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Pub. No.:    WO/2006/084030    International Application No.:    PCT/US2006/003676
Publication Date: 10.08.2006 International Filing Date: 01.02.2006
C07D 473/40 (2006.01), C07D 473/34 (2006.01), A61K 31/52 (2006.01), A61P 35/00 (2006.01), A61P 35/02 (2006.01), A61K 101/00 (2006.01), A61K 51/00 (2006.01)
Applicants: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH [US/US]; Office of Industrial Affairs, 1275 York Avenue, New York, NY 10021 (US) (For All Designated States Except US).
CHIOSIS, Gabriela [RO/US]; (US) (For US Only).
HUAZHONG, He [US/US]; (US) (For US Only).
LLAUGER-BUFI, Laura [IT/US]; (US) (For US Only).
KIM, Joungnam [KR/US]; (US) (For US Only).
LARSON, Steve, M. [US/US]; (US) (For US Only).
SMITH-JONES, Peter [GB/US]; (US) (For US Only)
Inventors: CHIOSIS, Gabriela; (US).
KIM, Joungnam; (US).
LARSON, Steve, M.; (US).
Agent: LARSON, Marina, T.; MARIAN LARSON & ASSOCIATES, LLC, P.o. Box 4928, Dillon, Colorado 80435 (US)
Priority Data:
60/649,322 01.02.2005 US
Abstract: front page image
(EN)Hsp90 inhibitors havin are rovided havin the formula: (I) with a 2',4',5'-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4' and 5' positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2-alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C=SR2 NSO2X5, C=OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5'-position and the other at the 4'-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.
(FR)L'invention porte sur des inhibiteurs du Hsp90 de formule (I) présentant un motif de substitution en 2',4',5'- du côté droit du fragment aryle. Dans ladite formule: X1 représente deux substituants, identiques ou différents, disposés dans les positions 4' et 5' du groupe aryle, X1 étant sélectionné parmi: halogène, alkyle, alkoxy, alkoxy halogéné, hydroxyalkyle, pyrollyle, aryloxy facultativement substitué, alkylamino, dialkylamino, carbamyle, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalométhoxy, trihalocarbone, thioalkyle, SO2-alkyle, COO-alkyle, KH2, OH, CN, SO2X5, NO2, NO, C=SR2 NSO2X5, C=OR2, X5 est F, NH2, alkyle ou H, et R2 est alkyle, NH2, NH-alkyle ou O-alkyle, C1 à C6 alkyle ou alkoxy; ou bien X1 présentant la formule -0-(CH2)n-0-, dans laquelle: n est un entier de O à 2, de préférence 1 ou 2, et l'un des oxygènes étant lié en position 5'- position et l'autre en position 4'- du cycle aryle. Lesdits composés s'avèrent utiles en thérapie du cancer et comme ligands de radioimagerie.
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)