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

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

A - Human Necessities

61

K

A61K 31/00 (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) C07K 2/00 (2006.01) C07K 4/00 (2006.01) G01N 33/53 (2006.01) G01N 33/543 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2321191

Disclosed are novel multi-binding compounds (agents) which bind 5-HT3 receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such receptors thereby modulating the biological processes/functions thereof. Each of the ligands is covalently attached to a linker or linkers which may be the same or different to provide for the multi- binding compound. The linker is selected such that the multi-binding compound so constructed demonstrates increased modulation of the biological processes mediated by the 5-HT3 receptor.

La présente invention concerne des composés ou agents à plusieurs liaisons et qui se lient aux récepteurs 5-HT¿3?. Ces composés comportent une pluralité de ligands dont chacun peut se lier à de tels récepteurs, modulant ainsi les fonctions ou processus biologiques de ces récepteurs. Chacun des ligands est attaché par covalence à un lieur ou à des lieurs qui peuvent être identiques ou différents, et ce, de façon à constituer un composé capable de liaisons multiples. Le choix du lieur est fait pour que le composé à liaisons multiples fasse preuve d'une modulation accrue des processus biologiques à médiation du récepteur 5-HT¿3?.

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