931409-69-7Relevant academic research and scientific papers
Inhalation by design: Novel tertiary amine muscarinic M3 receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease
Glossop, Paul A.,Watson, Christine A. L.,Price, David A.,Bunnage, Mark E.,Middleton, Donald S.,Wood, Anthony,James, Kim,Roberts, Dannielle,Strang, Ross S.,Yeadon, Michael,Perros-Huguet, Christelle,Clarke, Nicholas P.,Trevethick, Michael A.,MacHin, Ian,Stuart, Emilio F.,Evans, Steven M.,Harrison, Anthony C.,Fairman, David A.,Agoram, Balaji,Burrows, Jane L.,Feeder, Neil,Fulton, Craig K.,Dillon, Barry R.,Entwistle, David A.,Spence, Fiona J.
, p. 6888 - 6904 (2011)
A novel tertiary amine series of potent muscarinic M3 receptor antagonists are described that exhibit potential as inhaled long-acting bronchodilators for the treatment of chronic obstructive pulmonary disease. Geminal dimethyl functionality pr
Development of a scaleable synthesis of a geminal dimethyl tertiary amine as an inhaled muscarinic antagonist for the treatment of COPD
Dillon, Barry R.,Roberts, Dannielle F.,Entwistle, David A.,Glossop, Paul A.,Knight, Craig J.,Laity, Daniel A.,James, Kim,Praquin, Celine F.,Strang, Ross S.,Watson, Christine A. L.
supporting information; experimental part, p. 195 - 203 (2012/06/05)
An efficient and scalable process for the synthesis of muscarinic antagonist, PF-3635659 1, is described, illustrating redesign of an analogue-targeted synthesis which contained a scale-limiting rhodium-activated C-H amination step. The final route includes a reproducible modified Bouveault reaction which has not previously been reported on a substrate of this complexity, or on such a scale with over 5 kg of the requisite gem-dimethylamine prepared via this methodology.
CARBOXAMIDE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS
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Page/Page column 41, (2008/06/13)
The invention relates to compounds of Formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
