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Title:
CORTICOSTEROID 17-ALKYL CARBONATE 21-(O)-CARBOXYLIC ACID CARBONIC ESTER, PRODUCTION THEREOF, AND MEDICINE COMPOSITION CONTAINING THE SAME
Document Type and Number:
Japanese Patent JPH0789982
Kind Code:
A
Abstract:

PURPOSE: To obtain a corticosteroid 17-alkyl carbonate 21-[0]-carboxylic acid carbonic ester which has a very strong local and topical anti-inflammatory action and is effctive in treating inflammatory dermatosis by reacting a specific alkyl carbonate with a specific activated carboxylic acid.

CONSTITUTION: The objective compd. is represented by formula I [wherein A is CHOH, CHCl, CH2, C=O, or a 9(11) double bond and is arbitrarily sterically arranged; Y is H, F, or Cl; Z is H, F, or methyl; R(1) is (substd.) aryl or hetaryl; n and m are each 0 or 1; R(2) is 1-8C alkyl or -(CH2)2-OCH3; and R(3) is H or methyl]. An example is prednisolone 17-ethyl carbonate 21- benzoic ester. The compd. is prepd. by reacting a compd. of formula II [wherein R(5) is OH] with an activated carboxylic acid of formula III [wherein R(6) is Cl, Br, or the like] (pref. a halide, anhydride, or azolide thereof).


Inventors:
Stache, Ulrich
Alpermann, Hans-georg
Duerckheimer, Walter
Bohn, Manfred
Application Number:
JP1994000223963
Publication Date:
April 04, 1995
Filing Date:
August 26, 1994
Export Citation:
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Assignee:
HOECHST AG
International Classes:
A61K31/57; A61P17/00; A61P29/00; C07J5/00; C07J17/00; C07J31/00; C07J33/00; C07J41/00; C07J43/00; (IPC1-7): C07J5/00; A61K31/57; C07J17/00; C07J33/00; C07J43/00
Attorney, Agent or Firm:
高木 千嘉 (外2名)



 
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