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1. (WO2017185031) DEGRADATION OF CYCLIN-DEPENDENT KINASE 4/6 (CDK4/6) BY CONJUGATION OF CDK4/6 INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Pub. No.: WO/2017/185031 International Application No.: PCT/US2017/028941
Publication Date: 26.10.2017 International Filing Date: 21.04.2017
IPC:
C07D 487/04 (2006.01) ,C07D 471/04 (2006.01) ,C07D 401/14 (2006.01) ,A61K 31/519 (2006.01)
Applicants: DANA-FARBER CANCER INSTITUTE, INC.[US/US]; 450 BROOKLINE AVENUE Boston, Massachusetts 02215, US
Inventors: GRAY, Nathanael; US
ZHANG, Tinghu; US
OLSON, Calla M.; US
LIANG, Yanke; US
KWIATKOWSKI, Nicholas; US
Agent: ERLACHER, Heidi; US
CHEN, Chen; US
Priority Data:
62/326,57122.04.2016US
Title (EN) DEGRADATION OF CYCLIN-DEPENDENT KINASE 4/6 (CDK4/6) BY CONJUGATION OF CDK4/6 INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
(FR) DÉGRADATION DE LA KINASE 4/6 CYCLINE-DÉPENDANTE (CDK4/6) PAR CONJUGAISON D'INHIBITEURS DE CDK4/6 AVEC UN LIGAND DE TYPE LIGASE E3 ET LEURS PROCÉDÉS D'UTILISATION
Abstract: front page image
(EN) The present application provides bifunctional compounds of Formula (I), or Targeting Ligand, or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.
(FR) La présente demande concerne des composés bifonctionnels de formule (I), ou ligand de ciblage, ou sel pharmaceutiquement acceptable, hydrate, solvate, promédicament, stéréoisomère ou tautomère de ceux-ci, qui agissent comme des fragments induisant la dégradation protéique pour la kinase 4 cycline-dépendante (CDK4) et/ou la kinase 6 cycline-dépendante (CDK6). Des procédés de dégradation ciblée de CDK4 et/ou CDK6 par utilisation des composés bifonctionnels qui lient un fragment se liant à un fragment d'ubiquitine ligase à un ligand capable de se lier à CDK4 et/ou CDK6 et peuvent être utilisés dans le traitement des troubles modulés par CDK4 et/ou CDK6 sont en outre décrits.
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)