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1. (WO2006087752) CATIONIC LIPIDS FOR THE TRANSFECTION OF NUCLEIC ACIDS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2006/087752    International Application No.:    PCT/IT2006/000072
Publication Date: 24.08.2006 International Filing Date: 13.02.2006
IPC:
C07D 251/54 (2006.01), A61K 31/53 (2006.01), C12N 15/00 (2006.01)
Applicants: POLITECNICO DI MILANO [IT/IT]; Piazza Leonardo da Vinci, 32, I-20133 Milano (IT) (For All Designated States Except US).
ZANDA, Matteo [IT/IT]; (IT) (For US Only).
BRUCHE', Luca [IT/IT]; (IT) (For US Only).
FRIGERIO, Massimo [IT/IT]; (IT) (For US Only).
VIANI, Fiorenza [IT/IT]; (IT) (For US Only).
CHIAMENTI, Luca [IT/IT]; (IT) (For US Only).
PANZERI, Walter [IT/IT]; (IT) (For US Only).
ZAFFARONI, Nadia [IT/IT]; (IT) (For US Only).
FOLINI, Marco [IT/IT]; (IT) (For US Only).
GRECO, Maria Angela [IT/IT]; (IT) (For US Only)
Inventors: ZANDA, Matteo; (IT).
BRUCHE', Luca; (IT).
FRIGERIO, Massimo; (IT).
VIANI, Fiorenza; (IT).
CHIAMENTI, Luca; (IT).
PANZERI, Walter; (IT).
ZAFFARONI, Nadia; (IT).
FOLINI, Marco; (IT).
GRECO, Maria Angela; (IT)
Agent: LONG, Giorgio; Jacobacci & Partners S.p.A., Via Senato, 8, I-20121 Milano (IT)
Priority Data:
MI2005A000222 15.02.2005 IT
Title (EN) CATIONIC LIPIDS FOR THE TRANSFECTION OF NUCLEIC ACIDS
(FR) LIPIDES CATIONIQUES POUR LA TRANSFECTION D'ACIDES NUCLEIQUES
Abstract: front page image
(EN)The present invention relates to cationic lipids capable of forming complexes with nucleic acids and the use thereof for the transfection of eukaryotic cells. The cationic lipids according to the invention have general formulas (I) and (Ia): (see formulas (I) and (Ia), wherein E is a heteroaryl; Rl and R2 are selected from H, -R7-NH2, -CH-NH-NH2, alkyl; R7 is selected from alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl- (C0-C20) alkyl; R3 and R4 are selected from: H, -R8-SH, -R8-NH-NH2/ -R8-CO-R9 or - R8-NH2; R8 is selected from: alkyl, alkenyl, aryl, (C1- C20) alkyl-aryl- (C0 -C20 ) alkyl; R9 is selected from: H, alkyl; R5 and R6 are selected from: H, alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl.
(FR)La présente invention concerne, d'une part des lipides cationiques capables de former des complexes avec des acides nucléiques, et d'autre part leur utilisation pour la transfection de cellules eucariotes. Les lipides cationiques selon l'invention sont représentés par les formules générales (I) et (Ia). Dans ces formules, E est hétéroaryle. R1 et R2 sont H, -R7-NH2, -CH-NH-NH2, ou alkyle; R7 est alkyle, alcényle, aryle, (C1-C20) alkylaryle- (C0-C20) alkyle; R3 et R4 sont H, -R8-SH, -R8-NH-NH2/ -R8-CO-R9 ou - R8-NH2; R8 est alkyle, alcényle, aryle, (C1-C20) alkylaryle- (C0-C20) alkyle; R9 est H ou alkyle; enfin, R5 et R6 sont H, alkyle, alcényle, aryle ou (C1-C20) alkyl-aryl.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, 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 (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, 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: Italian (IT)