54236-99-6Relevant academic research and scientific papers
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X3/P2X2/3 antagonist for the treatment of pain
Carter, David S.,Alam, Muzaffar,Cai, Haiying,Dillon, Michael P.,Ford, Anthony P.D.W.,Gever, Joel R.,Jahangir, Alam,Lin, Clara,Moore, Amy G.,Wagner, Paul J.,Zhai, Yansheng
scheme or table, p. 1628 - 1631 (2009/11/30)
P2X purinoceptors are ligand-gated ion channels whose endogenous ligand is ATP. Both the P2X3 and P2X2/3 receptor subtypes have been shown to play an important role in the regulation of sensory function and dual P2X3/P2X2/3 antagonists offer significant potential for the treatment of pain. A high-throughput screen of the Roche compound collection resulted in the identification of a novel series of diaminopyrimidines; subsequent optimization resulted in the discovery of RO-4, a potent, selective and drug-like dual P2X3/P2X2/3 antagonist.
Process for substituted 5-benzyl-2,4-diamino-pyrimidines
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, (2008/06/13)
A process for preparing a compound of the formula STR1 wherein R1 and R2 are lower alkoxy or taken together are METHYLENEDIOXY; R3 is lower alkyl or hydrogen, which comprises the step of reacting an aromatic compound of the formula STR2 wherein R1, R2 and R3 are as previously described, with a diamino-pyrimidine of the formula STR3 wherein R4 is lower alkoxy, benzyloxy, hydroxy or halogen, in the presence of an inorganic or organic acid selected from the group consisting of ortho-phosphoric acid, poly-phosphoric acid, hydrohalic acids and tri-haloacetic acids, at a temperature in the range of from about 50° C. to about 110° C., is described.
