Novel Heterocyclic Nicotinic Agents

University of California System: University of California, Berkeley
posted on 05/28/2009

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Novel compounds are provided that modulate the neuronal nicotinic acetylcholine receptor (nAChR), particularly the mammalian nAChR (m-nAChR). The compounds are substituted pyridine derivatives such as analogs of 1-[(6-chloro-3-pyridinyl)methyl]-2-imidazolidine and 1-[(6-chloro-3-pyridinyl)methyl]-2-iminothiazole. Methods of using the novel m-nAChR modulators are also provided, including methods of using the compounds as m-nAChR probes and as therapeutic agents to treat mammalian individuals suffering from conditions, disorders or diseases that are responsive to administration of an m-nAChR modulator. The compounds are useful in treating (1) CNS disorders such as Alzheimer’s disease, AIDS-associated dementia, Tourette’s Syndrome, attention deficit disorder, and attention deficit disorder, (2) inflammation and inflammatory diseases, (3) conditions caused by or associated with smooth muscle contractions, and (4) withdrawal symptoms associated with cessation of chemical substance abuse. The compounds are also useful as non-opiate analgesics, to treat mild, moderate or severe pain. Pharmaceutical formulations containing an m-nAChR modulator of the invention are provided as well.

See also: J. Med Chem., 1999, 42, 2227-2234.

Inflammation and inflammatory diseases.
CNS disorders such as Alzheimer’s disease
Non-opiate analgesics
Conditions caused by or associated with smooth muscle contractions.
Withdrawl symptoms associated with cessation of chemical substance abuse.
Attention deficit disorder
AIDS-associated dementia.
Tourette’s Syndrome.

The compounds may be used as m nAChR probes and as therapeutic agents to treat diseases that are responsive to m-nAChR modulation.