3-piperidinylmethylcarboxylate substituted indoles

C - Chemistry – Metallurgy – 07 – D

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C07D 401/12 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) C07D 209/12 (2006.01) C07D 401/00 (2006.01)

Patent

CA 2105179

2105179 9214727 PCTABS00015 Indole derivatives of formula (I) wherein R1 represents a hydrogen or a halogen atom, or a C1-6alkyl, C1-6alkoxy or hydroxy group; R2 represents a hydrogen atom or a C1-6alkyl, -CH2C2-5alkenyl or -CH2C2-5alkynyl group; R3 represents a hydrogen atom or a C1-6alkyl or C1-6alkoxy group; n represents 2 or 3; R4 represents a group selected from cyano, hydroxyl, C1-6alkoxy, phenoxy, C(O)C1-6alkyl, C(O)C6H5, -CONR5R6, -NR5COR6, -SO2NR5R6 or -NR5SO2R6 (wherein each of R5 and R6 independently represent a hydrogen atom, a C1-6alkyl or phenyl group); and quaternary ammonium derivatives, piperidine N-oxides and pharmaceutically acceptable salts and solvates thereof; which compounds are potent and specific antagonists of 5-hydroxytryptamine (5-HT; seretonin).

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