24-12-2015 дата публикации
Номер: US20150368259A1
Принадлежит:
The present invention relates to the field of medicinal chemistry, and in particular relates to 4-(five-membered heterocyclic pyrimidine/pyridine substituted) amino-1H-3-pyrazolecarboxamide derivatives, the preparation method thereof, pharmaceutical compositions containing these compounds and the medicinal use thereof, especially as protein kinase inhibitors for anti-tumour use. 2. The compound according to claim 1 , wherein:{'sup': 1', '2', '3, 'R, Rand Reach independently represent H, alkyl, cyano, halogen, haloalkyl, hydroxyl, thiol, alkoxyl, alkylthiol, alkoxylalkyl, aralkyl or aryl;'}{'sup': 4', '4, 'X and Y each independently represent N atom or CH group, wherein the CH group can optionally be substituted by R, and Rmay be H, alkyl, cyano, halogen, haloalkyl, hydroxyl, thiol, alkoxyl, alkylthiol, alkoxylalkyl, aralkyl or aryl;'}{'sup': 5', '5, 'Z and M each independently represent NH, O, S or CH group with the proviso that one of Z and M is NH, O or S, wherein the CH or NH group can each optionally and independently be substituted by R, and Rmay be H, alkyl, cyano, halogen, haloalkyl, hydroxyl, thiol, alkoxyl, alkylthiol, alkoxylalkyl, aralkyl or aryl;'}{'sup': 1', '6', '6, 'Aindependently represents NH, O, S or alkylene group, wherein the NH or alkylene group can each optionally and independently be substituted by R, and Rmay be H, alkyl, cyano, halogen, haloalkyl, hydroxyl, thiol, alkoxyl, alkylthiol, alkoxylalkyl, aralkyl or aryl;'}{'sup': 2', '7', '7, 'Aindependently represents alkylene, C(O)NH, C(O), NHC(O), alkylene-C(O), C(O)-alkylene, alkylene-C(O)-alkylene or NHC(O)NH, wherein the above groups can each optionally and independently be substituted by R, and Rmay be H, alkyl, cyano, halogen, haloalkyl, hydroxyl, thiol, alkoxyl, alkylthiol, alkoxylalkyl, aralkyl or aryl;'}{'sup': 1', '8', '8, 'Qis selected from aryl or Het, wherein the aryl or Het can each optionally and independently be substituted by one or more R, and Rmay be H, alkyl, cyano, halogen, ...
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