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Machine translation
1. (WO2006090094) PYRIMIDOTHIOPHENE COMPOUNDS FOR USE AS HSP90 INHIBITORS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2006/090094    International Application No.:    PCT/GB2005/000736
Publication Date: 31.08.2006 International Filing Date: 28.02.2005
IPC:
C07D 495/04 (2006.01), A61K 31/381 (2006.01), A61K 31/519 (2006.01), A61P 35/00 (2006.01)
Applicants: VERNALIS R & D LTD [GB/GB]; Oakdene Court, 613 Reading Road, Winnersh, Wokingham, Berkshire RG41 5UA (GB) (For All Designated States Except US).
BROUGH, Paul, Andrew [GB/GB]; (GB) (For US Only).
BARRIL-ALONSO, Xavier [ES/GB]; (GB) (For US Only).
DRYSDALE, Martin, James [GB/GB]; (GB) (For US Only)
Inventors: BROUGH, Paul, Andrew; (GB).
BARRIL-ALONSO, Xavier; (GB).
DRYSDALE, Martin, James; (GB)
Agent: ALAN, Walls, J.; Vernalis R & D Ltd, Oakdene Court, 613 Reading Road, Winnersh, Wokingham, Berkshire RG41 5UA (GB)
Priority Data:
Title (EN) PYRIMIDOTHIOPHENE COMPOUNDS FOR USE AS HSP90 INHIBITORS
(FR) COMPOSES DE PYRIMIDOTHIOPHENE POUR UNE UTILISATION EN TANT QU’INHIBITEURS DE L’HSP90
Abstract: front page image
(EN)Certain specific compounds of formula (I) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: formula (I) wherein R2 is a group of formula -(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=0)-, -(C=S)-, -SO2-, -C(=0)O-, -C(=O)NRA- , -C(=S)NRA-, -SO2NRA-, -NRAC(=0)-, -NRASO2- or -NRA-wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
(FR)Certains composés spécifiques de formule (I) sont des inhibiteurs de l’activité de l’HSP90 in vitro ou in vivo, et utiles dans le traitement du cancer entre autres : R2 étant un groupe de formule (Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q, dans laquelle Ar1 est un radical aryle ou hétéroaryle facultativement substitué, Alk1 et Alk2 sont des radicaux alkylène en C1-C3 ou alcénylène en C2-C3 divalents facultativement substitués, m, p, r et s valent indépendamment 0 ou 1, Z est -0-, -S-, -(C=0)-, -(C=S)-, -SO2-, -C(=0)O-, -C(=O)NRA-, -C(=S)NRA-, -SO2NRA-, -NRAC(=0)-, -NRASO2- ou -NRA-, où RA est un hydrogène ou un alkyle en C1-C6, et Q est un hydrogène ou un radical carbocyclique ou hétérocyclique facultativement substitué ; R3 étant un hydrogène, un substituant facultatif ou un radical alkyle, aryle ou hétéroaryle en C1-C6 facultativement substitué ; et R4 étant un ester carboxylique, un groupe carboxamide ou sulfonamide.
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, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, 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, 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)