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1. (WO2017153518) PRMT5 INHIBITORS
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Pub. No.: WO/2017/153518 International Application No.: PCT/EP2017/055535
Publication Date: 14.09.2017 International Filing Date: 09.03.2017
IPC:
C07D 237/32 (2006.01) ,C07D 498/08 (2006.01) ,A61K 31/502 (2006.01) ,A61P 7/00 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
237
Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
26
condensed with carbocyclic rings or ring systems
30
Phthalazines
32
with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
08
Bridged systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
50
Pyridazines; Hydrogenated pyridazines
502
ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
CTxT PTY LIMITED [AU/AU]; 343 Royal Parade Parkville, Victoria 3052, AU
Inventors:
STUPPLE, Paul Anthony; AU
WALKER, Scott Raymond; AU
CAMERINO, Michelle Ang; 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:
1604027.109.03.2016GB
Title (EN) PRMT5 INHIBITORS
(FR) INHIBITEURS DE PRMT5
Abstract:
(EN) A compound of formula (Ia), (Ib) or (Ic) wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, -NH2, -C(=O)NH2, and -CH2OH; R4b is either H or Me; X is either N or CH; R7 is selected from H and C1-4 alkyl; (a) one of R8a, R8b, R8c and R8d is selected from H, halo, C1-4 alkyl, C1-4 alkoxy, NHC1-4 alkyl; (b) another of R8a, R8b, R8c and R8d is selected from H, C1-4 alkyl, C1-4 fluoroalkyl, C3-6 cycloalkyl, C5-6 heteroaryl, C5-6 heteroaryl methyl, C4-6 heterocyclyl, C4-6 heterocyclyl methyl, phenyl, benzyl, halo, amido, amidomethyl, acylamido, acylamidomethyl, C1-4 alkyl ester, C1-4 alkyl ester methyl, C1-4 alkyl carbamoyl, C1-4 alkyl carbamoyl methyl, C1-4 alkylacyl, C1-4 alkylacyl methyl, phenylcarbonyl, carboxy, carboxymethyl, ether, amino, amino methyl, sulfonamido, sulfonamino, sulfone, sulfoxide, nitrile and nitrilemethyl; (c) the others of R8a, R8b, R8c and R8d are H.
(FR) L'invention concerne un composé de formule (Ia), (Ib) ou (Ic). n est 1 ou 2 ; RN est H ou Me ; R1 est éventuellement un ou plusieurs groupes halo ou méthyle ; R2a et R2b sont indépendamment choisis parmi le groupe constitué de ce qui suit : (i) F ; (ii) H ; (iii) Me ; et (iv) CH2OH ; R2c et R2d (s’ils sont présents) sont indépendamment choisis parmi le groupe constitué de ce qui suit : (i) F ; (ii) H ; (iii) Me ; et (iv) CH2OH ; R3a et R3b sont indépendamment choisis parmi H et Me ; R4a est choisi parmi OH, -NH2, -C(=O)NH2, et -CH2OH ; R4b est soit H, soit Me ; X est soit N, soit CH ; R7 est choisi parmi H et alkyle en C1-4 ; (a) un élément parmi R8a, R8b, R8c, et R8d est choisi parmi H, halo, alkyle en C1-4, alcoxy en C1-4, NHC1-4 alkyle ; (b) un autre élément parmi R8a, R8b, R8c et R8d est choisi parmi H, alkyle en C1-4, fluoroalkyle en C1-4, cycloalkyle en C3-6, hétéroaryle en C5-6, hétéroaryle méthyle en C5-6, hétérocyclyle en C4-6 , hétérocyclyle méthyle en C4-6, phényle, benzyle, halo, amido, amidométhyle, acylamido, acylamidométhyle, ester d’alkyle en C1-4, ester d’alkyle méthyle en C1-4, alkyle carbamoyle en C1-4, alkyle carbamoyle méthyle en C1-4, alkylacyle C1-4, alkylacyle méthyle en C1-4, phénylcarbonyle, carboxy, carboxyméthyle, ether, amino, amino méthyle, sulfonamido, sulfonamino, sulfone, sulfoxyde, nitrile and nitrile-méthyle ; (c) les autres éléments parmi R8a, R8b, R8c et R8d sont H.
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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)