- Effect of Oligoethylene Chains on the Formation of Photoresponsive Nanotubes by Azobenzene Dyad
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Azobenzene dyad 1 possessing hydrophobic side chains has previously been reported to assemble into toroidal nanostructures, which can further stack to afford nanotubes in nonpolar media. In this study, amphiphilic dyad 2 was synthesized to obtain nanotubes with the hydrophilic interior. Dyad 2 directly assembled into nanotubes without forming isolatable toroidal nanostructures. UV light irradiation to the nanotubes resulted in monomerization by trans→cis photoisomerization, but following reconstruction by visible light irradiation afforded amorphous films, suggesting a kinetic trap of trans-2 by residual cis-2 through co-aggregation.
- Saito, Takuho,Yagai, Shiki
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Read Online
- Poly(oligo(ethylene glycol) vinyl acetate)s: A Versatile Class of Thermoresponsive and Biocompatible Polymers
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Polymers with a thermally triggered phase transition are important in the design of materials for biological applications, where their behavior can be used to trigger release or (dis)assembly events. Despite their advantages, a system with tunable thermal response, end-group reactive sites, low toxicity, and controlled main-chain degradability has not been realized, yet this would be a significant advance. The versatile new poly(oligo(ethylene glycol) vinyl acetate)s are presented with excellent control over their molecular properties obtained through RAFT/MADIX polymerization. Furthermore, we demonstrate structure-controlled thermal transitions, conjugation to human lysozyme through the retained end-group, and moreover show that this class of polymers can uniquely be copolymerized with 2-methylene-1,3-dioxepane (MDO) to generate polymers in which the degradability and cloud point can be independently tuned to create materials that display the same cloud point but degrade differently.
- Hedir, Guillaume G.,Arno, Maria C.,Langlais, Marvin,Husband, Jonathan T.,O'Reilly, Rachel K.,Dove, Andrew P.
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Read Online
- NOVEL TRITERPENE DERIVATIVES AS HIV INHIBITORS
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The present invention relates to novel triterpene derivatives of formula (I); and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and ring are as defined herein. The invention also relates to novel triterpene derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
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Page/Page column 54-55
(2020/08/28)
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- ARYL HYDROCARBON RECEPTOR MODULATOR
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Disclosed is an aryl hydrocarbon receptor modulator of formula (I), and a pharmaceutically acceptable salt thereof, wherein R′ is H, CN, CH2(OH)R0, CmH2m+1, CnH2n-1, CnH2n-3, two Ra are independently H or two Ra together form ═O or ═N—W3—R1; A is a C6 to C10 aromatic ring unsubstituted or substituted with 1 to 3 R, or a C2-C10 heteroaromatic ring interrupted by 1 to 5 heteroatoms selected from N, O, and S or a 4 to 7 membered nonaromatic heterocyclic ring containing C═N and interrupted by 1 to 3 heteroatoms selected from N, O, and S, with either one unsubstituted or substituted with 1 to 3 R; Q is R, or is a C6 to C10 aromatic ring or a C2 to C10 heteroaromatic ring unsubstituted or substituted with 1 to 3 R and interrupted by 1 to 5 heteroatoms selected from N, O, and S; and R is Rc which is C-attached or RN which is N-attached. The compounds of formula (I) of the present invention can regulate AhR activity, and can be used to inhibit the growth of cancer cells and inhibit the metastasis and invasion of tumor cells.
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Paragraph 0053-0054
(2019/10/20)
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- BENZODICYCLOALKANE DERIVATIVE, PREPARATION METHOD AND USE THEREOF
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It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.
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- A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
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- Monodisperse oligoethylene glycols modified Propofol prodrugs
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The low water solubility of Propofol resulted in complicated formulation and adverse effects during its clinical application. To improve its water solubility and maintain its anesthetic effects, Propofol prodrugs with monodisperse oligoethylene glycols as solubility enhancer were designed and synthesized. Monodisperse oligoethylene glycols enable the concise manipulation of water solubility, biocompatibility and anesthetic effects. Through the physicochemical and biological assay, a few water soluble prodrugs of Propofol were identified as promising anesthetic to overcome the drawbacks associated with Propofol.
