does not require the protection of the ascomycin C-24 hydroxyl group or the purification of the activated ascomycin derivative.

Claims

exact text as granted — not AI-modified
1 . Pimecrolimus having a purity of at least about 95% area by HPLC.  
   
   
       2 . The pimecrolimus of  claim 1 , having a purity of at least about 98% area by HPLC.  
   
   
       3 . A pharmaceutical formulation comprising a therapeutically effective amount of the pimecrolimus of  claim 1 .  
   
   
       4 . A method for treating a patient suffering from atopic dermatitis, comprising the step of administering to the patient the pharmaceutical formulation of  claim 3.

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