Novel Tropane Analogs
Section: For Industry
Category(ies): CNS Disorders
Reference #: KOAL422420
OTC Contact: David Odelson, Ph.D. (Directory Information | Send a Message)
Description
Currently two generations of antidepressants are utilized by physicians. The first generation of drugs consists of tricyclic antidepressants (TCA) and monoamine oxidase inhibitors, both of which have serious side effects and exhibit toxicity in overdose. As a result of these shortcomings a second generation of antidepressants with an improved safety profile was developed. This second generation includes selective serotonin reuptake inhibitors and reversible monoamine oxidase inhibitors. These compounds have proven to be safer but have a generally slower onset of action and tend to lose efficacy over time. The present invention is a group of novel tropane analogs, capable of acting as inhibitors of reuptake monoamines. These compounds have shown efficacy as selective inhibitors of serotonin and/or norepinephrine reuptake
Applications
- Treatment of mental disorders including depression
- Treating cocaine addiction
- Greater efficacy versus traditional serotonin reuptake inhibitors.
- Rapid onset of therapeutic activity on the scale of days rather than weeks.
- The ability to act on more than one target site
Advantages
Stage of Development
Stage of Development: Studies done to validate the compounds in-vitro.
Relevant Publications
"Novel Conformationally Constrained Tropane Analogues by 6-endo-trig Radical Cyclization and Stille Coupling--Switch of Activity Toward the Serotonin and/or Norepinephrine Transporter", Kozikowski et al, J. Med. Chem. 43: 2064-2071, (2000).
Patent Status
US patent # 6,982,271, entitled, “Novel Tropane Analogs” issued on January 6, 2006.
