Bi- and tri-cyclic aza compounds and their uses

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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Details

546112, 546183, A61K 3144, C07D22102

Patent

active

061503762

ABSTRACT:
The present invention provides tropane-derived monoamine neurotransmitter re-uptake inhibitors which predictably exhibit selectivity for either the serotonin or dopamine transporter, pharmaceutical compositions thereof and methods for their use. The serotonin-selective re-uptake inhibitors are particularly useful for treating neurological disorders associated with the serotonergic neural system of the brain, such as depression, with significantly reduced side-effects. The dopamine-selective re-uptake inhibitors are particularly useful for treating disorders associated with dopamine re-uptake and/or acetylcholine release.

REFERENCES:
patent: 5998405 (1999-12-01), Scheel-Kruger et al.
Abraham et al., 1992, "N-Modified Analogues of Cocaine: Synthesis and Inhibition of Binding to the Cocaine Receptor," J. Med. Chem. 35:141-144.
Kozikowski et al., 1994, "Structure-Activity Relationship Studies of N-Sulfonyl Analogs of Cocaine: Role of Ionic Interaction in Cocaine Binding," J. Med. Chem. 37:3440-3442.
Madras et al., 1996, "Nitrogen-Based Drugs Are Not Essential for Blockade of Monoamine Transporters," Synapse 24:340-348.
Smith et al., 1998, "The Synthesis of Tricyclic Cocaine Analogs via the 1,3-Dipolar Cycloaddition of Oxidopyridinium Betaines," Tetrahedron Letters 39:197-200.
Stoelwinder et al., 1994, "Differential Binding and Dopamine Uptake Activity of Cocaine Analogues Modified at Nitrogen," Bioorganic & Medicinal Chemistry Letters 4:303-308.
Thakore et al., 1996, "Treating depression with specific serotonergic acting agents," Journal of Serotonin Research 3:145-160.

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