A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/495 (2006.01) A61K 31/505 (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 403/06
Patent
CA 2319496
Disclosed are multibinding compounds which are agonists, partial agonists, inverse agonists, partial inverse agonist or antagonists of the GABA 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, partial inverse agonist or antagonist of the GABA receptors. The multibinding compounds of this invention are useful in the treatment of neurological disorders such as anxiety, depression, sleep and seizure disorders, emesis and overdoses of benzodiazepine-type drugs, and producing sedation, hypnosis, retrograde amnesia, and enhancing alertness and the like.
L'invention concerne des composés de liaison multiple, lesquels constituent des agonistes, des agonistes partiels, des agonistes inverses, des agonistes ou antagonistes partiels inverses des récepteurs de GABA (acide .gamma.-amino-butyrique) impliqués dans des troubles neurologiques. Les composés de liaison multiple de l'invention contiennent 2 à 10 ligands, liés de manière covalente à un ou plusieurs segments de liaison. Chaque ligand constitue un agoniste, un agoniste partiel, un agoniste inverse, un agoniste ou antagoniste partiel inverse des récepteurs de GABA. Les composés de liaison multiple de l'invention sont utiles dans le traitement de troubles neurologiques tels que l'anxiété, la dépression, les troubles du sommeil et les crises d'épilepsie, les vomissements et overdoses de médicaments du type benzodiazépines; ils sont également utiles pour produire la sédation et l'hypnose, l'amnésie rétrograde, et pour accroître la vigilance et analogue.
Beattie David T.
Griffin John H.
Moran Edmund J.
Advanced Medicine Inc.
Theravance Inc.
Torys Llp
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