Publication details

Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors

Authors

GUZI Timothy PARUCH Kamil DWYER Michael

Year of publication 2007
Type Patent
MU Faculty or unit

Faculty of Science

Publisher Unitedf States Patent Office
State Ukraine
Patent's number US 2007/0072880 A1
Description Title compds. I [R2 = alkyl, alkynyl, alkynylalkyl, etc.; R3 = H, halo, alkyl, etc.; R4 = H, halo or alkyl; R5 = (un)substituted aryl which may optionally be fused with one or more heteroaryl], and their pharmaceutically acceptable salts, are prepd. and disclosed as inhibitors of cyclin dependent kinases (CDKs). Thus, e.g., II (R = H) was prepd. by substitution of III (prepn. given) with aniline, followed by deprotection. In in vitro kinase assays, II (R = pyrazo-1-yl) was found to possess an IC50 = 0.2 (.mu.M). Further disclosed are pharmaceutical compns. contg. 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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