Benzimidazolone derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/14 (2006.01) A61K 31/454 (2006.01) A61K 31/4545 (2006.01) A61K 31/497 (2006.01) A61K 31/55 (2006.01) A61P 1/00 (2006.01) A61P 1/08 (2006.01) A61P 1/16 (2006.01) A61P 1/18 (2006.01) A61P 13/00 (2006.01) A61P 17/00 (2006.01) A61P 17/04 (2006.01) A61P 25/04 (2006.01) A61P 25/14 (2006.01) A61P 25/16 (2006.01) A61P 43/00 (2006.01) C07D 409/14 (2006.01)

Patent

CA 2444595

Benzimidazolone derivatives typified by compounds represented by the following general formula [I] and so on: wherein R1 and R2 represent each hydrogen, etc.; R3a, R3b, R4 and R5 represent each hydrogen, alkyl, etc.; R6 represents aryl, heteroaryl, etc.; the ring A represents a 5- to 8-membered aliphatic heterocycle having a nitrogen atom; and Z represents carbonyl or sulfonyl. Because of having an antagonistic effect to muscarinic acetylcholine receptor, the above benzimidazolone derivatives are useful as remedies and/or preventives for, e.g., Parkinson's disease, drug-induced Parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary mobility function error, achalasia, pain, itch, choline urticaria, irritable bowel syndrome, vomiting, vomiturition, stagger, Meniere's disease, rolling diseases such as space sickness, sea sickness and car sickness and urinary errors.

L'invention concerne des dérivés de benzimidazolone caractérisés par des composés représentés par la formule générale (I), dans laquelle R?1¿ et R?2¿ représentent chacun hydrogène, etc. ; R?3a¿, R?3b¿, R?4¿ et R?5¿ représentent chacun hydrogène, alkyle, etc. ; R?6¿ représente aryle, hétéroaryle, etc. ; le cycle A est un hétérocycle aliphatique à 5, 6, 7 ou 8 chaînons renfermant un atome d'azote et Z représente carbonyle ou sulfonyle. Du fait de leur effet antagoniste au niveau du récepteur de l'acétylcholine muscarinique, les dérivés de benzimidazolone susmentionnés sont utilisés comme remèdes curatifs et/ou prophylactiques contre, p. ex., la maladie de Parkinson, le parkinsonisme médicamenteux, la dystonie, l'akinésie, la pancréatite, les calculs biliaires/la cholécystite, le dysfonctionnement de la mobilité biliaire, l'achalasie, les douleurs, le prurit, l'urticaire cholinergique, le syndrome du côlon irritable, les vomissements, la vomiturition, les vertiges, la maladie de Ménière, les maladies des transports telles que le mal de l'espace, le mal de mer et le mal de l'automobile ainsi que des troubles urinaires.

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