- IONIZABLE LIPIDS AND NANOPARTICLE COMPOSITIONS THEREOF
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Provided herein are ionizable lipids represented by the Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R1, R2, R3, R4, R5,R6, m, and n are as defined herein. Also provided herein are lipid nanoparticle (LNP) compositions comprising an ionizable lipid of the invention and a capsid-free, non-viral vector (e.g., ceDNA). These LNPs can be used to deliver a capsid-free, non-viral DNA vector to a target site of interest (e.g., cell, tissue, organ, and the like).
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Page/Page column 90; 99-100
(2021/05/29)
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- Direct Addition of Amides to Glycals Enabled by Solvation-Insusceptible 2-Haloazolium Salt Catalysis
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The direct 2-deoxyglycosylation of nucleophiles with glycals leads to biologically and pharmacologically important 2-deoxysugar compounds. Although the direct addition of hydroxyl and sulfonamide groups have been well developed, the direct 2-deoxyglycosylation of amide groups has not been reported to date. Herein, we show the first direct 2-deoxyglycosylation of amide groups using a newly designed Br?nsted acid catalyst under mild conditions. Through mechanistic investigations, we discovered that the amide group can inhibit acid catalysts, and the inhibition has made the 2-deoxyglycosylation reaction difficult. Diffusion-ordered two-dimensional NMR spectroscopy analysis implied that the 2-chloroazolium salt catalyst was less likely to form aggregates with amides in comparison to other acid catalysts. The chlorine atom and the extended π-scaffold of the catalyst played a crucial role for this phenomenon. This relative insusceptibility to inhibition by amides is more responsible for the catalytic activity than the strength of the acidity.
- Nakatsuji, Yuya,Kobayashi, Yusuke,Takemoto, Yoshiji
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supporting information
p. 14115 - 14119
(2019/09/13)
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- COMPOSITIONS AND METHODS FOR DELIVERY OF THERAPEUTIC AGENTS
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This disclosure provides improved lipid-based compositions, including lipid nanoparticle compositions, and methods of use thereof for delivering agents in vivo including nucleic acids and proteins. These compositions are not subject to accelerated blood clearance and they have an improved toxicity profile in vivo.
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Page/Page column 339
(2017/07/18)
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- A METHOD OF TREATING PERIPHERAL INFLAMMATORY DISEASE
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An active for use in the treatment or inhibition of an inflammatory disease associated with over-activation of Toll-like Receptor 4 (TLR4), Toll-like Receptor 2 (TLR2) and Myeloid differentiating protein 88 (Myd88) adaptor-like protein (Mal) while maintaining a subject's ability to respond normally to a pathogen, in which the active is an oleamide or a derivative thereof.
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Paragraph 0078-0084
(2016/12/01)
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- Synthesis of fatty N-alkyl amides
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Fatty N-alkyl amides are synthesized directly from glycerides (preferably triglycerides) and amines in the absence of a catalyst, and preferably without a solvent. The method provides for products suitable for use without further purification, preferably after separating the glycerol and amide products. The disclosed method is also useful for the synthesis of glycerol from glycerides and ammonia and/or primary amines.
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