Substituted tetracyclic oxazepine and thiazepine derivatives...

Details Substituted tetracyclic oxazepine and thiazepine derivatives... Substituted tetracyclic oxazepine and thiazepine derivatives...

C - Chemistry, Metallurgy

07

D

C07D 498/04 (2006.01) A61K 31/55 (2006.01) C07D 267/20 (2006.01) C07D 281/16 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2203664

This invention concerns the compounds of Formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. In said formula, R1 and R2 each independently are hydrogen; C1-6 alkyl; C1-6 alkylcarbonyl; trihalomethylcarbonyl; C1-6 alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6 alkylcarbonyloxy, C1-6 alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 to R10 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluormethoxy, carboxyl, nitro, amino, mono-or di(C1- 6alkyl)amino, C1-6 alkylcarbonylamino, aminosulfonyl, mono-or di(C1-6alkyl)- aminosulfonyl, C1-6 alkyl, C1-6 alkyloxy, C1-6alkylcarbonyl, C1-6 alkyloxycarbonyl; R11 is hydrogen, C1-6alkyl, or trifluoromethyl; R12 is hydrogen, C1-6 alkyl, cyano, or trifluorotmethyl; n is zero to 6; and X is O, S, S(=O) or S(=O)2. The compounds of formula (I)may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

La présente invention concerne les composés représentés par la formule générale (I), leurs sels acceptables du point de vue pharmaceutique, leurs formes stéréo-isomères, ainsi que leurs formes N-oxyde. Dans cette formule, R?1¿ et R?2¿ sont chacun indépendamment hydrogène, C¿1-6?alkyle, C¿1-6?alkylocarbonyle, C¿1-6?alkylocarbonyloxy, C¿1-6?alkylocarbonyle, ou aryle; ou bien, R?1¿ et R?2¿ pris ensemble avec l'atome d'azote auquel ils sont attachés peuvent former un noyau morpholinyle ou un hétérocycle éventuellement substitué; R?3¿ à R?10¿ sont chacun indépendamment hydrogène, halo, cyano, hydroxy, trifluorométhyle, trifluorométhoxy, carboxyle, nitro, amino, mono- ou di(C¿1-6?alkyl)-amino, C¿1-6?alkylocarbonylamino, aminosulfonyle, mono- ou di(C¿1-6?alkyl)-aminosulfonyle, C¿1-6?alkyloxy-carbonyle; R?7¿ et R?8¿ sont chacun indépendamment hydrogène, hydroxy, C¿1-6?alkyle, C¿1-6?alkyloxy, C¿1-6?alkylocarbonyle, C¿1-6?alkyloxy-carbonyle; R?11¿ est hydrogène, C¿1-6?alkyle ou trifluorométhyle; R?12¿ est hydrogène, C¿1-6?alkyle, cyano ou trifluorométhyle; n est un entier valant de zéro à 6, et X appartient au groupe formé par les O, S, S(=O) ou S(=O)¿2?. Ces composés représentés par la formule (I) sont utilisables comme agents thérapeutiques dans le traitement ou la prévention des troubles du système nerveux central, des troubles cardio-vasculaires ou des troubles gastro-intestinaux.

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