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Title:
8-OXO-5,8-DIHYDRO-6H-DIBENZO(A,G)-QUINOLIZINE-13-PROPANOIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
Document Type and Number:
Japanese Patent JPH08239383
Kind Code:
A
Abstract:

To provide the subject novel derivative that is a specific 8-oxo-5,8- dihydro-6H-dibenzo[a,g]quinolizine-13-propanoic acid derivative and can treat the complaint as an anxiety accompanied by GABA transmission disorder of the GABAA receptor.

This novel compound is a free base represented by formula I [X is H, a halogen, a 1-3C alkyl, a 1-3C alkoxy, trifluoromethyl; Y is H, a halogen, a 1-3C alkyl, a 1-3C alkoxy; R is OH, methoxy, NR2R3 (R2 and R3 are each H, a 1-4C alkyl, 2-aminoethyl, R2 and R3 form together with N bonding to them morpholinyl or pyrrolidinyl or the like) or the like] or its salt and is useful for treating the complaint accompanied by GABA transmission trouble of GABAA acceptor including α5 subunit. This compound is prepared by reaction of an acid anhydride of formula II with an imine of formula III to form a compound of formula IV, converting the carboxyl group to an aldehyde group and chain-extending the product by treating it with methyl (dimethoxyphosphinyl)acetate.


Inventors:
BENOWA MARABOO
MIREEYU SEBURAN
JIYATSUKU FUROWATSUSAN
EMANIYUERU DASHIYARII
Application Number:
JP34262095A
Publication Date:
September 17, 1996
Filing Date:
December 28, 1995
Export Citation:
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Assignee:
SYNTHELABO (FR)
International Classes:
A61K31/435; A61K31/445; A61K31/47; A61K31/4745; A61K31/495; C07D455/03; A61K31/496; A61K31/535; A61K31/5377; A61P5/02; A61P21/02; A61P25/00; A61P25/04; A61P25/18; A61P25/20; A61P25/24; A61P25/26; A61P25/30; C07D455/02; (IPC1-7): C07D455/03; A61K31/435; A61K31/445; A61K31/495; A61K31/535
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)