4-oxoimidazolidine-2-spiropiperidine derivatives

Details 4-oxoimidazolidine-2-spiropiperidine derivatives 4-oxoimidazolidine-2-spiropiperidine derivatives

C - Chemistry, Metallurgy

07

D

C07D 471/10 (2006.01) A61K 31/438 (2006.01) A61P 1/00 (2006.01) A61P 3/04 (2006.01) A61P 7/12 (2006.01) A61P 11/06 (2006.01) A61P 11/08 (2006.01) A61P 11/14 (2006.01) A61P 15/10 (2006.01) A61P 23/00 (2006.01) A61P 25/04 (2006.01) A61P 25/16 (2006.01) A61P 25/18 (2006.01) A61P 25/20 (2006.01) A61P 25/22 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01) A61P 25/36 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2454785

The invention relates to 4-oxoimidazolidine-2-spiropiperidine derivatives represented by a general formula [I] (see formula I) [in which A1, A2, A3, A4 and A5 stand for optionally halogen- substituted methine, or nitrogen atom; R1 and R2 stand for lower alkyl or the like; R3 stands for hydrogen or lower alkyl; R4 and R5 stand for hydrogen, or lower alkyl which is optionally substituted with hydroxy, or the like] or salts thereof. These compounds act as nociceptin receptor agonist, and are useful as analgesic, reliever from tolerance to narcotic analgesic, reliever from dependence on narcotic analgesic, analgesic enhancer, antiobestic, drug for ameliorating brain function, remedy for schizophrenia, drug for treating regressive neurodegenerative diseases, antianxiety agent or antidepressant and remedy for diabetes insipidus and polyuria; and the like.

L'invention concerne un dérivé de 4-oxoimidazolidine-2-spiropipéridine représenté par la formule générale (I) (dans laquelle A¿1?, A¿2?, A¿3?, A¿4? et A¿5? représentent chacun un groupe méthine facultativement halogéné ou l'azote; R?1¿ et R?2¿ représentent chacun alkyle inférieur, etc.; R?3¿ représente hydrogène ou alkyle inférieur; et R?4¿ ainsi que R?5¿ représentent chacun hydrogène ou alkyle inférieur facultativement substitué par hydroxy, etc.) ou bien un sel du dérivé. Le composé fait office d'agoniste du récepteur de nociceptine et il est utile en tant qu'analgésique, agent destiné à vaincre la tolérance aux analgésiques narcotiques, activateur d'analgésie, agent antiobestique, améliorant des fonctions cérébrales, remède contre la schizophrénie, remède contre les maladies nerveuses dégénératives, agent anxiolytique ou antidépresseur, agent thérapeutique contre le diabète insipide, remède contre la polyurie, etc.

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