Benzimidazole derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 235/12 (2006.01) A61K 31/496 (2006.01) A61P 3/04 (2006.01) A61P 9/00 (2006.01) A61P 13/02 (2006.01) A61P 25/04 (2006.01) A61P 25/14 (2006.01) A61P 25/16 (2006.01) A61P 25/18 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01) A61P 25/36 (2006.01) A61P 43/00 (2006.01) C07D 235/14 (2006.01) C07D 235/24 (2006.01) C07D 401/06 (2006.01) C07D 403/04 (2006.01) C07D 403/08 (2006.01) C07D 403/14 (2006.01) C07D 405/06 (2006.01) C07D 405/14 (2006.01)

Patent

CA 2485753

It is intended to provide compounds represented by the following general formula [I]: [I] wherein X represents hydrogen or halogeno; B represents halogeno, cyano or optionally fluorinated lower alkyl; D represents a 3- to 10- membered aliphatic nitrogen-containing heterocycle; R3, R4 and R5 are the same or different and each represents hydrogen, optionally substituted lower alkyl, etc.; and a is 0 or 1. Because of having a high affinity for nociceptin receptor and thus inhibiting the effect of nociceptin, these compounds are useful as analgesics, antiobestics, brain function-improving drugs, drugs for treating Alzheimer~s, drugs for treating dementia, remedies for schizophrenia, remedies for retrograde neurodegenerative diseases, antidepressants, remedies for diabetes insipidus, remedies for polyuria, remedies for hypotension, etc.

L'invention concerne des composés représentés par la formule générale [I], dans laquelle X représente hydrogène ou halogéno ; B représente halogéno, cyano ou alkyle inférieur éventuellement fluoré ; D représente un hétérocycle azoté aliphatique possédant de 3 à 10 chaînons ; R?3¿, R?4¿ et R?5¿ sont identiques ou différents, et chacun représente hydrogène, alkyle inférieur éventuellement substitué, etc. ; et a égale 0 ou 1. En raison de leur forte affinité pour le récepteur de la nociceptine, et par conséquent de leur capacité à inhiber l'effet de la nociceptine, ces composés sont utiles comme analgésiques, agents anti-obésité, médicaments améliorant la fonction cérébrale, traitements de la maladie d'Alzheimer, de la démence, de la schizophrénie, de maladies neurodégénératives rétrogrades, antidépresseurs, traitements du diabète insipide, de la polyurée, de l'hypotension, etc..

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