Phenylalkynes to treat histamine mediated conditions

Abstract

With the identification of additional receptor subtypes for histamine, research into the discovery of compounds capable of regulating this neurotransmitter has rapidly expanded. This patent application, one of many recent publications from Ortho-McNeil, discloses a unique series of non-imidazole histamine receptor ligands designed to treat CNS and upper respiratory system disorders. The compounds included in this case incorporate an arylacetylene fragment that serves as a spacer between two basic amine groups; in vitro binding values are presented but no information is provided regarding selectivity for histamine H₃ over other histamine receptor subtypes or other G-protein-coupled receptors.

• allergic rhinitis
• CNS disorders
• H3
• histamine
• phenylalkyne