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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 8232270 B1

PDFFull Text
Date of Patent:
Jul. 31, 2012

Filed:

Jul. 24, 2007

Bivalent (−)-meptazinol compounds and/or their salts, and their preparation and futilization

Applicants:

Zhuibai Qiu, Shanghai, CN;

Qiong Xie, Shanghai, CN;

Hongzhuan Chen, Shanghai, CN;

Hao Wang, Shanghai, CN;

Zheng Xia, Shanghai, CN;

Meiyan LU, Shanghai, CN;

Xinghai Wang, Shanghai, CN;

Inventors:

Zhuibai Qiu, Shanghai, CN;

Qiong Xie, Shanghai, CN;

Hongzhuan Chen, Shanghai, CN;

Hao Wang, Shanghai, CN;

Zheng Xia, Shanghai, CN;

Meiyan Lu, Shanghai, CN;

Xinghai Wang, Shanghai, CN;

Assignee:

Other;

Attorney:
Primary Examiner:

Brenda Coleman

Int. Cl.
CPC ...
A61P 25/04 (2006.01); A61P 25/16 (2006.01); A61P 25/28 (2006.01); A61K 31/55 (2006.01); C07D 223/04 (2006.01);
U.S. Cl.
CPC ...
Abstract

The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (−)-meptazinol compounds and/or their salts, as well as the preparation and utilization of the compounds in the treatment of neurodegenerative disorders and dementias such as Alzheimer's Disease (AD). In the present invention, bivalent (−)-meptazinol compounds were synthesized, from the starting material (−)-meptazinol, successively by N-demethylation forming (−)-nor-meptazinol and then by acylation with α,ω-alkanediacyl dihalides or alkylation with α,ω-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced Aβ aggregation test demonstrated that the bivalent (−)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both AChE and Aβ aggregation. The most potent compound inhibited both AChE and BChE at nM level, which was 10000 and 1500 times more potent than (−)-MEP hydrochloride, respectively. It inhibited AChE-induced Aβ aggregation by a factor of 2 compared with propidium.

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