GUZI, Timothy, Kamil PARUCH, Michael DWYER, Ronald DOLL, Viyyoor GIRIJAVALLABHAN, Carmen ALVAREZ, Tin-Yau CHAN, Chad KNUTSON, Vincent MADISON, Thierry FISCHMANN, Lawrence DILLARD, Vinh TRAN, Zhen HE, Ray JAMES and Haengsoon PARK. Novel Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors. 2004.
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Basic information
Original name Novel Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors
Name in Czech Novel Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors
Authors GUZI, Timothy (840 United States of America), Kamil PARUCH (203 Czech Republic, guarantor), Michael DWYER (840 United States of America), Ronald DOLL (840 United States of America), Viyyoor GIRIJAVALLABHAN (840 United States of America), Carmen ALVAREZ (840 United States of America), Tin-Yau CHAN (840 United States of America), Chad KNUTSON (840 United States of America), Vincent MADISON (840 United States of America), Thierry FISCHMANN (840 United States of America), Lawrence DILLARD (840 United States of America), Vinh TRAN (840 United States of America), Zhen HE (840 United States of America), Ray JAMES (840 United States of America) and Haengsoon PARK (840 United States of America).
Edition Number: WO 2004/026229 A2, Publisher: World Intellectual Property Organization, Place of publication: USA, Owner's name: Schering-Plough; Pharmacopeia, 2004.
Other information
Original language English
Type of outcome Patent
Field of Study 10401 Organic chemistry
Country of publisher United States of America
Confidentiality degree is not subject to a state or trade secret
RIV identification code RIV/00216224:14310/04:00036031
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
Changed by Changed by: doc. Mgr. Kamil Paruch, Ph.D., učo 108413. Changed: 25/6/2009 14:38.
Abstract
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.
Abstract (in Czech)
viz Anotace
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