Novel lipids and compositions for the delivery of therapeutics

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专利权人:

Arbutus Biopharma Corporation

发明人:

Manoharan, Muthiah,Rajeev, Kallanthottathil G.,Jayaraman, Muthusamy,Butler, David,Narayanannair, Jayaprakash K.,Maier, Martin,Eltepu, Laxman

申请号：

AU2017279739

公开号：

AU2017279739A1

申请日:

2017.12.21

申请国别(地区):

AU

年份:

2018

代理人:

摘要：

#$%^&*AU2017279739A120180125.pdf#####NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure (I) wherein R1 and R2 are each independently for each occurrence optionally substituted Cio-C30 alkyl, optionally substituted C10-C 30 alkenyl, optionally substituted C10 -C30 alkynyl, optionally substituted Cio-C30 acyl, or -linker-ligand； R3 is H, optionally substituted C1 -Cio alkyl, optionally substituted C 2-Cio alkenyl, optionally substituted C 2 -Cio alkynyl, alkylheterocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, o-aminoalkyls, (o-(substituted)aminoalkyls, o-phosphoalkyls, to othiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand； E is 0, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O) 2N(Q), S(O) 2 , N(Q)S(O) 2 , SS, O=N, aryl, heteroaryl, cyclic or heterocycle； and, Q is H, alkyl, o-aminoalkyl, o-(substituted)aminoalkyl, o-phosphoalkyl or o-thiophosphoalkyl. Figure L X= NH(CO), (CO)NH, NH(CO)O O(CO)NH, 0, NH(CO)Nt. S-S R= CH3, (CH2)io-. Y= (01- GuCNAc, Maaose, Lactose, Glucose, Fucose Ym (CH2a- (GaiNAc)2, (Mannose) 2 ,( Lactose)2, (Glucose)2, (FuCose2 Y= (CH2)n- (GalNAc)*. (Mannose),( Laclose). (Glucose)3 , (Fucose3 Y= (CHr-CrO)- GaINAc, Mannose, Lactose, Glucose, rucose Y' (CHrCH2rO)a- (GaINAc) 2, (Mannose,(2. Lactose)2, (Glucosai 2, (Fucosea Y& (CH2-CH2 Oa- (GaJNAch, (Mannose) 3,( Lactose),. (Glucose 3 , (Fucose)3 n 1-10 X= NH(0O3, (CO)NH. NI-4(O)O OfCO)NH, 0, NH(C)IH, 3-3 R=CH3.-(H)Y= (Cz)t1- GaINA, Mannose, Laciose Glucosa Fucose Y= (CH2)n- (GalNAc)g, (Mannose)2.(

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