发明名称 Aminopyrimidine derivatives, their preparation, and pharmaceutical compositions thereof; useful for inhibiting nitric oxide synthase activity
摘要 A compound of formula (I) and a process for preparing this compound, wherein: R1 is H, alkyl, alkoxy, halogen or trifluoromethyl; R2 represents H or alkyl; A represent a five membered heterocyclic aromatic ring containing 1-3 heteroatoms which may be the same or different and which are selected from O, N and S; or A is a six membered heterocyclic aromatic ring containing 1-3 N atoms; i) R3 represents phenyl, or a six membered heterocyclic aromatic ring containing 1-3 N atoms, or a five-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may be the same or different and are selected from O, N and S, which phenyl or heterocyclic aromatic ring may be optionally substituted; and R4 represents H or alkyl; or ii) R3 represents alkyl, alkenyl, or alkynyl and R4 represents H or alkyl; or iii) R3 and R4 together represent (CH2)a -Z-(CH2)b, where Z represents N(COOR7), or iv) R3 and R4 together represent (CH2)a -Z-(CH2)b, where Z represents N(COR8); a and b are 1-3 (provided that a + b is 3 or 4); R7 and R8 are as defined in the specification; or a pharmaceutically acceptable salt, enantiomer, racemate or tautomer thereof. The compounds of formula (I) can be used to prepare pharmaceutical compositions, and are useful for the treatment or prophylaxis of human diseases or conditions in which the inhibition of nitric oxide synthase activity is beneficial.
申请公布号 NZ338006(A) 申请公布日期 2001.04.27
申请号 NZ19980338006 申请日期 1998.04.07
申请人 ASTRAZENECA AB 发明人 MCINALLY, THOMAS;TINKER, ALAN
分类号 A61P25/04;A61K31/505;A61K31/519;A61K31/527;A61P11/06;A61P29/00;A61P31/00;A61P43/00;C07D471/04;C07D471/10;C07D471/20;C07D495/04;C07D495/10;C07D495/20;(IPC1-7):C07D471/20 主分类号 A61P25/04
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