Quarternary ammonium compounds and their use as...

C - Chemistry – Metallurgy – 07 – C

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C07C 215/66 (2006.01) A61K 31/14 (2006.01) A61K 31/222 (2006.01) A61K 31/40 (2006.01) A61K 31/452 (2006.01) A61K 31/55 (2006.01) A61P 11/00 (2006.01) C07C 217/62 (2006.01) C07C 219/28 (2006.01) C07D 295/096 (2006.01)

Patent

CA 2464223

Novel quaternary ammonium compounds of the formula (I) and any stereoisomers thereof, wherein, R1, R2, and R3 independently represent C1-C6 alkyl, optionally substituted with phenyl or hydroxyl, or both, and wherein any two of R1, R2 and R3 may form a ring together with the quaternary ammonium nitrogen; R4 represents -H, -CH3, or -CO-R4-1, wherein R4-1 represents -(C1-C4 alkyl), -(C1-C4 alkoxy), or NR4-2R4-3, wherein R4-2 and R4-3 independently represent -H or -(C1-C4 alkyl); R5, R6 and R7 independently represent -H, - OCH3, -OH, -CONH2, -SO2NH2, -F, -Cl, -Br, -I, -CF3, or -(C1-C4 alkyl), optionally substituted with one or two -OH, -(C1-C4 alkoxy), -COOH, or -CO-O- (C1-C3 alkyl); and X represents an anion of a pharmaceutically acceptable acid, the compounds for use as medicaments, use of the compounds for the manufacture of specific medicaments, and pharmaceutical compositions comprising the compounds. The present invention also concerns a method of treatment involving administration of the compounds.

Nouveaux composés d'ammonium quaternaire représentés par formule (I) et leurs stéréoisomères, dans laquelle R¿1?, R¿2?, et R¿3? Représentent indépendamment alkyle C¿1?-C¿6?, éventuellement substitué par phényle ou hydorxyle ou les deux et dans laquelle toute paire constituée par R¿1?, R¿2? ou R¿3? peut constituer un noyau avec l'azote de l'ammonium quaternaire; R¿4? représente -H, -CH¿3?, ou -CO-R¿4-1?, R¿4-1? représentant alkyle C¿1?-C¿4?, alkoxy C¿1?-C¿4?, ou NR¿4-2?R¿4-3?, R¿4-2? et R¿4-3? représentant indépendamment -H ou alkyle C¿1?-C¿4?; R¿5?, R¿6? et R¿7? représentent indépendamment -H, -OCH¿3?, -OH, -CONH¿2?, -SO¿2?NH¿2?, -F, -Cl, -Br, -I, -CF¿3?, ou alkyle C¿1?-C¿4? éventuellement substitué par un ou deux -OH, alkoxy C¿1?-C¿4?, -COOH, ou -CO-O- alkyle C¿1?-C¿3?; X représente un anion d'acide acceptable sur le plan pharmaceutique, ces composés étant conçus pour être utilisés comme médicaments spécifiques. L'invention concerne également des compositions pharmaceutiques contenant ces composés, ainsi qu'une méthode de traitement consistant à administrer ces composés.

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