title: Novel dihydroquinoline-based MABAs; clues to the identity of LAS-190792: evaluation of WO20111411802.
abstract: Bifunctional aromatic compounds are claimed to contain a β(2) agonist pharmacophore linked by a flexible lipophilic spacer incorporating a trans-4-aminocyclohexanol group to a muscarinic antagonist pharmacophore. The compounds display nanomolar affinity at both β(2) and M(3) receptors and a prolonged duration of action in animal models. This application is the first from Almirall claiming such compounds although it has recently disclosed that LAS-190792 is progressing toward clinical development.
authors.affiliation: Norman Consulting, 18 Pink Lane, Burnham, Bucks, SL1 8JW, UK. peter.norman2@btinternet.com
authors.forename: Peter
authors.initials: P
authors.lastname: Norman
mesh_terms: D058666:Adrenergic beta-2 Receptor Agonists / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001993:Bronchodilator Agents / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D018727:Muscarinic Antagonists / Q000737:chemistry / Q000494:pharmacology*; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy* / Q000503:physiopathology; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D058666:Adrenergic beta-2 Receptor Agonists; D001993:Bronchodilator Agents; D018727:Muscarinic Antagonists; D011804:Quinolines