Publication details

Pyrazolopyrimidines as protein kinase inhibitors

Authors

PARUCH Kamil GUZI Timothy DWYER Michael

Year of publication 2007
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 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.

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