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1. (WO2010088537) IMPROVED LIPID FORMULATION FOR THE DELIVERY OF NUCLEIC ACIDS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/088537 International Application No.: PCT/US2010/022614
Publication Date: 05.08.2010 International Filing Date: 29.01.2010
IPC:
A61K 9/127 (2006.01) ,A61K 48/00 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
10
Dispersions; Emulsions
127
Liposomes
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
48
Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
Applicants:
ALNYLAM PHARMACEUTICALS, INC. [US/US]; 300 Third Street Cambridge, MA 02142, US (AllExceptUS)
AKINC, Akin [US/US]; US (UsOnly)
QUERBES, William; US (UsOnly)
WONG, Frances; US (UsOnly)
DORKIN, Joseph, Robert; US (UsOnly)
QIN, Xiaojun; US (UsOnly)
CANTLEY, William; US (UsOnly)
BORODOVSKY, Anna; US (UsOnly)
DE, Soma; US (UsOnly)
MANOHARAN, Muthiah [US/US]; US (UsOnly)
JAYARAMAN, Muthusamy; US (UsOnly)
RAJEEV, Kallanthottathil, G. [IN/US]; US (UsOnly)
Inventors:
AKINC, Akin; US
QUERBES, William; US
WONG, Frances; US
DORKIN, Joseph, Robert; US
QIN, Xiaojun; US
CANTLEY, William; US
BORODOVSKY, Anna; US
DE, Soma; US
MANOHARAN, Muthiah; US
JAYARAMAN, Muthusamy; US
RAJEEV, Kallanthottathil, G.; US
Agent:
MCCARTY, Catherine, M.; Lowrie, Lando & Anastasi LLP One Main Street, Eleventh Floor Cambridge, MA 02142, US
Priority Data:
61/148,36629.01.2009US
61/156,85102.03.2009US
61/185,71210.06.2009US
61/228,37324.07.2009US
61/239,68603.09.2009US
Title (EN) IMPROVED LIPID FORMULATION FOR THE DELIVERY OF NUCLEIC ACIDS
(FR) PRÉPARATION LIPIDIQUE AMÉLIORÉE
Abstract:
(EN) The invention features an improved lipid formulation comprising a cationic lipid of formula (A), a neutral lipid, a sterol and a PEG or PEG-modified lipid, where R1 and R2 are independently alkyl, alkenyl or alkynyl, each can be optionally substituted, and R3 and R4 are independently lower alkyl or R3 and R4 can be taken together to form an optionally subsituted heterocyclic ring. In one embodiment, R1 and R2 are independently selected from oleoyl, pamitoyl, steroyl, linoleyl and R3 and R4 are methyl. Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.
(FR) La présente invention concerne une préparation lipidique améliorée comprenant un lipide cationique de formule (A), un lipide neutre, un stérol et un lipide PEG ou modifié par PEG, où R1 et R2 sont indépendamment un groupe alkyle, alcényle ou alcynyle, chacun pouvant être facultativement substitué, et R3 et R4 sont indépendamment un groupe alkyle inférieur ou R3 et R4 peuvent être pris ensemble pour former un anneau hétérocyclique facultativement substitué. Dans un mode de réalisation, R1 et R2 sont indépendamment choisis parmi un groupe oléoyl, palmitoyl, stéaroyl, linoleyl et R3 et R4 sont un groupe méthyle. L'invention concerne également des lipides ciblants et des préparations lipidiques spécifiques comprenant de tels lipides ciblants.
front page image
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 (ARIPO) (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, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, 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: English (EN)
Filing Language: English (EN)
Also published as:
EP2391343US20120101148CA2751342AU2010208035EP3243504