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1. (WO2018226542) MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE
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Pub. No.: WO/2018/226542 International Application No.: PCT/US2018/035748
Publication Date: 13.12.2018 International Filing Date: 01.06.2018
IPC:
C07D 417/14 (2006.01) ,C07D 401/14 (2006.01) ,A61K 31/47 (2006.01) ,A61K 31/4725 (2006.01) ,A61P 35/00 (2006.01) ,A61P 29/00 (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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
47
Quinolines; Isoquinolines
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
47
Quinolines; Isoquinolines
472
Non-condensed isoquinolines, e.g. papaverine
4725
containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
Applicants:
ARVINAS, INC. [US/US]; 5 Science Park New Haven, CT 06511, US
YALE UNIVERSITY; Office of Cooperative Research 2 Whitney Avenue New Haven, CT 06510, US
Inventors:
CREW, Andrew P.; US
DONG, Hanqing; US
WANG, Jing; US
CREWS, Craig M.; US
JAIME-FIGUEROA, Saul; US
Agent:
ZERHUSEN, Bryan Daniel; US
Priority Data:
62/517,58109.06.2017US
62/563,61226.09.2017US
Title (EN) MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE
(FR) MODULATEURS DE PROTÉOLYSE ET PROCÉDÉS D'UTILISATION ASSOCIÉS
Abstract:
(EN) The present disclosure relates to bifunctional compounds, which find utility as modulators of c-Met and/or p38 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
(FR) La présente invention concerne des composés bifonctionnels qui sont utiles en tant que modulateurs de c-Met et/ou de p38 (protéine cible). En particulier, la présente invention concerne des composés bifonctionnels, qui contiennent, sur une extrémité, un ligand de Von Hippel-Lindau, de céréblon, d'inhibiteurs de protéines d'apoptose ou d'homologue 2 de double-minute de souris, qui se lie à l'ubiquitine ligase E3 respective, et, sur l'autre extrémité, une fraction qui se lie à la protéine cible, de sorte que la protéine cible se trouve à proximité de l'ubiquitine ligase pour effectuer la dégradation (et l'inhibition) de la protéine cible. La présente invention présente une large plage d'activités pharmacologiques associées à la dégradation/l'inhibition de la protéine cible. Les composés et les compositions de la présente invention sont destinés à être utilisés dans le traitement ou la prévention de maladies ou de troubles résultant de l'agrégation ou de l'accumulation de la protéine cible.
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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)