Condensed benzazepine derivative and pharmaceutical...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/55 (2006.01) C07C 233/81 (2006.01) C07D 209/48 (2006.01) C07D 223/16 (2006.01) C07D 498/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2167673

This invention relates to nitrogen-containing aromatic 5-membered ring-condensed benzazepine derivatives represented by the general formula (I) Image (symbols in the formula have the following meanings; ring B: a nitrogen-containing aromatic 5-membered ring having at least 1 nitrogen atom and optionally one oxygen or sulfur atom, which may optionally have substituent(s), R1 and R2: these may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group which may optionally be substituted by lower alkyl group(s), or a lower alkoxy group, A: a single bond; a group represented by the formula -NHCO-(CR3R4)n-, n: 0 or an integer of from 1 to 3, R3 and R4: these may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group (provided that R3 and R4 may together form a lower alkylene group having 2 to 7 carbon atoms), and ring C: a benzene ring which may optionally have substituent(s)) and salts thereof; to pharmaceutical compositions which contain these compounds as an active ingredient and to intermediates which are useful in synthesizing these compounds. The compounds of this invention are useful as arginine vasopressin antagonists.

Dérivé de benzazépine de fusion à 5 éléments aromatiques azotés, représenté par la formule générale (I), utile comme antagoniste de l'arginine-vasopressine, ou sel de ce dérivé et composition pharmaceutique renfermant ce dérivé comme principe actif. Dans cette formule B représente une liaison à 5 éléments aromatiques azotés pouvant être substitués et comportant au moins un atome d'azote et, éventuellement, un atome d'oxygène ou un atome de soufre; R<1> et R<2> représente chacun indépendamment hydrogène, halogène, alkyle inférieur, amino pouvant être substitué par alkyle inférieur, ou alkoxy inférieur; A représente une liaison unique ou -NHCO-(CR<3>R<4>)n-; n représente un entier de 0 à 3; R<3> et R<4> représente chacun indépendamment hydrogène ou alkyle inférieur, sous réserve que R<3> et R<4> puissent être combinés ensemble pour former C2-C7 alkylène; et C représente une liaison benzènique facultativement substituée.

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