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 JP3780007
Kind Code:
B2
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:
Ulrich Syuthage
Hans-Georg Alperman
Walter de Jürkheimer
Manfred Bourne
Hans-Georg Alperman
Walter de Jürkheimer
Manfred Bourne
Application Number:
JP22396394A
Publication Date:
May 31, 2006
Filing Date:
August 26, 1994
Export Citation:
Assignee:
Hoechst Gesellschaft Mito Beschlenktel Haftung
International Classes:
A61K31/57; C07J5/00; A61K31/573; A61P17/00; A61P29/00; C07J17/00; C07J31/00; C07J33/00; C07J41/00; C07J43/00; (IPC1-7): C07J5/00; A61K31/57; A61K31/57; C07J17/00; C07J33/00; C07J43/00
Domestic Patent References:
| JP54036248A |
Foreign References:
| EP0072200A1 |
Attorney, Agent or Firm:
Chika Takagi
Tatsuo Sato
Kosuke Nishimura
Tatsuo Sato
Kosuke Nishimura