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Machine translation
1. (WO2006086103) SYNTHESIS OF INHIBITORS OF P90RSK
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2006/086103    International Application No.:    PCT/US2006/000709
Publication Date: 17.08.2006 International Filing Date: 10.01.2006
IPC:
A01N 43/04 (2006.01), A61K 31/70 (2006.01), C07H 15/00 (2006.01), C07H 17/00 (2006.01)
Applicants: UNIVERSITY OF VIRGINIA PATENT FOUNDATION [US/US]; 250 West Main Street, Suite 300, Charlottesville, Virginia 22902 (US) (For All Designated States Except US).
HECHT, Sidney, M. [US/US]; (US) (For US Only).
MALONEY, David [US/US]; (US) (For US Only)
Inventors: HECHT, Sidney, M.; (US).
MALONEY, David; (US)
Agent: SPARKS, Rodney, L.; UNIVERSITY OF VIRGINIA PATENT FOUNDATION, 250 West Main Street, Suite 300, Charlottesville, Virginia 22902 (US)
Priority Data:
60/642,539 10.01.2005 US
Title (EN) SYNTHESIS OF INHIBITORS OF P90RSK
(FR) SYNTHESE D'INHIBITEURS DE P90RSK
Abstract: front page image
(EN)The synthesis of the naturally occurring kaempferol glycoside SLO1O1-1, as well as analogs thereof, has been accomplished, as has its biochemical evaluation. SLO1O1-1 exhibits selective and potent p90 Rsk inhibitory activity at nanomolar concentrations without inhibiting the function of upstream kinases such as MEK, Raf, or PKC. The synthetic scheme of the invention verified the structural assignment of the natural product and has provided access to material sufficient for detailed biological evaluation.
(FR)Selon l'invention, on a réalisé la synthèse de glycoside de kaempférol naturel SL0101-1 et d'analogues de ce composé, de même que son évaluation biochimique. Le SL0101-1 présente une activité inhibitrice de la p90Rsk sélective et puissante à des concentrations nanomolaires sans inhibition de la fonction des kinases en amont telles que MEK, Raf ou PKC. Le système de synthèse de l'invention a permis de vérifier l'attribution structurale du produit naturel et a fourni un accès à la matière suffisant pour une évaluation biologique détaillée.
Designated States: 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, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, 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, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)