Multivalent agonists, partial agonists, inverse agonists and...

A - Human Necessities – 61 – K

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A61K 31/40 (2006.01) A61K 31/495 (2006.01) A61K 38/00 (2006.01) A61K 39/00 (2006.01) A61K 39/395 (2006.01) A61K 39/44 (2006.01) A61K 51/00 (2006.01) C07B 61/00 (2006.01) C07C 215/60 (2006.01) C07C 217/08 (2006.01) C07C 323/62 (2006.01) C07D 211/42 (2006.01) C07D 211/56 (2006.01) C07D 213/74 (2006.01) C07D 213/80 (2006.01) C07D 263/32 (2006.01) C07D 263/34 (2006.01) C07D 265/32 (2006.01) C07D 277/24 (2006.01) C07D 277/28 (2006.01) C07D 277/34 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12

Patent

CA 2319751

Disclosed are multibinding compounds which are agonists, partial agonists, inverse agonists or antagonists of the 5HT2 receptors, which are involved in neurological disorders. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is an agonist, partial agonist, inverse agonist or antagonist of the 5HT2 receptors. The multibinding compounds of this invention are useful for the prophylaxis and treatment of various neurological disorders such as depression, anxiety, epilepsy, psychosis, schizophrenia, Alzheimer's disease, drug addiction, sleep and eating disorders, migraine and pain.

La présente invention concerne des composés à liaisons multiples qui sont des agonistes, des agonistes partiels, des agonistes inverses ou des antagonistes des récepteurs 5HT¿2?, et qui sont impliqués dans des troubles neurologiques. Les composés à liaisons multiples de l'invention comportent de 2 à 10 ligands reliés par covalence à au moins un lieur. Chacun des ligands est un agoniste, un agoniste partiel, un agoniste inverse ou un antagoniste des récepteurs 5HT¿2?. Les composés à liaisons multiples de l'invention conviennent à la prophylaxie et au traitement de divers troubles neurologiques tels que la dépression, l'anxiété, l'épilepsie, la psychose, la schizophrénie, la maladie d'Alzheimer, la toxicomanie, les troubles du sommeil et de l'alimentation, la migraine et la douleur.

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