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Title:
17-DEOXYCORTICOSTEROID-21-(O)-CARBOXYLIC ACID ESTER, ITS PRODUCTION AND PHARMACEUTICAL CONTAINING SAME
Document Type and Number:
Japanese Patent JP3902255
Kind Code:
B2
Abstract:

PROBLEM TO BE SOLVED: To provide the subject new compound having excellent antiinflammatory action and low systemic side actions and useful e.g. for an extremely strong local antiinflammatory agent by reacting deoxymethasone, etc., with an activated aromatic alkylcarboxylic acid.
SOLUTION: This new 17-deoxycorticosteroid-21-[O]-carboxylic acid ester having excellent antiinfl,ammatory action and low systemic side actions and useful e.g. for an extremely strong local antiinflammatory agent is expressed by the formula I [A is CHOH, CHCI, CH2, C=O or 9(11) double bond each having arbitrary steric configuration; Y is H, F or Cl; Z is H, F or methyl; R(1) is a (substituted)aryl or a heteroaryl; R(2) is H, α-methyl or β-methyl]. The compound can be produced by reacting a compound of the formula II [R(4) is OH] (e.g. deoxymethasone) with an active carboxylic acid of the formula III [R(5) is Cl, Br, OC(O)CF3, an active acid group or the like] (e.g. 3- phenylpropionyl, chloride).


Inventors:
Ulrich Schyuterhier
Hans-Georg Alperman
Manfred Bourne
Application Number:
JP23939895A
Publication Date:
April 04, 2007
Filing Date:
September 19, 1995
Export Citation:
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Assignee:
Hoechst Gesellschaft Mito Beschlenktel Haftung
International Classes:
A61K31/575; A61K31/57; C07J43/00; A61K31/573; A61K31/58; A61P17/00; A61P17/04; A61P29/00; C07J5/00; C07J7/00; C07J9/00; C07J17/00; C07J31/00; C07J33/00; C07J41/00; (IPC1-7): C07J43/00; A61K31/575; A61K31/58; C07J9/00; C07J17/00; C07J31/00; C07J33/00
Domestic Patent References:
JP53127456A
JP60041696A
Foreign References:
CH495969A5
US2755292
Other References:
J. Med. Chem.,1969, Vol.12,p.810-818
Attorney, Agent or Firm:
Chika Takagi
Tatsuo Sato
Kosuke Nishimura