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CAPLUS COPYRIGHT 2004 ACS on STN
| TITLE:
| Preparation of pyrazolopyrimidines as cyclin-dependent kinase inhibitors |
| INVENTOR(S):
| Guzi, Timothy J.; Paruch, Kamil; Dwyer, Michael P.; Doll, Ronald J.; Girijavallabhan, Viyyoor Moopil; Mallams, Alan; Alvarez, Carmen S.; Keertikar, Kartik M.; Rivera, Jocelyn; Chan, Tin-yau; Madison, Vincent; Fischmann, Thierry O.; Dillard, Lawrence W.; Tran, Vinh D.; He, Zhen Min; James, Ray Anthony; Park, Haengsoon; Paradkar, Vidyadhar M.; Hobbs, Douglas Walsh |
| PATENT ASSIGNEE(S):
| Schering Corporation, USA; Pharmacopeia, Inc. |
| SOURCE:
| PCT Int. Appl., 609 pp. CODEN: PIXXD2 |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- --------------- --------
WO 2004022561 A1 20040318 WO 2003-US27555 20030903
W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN,
CO, CR, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, HR, HU,
ID, IL, IN, IS, JP, KG, KR, KZ, LC, LK, LR, LT, LU, LV, MA, MD,
MG, MK, MN, MX, MZ, NI, NO, NZ, PG, PH, PL, PT, RO, RU, SC, SE,
SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UZ, VC, VN, YU, ZA,
ZM, AM, AZ, BY, KG, KZ, MD, RU, TJ, TM
RW: GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, ZW, AT, BE, BG,
CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IT, LU, MC,
NL, PT, RO, SE, SI, SK, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GQ,
GW, ML, MR, NE, SN, TD, TG
ABSTRACT:
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 compn. comprising the compd. I is claimed. This is a Part I of I-III series.
Updated 5/8/2007 10:27:17 AM
