61310-39-2Relevant articles and documents
2, 6 BISHETEROARYL-4-AMINOPYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS
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Page/Page column 103, (2010/02/12)
4-Aminopyrimidine derivatives of formula (I) FORMULA heteroaryl groups, including pharmaceutically acceptable salts thereof, wherein R1 and R2 are adenosine A2A receptor antagonists useful in the treatment of movement disorders such as Parkinson's disease.
N-[2-(pyridinyl)-4-pyrimidinyl]ureas
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, (2008/06/13)
Compounds useful as anti-allergic agents are N-R3 -N-R4 -N'-R-N'-(2-Q-5-R1 -6-R2 -4-pyrimidinyl)ureas (I), where Q is 4- or 3- or 2-pyridinyl or 4- or 3- or 2-pyridinyl having one or two lower-alkyl substituents or N-oxide thereof, R is hydrogen or lower-alkyl, R1 is hydrogen, lower-alkyl or cyano, R2 is hydrogen or lower-alkyl, R3 is hydrogen, lower-alkyl or lower-hydroxyalkyl, R4 is hydrogen, lower-alkyl, lower-hydroxyalkyl, lower-alkenyl or lower-cycloalkyl. Said ureas are prepared by reacting 2-Q-4-RNH-5-R1 -6-R2 -pyrimidine (II) with a carbamylating agent selected from an R4 '-isocyanate of the formula R4 'N=C=O to produce N-R4 '-N'-R-N'-(2-Q-5-R1 -6-R2 -4-pyrimidinyl)urea (IA), an N-R3 '-N-R4 '-carbamyl halide of the formula R3 'R4 'NC(=O)-halide to produce N-R3 '-N-R4 'N'-R-N'-(2-Q-5-R1 -6-R2 -4-pyrimidinyl)urea (IB) or 1,1'-carbonyldiimidazole to produce N-(2-Q-5-R1 -6-R2 -4-pyrimidinyl)-N-R-imidazole-1-carboxamide and then reacting said 1-carboxamide with R3 R4 NH to produce I.
N-(2-(pyridinyl)-4-pyrimidinyl)-aminomethylenemalonates and analogs
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, (2008/06/13)
Compounds useful as anti-allergic agents are 2-Q-4-[XZC=C(R)NH]-5-R1 -6-R2 -pyrimidines (I), where Q is 4- or 3- or 2-pyridinyl or 4- or 3- or 2-pyridinyl having one or two lower-alkyl substituents or N-oxide thereof, R is hydrogen or lower-alkyl, R1 is hydrogen, lower-alkyl or cyano, R2 is hydrogen, lower-alkyl, hydroxy or halo, X and Z are the same or different and are each selected from lower-carbalkoxy, lower-alkanoyl, carbamyl and cyano, or STR1 where R3 and R4 are each lower-alkyl, or X is hydrogen, are prepared by reacting 4-amino-2-Q-5-R1 -6-R2 -pyrimidine (II where Q' is amino) with R'O-C-(R)=CXZ (III). Preparations of II are given. Also shown as intermediates and/or anti-allergic agents are 4-(AcNH)-2-Q-5-R1 -6-R2 -pyrimidines (IV) and 4-(R5 R6 N)-2-Q-5-R1 -6-R2 -pyrimidines (V) where Ac is lower-alkanoyl or lower-carbalkoxy, R5 is hydrogen, lower-alkyl or lower-hydroxyalkyl, and R6 is lower-alkyl or lower-hydroxyalkyl.