Discovery of Clinical Candidate CHF-6366: A Novel Super-soft Dual Pharmacology Muscarinic Antagonist and β2 Agonist (MABA) for the Inhaled Treatment of …

L Carzaniga, ID Linney, A Rizzi… - Journal of Medicinal …, 2022 - ACS Publications
The development of molecules embedding two distinct pharmacophores acting as
muscarinic antagonists and β2 agonists (MABAs) promises to be an excellent opportunity to …

Discovery, Multiparametric Optimization, and Solid-State Driven Identification of CHF-6550, a Novel Soft Dual Pharmacology Muscarinic Antagonist and β2 Agonist …

L Carzaniga, ID Linney, A Rizzi… - Journal of Medicinal …, 2024 - ACS Publications
Clinical guidelines for COPD and asthma recommend inhaled β-adrenergic agonists,
muscarinic antagonists, and, for frequent exacerbators, inhaled corticosteroids, with the …

Dual-Pharmacology Muscarinic Antagonist and β2 Agonist Molecules for the Treatment of Chronic Obstructive Pulmonary Disease

AD Hughes, LH Jones - Future Medicinal Chemistry, 2011 - Taylor & Francis
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 …

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 …

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 receptor antagonists for the treatment of respiratory disease

M Cazzola, C Page, MG Matera - Pulmonary Pharmacology & Therapeutics, 2013 - Elsevier
The use of muscarinic receptor antagonists in the treatment of chronic obstructive pulmonary
disease (COPD) is well established. More recently, the potential for long-acting muscarinic …

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 …

Pharmacological preclinical characterization of LAS190792, a novel inhaled bifunctional muscarinic receptor antagonist/β2-adrenoceptor agonist (MABA) molecule

M Aparici, C Carcasona, I Ramos, JL Montero… - Pulmonary …, 2017 - Elsevier
LAS190792 is a novel muscarinic antagonist and β 2-adrenoceptor agonist in development
for chronic respiratory diseases. This study investigated the pharmacological profile of …

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 …