Dimeric Compounds
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.
1. The compounds can be synthesized easily
2. The compounds have high potency used for neruodegenerative diseases treatment
3. Lower production cost
- Provide effective treatment in Alzheimer's Disease and myasthenia gravis
Patent Number: US6472408B1
Application Number: US2001784034A
Inventor: Carlier, Paul R. | Han, Yifan | Pang, Yuan Ping | Du, Da Ming
Priority Date: 16 Feb 2000
Priority Number: US6472408B1
Application Date: 16 Feb 2001
Publication Date: 29 Oct 2002
IPC Current: A61P002528 | C07D0215227 | C07D021522
US Class: 514312 | 514311 | 514314 | 546153 | 546157
Assignee Applicant: The Hong Kong University of Science & Technology
Title: Dimeric compounds
Usefulness: Dimeric compounds
Summary: Used for treating neurodegenerative diseases, particularly Alzheimer's disease and myasthenia gravis.
Novelty: New dimeric compounds useful for treating e.g. Alzheimer's disease, comprises two 5-amino-5,6,7,8-tetrahydroquinoline fragments joined by divalent linking group
生物医学
医药成分
16 Feb 2001
US 6472408
TTC.PA.111
香港
