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1. (WO2017153513) TETRAHYDROISOQUINOLINES AS PRMT5 INHIBITORS
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Pub. No.: WO/2017/153513 International Application No.: PCT/EP2017/055529
Publication Date: 14.09.2017 International Filing Date: 09.03.2017
IPC:
C07D 401/14 (2006.01) ,C07D 405/14 (2006.01) ,C07D 217/16 (2006.01) ,C07D 401/12 (2006.01) ,C07D 413/12 (2006.01) ,C07D 471/04 (2006.01) ,C07D 498/08 (2006.01) ,A61K 31/4725 (2006.01) ,A61K 31/437 (2006.01) ,A61P 7/00 (2006.01) ,A61P 35/00 (2006.01)
[IPC code unknown for C07D 401/14][IPC code unknown for C07D 405/14][IPC code unknown for C07D 217/16][IPC code unknown for C07D 401/12][IPC code unknown for C07D 413/12][IPC code unknown for C07D 471/04][IPC code unknown for C07D 498/08][IPC code unknown for A61K 31/4725][IPC code unknown for A61K 31/437][IPC code unknown for A61P 7][IPC code unknown for A61P 35]
Applicants:
CTxT PTY LIMITED [AU/AU]; 343 Royal Parade Parkville, Victoria 3052, AU
Inventors:
BERGMAN, Ylva Elisabet; AU
CAMERINO, Michelle Ang; AU
WALKER, Scott Raymond; AU
STUPPLE, Paul Anthony; AU
Agent:
WATSON, Robert; GB
ADDISS, John; GB
ANDREWS, Robert; GB
BAILEY, Sam; GB
BRASNETT, Adrian; GB
BREARLEY, Sarah; GB
CARLISLE, Julie; GB
CARTER, Stephen; GB
CASLEY, Christopher; GB
CLEGG, Richard; GB
CRIPPS, Joanna; GB
DALE, Elizabeth; GB
DENISON, Christopher; GB
DUNNE, Paul; GB
FORREST, Graham; GB
GILL, Stephen; GB
GRAHAM, Emma; GB
GREEN, Katherine; GB
GREGORY, Adam; GB
HACKNEY, Nigel; GB
HARRISON, Susan; GB
HAYES, Emily; GB
HODSDON, Stephen; GB
JOHNSON, Richard; GB
JONES, Rachel; GB
KEIRSTEAD, Tanis; GB
KIDDLE, Simon; GB
KREMER, Simon; GB
LEACH, James; GB
LENTHALL, Joseph; GB
LYONS, June; GB
MCGUINN, Callum; GB
MOORE, Graeme; GB
NAYLOR, Matthew; GB
NICHOLLS, Kathryn; GB
OXLEY, Rachel; GB
PARRY, Simon; GB
SALISBURY, Frances; GB
SMITH, Matthew; GB
STONER, Patrick; GB
SUTCLIFFE, Nicholas; GB
TOLLERVEY, Rebecca; GB
WALTON, Seán; GB
WARD, Eliot; GB
WEBSTER, Jeremy; GB
WESCOTT, Rhiannon; GB
WILLS, Jonathan; GB
WOOLLEY, Lindsey; GB
WYTENBURG, Wilhelmus; GB
Priority Data:
1604020.609.03.2016GB
Title (EN) TETRAHYDROISOQUINOLINES AS PRMT5 INHIBITORS
(FR) TÉTRAHYDRO-ISOQUINOLÉINES EN TANT QU'INHIBITEURS DE PRMT5
Abstract:
(EN) A compound of formula (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from the group consisiting of H, halo, C1-4 alkoxy, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH-C1-4 alkyl and cyano; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2e is H or Me; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl; wherein when R2e is H, at least one of R1a, R1b, R1c and R1d is selected from C1-4 alkoxy, C2-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH-C1-4 alkyl and cyano.
(FR) L'invention concerne un composé de formule (I) dans laquelle : n vaut 1 ou 2 ; p vaut 0 ou 1 ; R1a, R1b, R1c et R1d sont choisis indépendamment dans le groupe constitué par H, halogéno, C1-4-alcoxy, C1-4-alkyle, C1-4-fluoroalkyle, C3-4-cycloalkyle, NH-C1-4-alkyle et cyano ; R2a et R2b sont choisis, indépendamment, dans le groupe constitué par : (i) F ; (ii) H ; (iii) Me ; et (iv) CH2OH ; R2c et R2d sont choisis, indépendamment, dans le groupe constitué par : (i) F ; (ii) H ; (iii) Me ; et (iv) CH2OH ; R2e représente H ou Me ; R3a et R3b sont choisis, indépendamment, parmi H et Me ; R4 représente soit H, soit Me ; R5 représente soit H, soit Me ; R6a et R6b sont choisis, indépendamment, parmi H et Me ; A est soit (i) phényle éventuellement substitué ; (ii) naphtyle éventuellement substitué ; ou (iii) C5-12-hétéroaryle éventuellement substitué ; où, lorsque R2e représente H, au moins l'un parmi R1a, R1b, R1c et R1d est choisi parmi C1-4-alcoxy, C2-4-alkyle, C1-4-fluoroalkyle, C3-4-cycloalkyle, NH-C1-4-alkyle et cyano.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)