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Title:
CARBOXYLIC ACID AMIDE DERIVATIVE
Document Type and Number:
Japanese Patent JP3391038
Kind Code:
B2
Abstract:

PURPOSE: To obtain a new carboxylic acid amide derivative, having calpain inhibiting activity and useful as a therapeutic agent for ischemic diseases, inflam mation, myodystrophia, cataract, immunopathy, essential hypertension, etc.
CONSTITUTION: The objective compound of formula I [R1 is aromatic hydrocarbon group; heterocyclic group, alkyl, alkenyl or X-R3 (X is O or S; R3 is aromatic hydrocarbon group, heterocyclic group or alkyl); Y is saturated heterocyclic group containing N or monocyclic saturated hydrocarbon group; R2 is substituted alkyl, substituted alkenyl, acyl, substituted sulfonyl, alkoxycarbonyl, substituted carbamoyl or substituted thiocarbamoyl; n is 0-5], e.g. (2R,2S)-1- benzyloxycarbonyl-azetidine-2-carboxylic acid-(1S)-(1-formyl-3-methylthio)propylamide. This compound of formula I is obtained by reacting a carboxylic acid derivative of formula II with an amine derivative of formula III, preferably in the presence of a condensing agent and then oxidizing the resultant alcoholic derivative of formula IV.


Inventors:
Akihiko Hosoda
Naoko Tanabe
Masahiro Shibata
Jiro Inaba
Hiroshi Ikawa
Tetsuaki Yamaura
Application Number:
JP35875092A
Publication Date:
March 31, 2003
Filing Date:
December 28, 1992
Export Citation:
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Assignee:
Fujirebio Co., Ltd.
International Classes:
A61K31/16; A61K31/215; A61K31/395; A61K31/397; A61K31/40; A61K31/403; A61K31/404; A61K31/4427; A61K31/4433; A61K31/445; A61K31/4465; A61P9/10; A61P9/12; A61P27/02; A61P27/12; A61P29/00; A61P43/00; C07C233/31; C07C233/58; C07C233/76; C07C235/06; C07C235/40; C07C271/12; C07C271/22; C07C271/28; C07C271/30; C07C275/16; C07C323/41; C07C323/59; C07C333/08; C07D205/04; C07D207/16; C07D209/14; C07D209/18; C07D211/36; C07D211/60; C07D211/62; C07D211/96; C07D333/18; C07D401/06; C07D401/12; C07D401/14; C07D409/06; (IPC1-7): C07C233/31; C07C233/58; C07C233/76; C07C235/06; C07C235/40; C07C271/12; C07C271/22; C07C271/28; C07C271/30; C07C275/16; C07C323/41; C07C323/59; C07C333/08; C07D205/04; C07D207/16; C07D209/14; C07D209/18; C07D211/36; C07D211/60; C07D211/62; C07D211/96; C07D333/18; C07D401/06; C07D401/12; C07D401/14; C07D409/06
Domestic Patent References:
JP2256654A