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1. (WO2009066072) INHIBITORS OF 17BETA-HYDROXYSTEROID DEHYDROGENASE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2009/066072    International Application No.:    PCT/GB2008/003889
Publication Date: 28.05.2009 International Filing Date: 19.11.2008
IPC:
C07C 209/14 (2006.01), C07C 211/50 (2006.01), C07C 233/43 (2006.01), C07C 237/42 (2006.01), C07D 207/26 (2006.01), C07D 211/58 (2006.01), C07D 211/62 (2006.01), C07D 317/66 (2006.01), A61K 31/167 (2006.01), A61K 31/4409 (2006.01), A61K 31/36 (2006.01), A61P 35/00 (2006.01), A61P 5/24 (2006.01)
Applicants: STERIX LIMITED [GB/GB]; 190 Bath Road Slough Berkshire SL1 3XE (GB) (For All Designated States Except US).
VICKER, Nigel [GB/GB]; (GB) (For US Only).
BAILEY, Helen, Victoria [GB/GB]; (GB) (For US Only).
HEATON, Wesley [GB/GB]; (GB) (For US Only).
DAY, Joanna, Mary [GB/GB]; (GB) (For US Only).
PUROHIT, Atul [GB/GB]; (GB) (For US Only).
POTTER, Barry, Victor, Lloyd [GB/GB]; (GB) (For US Only)
Inventors: VICKER, Nigel; (GB).
BAILEY, Helen, Victoria; (GB).
HEATON, Wesley; (GB).
DAY, Joanna, Mary; (GB).
PUROHIT, Atul; (GB).
POTTER, Barry, Victor, Lloyd; (GB)
Agent: ALCOCK, David; D Young & Co LLP 120 Holborn London EC1N 2DY (GB)
Priority Data:
0722779.6 20.11.2007 GB
Title (EN) INHIBITORS OF 17BETA-HYDROXYSTEROID DEHYDROGENASE
(FR) COMPOSÉ
Abstract: front page image
(EN)There is provided a compound having Formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, -OC(R13)3, -OCH(R13)2, -OCH2R13, -C(R13)3, -CH(R13)2, or -CH2R13 wherein R13 is a halogen; (c) -CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (I) aryloxy; (m) -SO2-alkyl; and (n) -N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (T) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=O, S(=O)2, C=O, S(=O)2NR16, C=ONR17, NR18, in which R16, R17, and R18 are independently selected from H and hydrocarbyl, R10 is selected from H and hydrocarbyl, R11 is selected from CR19R20 and C=O, in which R19 and R20 are independently selected from H and hydrocarbyl, R12 is selected from a substituted five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring, and wherein the one or more substituents are selected from hydrocarbyl groups.
(FR)L'invention porte sur un composé représenté par la Formule (I), dans laquelle R1, R2, R3, R4, R5, R6, R7, R8 et R9 sont indépendamment choisis parmi (a) H, (b) R13, -OC(R13)3, -OCH(R13)2, -OCH2R13, -C(R13)3, -CH(R13)2 ou -CH2R13 où R13 représente un halogène; (c) -CN; (d) alkyle facultativement substitué, (e) hétéroalkyle facultativement substitué; (f) aryle facultativement substitué; (g) hétéroaryle facultativement substitué; (h) arylalkyle facultativement substitué; (i) hetéroarylalkyle facultativement substitué; (j) hydroxy; (k) alcoxy; (l) aryloxy; (m) -SO2-alkyle; et (n) -N(R14)C(O)R15, où R14 et R15 sont choisis indépendamment parmi H et hydrocarbyle, les substituants facultatifs de (d) (e) (f) (g) (h) et (i) étant choisis dans le groupe constitué par : alkyle en C1-6, halo, cyano, nitro, haloalkyle, hydroxy, alcoxy en C1-6, carboxy, carboxyalkyle, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyle, sulfonamido, aryle et hétéroaryle; n et p sont indépendamment choisis parmi 0 et 1; X est un groupe facultatif choisi parmi O, S, S=O, S(=O)2, C=O, S(=O)2NR16, C=ONR17, NR18, où R16, R17, et R18 sont choisis indépendamment parmi H et hydrocarbyle, R10 est choisi parmi H et hydrocarbyle, R11 est choisi parmi CR19R20 et C=O, où R19 et R20 sont choisis indépendamment parmi H et hydrocarbyle, R12 est choisi parmi les cycles carbonés à cinq ou six chaînons substitués, contenant facultativement un ou plusieurs hétéroatomes choisis parmi N, S et O et présentant facultativement, fusionné à ceux-ci, un autre cycle, et où le ou les substituants sont choisis parmi les groupes hydrocarbyles.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 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, HR, HU, IE, IS, IT, LT, LU, LV, MC, MT, NL, NO, 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)