The Identification of Indacaterol as an Ultralong-Acting Inhaled β2-Adrenoceptor Agonist

F Baur, D Beattie, D Beer, D Bentley… - Journal of medicinal …, 2010 - ACS Publications
Following a lipophilicity-based hypothesis, an 8-hydroxyquinolinone 2-aminoindan derived
series of β2-adrenoceptor agonists have been prepared and evaluated for their potential as …

In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5, 6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel …

C Battram, SJ Charlton, B Cuenoud, MR Dowling… - … of Pharmacology and …, 2006 - ASPET
Here, we describe the preclinical pharmacological profile of 5-[(R)-2-(5, 6-diethyl-indan-2-
ylamino)-1-hydroxy-ethyl]-8-hydroxy-1 H-quinolin-2-one (indacaterol), a novel, chirally pure …

Pharmacological characterization of indacaterol, a novel once daily inhaled β2 adrenoceptor agonist, on small airways in human and rat precision-cut lung slices

RG Sturton, A Trifilieff, AG Nicholson… - Journal of Pharmacology …, 2008 - ASPET
Indacaterol is a novel once daily inhaled β2 adrenoceptor agonist in clinical development.
This study compared the properties of indacaterol with salmeterol, formoterol, and albuterol …

In vitro and in vivo preclinical profile of abediterol (LAS100977), an inhaled long-acting β2-adrenoceptor agonist, compared with indacaterol, olodaterol and vilanterol

M Aparici, A Gavaldà, I Ramos, C Carcasona… - European Journal of …, 2016 - Elsevier
Abediterol is a novel long-acting β 2-adrenoceptor agonist (LABA) currently in development
for once-daily combination maintenance therapy of asthma and COPD. This study …

Indacaterol, a novel inhaled β2-agonist, provides sustained 24-h bronchodilation in asthma

KM Beeh, E Derom, F Kanniess… - European …, 2007 - Eur Respiratory Soc
The present study examined the bronchodilator and safety profiles of single-dose
indacaterol in intermittent or persistent asthma. In the present double-blind crossover study …

Pharmacological characterization of abediterol, a novel inhaled β2-adrenoceptor agonist with long duration of action and a favorable safety profile in preclinical …

M Aparici, M Gomez-Angelats, D Vilella, R Otal… - … of Pharmacology and …, 2012 - ASPET
Abediterol is a novel potent, long-acting inhaled β2-adrenoceptor agonist in development for
the treatment of asthma and chronic obstructive pulmonary disease. Abediterol shows …

The discovery of indole-derived long acting β2-adrenoceptor agonists for the treatment of asthma and COPD

AD Brown, ME Bunnage, PA Glossop… - Bioorganic & medicinal …, 2007 - Elsevier
The design and profile of a series of indole containing long acting β2-adrenoceptor agonists
is described. Evaluation of these analogues using an in vitro guinea pig trachea tissue …

Effect of indacaterol, a novel long-acting β2-agonist, on isolated human bronchi

E Naline, A Trifilieff, RA Fairhurst… - European …, 2007 - Eur Respiratory Soc
Indacaterol is a novel β2-adrenoceptor agonist in development for the once-daily treatment
of asthma and chronic obstructive pulmonary disease. The present study evaluated the …

An investigation into the structure–activity relationships associated with the systematic modification of the β2-adrenoceptor agonist indacaterol

D Beattie, D Beer, ME Bradley, I Bruce… - Bioorganic & medicinal …, 2012 - Elsevier
The synthesis of a series of indacaterol analogues in which each of the three structural
regions of indacaterol are modified in a systematic manner is described. Evaluation of the …

Efficacy and Safety of Indacaterol, a New 24-hour β 2-Agonist, in Patients with Asthma: A Dose-Ranging Study

F Kanniess, LP Boulet, W Pierzchala… - Journal of …, 2008 - Taylor & Francis
Background. Indacaterol is a new once-daily inhaled β2-agonist in clinical development for
asthma as a component of a fixed-dose combination with an inhaled corticosteroid …