Publication details

Novel Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors

Authors

GUZI Timothy PARUCH Kamil DWYER Michael DOLL Ronald GIRIJAVALLABHAN Viyyoor ALVAREZ Carmen CHAN Tin-Yau KNUTSON Chad MADISON Vincent FISCHMANN Thierry DILLARD Lawrence TRAN Vinh HE Zhen JAMES Ray PARK Haengsoon

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 2004/026229 A2
Description In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compds. I [R = (un)substituted aryl; R2 = halo, CN, (un)substituted alkyl, etc.; R3 = H, halo, (un)substituted-alkyl, -alkynyl, -aryl, etc.; R4 = H, halo or alkyl] as inhibitors of cyclin dependent kinases, methods of prepg. such compds., pharmaceutical compns. contg. one or more such compds., 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. Thus, e.g., II was prepd. by substitution of 3-bromo-7-chloro-5-(2-chlorophenyl)-pyrazolo[1,5-a]pyrimidine (prepn. given) with aniline. I exhibit excellent CDK inhibitory properties as demonstrated by II which possessed a IC50 value of 0.51 uM in kinase activity assays.

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