7-Phenylsulfonyl-tetrahydro-3-benzazepine derivatives as antipsychotic agents

Abstract

A series of structurally related arylsulfonyl substituted 3-benzazepines displaying dopamine and serotonin antagonist activities, with pK_i values in the range of 6.7 – 8.8, are disclosed in three applications from Glaxo. These compounds are claimed to have potential for the treatment of schizophrenia and other CNS disorders, either alone or in combination with other medications. WO2005051399 describes the synthesis and physicochemical properties of 7-[4-(3-fluoro-4-methylbenzyl)-benzensulfonyl]-8-methoxy-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and its tosylate.

Keywords::

• benzazepine
• cognition
• dopamine
• schizophrenia
• serotonin