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Title: Dimeric compounds
Authors: Carlier, Paul R.
Han, Yi-Fan
Pang, Yuan-Ping
Du, Da-Ming
Keywords: Drugs
Alzheimer's Disease
Issue Date: 5-May-2004
Citation: UK Patent GB 2 360 518 B, 2006
Abstract: Huperzine A is a selective and potent reversible acetylcholinesterase (AChE) inhibitor isolated from club moss Huperzia serrata which shows considerable promise for the palliative treatment of Alzheimer's Disease. However, the synthesis of this compound requires many steps. More easily synthesised and potent analogues of huperzine A have been developed, but these compounds are relatively weak AChE inhibitors or contain toxic tacrine moieties. The invention relates to dimeric compounds comprising two 5-amino-5,6,7,8-tetrhydroquinoline fragments joined together by a divalent link group. This synthesized compound exhibit high potency as cholinesterase. The optimum dimers are twice as potent as huperzine A. Moreover, this dimeric compound does not contain any toxic tacrine moieties and can be synthesized in just nine steps from commercially available starting materials. The dimeric compounds and compositions of the invention are useful as cholinesterase inhibitors and inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The invention can be used in the treatment of neurodegenerative diseases, especially Alzheimer's Disease and myasthenia gravis.
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