| 摘要 |
The present invention relates to a kind of new hydroximic acid derivatives, in particular, hydroximic acid derivatives of pyrazolopyrimidine and their medical applications, which have inhibition to histone deacetylase 1 and two kinds of tyrosine kinases (vascular endothelial cell growth factor receptors as well as platelet-derived growth factor receptors) simultaneously, and thus can be used for treatment of diseases related to those three kinds of enzymes. This kind of compounds both exerts a synergistic effect sufficiently to increase biological activity, and avoids problems caused by different properties and metabolisms, therefore is more practical and has good prospects. |
| 主权项 |
1. A compound of formula I, and a pharmaceutically acceptable salt, a hydrate, a pro-drug and a metabolite produced in any type of metabolism thereof, in formula I, R1, R2 and R3 are independently selected from hydrogen, alkyl and hetero alkyl; R4 is selected from the group consisting of: halogen; hydroxyl; sulfhydryl; cyano; amino or alkyl-substituted amino; nitryl; C1˜C6 alkyl unsubstituted or substituted by one or more of halogen, hydroxyl, sulfhydryl, cyano, amino, alkyl-substituted amino and nitryl; C1˜C6 alkoxy unsubstituted or substituted by one or more of halogen, hydroxyl, sulfhydryl, cyano, amino, alkyl-substituted amino and nitryl; COR5; CONHR6; COOR7; NHCOR8; OCOR9; M is N or CH; Y is CH2, CH(CH3) or C═O; Z has a straight-chain structure consisting of 3˜12 atoms and connecting Y and carbonyl of compound of formula I; x is an integer between 0 and 5; R5, R6, R7, R8 and R9 are independently selected from C1˜C6 alkyl unsubstituted or substituted by halogen. |
