2-(4-piperidinyl)-1h-pyrido¬4,3-b|indol-1-ones and related...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/445 (2006.01) A61K 31/55 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/00 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01)

Patent

CA 2052424

The present invention relates to novel 2-(4-piperidinyl)-1H-pyrido[4,3-b]indol- 1- ones and related compounds, intermediates and processes for the preparing thereof. In particular, the present invention provides compounds of formula 1 (see formula I) wherein R1 is hydrogen, loweralkyl, phenyl, phenyl substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups, phenylloweralkyl or phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups; R2 is hydrogen, loweralkyl, furanylloweralkyl, thienylloweralkyl, pyrrolylloweralkyl, pyridinylloweralkyl, phenylloweralkyl, phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups, or a group of the formula (see formula II) wherein R3 is loweralkyl, haloloweralkyl, haloloweralkyl, phenyl, phenyl substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups, phenylloweralkyl, or phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups; X is hydrogen, loweralkyl, loweralkoxy, halogen, or trifluoromethyl; m is 0, 1, or 2; n is 1 or 2; an optical isomer thereof, or a pharmaceutically acceptable salt thereof. The compounds of the invention show antipsychotic activity and can therefore be used as medicaments.

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