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1. (WO2018081204) DEUTERATED N-(5-((4-ETHYLPIPERAZIN-1-YL)METHYL) PYRIDIN-2-YL)-5-FLUORO-4-(4-FLUORO-1-ISOPROPYL-2-METHYL-1H-BENZO[d]IMIDAZOL-6-YL)PYRIMIDIN-2-AMINE
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Pub. No.: WO/2018/081204 International Application No.: PCT/US2017/058191
Publication Date: 03.05.2018 International Filing Date: 25.10.2017
IPC:
A61K 31/517 (2006.01) ,A61K 31/519 (2006.01) ,A61K 31/655 (2006.01)
[IPC code unknown for A61K 31/517][IPC code unknown for A61K 31/519][IPC code unknown for A61K 31/655]
Applicants:
LI, George, Y.; US
HOU, Duanjle; US (AllExceptUS)
Inventors:
LI, George, Y.; US
HOU, Duanjle; US
Agent:
LIU, Lance; US
Priority Data:
62/412,83526.10.2016US
Title (EN) DEUTERATED N-(5-((4-ETHYLPIPERAZIN-1-YL)METHYL) PYRIDIN-2-YL)-5-FLUORO-4-(4-FLUORO-1-ISOPROPYL-2-METHYL-1H-BENZO[d]IMIDAZOL-6-YL)PYRIMIDIN-2-AMINE
(FR) N-(5-((4-ÉTHYLPIPÉRAZINE-1-YL)MÉTHYL) PYRIDIN-2-YL)-5-FLUORO-4-(4-FLUORO-1-ISOPROPYL-2-MÉTHYL-1H-BENZO[D]IMIDAZOL-6-YL)PYRIMIDIN-2-AMINE DEUTÉRÉ
Abstract:
(EN) The present invention is related to compounds of Formula (I): (I) or a pharmaceutically acceptable salt thereof; wherein: Y1, Y2, Y3, Y4, Y4,, Y5, Y5,, Y6,Y6,, Y7, Y7,8, Y8', Y9, Y9', Y10, Y10', YI0", Y11, Y12, Y13, Y14, Y I4', Y14", Υ15, Y16, Υ16', Y16", Y17, Y17' and Y17" are selected from the group consisting of hydrogen or deuterium, wherein at least one of Y1, Y2, Y3, Y4, Y4,,Y5 Y5,, Y6, Y6,, Y7, Y7,, Y8, Y8', Y9, Y9', Y10, Y10', Y10", Υ11, Y12, Y13, Y14, Y14', Y14", Y15, Y16, Y16', Y16", Y17, Y17', and Y17'' is deuterium; and each carbon is independently optionally replaced with 13C. It also relates to pharmaceutical compositions comprising the compounds of Formula (I) and the use of these compounds as selective CDK4/6 inhibitors with the potential for treatment of pRb-positive tumor types including HR (hormone-receptor)-positive aid HER2 (human epidermal growth factor receptor 2)- negative breast cancer, melanoma, liposarcoma and non-small-cell lung cancer, alone or in combination with additional agents.
(FR) La présente invention concerne des composés de Formule (I): (I) ou un sel pharmaceutiquement acceptable de ceux-ci; dans laquelle : Y1, Y2, Y3, Y4, Y4,, Y5, Y5,, Y6,Y6,, Y7, Y7,8, Y8', Y9, Y9', Y10, Y10', YI0", Y11, Y12, Y13, Y14, Y I4', Y14", Υ15, Y16, Υ16', Y16", Y17, Y17' and Y17" sont choisis dans le groupe constitué par l'hydrogène ou le deutérium, au moins l'un parmi Y1, Y2, Y3, Y4, Y4,,Y5 Y5,, Y6, Y6,, Y7, Y7,, Y8, Y8', Y9, Y9', Y10, Y10', Y10", Υ11, Y12, Y13, Y14, Y14', Y14", Y15, Y16, Y16', Y16", Y17, Y17', et Y17'' étant un deutérium ; et chaque carbone est éventuellement remplacé indépendamment par 13C. L’invention concerne également des compositions pharmaceutiques comprenant les composés de Formule (I) et l'utilisation de ces composés en tant que inhibiteurs sélectifs de CDK4/6 avec le potentiel pour le traitement de types de tumeurs pRb positifs comprenant le cancer du sein négatif au HER2 (récepteur du facteur de croissance épidermique humain-2) et positif au HR (récepteur hormonal), le mélanome, le liposarcome et le cancer bronchique non à petites cellules, seuls ou en combinaison avec d'autres agents.
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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, JO, 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)