Dual-acting β₂ agonists/muscarinic antagonists

Abstract

Bifunctional aromatic derivatives that act as both β₂ agonists and muscarinic receptor antagonists are claimed. The compounds use two separate pharmacophoric groups, coupled by a long lipohilic chain, to provide the desired biological activities and with the aim of providing a long duration of action. The compounds are claimed to be useful in the treatment of both asthma and chronic obstructive pulmonary disease and represent the first disclosure of a new concept – muscarinic antagonist–β₂ agonists.

Keywords::

• bronchodilator
• COPD
• muscarinic antagonist–β₂ agonist

Patent details

• Title Dual-acting β₂ agonists/muscarinic antagonists

• Assignee Theravance Inc.

• Inventors Mammen M, Mischki T.

• Priority date 16/08/04

• Filing date 15/08/05

• Publication date 02/03/06

• Publication no. WO2006023457