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1. (WO2018127292) SELECTIVE AURORA A KINASE INHIBITORS
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Pub. No.: WO/2018/127292 International Application No.: PCT/EP2017/050283
Publication Date: 12.07.2018 International Filing Date: 06.01.2017
IPC:
C07D 417/08 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
08
linked by a carbon chain containing alicyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
UNIVERSITÄT BERN [CH/CH]; Verwaltungsdirektion Hochschulstrasse 6 CH-3012 Bern, CH
Inventors:
REYMOND, Jean-Louis; CH
KILCHMANN, Falco; CH
Agent:
BOLSINGER, Jens; DE
Priority Data:
Title (EN) SELECTIVE AURORA A KINASE INHIBITORS
(FR) INHIBITEURS SÉLECTIFS DE LA KINASE AURORA A
Abstract:
(EN) The invention relates to a compound (F) (1a) or (1b) wherein R1 is selected from -I, -Br, -CI, -F, C1C6-alkyl, -O(CH2)mCH3, -(CH2)mOCH3, C1C6-haloalkyl, a cycloalkyl, a heterocycle, a aryl or heteroaryl, wherein R2 is selected from H, C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-cycloalkyl, -CH2-(C3-C6-cycloalkyl), or -(CH2)rOCH3, wherein R3 is -NH2, -NH-R4, -NHC(=0)-R4, -NHC(=O)NH-R4, -NHC(=S)-R4 or -NHC(=S)NH-R4, wherein R4 is selected from a cycloalkyl, a heterocycle, a aryl or a heteroaryl, or -L-R5, wherein L is selected from C1-C5-alkyl, a cycloalkyl, a heterocycle, a aryl, or a heteroaryl, and R5 is selected from -OH, -CH2OH, -NH2, -COOH, -CONH2, -CONH-R6 or carboxylic acid isosteres, wherein R6 is selected from C1-C4-alkyl, with n, m and r being 0, 1, 2, 3, 4 or 5 and their use.
(FR) L'invention concerne un composé (F) (1a) ou (1b) dans lequel R1 est choisi parmi -I, -Br, -CI, -F , un alkyle en C1C6, -O(CH2)mCH3, -(CH2)mOCH3, un haloalkyle en C1C6, un cycloalkyle, un hétérocycle, un aryle ou un hétéroaryle, R2 étant choisi parmi H, un alkyle en C1-C6, un haloalkyle en C1-C6, un cycloalkyle en C3-C6, un cycloalkyle en -CH2-(C3-C6), ou -(CH2)rOCH3, R3 étant -NH2, -NH-R4, -NHC(=0)-R4, -NHC(=O)NH-R4, -NHC(=S)-R4 ou -NHC(=S)NH-R4, R4 étant choisi parmi un cycloalkyle, un hétérocycle, un aryle ou un hétéroaryle, ou -L-R5, L étant choisi parmi un alkyle en C1-C5, un cycloalkyle, un hétérocycle, un aryle, ou un hétéroaryle et R5 est choisi parmi -OH, -CH2OH, -NH2, -COOH, -CONH2, -CONH-R6 ou des isostères d'acide carboxylique, R6 étant choisi parmi un alkyle C1-C4, avec n, m et r étant 0, 1, 2, 3, 4 ou 5. L'invention concerne également une utilisation associée dudit composé.
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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)