Dual inhibitors of the histamine H1 and neurokinin NK1 receptors for the treatment of allergic diseases

Abstract

Both histamine and substance P are present during an acute allergic reaction. Interaction of these mediators with their respective receptors, i.e., the H₁ receptor and the NK₁ receptor, results in very similar symptoms, including bronchoconstriction, plasma extravisation and mucus secretion. Simultaneous blockade of both of these receptors may therefore lead to compounds with increased clinical efficacy over the corresponding monotherapies. These patents disclose novel compounds based on the H₁ antihistamine astemizole and the NK₂ antagonist SR 48968 which are claimed to be dual antagonists of the H₁ and NK₁ receptors.

• dual antagonists
• H1 antagonist
• histamine
• NK1
• substance P
• tachykinins