Publication details

Pyrazolopyrimidines as Protein Kinase Inhibitors

Authors

PARUCH Kamil GUZI Timothy DWYER Michael SHIPPS Gerald

Year of publication 2006
Type Patent
MU Faculty or unit

Faculty of Science

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.

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