- Deng, Tao,Mao, Xianglan,Li, Yu,Bo, Shaowei,Yang, Zhigang,Jiang, Zhong-Xing
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p. 3502 - 3505
(2018/10/15)
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- Preparation and application of monodisperse polyethylene glycol monomethyl ether modified propofol prodrug
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Belonging to the field of organic chemistry and pharmaceutical chemicals, the invention discloses preparation and application of a monodisperse polyethylene glycol monomethyl ether modified propofol prodrug with a novel structure. Monodisperse polyethylene glycol monomethyl ether and propofol can be connected by an in-vivo degradable chemical bond to prepare a series of carbonic ester type and acetic ester type prodrugs respectively. By adjusting the length of the monodisperse polyethylene glycol monomethyl ether chain, the method can synthesize corresponding water-soluble propofol prodrugs, the longer the monodisperse polyethylene glycol monomethyl ether chain is, the better the water solubility is, along with the improvement of the water solubility, the prodrug can be made into aqueous solution preparations so as to avoid the defects of fat emulsion in propofol fat emulsions. The method provided by the invention has the advantages of simple reaction, mild conditions and low cost, andis convenient for industrial production.
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Paragraph 0042; 0043; 0046; 0047
(2018/07/06)
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- ALKYNYL INDAZOLE DERIVATIVE AND USE THEREOF
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The main object of the present invention is to provide a novel compound which has a VEGF receptor tyrosine kinase inhibitory activity and is useful as an active ingredient for the treatment of diseases accompanying angiogenesis or edema, for example, age-related macular degeneration or the like. The present invention includes, for example, an alkynyl indazole derivative represented by the following general formula (I), a pharmaceutical acceptable salt thereof, and a medicine containing thereof.
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Paragraph 0202; 0203
(2017/02/24)
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- Phenothiazine derivatives and methods of use thereof
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The present disclosure relates to phenothiazine derivatives such as conjugates of phenothiazine compounds, as well as pharmaceutical compositions thereof. The present disclosure also relates to a method of making and the use of such compounds for treating cancer, e.g., a lung cancer, a colon cancer, breast cancer or pancreatic cancer.
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Page/Page column 45
(2017/08/01)
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- Regulatory effect of hydroquinone-tetraethylene glycol conjugates on zebrafish pigmentation
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We synthesized two hydroquinone-tetraethylene glycol conjugates (HQ-TGs) and investigated their log P, photophysical stability, and redox chemical stability. HQ-TGs are a little more hydrophilic than hydroquinone (HQ) and show an enhanced photophysical an
- Le, Hoa Thi,Hong, Bin Na,Lee, Yeong Ro,Cheon, Ji Hyun,Kang, Tong Ho,Kim, Tae Woo
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supporting information
p. 699 - 705
(2016/01/09)
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- Short Soluble Coumarin Crosslinkers for Light-Controlled Release of Cells and Proteins from Hydrogels
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Materials that degrade or dissociate in response to low power light promise to enable on-demand, precisely localized delivery of drugs or bioactive molecules in living systems. Such applications remain elusive because few materials respond to wavelengths
- De Gracia Lux, Caroline,Lux, Jacques,Collet, Guillaume,He, Sha,Chan, Minnie,Olejniczak, Jason,Foucault-Collet, Alexandra,Almutairi, Adah
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p. 3286 - 3296
(2015/10/20)
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- Protein fixing surface modification material
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PROBLEM TO BE SOLVED: To provide a new compound which is a silane compound, with which a hydroxysuccinimido ester group for immobilizing protein is introduced onto a substrate surface with one step, and which yields a modification material capable of building a high density monomolecular film applicable to a highly sensitive sensing element substrate for a biosensor. SOLUTION: The hydroxysuccinimido ester-silane compound is represented by chemical formula (1) (wherein each of X1to X3independently represents a halogen, a 1-3C alkoxy group, or a 1-3C alkyl group, R1represents a 1-10C straight alkyl chain, and R2represents -(CH2)m-(OCH2CH2)n- or -(CH2CH2O)n-(CH2)m-; m is an integer of 3-30, n is an integer of 0-20, and m+n≥3). COPYRIGHT: (C)2013,JPOandINPIT
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Paragraph 0029
(2016/10/10)
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- Ceria supported gold-platinum catalysts for the selective oxidation of alkyl ethoxylates
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This work covers the development of a ceria based AuPt catalyst for the selective aerobic oxidation of alkyl ethoxylates to their corresponding carboxylic acids. By optimizing metal loading and the Au to Pt ratio the activity of the catalyst could be increased significantly, while maintaining total selectivity. Although the choice of ceria as a support helped to suppress intermediate metal leaching, the catalyst still showed poor long-term stability in repeated batches. The cause for deactivation could finally be identified by TPR studies as over-oxidation. These suspicions were confirmed by a long-term stability study in continuous-mode. It proved to be possible to deactivate the catalyst on purpose by employing unfavourable oxidising reaction conditions, i.e. low substrate concentrations and excess oxygen. By avoiding such unfavourable conditions either in continuous-flow mode or in repeated batches, the long-term stability of the catalyst increased tremendously. A substrate screening of various ethoxylates showed that the catalyst was very well-suited to selectively oxidize a wide range of alkyl ethoxylates.
