Ligands for monoamine receptors and transporters, and...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 295/16 (2006.01) A61K 31/435 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01) C07B 61/00 (2006.01) C07C 255/46 (2006.01) C07D 205/02 (2006.01) C07D 207/06 (2006.01) C07D 207/08 (2006.01) C07D 207/09 (2006.01) C07D 211/12 (2006.01) C07D 211/16 (2006.01) C07D 211/18 (2006.01) C07D 211/20 (2006.01) C07D 211/26 (2006.01) C07D 211/32 (2006.01) C07D 211/40 (2006.01) C07D 211/42 (2006.01) C07D 211/60 (2006.01) C07D 213/30 (2006.01) C07D 223/04 (2006.01) C07D 223/10 (2006.01) C07D 233/04 (2006.01) C07D 233/

Patent

CA 2422055

One aspect of the present invention relates to heterocyclic compounds formula A; whereof the substituents are defined in the description. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous aliments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

Selon un premier aspect, la présente invention concerne des composés hétérocycliques. Selon un deuxième aspect, la présente invention concerne l'utilisation de composés hétérocycliques comme des ligands pour divers récepteurs cellulaires de mammifères, y compris, la dopamine, la sérotonine ou les transporteurs de norépinéphrine. Ces composés, selon l'invention, peuvent être utilisés dans le traitement de nombreux troubles, états et maladies qui touchent les mammifères. Ils permettent de soigner, mais sans s'y limiter, la toxicomanie, l'anxiété, la dépression, les troubles sexuels, l'hypertension, la migraine, la maladie d'Alzheimer, l'obésité, les vomissements, la psychose, la schizophrénie, la maladie de Parkinson, les douleurs inflammatoires, les douleurs neuropathiques, le syndrome de Lesch-Nyhan, la maladie de Wilson et le syndrome de Tourette. Selon un autre aspect, la présente invention concerne la synthèse de bibliothèques de combinaison des composés hétérocycliques, et le dosage de ces bibliothèques afin de déterminer l'activité biologique, par exemple, dans des dosages fondés sur les transporteurs de dopamine.

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