Publication details
Novel Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors
| Authors | |
|---|---|
| Year of publication | 2006 |
| Type | Patent |
| MU Faculty or unit | |
| Publisher | United States Patent and Trademark Office |
| State | United States of America |
| Patent's number | US 2006/040958 A1 |
| Description | The title compds. pyrazolo[1,5-a]pyrimidines I [R18 = alkyl or heterocyclyl (wherein heterocyclyl is linked to the isothiazole ring via a carbon atom on heterocyclyl)], useful as inhibitors of cyclin dependent kinases, were prepd. Thus, reacting II (prepn. given) with 5-amino-3-methylisothiazole hydrochloride followed by treating with Boc2O, coupling of the resulting intermediate with 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole and Boc-deprotection afforded I [R18 = Me]. The compds. I are tested in in vitro cyclin E/CDK2 kinase assay (no data given). The invention also provides pharmaceutical compns. contg. one or more compds. 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. |