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1. (WO2013106643) COMPOUNDS & METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS & OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2013/106643 International Application No.: PCT/US2013/021136
Publication Date: 18.07.2013 International Filing Date: 11.01.2013
IPC:
C07K 19/00 (2006.01) ,C07D 413/12 (2006.01) ,C07D 413/14 (2006.01) ,C07D 207/26 (2006.01) ,C07J 9/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
19
Hybrid peptides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18
having one double bond between ring members or between a ring member and a non-ring member
22
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
24
Oxygen or sulfur atoms
26
2-Pyrrolidones
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
9
Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
Applicants:
YALE UNIVERSITY [US/US]; Two Whitney Avenue New Haven, CT 06511, US
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED [GB/GB]; 980 Great West Road Brentford, Middlesex TW8 9GS, GB
CAMBRIDGE ENTERPRISE LIMITED UNIVERSITY OF CAMBRIDGE [GB/GB]; Hause Forum 3 Charles Babbage Road Cambridge CB3 0GT, GB
Inventors:
CREWS, Craig, M.; US
BUCKLEY, Dennis; US
CIULLI, Alessio; GB
JORGENSEN, William; US
GAREISS, Peter, C.; US
MOLLE, Inge, Van; GB
GUSTAFSON, Jeffrey; US
TAE, Hyun-Seop; US
MICHEL, Julien; GB
HOYER, Dentin, Wade; US
ROTH, Anke, G.; DE
HARLING, John, David; GB
SMITH, Ian Edward, David; GB
MIAH, Afjal, Hussain; GB
CAMPOS, Sebastien, Andre; GB
LE, Joelle; GB
Agent:
COLEMAN, Henry, D.; Coleman Sudol Sapone, P.C. 714 Colorado Avenue Bridgeport, CT 06605-1601, US
Priority Data:
61/585,76912.01.2012US
Title (EN) COMPOUNDS & METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS & OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE
(FR) COMPOSÉS ET PROCÉDÉS POUR LA DÉGRADATION AMÉLIORÉE DE PROTÉINES CIBLES ET D'AUTRES POLYPEPTIDES PAR UNE E3 UBIQUITINE LIGASE
Abstract:
(EN) The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
(FR) La présente invention concerne des composés bifonctionnels, qui sont utiles en tant que modulateurs de l'ubiquitination ciblée, en particulier en tant qu'inhibiteurs d'une variété de polypeptides et d'autres protéines qui sont dégradées et/ou autrement inhibées par des composés bifonctionnels selon la présente invention. En particulier, la présente invention concerne des composés qui contiennent à une extrémité un ligand VHL qui se lie à l'ubiquitine ligase et à l'autre extrémité une fraction qui se lie à une protéine cible de telle sorte que la protéine cible est placée à proximité à l'ubiquitine ligase pour permettre la dégradation (et l'inhibition) de cette protéine. La présente invention concerne un large éventail d'activités pharmacologiques associées à des composés selon la présente invention, cohérentes avec la dégradation/l'inhibition des polypeptides ciblés.
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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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, 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, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)