Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X3/P2X2/3 antagonist for the treatment of pain
The purinoceptor subtypes P2X3 and P2X2/3 have been shown to play a pivotal role in models of various pain conditions. Identification of a potent and selective dual P2X3/P2X2/3 diaminopyrimidine antagonist RO-4
Jahangir, Alam,Alam, Muzaffar,Carter, David S.,Dillon, Michael P.,Bois, Daisy Joe Du,Ford, Anthony P.D.W.,Gever, Joel R.,Lin, Clara,Wagner, Paul J.,Zhai, Yansheng,Zira, Jeff
scheme or table
p. 1632 - 1635
(2009/10/15)
Diaminopyrimidines as P2X3 and P2X2/3 modulators
Compounds of formula (I): wherein R1 and R2 are as defined herein. Also disclosed are methods of making and using the subject compounds.
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Page/Page column 19
(2008/12/08)
Process for synthesis of phenoxy diaminopyrimidine derivatives
A method for preparing a compound of formula I the method comprising treating a compound of formula d with an iodination reagent, to form the compound of formula I, wherein R1, R2 and R3 are as defined herein.
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Page/Page column 21-23
(2010/11/26)
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