Bivalent (−)-meptazinol compounds and/or their salts, and their preparation and futilization
US8232270B2 · kind B2 · utility
Inventors
Key dates
| Filing date | Jul 24, 2007 |
| Grant date | Jul 31, 2012 |
| Priority date | — |
| Expiry date | Jan 29, 2029 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P25/28
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.