Scaffold-hopping with zwitterionic CCR3 antagonists: Identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092
The discovery and optimisation of a series of zwitterionic CCR3 antagonists is described. Optimisation of the structure led to AZ12436092, a compound with excellent selectivity over activity at hERG and outstanding pharmacokinetics in preclinical species.
Barton, Patrick,Caffrey, Moya V.,Linannen, Tero,Luckhurst, Christopher A.,Mochel, Tobias,Perry, Matthew W. D.,Springthorpe, Brian,Stein, Linda,Bahl, Ash,Bowers, Keith,Gilmour, Peter,Hawley, Shaun,Denton, Rebecca,Riley, Robert J.,Roe, Emma,Webborn, Peter
supporting information
p. 6694 - 6699,6
(2012/12/12)
NOVEL PIPERIDINE DERIVATIVES
The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.
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Page/Page column 55-56
(2010/11/25)
CHEMICAL COMPOUNDS
The present invention provides a compound of a formula (I) wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
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Page 39
(2008/06/13)
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