MEPTAZINOL BILIGAND DERIVATIVES AND/OR THEIR SALTS, PREPARATION METHOD AND USES THEREOF

Title:

MEPTAZINOL BILIGAND DERIVATIVES AND/OR THEIR SALTS, PREPARATION METHOD AND USES THEREOF

Document Type and Number:

WIPO Patent Application WO/2008/019572

Kind Code:

A1

Abstract:

This invention belongs to pharmacy field. Meptazinol biligand derivatives,salts, preparation method and uses thereof in the treatment CNS degenerative diseases including Alzheimer's type and dementia. The method comprises crude materials (-)meptazinol undergoing N-demethyl reaction to form (-)-N-demethyl-meptazinol following by reacting with diacid chloride or dihalohydrocarbon to be condensed into (-)meptazinol biligand derivatives. It is approved by in vitro choline esterase restrain activity and Aβ gathering inhibition experiments that (-)meptazinol biligand derivatives and their salts are new type dimolecular inhibitor which can inhibit both AchE and Aβgathering. The inhibition activity of the derivatives with the strongest activity reaches nM grade for both AchE and BchE, which respectively increases by 10,000 and 1500 times contrasting against (-)meptazinol hydrochloric and is three times of inhibition intensity for Aβ gathering induced by AchE contrasting against controlled propyldine iodide.

Inventors:

QIU ZHUIBAI (CN)
XIE QIONG (CN)
CHEN HONGZHUAN (CN)
WANG HAO (CN)
XIA ZHENG (CN)
LU MEIYAN (CN)
WANG XINGHAI (CN)

Application Number:

PCT/CN2007/002243

Publication Date:

February 21, 2008

Filing Date:

July 24, 2007

Export Citation:

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Assignee:

UNIV FUDAN (CN)
QIU ZHUIBAI (CN)
XIE QIONG (CN)
CHEN HONGZHUAN (CN)
WANG HAO (CN)
XIA ZHENG (CN)
LU MEIYAN (CN)
WANG XINGHAI (CN)

International Classes:

C07D223/04; A61K31/55; A61P25/04; A61P25/16; A61P25/28

Foreign References:

CN1974558A	2007-06-06
CN1569839A	2005-01-26
US4021550A	1977-05-03
CN200410017499A	2004-04-07
CN200610025390A	2006-03-31

Other References: