DWYER, MICHAEL P,GUZI, TIMOTHY J,PARUCH, KAMIL,DOLL, RONALD J,GIRIJAVALLABHAN, VIYYOOR MOOPIL,MALLAMS, ALAN,ALVAREZ, CARMEN S,KEERTIKAR, KARTIK M,RIVERA, JOCELYN,CHAN, TIN-YAU,MADISON, VINCENT,FISCHMA
申请号:
NZ59048005
公开号:
NZ590480A
申请日:
2005.02.08
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are specific 7-amino-pyrazolo[1,5-a]pyrimidine compounds as represented by the general formula (I), wherein R2 is a group such as alkyl, cycloalkyl, or bromo R3 is a group such as phenyl, an alkylamino group, or a nitrogen linked heterocycle R4 is hydrogen and R is an arylmethyl group or a heteroarylmethyl group. Some of the specific compounds disclosed herein include 3-ethyl-5-(2-(hydroxyethyl)-piperidin-1-yl)-7-[{ (pyridin-3-yl)methyl} amino]-pyrazolo[1,5-a]pyrimidine 3-ethyl-5-[{ 2-(hydroxymethyl)-cyclohexy} amino]-7-[{ (2-amino-pyrimidin-5-yl)methyl} amino]-pyrazolo[1,5-a]pyrimidine, 5-ethoxy-3-[{ (3-ethyl-5-phenyl-pyrazolo[1,5-a]pyrimidin-7-yl)amino} methyl]-pyridine N-oxide, 3-[{ (3-cyclopropyl-5-(2-(hydroxyethyl)-piperidin-1-yl)-pyrazolo[1,5-a]pyrimidin-7-yl)amino} methyl]-pyridine N-oxide and 3-[{ (3-ethyl-5-(2-(hydroxyethyl)-piperidin-1-yl)-pyrazolo[1,5-a]pyrimidin-7-yl)amino} methyl]-pyridine N-oxide. Further disclosed is a pharmaceutical composition which comprises at least one compound as defined above or a pharmaceutically acceptable salt or solvate thereof in combination with at least one pharmaceutically acceptable carrier for the treatment of cancer, squamous cell carcinoma, leukemia, fibrosarcoma, melanoma, seminoma, teratocarcinoma, osteosarcoma, xenoderoma pigmentosum, keratoctanthoma, thyroid follicular cancer, Kaposis sarcoma etc.