PURPOSE: To obtain the novel derivative useful for preventing and treating higher tension, heart disease, asrthma, inflammation, etc., having inhibitory activity against CGMP phosphodiesterase and inhibitory activity against thromboxane A2 synthase, comprising a 4-aminopyrimidine derivative.
CONSTITUTION: A new 4-aminopyrimidine derivative of formula I (A is single bond, 1-4C alkylene or 1-4C oxyalkylene; Y is single bond, 1-4C alkylene, 1-4C alkylenoxy or l-4C alkoxyphenylene ring; Z is single bond or vinylene; R1 is 4-to 15-membered hetero ring containing 1 to 2 nitrogen atoms, 5-15C carbon ring, etc.; R2 is 4- to 1-membered hetero ring containing 1 to 2 nitrogen atoms, 1 to 2 oxygen atoms and one sulfur atom, 4- to 15carbon ring, etc. ; R3 is 5- to 15-membered hetero ring containing 1 to 2 nitrogen atoms, one oxygen atom, one sulfur atom or one nitrogen atom and one sulfur atom, etc. ; (1) is 1 or 2). The compound is obtained by reacting a pyrimidine derivative of formula II (R1b is Z-R1, etc.) with an amine compound of the formula H2N-Y-R2.
KONISHI YOSHITAKA
ORESUTO TARASU MASHIINA
KONDOU NORIMOTO
DEINUEI TEIMU YUU
TAMARA AN MISUKOUSUKII
