Pyrrolo[3,2-c]quinoline derivatives containing haloalkoxy...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/47 (2006.01)

Patent

CA 2268166

The present invention relates to a novel pyrrolo[3,2-c]quinoline derivatives containing haloalkoxy group, represented by Formula (I), their pharmaceutically acceptable salts; process for preparation thereof; and pharmaceutical composition thereof for treating gastric ulcer. In said Formula R1 is haloatkoxy group of C1-C6 including trifluoromethoxy, difluoromethoxy and trifluoroethoxy group. R2 and R3, which are the same or different, are each hydrogen, halogen hydroxy, benzyloxy, alkyl group of C1-C6, alkoxy group of C1-C6. A is -CH2-CH2- or -CH=CH-, and R4 is hydrogen, halogen amino, alkylamino group of C1-C6 and NH(CH2)n OH in which n is 1-6. Pyrrolo[3,2-c]quinoline derivatives having haloalkoxy group, and their pharmaceutically acceptable salts, which reversibly inhibit gastric acid secretion of mammal, are usefully utilized for gastric ulcer therapeutics.

La présente invention concerne de nouveaux dérivés de pyrrolo[3,2-c]quinoline contenant un groupe haloalcoxy, représentés par la formule (I), leurs sels pharmaceutiquement acceptables, leur procédé de préparation ainsi que leur composition pharmaceutique utile dans le traitement de l'ulcère gastrique. Dans ladite formule R1 représente un groupe haloalcoxy de C1-C6 comprenant un groupe trifluorométhoxy, difluorométhoxy et trifluoroéthoxy. R2 et R3, identiques ou différents, représentent chacun hydrogène, halogène, hydroxy, benzyloxy, un groupe alkyle C1-C6, un groupe alcoxy C1-C6 . A représente -CH2-CH2- ou -CH=CH-, et R4 représente hydrogène, halogène, amino, un groupe alkylamino C1-C6 et NH(CH2)nOH où n est compris entre 1 et 6. Les dérivés de pyrrolo[3,2-c]quinoline présentant un groupe haloalcoxy, ainsi que leurs sels pharmaceutiquement acceptables, lesquels empêchent de manière réversible la sécrétion d'acide gastrique mammifère, sont utilisés utilement en thérapie de l'ulcère gastrique.

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