Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD.
SAR around alkyne-quinuclidine derivatives allowed the discovery of highly potent muscarinic antagonists displaying interesting preferential slow off-rates from the M3 receptor.
Starck
Jean-Philippe
JP
UCB, R&D, Chemin du Foriest, B-1420 Braine-L'Alleud, Belgium.
Provins
Laurent
L
Christophe
Bernard
B
Gillard
Michel
M
Jadot
Sophie
S
Lo Brutto
Patrick
P
Quéré
Luc
L
Talaga
Patrice
P
Guyaux
Michel
M
D000480:Alkynes / Q000737:chemistry*; D018680:Cholinergic Antagonists / Q000737:chemistry; D015394:Molecular Structure; D018727:Muscarinic Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy*; D011812:Quinuclidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D043585:Receptor, Muscarinic M2 / Q000378:metabolism; D043587:Receptor, Muscarinic M3 / Q000378:metabolism; D013329:Structure-Activity Relationship
D000480:Alkynes; D018680:Cholinergic Antagonists; D018727:Muscarinic Antagonists; D011812:Quinuclidines; D043585:Receptor, Muscarinic M2; D043587:Receptor, Muscarinic M3