Benzodiazepine derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 403/04 (2006.01) A61K 31/55 (2006.01) C07D 401/04 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01)

Patent

CA 2169089

A benzodiazepine derivative of formula I, or a pharmaceutically acceptable salt thereof: Image I wherein: (a) R4 is an alkyl, cycloalkyl or aryl group. (b) R10 is chosen from halo, OH, CH3, OCH3, NR11R12, NO2, NHCHO, CO2H and CN, and R11 and R12 are independently selected from H and alkyl (C1 - C5) or together NR11R12 form a cyclic structure II, Image II wherein a is 1 - 6; and (c) R2 is an aromatic 5- or 6-membered, substituted or unsubstituted heterocyclecontaining at least two heteroatoms of which at least one is nitrogen. These compounds are gastrin and/or CCK-B receptor antagonists.

Dérivé de benzodiazépine de la formule (I), ou sel pharmaceutiquement acceptable de celui-ci. Dans la formule, (a) R<4> représente un groupe alcoyle, cycloalcoyle ou aryle; (b) R<10> est sélectionné parmi halo, OH, CH3, OCH3, NR<11>R<12>, NO2; NHCHO, CO2H et CN, et R<11> et R<12> sont sélectionnés indépendamment entre H et alcoyle (C1-C5) ou NR<11>R<12> ensemble forment une structure cyclique (II), où a est compris entre 1 et 6; et (c) R<2> représente un hétérocycle aromatique à 5 ou 6 éléments, avec ou sans substitution, qui contient au moins deux hétéroatomes dont l'un au moins est un atome d'azote. Ces composés sont des antagonistes des récepteurs de la gastrine et/ou de la CCK-B.

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