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CAPLUS COPYRIGHT 2007 ACS on STN
| TITLE:
| Pyrrolo[2,3-b]pyridine derivatives as protein kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases |
| INVENTOR(S):
| Ibrahim, Prahbha N.; Artis, Dean R.; Bremer, Ryan; Mamo, Shumeye; Nespi, Marika; Zhang, Chao; Zhang, Jiazhong; Zhu, Yong-Liang; Tsai, James; Hirth, Klaus-Peter; Bollag, Gideon; Spevak, Wayne; Cho, Hanna; Gillette, Samuel J.; Wu, Guoxiam; Zhu, Hongyao; Shi, Shenghua |
| PATENT ASSIGNEE(S):
| Plexxikon, Inc., USA |
| SOURCE:
| PCT Int. Appl., 291 pp. CODEN: PIXXD2 |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
WO 2007002325 A1 20070104 WO 2006-US24361 20060621
W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH,
CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD,
GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP,
KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN,
MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU,
SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG,
US, UZ, VC, VN, ZA, ZM, ZW
RW: AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE,
IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR, BF, BJ,
CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG, BW, GH,
GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW, AM, AZ, BY,
KG, KZ, MD, RU, TJ, TM
ABSTRACT:
Compds. of formula I which are active on protein kinases are described, as well as methods of using such compds. to treat diseases and conditions assocd. with aberrant activity of protein kinases. Compds. of formula I wherein Q is (un)substituted (hetero)aryl, and (un)substituted indole; A is O, S, (un)substituted methylene, NH and derivs., CO, CS, SO and SO2; R4 - R6 are independently H, halo, (un)substituted lower alkyl, (un)substituted lower alkenyl, (un)substituted lower alkynyl, (un)substituted (hetero)cycloalkyl, (un)substituted (hetero)aryl, etc.; and their pharmaceutically acceptable salts, prodrugs, tautomer, and isomers thereof, are claimed. Example compd. II was prepd. by carboxylation of 2,4-difluoroaniline with benzyl chloroformate; the resulting benzyl 3-amino-2,6-difluorobenzoate underwent sulfonylation with propane-1-sulfonyl chloride to give benzyl 2,6-difluoro-3-(propylsulfonylamino)benzoate, which underwent hydrolysis to give the corresponding benzoic acid, which underwent chlorination and coupling with 5-bromo-7-azaindole to give compd. II. All the invention compds. were evaluated for their protein kinase inhibitory activity. Several of the invention compds. exhibited good inhibitory activity against various protein kinases.
Updated 8/24/2007 12:45:17 PM