- Heidkamp, Katharina,Aytemir, Memet,Vorlop, Klaus-Dieter,Pruesse, Ulf
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p. 2984 - 2992
(2013/11/06)
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- Ionic liquids
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Novel ionic liquids comprising polyethercarboxylates as anions, a process for preparing them and their use.
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Page/Page column 7
(2013/06/27)
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- Cholesterol-based nucleolipid-ruthenium complex stabilized by lipid aggregates for antineoplastic therapy
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A novel ruthenium complex, linked to a cholesterol-containing nucleolipid (named ToThyCholRu), stabilized by lipid aggregates for antineoplastic therapy is presented. In order to retard the degradation kinetics typically observed for several ruthenium-based antineoplastic agents, ToThyCholRu is incorporated into a liposome bilayer formed by POPC. The resulting nanoaggregates contain up to 15% in moles of the ruthenium complex, and are shown to be stable for several weeks. The liposomes host the ruthenium - nucleolipid complex with the metal ion surrounded by POPC lipid headgroups and the steroid moiety inserted in the more external acyl chain region. These rutheniumcontaining liposomes are more effective in inhibiting the growth of cancer cells than a model NAMI-A-like ruthenium complex, prepared for a direct evaluation of their antiproliferative activity. These results introduce new perspectives in the design of innovative transition-metal-based supramolecular systems for anticancer drug vectorization. (Graph Presented)
- Simeone, Luca,Mangiapia, Gaetano,Vitiello, Giuseppe,Irace, Carlo,Colonna, Alfredo,Ortona, Ornella,Montesarchio, Daniela,Paduano, Luigi
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p. 758 - 770
(2012/07/03)
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- Gold nanoparticles generated by thermolysis of "all-in-one" gold(i) carboxylate complexes
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Consecutive synthesis methodologies for the preparation of the gold(i) carboxylates [(Ph3P)AuO2CCH2(OCH 2CH2)nOCH3] (n = 0-6) (6a-g) are reported, whereby selective mono-alkylation of diols HO(CH2CH 2O)nH (n = 0-6), Williamson ether synthesis and metal carboxylate (Ag, Au) formation are the key steps. Single crystal X-ray diffraction studies of 6a (n = 0) and 6b (n = 1) were carried out showing that the P-Au-O unit is essentially linear. These compounds were applied in the formation of gold nanoparticles (NP) by a thermally induced decomposition process and hence the addition of any further stabilizing and reducing reagents, respectively, is not required. The ethylene glycol functionalities, providing multiple donating capabilities, are able to stabilise the encapsulated gold colloids. The dependency of concentration, generation time and ethylene glycol chain lengths on the NP size and size distribution is discussed. Characterisation of the gold colloids was performed by TEM, UV/Vis spectroscopy and electron diffraction studies revealing that Au NP are formed with a size of 3.3 (±0.6) to 6.5 (±0.9) nm in p-xylene with a sharp size distribution. Additionally, a decomposition mechanism determined by TG-MS coupling experiments of the gold(i) precursors is reported showing that 1 st decarboxylation occurs followed by the cleavage of the Au-PPh 3 bond and finally release of ethylene glycol fragments to give Au-NP and the appropriate organics. The Royal Society of Chemistry 2012.
