Novel Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors

GUZI, Timothy, Kamil PARUCH and Michael DWYER. Novel Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors. 2006.

Basic information

Original name

Novel Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors

Name in Czech

Novel Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors

Authors

GUZI, Timothy, Kamil PARUCH and Michael DWYER

Edition

Number: US 2006/040958 A1, Publisher: United States Patent and Trademark Office, Place of publication: USA, Owner's name: Schering-Plough, 2006

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Other information

Language

English

Type of outcome

Patent

Field of Study

10401 Organic chemistry

Country of publisher

United States of America

Confidentiality degree

není předmětem státního či obchodního tajemství

Organization unit

Faculty of Science

Keywords (in Czech)

cyclin dependent kinase; inhibitor; pyrazolopyrimidine

Keywords in English

cyclin dependent kinase; inhibitor; pyrazolopyrimidine

Tags

Cyclin dependent kinase, inhibitor, pyrazolopyrimidine

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Abstract

V originále

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.

In Czech

viz Anotace