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1. (WO2014093723) SYNTHÈSE GAP DE VELCADE, ANALOGUES DIMÈRES ET COMPOSÉS AMINÉS
Dernières données bibliographiques dont dispose le Bureau international   

N° de publication :    WO/2014/093723    N° de la demande internationale :    PCT/US2013/074830
Date de publication : 19.06.2014 Date de dépôt international : 12.12.2013
CIB :
C07F 9/36 (2006.01), C07F 9/34 (2006.01), C07F 9/06 (2006.01), A61K 33/42 (2006.01), A61P 35/00 (2006.01)
Déposants : NANJING UNIVERSITY [CN/CN]; Institute of Chemistry and Biomedical Sciences #22 Hankou Road Jiangsu Nanjing, 210093 (CN)
Inventeurs : LI, Guigen; (US)
Mandataire : WANG, Stephanie; DLA Piper LLP (US) 555 Mission Street, Suite 2400 San Francisco, CA 94105-2933 (US)
Données relatives à la priorité :
61/736,357 12.12.2012 US
61/761,131 05.02.2013 US
Titre (EN) GROUP-ASSISTANT-PURIFICATION (GAP) SYNTHESIS OF VELCADE, DIMERIC ANALOGS, AND AMINO COMPOUNDS
(FR) SYNTHÈSE GAP DE VELCADE, ANALOGUES DIMÈRES ET COMPOSÉS AMINÉS
Abrégé : front page image
Provided herein are novel methods of GAP synthesis of Velcade, Velcade analogs and amino compounds. The methods involve organic syntheses with chiral auxiliaries which allow pure products, often pure isomers, to be obtained simply by washing crude products with organic solvents. In preferred embodiments, chiral auxiliaries can be recycled easily after deprotection, in some cases without racemization of the chiral auxiliaries. The chiral auxiliaries can be phosphonyl or phosphinyl auxiliaries. The phosphonyl and phosphinyl auxiliaries can provide efficient asymmetric induction and control in organic transformations. Additionally, corresponding chiral products, mostly solidified, can be utilized to synthesize Velcade, Velcade analogs and amino compounds. Also provided herein are novel dimeric Velcade analogs and methods of synthesis thereof, which have potential use as alternatives to Velcade monomer cancer therapeutics.
États désignés : 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.
Organisation régionale africaine de la propriété intellectuelle (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Office eurasien des brevets (OEAB) (AM, AZ, BY, KG, KZ, RU, TJ, TM)
Office européen des brevets (OEB) (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)
Organisation africaine de la propriété intellectuelle (OAPI) (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Langue de publication : anglais (EN)
Langue de dépôt : anglais (EN)