C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/12 (2006.01) A61K 31/365 (2006.01) A61K 31/38 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/515 (2006.01) C07D 239/60 (2006.01) C07D 239/62 (2006.01) C07D 239/66 (2006.01) C07D 311/56 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/06 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01) C07D 413/12 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 473/08 (2006.01) C07D 487/
Patent
CA 2254744
Ligand inhibitors for increasing levels of free corticotropin-releasing factor (CRF) in the brain are disclosed. Such ligand inhibitors cause release of CRF from the CRF/CRF-bind protein complex. Administration of the ligand inhibitors provide improvement in learning and memory, result in decreased food intake and/or provide treatment for diseases associated with low levels of CRF in the brain, notably Alzheimer's disease. In the practice of this invention, the ligand inhibitor is one or more compounds having the structure (I), (II) or (III), including keto tautomers, stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, G and Xm of structure (I), R1', R2'R3', G and W of structure (II), and R1", R2", R3" and W of structure (III) are as disclosed in the description.
L'invention porte sur des ligands inhibiteurs servant à augmenter les taux du facteur libre libérant la corticotrophine (CRF) dans le cerveau. Ces ligands inhibiteurs provoquent la libération du facteur libérant la corticotrophine du complexe de protéines liantes CRF/CRF. L'administration des ligands inhibiteurs améliore les facultés d'apprentissage et la mémoire, entraîne une réduction de l'apport alimentaire et/ou permet de traiter les maladies liées à de faibles taux de CFR dans le cerveau, notamment la maladie d'Alzheimer. Dans la pratique, le ligand inhibiteur faisant l'objet de l'invention est constitué d'un ou plusieurs composés de structure (I), (II) ou (III), et comprenant des cétotautomères, des stéréo-isomères et des sels acceptables pharmacologiquement desdits composés, R¿1?, G et X¿m? de la structure (I), R¿1?', R¿2?' et R¿3?', G et W de la structure (II), et R¿1?'', R¿2?'', R¿3?'' et W de la structure (III) étant spécifiés dans la description.
Behan Dominic P.
Erickson Philip E.
Huang Charles Q.
Liu Zhengyu
Lowe Richard F.
Gowling Lafleur Henderson Llp
Neurocrine Biosciences Inc.
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