1-SUBSTITUTED ALKYLQUINOXALINE DERIVATIVE AND USE THEREOF

PURPOSE:To provide a new compound having high affinity for serotonin 1A receptor, thus useful as a medicine for serotonin neurally related diseases such as antianxiety agents, antidepressants, hypotensive agents, or antiemetic agents. CONSTITUTION:The compound of formula I (R1 is H or methyl; R2 is...

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Bibliographische Detailangaben
Hauptverfasser: SAITO SATORU, MOCHIZUKI DAISUKE, YASO MASAO, SUZUKI YUKIO
Format: Patent
Sprache:eng
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Zusammenfassung:PURPOSE:To provide a new compound having high affinity for serotonin 1A receptor, thus useful as a medicine for serotonin neurally related diseases such as antianxiety agents, antidepressants, hypotensive agents, or antiemetic agents. CONSTITUTION:The compound of formula I (R1 is H or methyl; R2 is 2-pyridyl, 2-pyrimidinyl, or 1,2-benzo-3-isothiazolyl; n is 2-4), e.g. 1-[2-{-(2-pyridinyl)-1- piperazinyl}ethyl]-1,2-dihydro-2-oxoquinoxaline. The compound of the formula I can be obtained by reaction of a compound of formula II (X is eliminable group) with a compound of formula III in an inert solvent (e.g. benzene) pref. in the presence of a deacidifying agent (e.g. triethylamine) at room temperature to elevated temperatures (e.g. the solvent refluxing temperature). Among the present compounds, there are those with high affinity for adrenaline alpha-1 receptor and those with low affinity therefor; thus, appropriate compounds can be selected from the present compounds and used depending on causes and symptoms corresponding to the diseases to be cured.