869112-31-2Relevant articles and documents
Quinuclidine derivative, method for preparing same and application of quinuclidine derivative
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Paragraph 0114-0115; 0124-0125, (2017/10/13)
The invention relates to a quinuclidine derivative, a pharmaceutically acceptable salt, pro-drug and solvent compound of the quinuclidine derivative, a method for preparing the quinuclidine derivative, a drug composition with the quinuclidine derivative and the pharmaceutically acceptable salt, pro-drug and solvent compound and pharmaceutical application of the quinuclidine derivative. The quinuclidine derivative, the pharmaceutically acceptable salt, pro-drug and solvent compound, the method, the drug composition and the pharmaceutical application have the advantage that the compound is excellent in M3 receptor antagonist activity and accordingly can be used as a novel efficient drug for chronic obstructive pulmonary diseases.
Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists
Lainé, Dramane I.,McCleland, Brent,Thomas, Sonia,Neipp, Christopher,Underwood, Brian,Dufour, Jeremy,Widdowson, Katherine L.,Palovich, Michael R.,Blaney, Frank E.,Foley, James J.,Webb, Edward F.,Luttmann, Mark A.,Burman, Miriam,Belmonte, Kristen,Salmon, Michael
experimental part, p. 2493 - 2505 (2010/03/04)
A novel 4-hydroxyl(diphenyl)methyl substituted quinuclidine series was discovered as a very promising class of muscarinic antagonists. The structure-activity relationships of the connectivity of the diphenyl moiety to the quinuclidine core and around the ring nitrogen side chain are described. Computational docking studies using an homology model of the M3 receptor readily explained the observed structure-activity relationship of the various compounds. Compound 14o was identified as a very potent, slowly reversible M3 antagonist with a very long in vivo duration of bronchoprotection.
Muscarinic acetylcholine receptor antagonists
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Page/Page column 11, (2008/06/13)
Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.