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; ZHEN Min; JAMES Ray; PARK Haengsoon; PARADKAR Vidyadhar; HOBBS Douglas
• Year of publication: 2004
• Type: Patent
• MU Faculty or unit: Faculty of Science
• Publisher: United States Patent and Trademark Office
• State: United States
• Patent's number: US 2004/209878 A1
• Description: The title compds. 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.