170304-76-4Relevant academic research and scientific papers
Ultra-Fast Synthesis of Multivalent Radical Nanoparticles by Ring-Opening Metathesis Polymerization-Induced Self-Assembly
Le, Dao,Dilger, Marco,Pertici, Vincent,Diabaté, Silvia,Gigmes, Didier,Weiss, Carsten,Delaittre, Guillaume
, p. 4725 - 4731 (2019)
We report the straightforward, time-efficient synthesis of radical core–shell nanoparticles (NPs) by polymerization-induced self-assembly. A nitroxide-containing hydrophilic macromolecular precursor was prepared by ring-opening metathesis copolymerization of norbornenyl derivatives of TEMPO and oligoethylene glycol and was chain-extended in situ with norbornene in ethanolic solution, leading to simultaneous amphiphilic block copolymer formation and self-assembly. Without any intermediate purification from the monomers to the block copolymers, radical NPs with tunable diameters ranging from 10 to 110 nm are obtained within minutes at room temperature. The high activity of the radical NPs as chemoselective and homogeneous, yet readily recyclable catalysts is demonstrated through oxidation of a variety of alcohols and recovery by simple centrifugation. Furthermore, the NPs show biocompatibility and antioxidant activity in vitro.
COMPOUNDS FOR THE MODULATION OF RIP2 KINASE ACTIVITY
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Page/Page column 80, (2017/04/11)
The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
CONJUGATES COMPRISING SELF-IMMOLATIVE GROUPS AND METHODS RELATED THERETO
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Page/Page column 115, (2017/06/27)
In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self- immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
CONJUGATES COMPRISING PEPTIDE GROUPS AND METHODS RELATED THERETO
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Page/Page column 125; 126, (2017/08/08)
In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody; a linker; and at least two active agents. In preferred embodiments, the linker comprises a peptide sequence of a plurality of amino acids, and at least two of the active agents are covalently coupled to side chains of the amino acids. The antibody-drug conjugate may comprise a self-immolative group, preferably two-self-immolative groups. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
ZWITTERIONIC POLYMERS WITH THERAPEUTIC MOIETIES
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Paragraph 0119, (2016/12/22)
The invention generally relates to zwitterionic polymers (including zwitterionic copolymers), such as polymethacrylic structures, with pendent functional moieties, such as therapeutic or biologic moieties. More particularly, the invention relates to phosphorylcholine-substituted methacrylic polymers prepared by free radical polymerization and click chemistry, for example, and compositions and products comprising same, as well as related methods and uses of the compositions, for example, as biological or therapeutic agents and in drug delivery thereof.
Antiviral agent-sensitive/resistant virus detection system
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Paragraph 0033-0037; 0039; 0040, (2017/01/02)
The present invention relates to a nanoparticle for detecting an antiviral agent-resistant virus. According to the present invention, an Oseltamivir (Tamiflu)-sensitive/resistant virus is rapidly and comfortably diagnosed/detected with naked eyes. Therefore, the nanoparticle is used in rapidly making a treatment plan of a patient inoculated by influenza virus.(AA,DD) Wild + Nanoprobe(BB,EE) Mutant + Nanoprobe(CC,FF) NanoprobeCOPYRIGHT KIPO 2016
Semisynthetic lectin-4-dimethylaminopyridine conjugates for labeling and profiling glycoproteins on live cell surfaces
Hayashi, Takahiro,Sun, Yedi,Tamura, Tomonori,Kuwata, Keiko,Song, Zhining,Takaoka, Yousuke,Hamachi, Itaru
supporting information, p. 12252 - 12258 (2013/09/23)
Glycoproteins on cell surfaces play important roles in biological processes, including cell-cell interaction/signaling, immune response, and cell differentiation. Given the diversity of the structure of glycans, labeling and imaging of selected glycoproteins are challenging, although several promising strategies have been developed recently. Here, we design and construct semisynthetic reactive lectins (sugar-binding proteins) that are able to selectively label glycoproteins. Congerin II, an animal galectin, and wheat germ agglutinin are conjugated with 4-dimethylaminopyridine (DMAP), a well-known acyl transfer catalyst by our affinity-guided DMAP method and Cu(I)-assisted click chemistry. Selective labeling of glycoproteins is facilitated by the DMAP-tethered lectin catalysts both in vitro and on living cells. Two-dimensional polyacrylamide gel electrophoresis (2D-PAGE) analysis enabled us to isolate labeled glycoproteins that are uniquely exposed on distinct cell lines. Furthermore, the combination of immunoprecipitation with mass spectrometry (MS)-fingerprinting techniques allowed us to characterize 48 glycoproteins endogenously expressed on HeLa cells, and some low-abundant glycoproteins, such as epidermal growth factor receptor (EGFR) and neuropilin-1, were successfully identified. Our results demonstrate that semisynthetic DMAP-tethered lectins provide a new tool for labeling and profiling glycoproteins on living cells.
1- [4- (SULFONYL) -PHENYL] -5- (BENZYL) -IH-I, 2, 4-TRIAZOL DERIVATIVES AS INHIBITORS OF CARBONIC ANHYDRASE FOR TREATING GLAUCOMA OR OCULAR HYPERTENSION
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Page/Page column 44-45, (2008/12/06)
The invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4 and RA through RE are as defined herein. The invention also relates to methods of treating glaucoma, ocular hypertension, age-related macular degeneration, diabetic macular edema, diabetic retinopathy, hypertensive retinopathy, retinal vasculopathies and intraocular pressure in mammals by administering the compounds of formula I, and to pharmaceutical compositions which contain the compounds of formula I for such treatments. The invention also relates to methods of preparing the compounds of formula (I).
Sugar balls: Synthesis and supramolecular assembly of [60]fullerene glycoconjugates
Kato, Haruhito,Boettcher, Christoph,Hirsch, Andreas
, p. 2659 - 2666 (2008/02/09)
The synthesis and characterization of fully deprotected C60 glycoconjugates 4 and 17 is reported. Bis(α-D-mannopyranosyl)malonamide 4 was obtained by using nucleophilic cyclopropanation chemistry, which in general is a very versatile method for
Linker arms for nanocrystals and compounds thereof
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, (2008/06/13)
A nanocrystal compound comprising: a nanocrystal, and attached thereto a compound of the following formula: n is 0 or an integer from 1 to 48; X and Z are independently O, NH, N—R, S, CH2, CO, COHN, NHCO, SO, SO2NH, NHSO2, carbamate and thio carbamate; R is alkyl or aryl; r is 0 or an integer from 1 to 15; and wherein S is the attachment point to a nanocrystal compound. The nanocrystal compounds of the present invention are useful fluorescent labels.
