Novel 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 Zhenmin; JAMES Ray; PARK Haengsoon; PARADKAR Vidyadhar; HOBBS Douglas; KIRSCHMEIER Paul; BANNERJI Rajat
• Year of publication: 2008
• Type: Patent
• MU Faculty or unit: Faculty of Science
• Publisher: United States Patent Office
• State: United States of America
• Patent's number: US 2008/0050384 A1
• Description: The title compds. [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 compns. comprising the compd. I alone or in combination with other therapeutic agents are claimed.