Indole derivatives and their use as serotonin receptor ligands

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 417/14 (2006.01) A61K 31/454 (2006.01) A61K 31/475 (2006.01) A61K 31/5415 (2006.01) A61K 31/549 (2006.01) C07D 209/34 (2006.01) C07D 215/22 (2006.01) C07D 215/227 (2006.01) C07D 215/36 (2006.01) C07D 285/10 (2006.01) C07D 285/16 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2351526

A pharmaceutical compound of formula (I) in which R1 and R2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, X is (1) or (2), Y is (3) or (4) where R4 and R5 are each hydrogen, C1-6 alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl, n is 0 or 1, and R3 is -SR6, -SOR6, - SO2R6, -COR6, -CH2OH or -CONHR7, where R6 is C1-6 alkyl and R7 is hydrogen or C1-6 alkyl; provided that when one of R1 and R2 is hydrogen and the other is fluoro, X is (1), Y is (4), R4 and R5 are each hydrogen or C1-6 alkyl, and n is 0, then R3 is not -COR6 or -CONHR7; and salts thereof.

L'invention concerne une composition pharmaceutique de la formule (I) et des sels de cette composition. Dans ladite formule, R?1¿ et R?2¿ sont chacun hydrogène, halo, cyano ou méthyle; la ligne pointillée représente une double liaison facultative, X est représenté par les formules (1) ou (2), Y par les formules (3) ou (4) (dans lesquelles R?4¿ et R?5¿ sont chacun hydrogène, alkyle C¿1-6?, cyclopropyle ou cyclopropyle-alkyle C¿1-6?); n est 0 ou 1; et R?3¿ est SR?6¿,SOR?6¿,SO¿2?R?6¿,COR?6¿,CH¿2?OH ou ONHR?7¿ (R?6¿ étant alkyle C¿1-6?, R?7¿ étant hydrogène ou alkyle C¿1-6?); à condition que, lorsque R?1¿ ou R?2¿ est hydrogène, l'autre soit fluoro, que X soit représenté par la formule (1), Y par la formule (4) (dans laquelle R?4¿ et R?5¿ sont chacun hydrogène ou alkyle C¿1-6?), que n soit 0, et que R?3¿ soit différent deCOR?6¿ ouCONHR?7¿.

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