146462-60-4Relevant academic research and scientific papers
LIPIDIC COMPOUNDS COMPRISING AT LEAST ONE TERMINAL RADICAL OF FORMULA -NH-CX-A OR -NH-CX-NH-A, COMPOSITIONS CONTAINING THEM AND USES THEREOF
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, (2022/01/24)
The disclosure concerns new lipid compounds, lipid nanoparticles (LNPs) containing them, and the use of lipid compounds or LNPs for nucleic acid administration. The lipid compounds according to the disclosure comprise at least one terminal radical of formula (I): *-NH-CX-(NH)n-A (I), wherein: -*- Represents a simple bond binding said radical of formula (I), directly or indirectly, to a lipophilic or hydrophobic tail group in C10 to C55; - n is 0 or 1; - X is an oxygen atom or a sulfur atom, and - A represents an unsaturated heterocyclic radical with 5 or 6 chains optionally substituted or a heteroaromatic cyclic radical with 5 or 6 links, both containing at least one nitrogen atom; or one of the pharmaceutically acceptable salts of said radical of formula (I); and said compound being in all possible racemic isomers, enantiomers and diastereoisomers.
DENDRITIC POLYETHYLENE GLYCOL DERIVATIVE, AND PREPARATION METHOD AND APPLICATION THEREOF
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Paragraph 0169, (2020/05/14)
The disclosure discloses a dendritic polyethylene glycol derivative and a preparation method and an application thereof. The dendritic polyethylene glycol derivative has a structure of formula (I), has multiple end functional groups, has a stronger water solubility in comparison with linear-chain polyethylene glycol, and can solve a problem of insufficient water solubility due to the increase of load when modifying an insoluble drug by the polyethylene glycol. The preparation method of the dendritic polyethylene glycol derivative provided by the disclosure has mild reaction conditions, is green and environmentally friendly, is low in cost, and is easy to implement industrialization.
Ligand-Phospholipid Conjugation: A Versatile Strategy for Developing Long-Acting Ligands That Bind to Membrane Proteins by Restricting the Subcellular Localization of the Ligand
Kawamura, Shuhei,Ito, Yoshihiko,Hirokawa, Takatsugu,Hikiyama, Eriko,Yamada, Shizuo,Shuto, Satoshi
supporting information, p. 4020 - 4029 (2018/05/07)
We hypothesized that if drug localization can be restricted to a particular subcellular domain where their target proteins reside, the drugs could bind to their target proteins without being metabolized and/or excreted, which would significantly extend the half-life of the corresponding drug-target complex. Thus, we designed ligand-phospholipid conjugates in which the ligand is conjugated with a phospholipid through a polyethylene glycol linker to restrict the subcellular localization of the ligand in the vicinity of the lipid bilayer. Here, we present the design, synthesis, pharmacological activity, and binding mode analysis of ligand-phospholipid conjugates with muscarinic acetylcholine receptors as the target proteins. These results demonstrate that ligand-phospholipid conjugation can be a versatile strategy for developing long-acting ligands that bind to membrane proteins in drug discovery.
HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 37; 38; 40, (2013/07/05)
The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
Radiofluorinated pyrimidine-2,4,6-triones as molecular probes for noninvasive MMP-targeted imaging
Breyholz, Hans-Joerg,Wagner, Stefan,Faust, Andreas,Riemann, Burkhard,Hoeltke, Carsten,Hermann, Sven,Schober, Otmar,Schaefers, Michael,Kopka, Klaus
scheme or table, p. 777 - 789 (2011/01/05)
Matrix metalloproteinases (MMPs) are zinc- and calcium-dependent endopeptidases. Representing a subfamily of the metzincin superfamily, MMPs are involved in the proteolytic degradation of components of the extracellular matrix. Unregulated MMP expression,
Synthesis and ligation ability of mono-aminooxy-functionalized dendrigraft poly-l-lysine (DGL)
Bondia, Andrea Molero,Larcher, Nicolas,Garrelly, Laurent,Rossi, Jean Christophe,Pascal, Robert
scheme or table, p. 3330 - 3333 (2010/07/10)
A bifunctional tetraethylene glycol (TEG) linker was prepared and used as an initiator for the synthesis of the first two generations of dendrigraft poly-l-lysines (DGL). The key steps involved the desymmetrization of TEG by introduction of an amine group
Synthesis of bifunctional integrin-binding peptides containing PEG spacers of defined length for non-viral gene delivery
Pilkington-Miksa, Michael A.,Sarkar, Supti,Writer, Michele J.,Barker, Susie E.,Shamlou, Parviz Ayazi,Hart, Stephen L.,Hailes, Helen C.,Tabor, Alethea B.
experimental part, p. 2900 - 2914 (2009/04/11)
Improving the buffer and serum stability of non-viral gene delivery vectors, and increasing their circulation time in vivo, is an important focus of current research in gene therapy. The most successful strategies to date have involved shielding the complexes with large polydisperse PEG adducts. However, this approach is accompanied by a fall in transfection efficiency. In this paper we describe the solid-phase synthesis of a series of bifunctional peptides bearing short PEG spacers of defined structure as components of lipopolyplex gene delivery vectors. Short, high-yielding routes to a series of PEG-amino acids are described: these PEG-amino acids can be used in varying combinations to afford bifunctional peptides with varying lengths of PEG spacers by using standard solid-phase synthesis techniques. A series of lipopolyplexes were formulated using these bifunctional peptides, and their transfection properties assessed. Dynamic light scattering measurements on the complex with the best transfection properties showed that in phosphate-buffered saline this complex was considerably more stable, and aggregated more slowly, than a complex formulated using a similar peptide lacking the short PEG spacer. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
Gold glyconanoparticles: Synthetic polyvalent ligands mimicking glycocalyx-like surfaces as tools for glycobiological studies
Barrientos, Africa G.,De la Fuente, Jesus M.,Rojas, Teresa C.,Fernandez, Asuncion,Penades, Soledad
, p. 1909 - 1921 (2007/10/03)
A simple and versatile methodology is described for tailoring sugar-functionalised gold nanoclusters (glyconanoparticles) that have 3D polyvalent carbohydrate display and globular shapes. This methodology allows the preparation of glyconanoparticles with biologically significant oligosaccharides as well as with differing carbohydrate density. Fluorescent glyconanoparticles have been also prepared for labelling cells in biological tests. The materials are water soluble, stable under physiological conditions and present an exceptional small core size. All of them have been characterised by 1H NMR, UV and IR spectroscopy, TEM and elemental analysis. Their highly polyvalent network can mimic glycosphingolipid clustering and interactions at the plasma membrane, providing an controlled system for glycobiological studies. Furthermore, they are useful building blocks for the design of nanomaterials.
Synthesis of New Glycerolipids Linked to Hydroxamate Derivatives Designed for Two-Dimensional Crystallization of Aminopeptidase M
Altenburger, Jean-Michel,Lebeau, Luc,Mioskowski, Charles,Schirlin, Daniel
, p. 2538 - 2544 (2007/10/02)
The synthesis of glycerolipids linked to hydroxamate derivatives designed for two-dimensional crystallization of aminopeptidase M is reported.The lipid moieties are readily obtained using a convergent pathway.Their structure allows the introduction of a w
