Discovery of substituted phenyl urea derivatives as novel long-acting β2-adrenoreceptor agonists

Lead Generation Approaches Delivering Inhaled β 2 ‐Adrenoreceptor Agonist Drug Candidates

“…Scientists at Almirall have reported on their research into the area of uLABAs and discussed their lead generation design concept based on the microkinetic theory in combination with an examination of the impact of lipophilicity [33]. In their approach, they chose to design a series of compounds based on the carbos tyryl moiety present in both indacaterol and carmoterol.…”

Discovery of a Rapidly Metabolized, Long-Acting β2 Adrenergic Receptor Agonist with a Short Onset Time Incorporating a Sulfone Group Suitable for Once-Daily Dosing

“…Other development candidates include Boehringer-Ingelheim’s olodaterol ( 5 ), Pfizer’s candidate PF-610355 ( 6 ), Chiesi’s carmoterol ( 7 ), and Theravance’s milveterol ( 8 ) . In addition further studies were published during the past year describing further compounds at the preclinical stage. − Furthermore, two reviews on bronchodilators were published recently. , Our group reported on sulfonamides including GlaxoSmithKline’s first candidate 9 , on vilanterol ( 4 ), on hydantoins, and on urea saligenin analogues.…”