Fused thiazole derivatives having affinity for the histamine H₃ receptor

Abstract

A group of structurally related thiazoloazepines displaying high affinity for histamine receptors of the H₃ subtype, with pK_i values in the range of 7.5 – 9.5, are disclosed in the latest of a series of such applications from Glaxo. These compounds have potential utility in the treatment of CNS disorders, in particular for the improvement of cognitive deficits and alleviation of some symptoms of Alzheimer’s disease, when administered either alone or in combination with other psychotherapeutic agents, for example, muscarinic M₁ agonists or acetylcholinesterase inhibitors.

Keywords::

• Alzheimer’s disease
• cognition
• H₃
• histamine

Patent details

• Title Fused thiazole derivatives having affinity for the histamine H₃ receptor

• Assignee Bailey N, Pickering PL,Wilson DM

• Inventors Glaxo Group Ltd

• Priority date 14/03/05

• Filing date 10/03/06

• Publication date 21/09/06

• Publication no. WO2006097691