Thienylazole compound and thienotriazolodiazepine compound

C - Chemistry – Metallurgy – 07 – D

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C07D 409/04 (2006.01) A61K 31/395 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 495/00 (2006.01) C07D 495/14 (2006.01)

Patent

CA 2191756

Thienylazole compounds (I) and thienotriazolodiazepine compounds (II) represented by respective general formulae (I) and (II) (wherein R1 and R2 represent each hydrogen, halogen, C1-C5 alkyl, etc.; -A=B- represents -N=N-, etc.; R3 and R19 represent each hydrogen, C1-C5 alkyl, etc.; Y represents - NHCO-, -NHCONH-, -NHCOO-, etc.; Z1 and Z2 represent each aryl, heteroaryl, etc.; Ar represents halogenated phenyl, etc.; and m represents an integer of 0, 1 to 5). These compounds have CCK and gastrin antagonisms, in particular, a potent CCK-A receptor antagonism and are useful as preventive or remedy for central and peripheral nerve system diseases, such as anxiety and schizophrenia, and digestive diseases, such as pancreatitis, gastrointestinal ulcer, irritable bowel syndrome and constipation.

L'invention concerne des composés thiénylazole (I) et thiénotriazolodiazépine (II). Dans cette formule, R?1¿ et R?2¿ représentent chacun un hydrogène, un halogène, un C¿1?-C¿5?alkyle, etc.; -A=B- représente -N=N-, etc.; R?3¿ et R?19¿ représentent chacun un hydrogène, un C¿1?-C¿5?alkyle, etc.; Y représente -NHCO-, -NHCONH-, -NHCOO-, etc.; Z?1¿ et Z?2¿ représentent chacun un aryle, un hétéroaryle, etc.; Ar représente un phényle halogéné, etc.; et m représente 0 ou un nombre entier entre 1 et 5. Ces composés sont des antagonistes de la CCK et de la gastrine, en particulier ce sont des antagonistes puissants des récepteurs CCK-A et ils sont utiles en thérapie préventive ou curative contre des troubles du système nerveux central et du système nerveux périphérique, tels que l'anxiété et la schizophrénie, ainsi que contre les troubles digestifs tels que la pancréatite, les ulcères gastro-intestinaux, l'irritation du côlon et la constipation.

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