Publication details

Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors

Authors

GUZI Timothy PARUCH Kamil DWYER Michael DOLL Ronald GIRIJAVALLABHAN Viyyoor MALLAMS Alan ALVAREZ Carmen KEERTIKAR Kartik RIVERA Jocelyn CHAN Tin-Yau MADISON Vincent FISCHMANN Thierry DILLARD Lawrence TRAN Vinh HE Zhen JAMES Ray PARK Haengsoon PARADKAR Vidyadhar HOBBS Douglas

Year of publication 2004
Type Patent
MU Faculty or unit

Faculty of Science

Publisher World Intellectual Property Organization
State United States of America
Patent's number WO 2004/022561 A1
Description The title pyrazolo[1,5-a]pyrimidines [I R = H, alkyl, cycloalkyl, etc.; R2 = alkyl, halo, aryl, etc.; R3 = H, halo, aryl, etc.; R4 = H, halo, alkyl], useful as inhibitors of cyclin dependent kinases for treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the CDKs such as cancer, were prepd. Thus, reacting II (prepn. given) with 4-aminomethylpyridine afforded 93% III which showed IC50 of 0.020 .mu.M and 0.029 .mu.M against CDK2 kinase (cyclin A or cyclin E-dependent). The pharmaceutical compn. comprising the compd. I is claimed.

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