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1. (WO2011135138) LIPOPHILIC DERIVATIVES OF NUCLEIC ACIDS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2011/135138    International Application No.:    PCT/ES2011/070293
Publication Date: 03.11.2011 International Filing Date: 25.04.2011
IPC:
A61K 48/00 (2006.01), A61K 47/48 (2006.01), C12N 15/87 (2006.01)
Applicants: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS (CSIC) [ES/ES]; Serrano, 117 E-28006 Madrid (ES) (For All Designated States Except US).
UNIVERSIDAD DE BARCELONA [ES/ES]; Avenida Diagonal, 645 E-08028 Barcelona (ES) (For All Designated States Except US).
CIBER-BBN [ES/ES]; Campus Rio Ebro. Edificio I+D. Bloque 5, 1ª Planta. Calle Poeta Mariano Esquilor, s/n E-50018 Zaragoza (ES) (For All Designated States Except US).
ERITJA CASADELLÁ, Ramón [ES/ES]; (ES) (For US Only).
OCAMPO, Sandra Milena [CO/ES]; (ES) (For US Only).
PERALES LOSA, José Carlos [ES/ES]; (ES) (For US Only).
GRIJALVO TORRIJO, Santiago [ES/ES]; (ES) (For US Only).
AVIÑO ANDRÉS, Ana [ES/ES]; (ES) (For All Designated States Except US)
Inventors: ERITJA CASADELLÁ, Ramón; (ES).
OCAMPO, Sandra Milena; (ES).
PERALES LOSA, José Carlos; (ES).
GRIJALVO TORRIJO, Santiago; (ES)
Agent: UNGRIA LÓPEZ, Javier; Avenida Ramón y Cajal, 78 E-28043 Madrid (ES)
Priority Data:
P201030611 27.04.2010 ES
Title (EN) LIPOPHILIC DERIVATIVES OF NUCLEIC ACIDS
(ES) DERIVADOS LIPOFÍLICOS DE ÁCIDOS NUCLEICOS
(FR) DÉRIVÉS LIPOPHILES D'ACIDES NUCLÉIQUES
Abstract: front page image
(EN)The invention relates to novel derivatives of siRNA. The siRNA modified according to the invention improves the introduction thereof into cells and the stability of same to nuclease-induced degradation, thereby increasing the inhibitory capacity of the siRNA. These novel compounds contain lipids bound to a bridge molecule at the terminal end of the siRNA duplex by means of ether type bonds. The invention also relates to the synthesis of said compounds.
(ES)En esta invención se describen nuevos derivados del pARNi. El pARNi modificado según la invención mejora su entrada en las células y su estabilidad a la degradación por nucleasas, aumentando la capacidad inhibitoria de los pARNi. Estos nuevos compuestos contienen lípidos unidos a una molécula puente presente en el extremo terminal del dúplex de pARNi mediante enlaces tipo éter. También se describe la síntesis de dichos compuestos.
(FR)L'invention concerne de nouveaux dérivés du pARNI. Le pARNi modifié selon l'invention améliore son entrée dans les cellules et sa stabilité face à la dégradation par des nucléases, augmentant la capacité inhibitrice des pARNI. Ces nouveaux composés contiennent des lipides liés à une molécule pont présente à l'extrémité terminale du duplex de pARNI au moyen de liaisons de type éther. L'invention concerne également la synthèse de ces composés.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, 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, PE, PG, PH, PL, PT, RO, RS, RU, 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, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, 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, ML, MR, NE, SN, TD, TG).
Publication Language: Spanish (ES)
Filing Language: Spanish (ES)