- LIPIDS FOR LIPID NANOPARTICLE DELIVERY OF ACTIVE AGENTS
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Compounds are provided having the following structure: (I) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein G1, R1, R2, L, and n are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.
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Page/Page column 54
(2020/05/21)
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- Synthesis method of ascorbyl tetraisopalmitate
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The invention discloses a synthesis method of ascorbyl tetraisopalmitate. The method comprises the following steps of reacting to generate 2-hexyldecanoyl chloride by utilizing 2-hexyldecanoic acid and a chlorinating reagent; enabling the 2-hexyldecanoyl chloride to react with L-ascorbic acid to generate the ascorbyl tetraisopalmitate; preparing the ascorbyl tetraisopalmitate through post treatment of extraction, water scrubbing, drying, concentration, purification and the like. The method is stable in yield, lower in cost, simple in equipment and less in investment and is easy to industriallyimplementation.
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Paragraph 0024-0027; 0030-0033; 0036-0039; 0042-0045
(2018/06/04)
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- LIPID DELIVERY OF THERAPEUTIC AGENTS TO ADIPOSE TISSUE
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A method of treating a disease mediated by protein expression in adipose tissue by intraperitoneally administering a composition comprising a lipid nanoparticle encapsulating or associated with a therapeutic agent (e.g., a nucleic acid), thereby delivering the therapeutic agent to adipose tissue of the subject and altering protein expression in the adipose tissue is provided herein. A method for delivering a therapeutic agent to adipose tissue of a subject in need thereof is also provided.
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Page/Page column 147-148
(2018/11/10)
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- Branched-chain and dendritic lipids for nanoparticles
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Lipid nanoparticles (LNPs) for drug-delivery applications are largely derived from natural lipids. Synthetic lipids, particularly those incorporating branched hydrocarbons and hyper-branched hydrocarbon architectures, may afford enhanced lipophilicity with enhanced fluidity and thereby lead to LNP stabilization. Hydrocarbon anchors based on serinol diesters were prepared from linear Cn (n = 14, 16, 18) and branched (n = 16) acids with Boc-protected serinol. These diesters were further dimerized on an iminodiacetamide backbone to provide eight branched-chain and dendritic lipid anchors. Derivatization of these core structures provided eight PEG-lipids and seven thiopurine linked lipid-drug conjugates. LNPs were prepared by microfluidic mixing from mixed lipids in ethanol diluted into aqueous media. The lipid-drug conjugates incorporated 5 mol% of a phosphocholine and 5 mol% of a commercial PEG-lipid to form LNPs with a thiopurine drug loading of 15 wt%. The PEG-lipids prepared were formulated at 1.5 mol% as a surface stabilizer to LNPs containing dsDNA lipoplexes. The stability of the LNPs was assessed under different storage conditions through monitoring of particle size. For both LNPs from lipid-Thiopurine conjugates and the PEG-lipid systems, there is strong preliminary evidence that hydrocarbon branching results in LNP stabilization. Four of the lipid-drug conjugate formulations were stable to cell culture conditions (10% serum, 37 °C) and the toxicity of these LNPs was assessed in two cell lines relative to the free thiopurines in the medium. The observed toxicity is consistent with cellular uptake of the LNPs and reductive release of the cargo thiopurine within the cell.
- Meanwell, Michael W.,O'Sullivan, Connor,Howard, Perry,Fyles, Thomas M.
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supporting information
p. 120 - 129
(2017/02/10)
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- Method for cleaving alpha carbon-carbon single bonds in ketone under condition of metal-free catalysis
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The invention discloses a method for selectively activating and cleaving alpha carbon-carbon single bonds in ketone under the condition of metal-free catalysis. The method is characterized in that the alpha carbon-carbon single bonds in the ketone are activated and cleaved by solvent induction and driving of intermediate structure factors formed by the ketone and hydrazine without metal catalysts. Transition metal for catalysis is omitted, the method is environmentally friendly, reaction cost is reduced to a certain degree, methodology of selective cleavage of the carbon-carbon single bonds is enriched, and a new idea is provided for activation of inertial chemical bonds under mild conditions.
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Paragraph 0017; 0020
(2017/10/07)
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- ALIPHATIC-AROMATIC HETEROCYCLIC COMPOUNDS AND USES THEREOF IN METAL EXTRACTANT COMPOSITIONS
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The invention relates to an aliphatic-aromatic heterocyclic compound A which comprises at least two heterocyclic rings B and C, to a metal extractant composition E comprising this aliphatic-aromatic heterocyclic compound A and an organic acid D having at least one carboxylic, sulfonic, sulfuric, phosphinic, phosphonic, or phosphoric acid group, and to a process to extract one or more metals M selected from the group consisting of Ni and Co from an aqueous acidic leach solution PL comprising ions of at least one of the metals M, and further, at least one kind of further ions selected from the group consisting of Fe ions, Al ions, Cu ions, Mg ions, Mn ions, and also silicate anions, by mixing the solution PL with an extractant composition E, separating the organic and aqueous phases, and recovering the metal M from the separated organic phase.
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Paragraph 0162-0163
(2016/09/26)
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- Organogel compositions comprising alkylated benzimidazolones
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Disclosed is a composition comprising an organogel which comprises: (a) an alkylated benzimidazolone compound; and (b) an organic liquid.
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Page/Page column 20-21
(2015/05/05)
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- SELF-ASSEMBLED NANOSTRUCTURES
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An alkylated benzimidazolone compound of the formula: wherein at least one of R1 to R4 is X—Rc, where X represents a linking group, and Ra, Rb, and Rc independently represents substituted or unsubstituted alkyl groups, provided that at least one of Ra and Rb represents H. The present disclosure provides alkylated benzimidazolone compounds and self-assembled nanostructures formed from alkylated benzimidazolone compounds.
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Page/Page column 12
(2011/11/30)
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- Bna Conjugates and Methods of Use
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Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, decreasing arterial blood pressure and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the hBNP compound are also disclosed, having an amino acid sequence that is other than the native sequence.
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Page/Page column 22
(2008/12/08)
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- Mild methods to assemble and pattern organic monolayers on hydrogen-terminated Si(111)
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Mild methods to assemble well-ordered organic monolayers of olefins on Si(111) using 2,2,6,6-tetramethyl-1-piperidinyloxy and to pattern these monolayers on the micrometer-size scale using soft lithography are reported. The Royal Society of Chemistry 2005.
- Arafat, Samer N.,Dutta, Samrat,Perring, Mathew,Mitchell, Michael,Kenis, Paul J. A.,Bowden, Ned B.
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p. 3198 - 3200
(2007/10/03)
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- Structural Effect of Mixed Micelles in the Selective Deacylation of p-Nitrophenyl Carboxylates by Specific Hydroxamic Acids
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Factors controlling the enhanced and selective deacylations of p-nitrophenyl carboxylates (Sn) possessing an appropriate acyl chain by several hydroxamic acids (C10, BHA, PAHA, and HDHA) with cationic surfactants (DTAC, CTAB, CEAB, CBzAC, and O
- Ueoka, Ryuichi,Matsumoto, Yoko
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p. 2660 - 2692
(2007/10/02)
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