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Title:
DIGITOXIGENIN AND DIHYDRODIGITOXIGENIN 3 BETA-DERIVATIVE AND PHARMACEUTICAL COMPOSITION
Document Type and Number:
Japanese Patent JPH0665285
Kind Code:
A
Abstract:

PURPOSE: To obtain a new compd. which is useful as a therapeutic drug for cardiovascular diseases such as heart failure and hypertension, is low toxic and which acts as a partial agonist for enzymic activity of Na+, K+-ATPase.

CONSTITUTION: This compd. is expressed by formula I (double lines of dotted lines and solid lines represent single bonds or double bonds; X is S, O; R is a 2-6C alkyl, a 3-6C alkenyl, alkynyl or the like), for example, 3β-(2-(trimethylammonium)ethoxy)-14β-hydroxy-5β-carbo-20(22)-enolidechloride. The compd. is obtd. by condensation of a compd. expressed by formula II with a compd. expressed by R-Y (Y is an electron attractive group). The condensation reaction is preferably carried out in an inert aprotic solvent such as THF in the presence of a strong base such as hydrogenated sodium at -20 to 110°C. The compd. expressed by formula I is preferably purified by flush chromatography on a silica gel.


Inventors:
PIERO MEROONI
RUIJI BERUNARUDEI
PATORITSUIA FUERAARI
MAURO GOBIINI
MARUKO TORI
ROREDANA BUARENTEINO
Application Number:
JP16123993A
Publication Date:
March 08, 1994
Filing Date:
June 30, 1993
Export Citation:
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Assignee:
SIGMA TAU IND FARMACEUTI
International Classes:
A61K31/58; A61P9/00; A61P9/12; C07J19/00; A61K31/585; C07J31/00; C07J41/00; C07J43/00; (IPC1-7): C07J19/00; A61K31/585; C07J31/00; C07J43/00
Attorney, Agent or Firm:
Aoyama Ryo (2 outside people)



 
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