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1. (WO2014201405) NOVEL ALLOSTERIC INHIBITORS OF PROTEASOME AND METHODS OF USE THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2014/201405    International Application No.:    PCT/US2014/042383
Publication Date: 18.12.2014 International Filing Date: 13.06.2014
IPC:
A61K 31/445 (2006.01), A01N 43/34 (2006.01), C07D 211/00 (2006.01)
Applicants: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM [US/US]; 201 W. 7th St. Austin, TX 78701 (US)
Inventors: OSMULSKI, Pawel, A.; (US).
GACZYNSKA, Maria, E.; (US)
Agent: HIGHLANDER, Steven L.; Parker Highlander PLLC 1120 S. Capital of Texas Highway Building One, Suite 200 Austin, TX 78746 (US)
Priority Data:
61/835,221 14.06.2013 US
Title (EN) NOVEL ALLOSTERIC INHIBITORS OF PROTEASOME AND METHODS OF USE THEREOF
(FR) NOUVEAUX INHIBITEURS ALLOSTÉRIQUES DU PROTÉASOME ET MÉTHODES D'UTILISATION ASSOCIÉES
Abstract: front page image
(EN)The present invention relates generally to novel allosteric regulators of proteasome activity, methods for preparation and use, and pharmaceutical compositions thereof. Specifically piperidine-2-carboxylic acid derivatives containing 1-oxo-aroyl group and a lipophilic ester side chain are disclosed as allosteric inhibitors of proteasome 2S activity, and as therapeutic agents for the treatment of proteasome-associated disorders in a subject.
(FR)L'invention concerne en général de nouveaux régulateurs allostériques de l'activité du protéasome, des méthodes de préparation et d'utilisation, ainsi que des compositions pharmaceutiques associées. L'invention concerne en particulier des dérivés d'acide pipéridine-2-carboxylique contenant un groupe 1-oxo-aroyle et une chaîne latérale d'ester lipophile, utilisés en tant qu'inhibiteurs allostériques de l'activité du protéasome 2S, ainsi que des agents thérapeutiques destinés au traitement des troubles liés au protéasome chez un patient.
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, IR, IS, JP, KE, KG, 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, 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 (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)