Publication details

Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors

Authors

GUZI Timothy PARUCH Kamil DWYER Michael LABROLI Marc KEERTIKAR Kartik

Year of publication 2007
Type Patent
MU Faculty or unit

Faculty of Science

Publisher United States Patent and Trademark Office
State United States
Patent's number US 2007/00772881 A1
Description Title compds. I [R = H, alkyl, alkenyl, etc.; R2 = H, CF3, alkyl, heterocyclyl, etc.; R3 = H, halo, OH, SH, alkyl, etc.; R4 = H, halo or alkyl], and their pharmaceutically acceptable salts, are prepd. and disclosed as inhibitors of cyclin dependent kinases (CDKs). Thus, e.g., II was prepd. by amination of III (prepn. given) followed by deprotection. Methods for in vitro kinase assays are described, e.g., II was found to possess an IC50 value of 10 (.mu.M). Further disclosed are pharmaceutical compns. contg. one or more of I, methods of prepg. pharmaceutical formulations comprising one or more such compds., and methods of treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the CDKs using such compds. or pharmaceutical compns.

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