| 摘要 |
A 5,6,7-trisubstituted-4-aminopyrido[2,3-d]pyrimidine derivative or a pharmaceutically acceptable salt or amide thereof has the formula (I) wherein: A) R1 and R2 are independently H, alkyl, arylalkyl or acyl or together with the nitrogen atom to which they are attached may form a 5 to 7 membered ring optionally containing 1-3 additional heteroatoms selected from N, O or S; R3 and R4 are independently alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or a heterocyclic group R5 is aryl, aralkyl, heteroaryl or a heterocyclic group and the dashed lines indicate a double bond is optionally present or B) R1 and R2 are independently H, alkyl, arylalkyl -C(O)-alkyl, -C(O)-aryl, -C(O)-heterocyclic or together with the nitrogen atom to which they are attached may form a 5 to 7 membered ring optionally containing 1-2 additional heteroatoms selected from N, O or S; R3 and R4 are independently alkyl, alkenyl, alkynyl, cycloalkyl, or optionally substituted heteroarylalkyl, aryl, arylalkyl, heteroarylalkenyl, arylalkenyl, arylalkynyl or heteroarylalkynyl and R5 is optionally substituted heteroarylalkyl, aryl, arylalkyl, heteroarylalkenyl, arylalkenyl, arylalkynyl or heteroarylalkynyl; with the proviso that the compound may not be: i) 4-amino-5-(4-chlorophenyl)-7-(4-nitrophenyl)pyrido[2,3-d]pyrimidine; ii) 4-amino-5-(4-methoxyphenyl)-7-(4-nitrophenyl)pyrido[2,3-d]pyrimidine; iii) 4-amino-5-(4-fluorophenyl)-7-(4-fluorophenyl)pyrido[2,3-d]pyrimidine; iv) 4-amino-5-(4-chlorophenyl)-7-(4-fluorophenyl)pyrido[2,3-d]pyrimidine; v) 4-amino-5-phenyl-7-(4-aminophenyl)pyrido[2,3-d]pyrimidine; vi) 4-amino-5-phenyl-7-(4-bromophenyl)pyrido[2,3-d]pyrimidine; vii) 4-amino-5-(4-methoxyphenyl)-7-(4-aminophenyl)pyrido[2,3-d]pyrimidine; viii) 4-amino-5-(4-methoxyphenyl)-7-(4-bromophenyl)pyrido[2,3-d]pyrimidine and ix) 4-amino-5,7-diphenylpyrido[2,3-d]pyrimidine. A pharmaceutical composition thereof is useful for inhibiting adenosine kinase, ischemia, neurological disorders, nociperception, inflammation, immunosuppression, gastrointestinal disjunctions, diabetes or sepsis.
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