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Publication details
Pyrazolopyrimidines as protein kinase inhibitors
Authors | |
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Year of publication | 2007 |
Type | Patent |
MU Faculty or unit | |
Publisher | United States Patent and Trademark Office |
State | United States of America |
Patent's number | US 2007/0082902 A1 |
Description | The title compds. I [R2 = H, alkyl, cycloalkyl, etc.; R3 = haloalkyl, alkenyl, aryl, etc.; R4 = H, halo, (halo)alkyl, etc.; R5 = H, halo, (halo)alkyl, etc.], useful as inhibitors of protein and/or checkpoint kinases, were prepd. E.g., a multistep synthesis of I [R2, R4 = H; R3 = Ph; R5 = NH2], starting from di-Et malonimidate dichloride, was given. Compd. I [R2, R4 = H; R3 = Ph; R5 = NH2] showed IC50 of 0.08 .mu.M against CDK2. This invention also relates to pharmaceutical compns. including one or more compds. I alone or in combination with therapeutic agents, methods of prepg. pharmaceutical formulations including one or more compds. I, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the protein or checkpoint kinases using such compds. or pharmaceutical compns. |