Publication details
Pyrazolopyrimidines as Protein Kinase Inhibitors
| Authors | |
|---|---|
| Year of publication | 2006 |
| Type | Patent |
| MU Faculty or unit | |
| Publisher | United States Patent and Trademark Office |
| State | United States of America |
| Patent's number | US 2006/094706 A1 |
| Description | The invention provides a novel class of pyrazolopyrimidines I [R2 = halo; R3 = satd. or partially unsatd. heterocyclyl radical; R4 = H, halo, haloalkyl, aryl, etc.] as inhibitors of protein and/or checkpoint kinases, methods of prepg. such compds., pharmaceutical compns. including one or more such compds., methods of prepg. pharmaceutical formulations including one or more such compds., 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. E.g., a multi-step synthesis of II, startting from 3-aminopyrazole and Et 2-ethylacetoacetate, was given. II showed IC50 of 0.1 .mu.M against CDK2 kinase. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compds. III [G1 = OH, cyano, CO2H, etc.; G2 and G3 = alkyl, cycloalkyl, aryl, etc.] and methods for inhibiting HCV RNA-dependent RNA polymerase enzymic activity. The compds. III inhibited HCV RNA-dependent RNA polymerase (RdRp) at the concn. from >10 to <1 .mu.M. The invention also provides compns. and methods for the prophylaxis and treatment of HCV infection. |