Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and β2 agonist (MABA) for the treatment of chronic obstructive pulmonary disease …

F Rancati, ID Linney, A Rizzi, M Delcanale… - Bioorganic & Medicinal …, 2021 - Elsevier
The targeting of both the muscarinic and β-adrenergic pathways is a well validated
therapeutic approach for the treatment of chronic obstructive pulmonary disease (COPD). In …

Dual-pharmacology muscarinic antagonist and β2 agonist molecules for the treatment of chronic obstructive pulmonary disease

AD Hughes, LH Jones - Future Medicinal Chemistry, 2011 - Future Science
Chronic obstructive pulmonary disease (COPD) is one of the leading causes of death in the
world today. Bronchodilators, particularly muscarinic antagonists and β2 agonists, are …

Multivalent dual pharmacology muscarinic antagonist and β2 agonist (MABA) molecules for the treatment of COPD

AD Hughes, A McNamara, T Steinfeld - Progress in medicinal chemistry, 2012 - Elsevier
Abstract Inhaled beta-2-adrenergic receptor (β 2) agonists and inhaled muscarinic
acetylcholine antagonists are the most frequently used bronchodilators in the treatment of …

Discovery of (R)-1-(3-((2-Chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1 …

AD Hughes, Y Chen, SS Hegde, JR Jasper, S Jaw-Tsai… - 2015 - ACS Publications
Through application of our multivalent approach to drug discovery we previously reported
the first discovery of dual pharmacology MABA bronchodilators, exemplified by 1. Herein we …

Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules

AD Hughes, KH Chin, SL Dunham, JR Jasper… - Bioorganic & medicinal …, 2011 - Elsevier
We sought to design dual pharmacology bronchodilators targeting both the M3 muscarinic
acetylcholine and beta-2 adrenergic (β2) receptors by applying our multivalent approach to …

Long acting muscarinic antagonists for the treatment of chronic obstructive pulmonary disease: a review of current and developing drugs

MA Mastrodicasa, CA Droege, AM Mulhall… - Expert opinion on …, 2017 - Taylor & Francis
Introduction: Long acting muscarinic receptor antagonists (LAMA) reverse airflow obstruction
by antagonizing para-sympathetic bronchoconstricting effects within the airways. For years …

Muscarinic antagonist-β-adrenergic agonist dual pharmacology molecules as bronchodilators: a patent review

NC Ray, L Alcaraz - Expert Opinion on Therapeutic Patents, 2009 - Taylor & Francis
Background: The proven efficacy of several anti-cholinergics and β2-agonists and their
combinations in both chronic obstructive pulmonary disease (COPD) and asthma strongly …

New dual-acting bronchodilator treatments for COPD, muscarinic antagonists and β2 agonists in combination or combined into a single molecule

P Norman - Expert Opinion on Investigational Drugs, 2013 - Taylor & Francis
Introduction: It has long been known that combining short-acting muscarinic antagonists and
β2 agonists produces additive effects on the lung function of patients with chronic obstructive …

Inhaled long-acting muscarinic antagonists in chronic obstructive pulmonary disease

J Busch-Petersen, DI Lainé - Future Medicinal Chemistry, 2011 - Future Science
In 2002, the first long-acting muscarinic antagonist, tiotropium bromide (Spiriva®), was
launched as a once-daily bronchodilating agent for the treatment of chronic obstructive …

Preclinical efficacy of THRX-200495, a dual pharmacology muscarinic receptor antagonist and β2-adrenoceptor agonist (MABA)

A McNamara, T Steinfeld, MT Pulido-Rios… - Pulmonary …, 2012 - Elsevier
Combinations of a muscarinic receptor antagonist (MA) and a β2-adrenoceptor agonist (BA)
improve bronchodilation in COPD patients to a greater extent than drugs with either …