- Tuchscherer,Schaarschmidt,Schulze,Hietschold,Lang
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scheme or table
p. 2738 - 2746
(2012/04/10)
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- Oligo(p-phenylene-ethynylene)s with backbone conformation controlled by competitive intramolecular hydrogen bonds
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A series of conjugated oligo(p-phenylene-ethynylene) (OPE) molecules with backbone conformations (that is, the relative orientations of the contained phenylene units) controlled by competitive intramolecular hydrogen bonds to be either co-planar or random
- Hu, Wei,Yan, Qifan,Zhao, Dahui
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supporting information; experimental part
p. 7087 - 7094
(2011/07/09)
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- Nucleolipid nanovectors as molecular carriers for potential applications in drug delivery
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Novel thymidine- or uridine-based nucleolipids, containing one hydrophilic oligo(ethylene glycol) chain and one or two oleic acid residues (called ToThy, HoThy and DoHu), have been synthesized with the aim to develop bio-compatible nanocarriers for drug d
- Simeone, Luca,Mangiapia, Gaetano,Irace, Carlo,Di Pascale, Antonio,Colonna, Alfredo,Ortona, Ornella,De Napoli, Lorenzo,Montesarchio, Daniela,Paduano, Luigi
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p. 3075 - 3086
(2012/08/08)
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- αvβ3 integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers
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RGD peptides are used in biomaterials science for surface modifications with a view to elicit selective cellular responses. Our objective is to replace peptides by small peptidomimetics acting similarly. We designed novel molecules targeting αvβ3 integrin and featuring spacer-arms (for surface grafting), which do not disturb the biological activity, from (L) N-(3-(trifluoromethyl)benzenesulfonyl) tyrosine used as scaffold. Various Arg-mimics were fixed on the phenol function, and the ortho position was used for the coupling of OEG spacers. All peptidomimetics were active in the nM range in a binding test toward human αvβ 3 integrin (IC50 = 0.1 to 1.7 nM) and selective versus platelet integrin αIIbβ3. Selected compounds revealed excellent ability to inhibit bone cells adhesion on vitronectin. Modeling and docking studies were performed for comparing the most active RGD peptidomimetic to cilengitide, i.e., cyclo-[RGDfN(Me)V]-. Lastly, the adhesion of endothelial cells on a cultivation support grafted with RGD peptidomimetics was significantly improved. 2009 American Chemical Society.
- Rerat, Vincent,Dive, Georges,Cordi, Alex A.,Tucker, Gordon C.,Bareille, Reine,Amédée, Jo?lle,Bordenave, Laurence,Marchand-Brynaert, Jacqueline
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supporting information; experimental part
p. 7029 - 7043
(2010/07/05)
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- Alkali metal oligoether carboxylates - A new class of ionic liquids
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A new group of ionic liquids (IL) based on small inorganic cations and oligoether carboxylate anions were synthesized. The physicochemical properties of the salts were also investigated, and possible reasons for the formation of ionic liquids with alkali metal ions were proposed. It was found that complexation of the alkali metal cations by their combined oligoether- carboxylate counter-ion was sufficient to generate room-temperature liquid salts. It was also found that the use of simple tri- and tetraalkylammonium instead of alkali metal ions could also yielded ionic liquids at ambient temperature that appear to display additional desirable properties such as low viscosity. The result also showed that the combination of the 2,5,8,1 l-tetraoxatridecan-13-oate (TOTO) anion with biological cations such as choline could also lead to the development of even greener ILs.
- Zech, Oliver,Kellermeier, Matthias,Thomaier, Stefan,Maurer, Eva,Klein, Regina,Schreiner, Christian,Kunz, Werner
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experimental part
p. 1341 - 1345
(2009/09/04)
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- Novel alkanoic acid derivaties
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There are provided according to the invention compounds of the formula (I) or a salt or solvate thereof, wherein: n represents an integer 1 to 6; N represents an integer 1 to 15; R1 represents (CO)xC1-9alkyl or (CO)xC1-9fluoroalkyl, which fluoroalkyl moiety contains at least 1 fluorine atom and not more than 3 consecutive perfluorocarbon atoms wherein x represents 0 or 1; and R2 and R3 independently represent C1-3alkyl or hydrogen. There are also provided pharmaceutical aerosol formulations employing said compounds as suspension stabilising agents.
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- Oligomeric aminodiol-containing compounds, libraries thereof, and process of preparing the same
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Oligomeric compounds comprising a plurality of aminodiol monomer subunits joined by linking groups are provided, as well as libraries of such compounds and processes for preparing the oligomeric compounds and libraries.
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- PEPTIDE NUCLEIC ACID CONJUGATES
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A novel class of peptide nucleic acids are described which include a conjugate attached thereto. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.
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- Combinatorial libraries having aminodiol monomer subunits
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Combinatorial libraries are constructed to include aminodiol monomer subunits connected by phosphodiester, phosphorothioate, or phosphoramidate linking moieties. Combinatorial libraries of the invention feature a plurality of functional groups attached to
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- Phosphate linked oligomers
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Novel ethylene glycol compounds bearing various functional groups are used to prepare oligomeric structures. The ethylene glycol monomers can be joined via standard phosphate linkages including phosphorothioate, phosphodiester, and phosphoramidate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.
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- Pyrrolidine-containing monomers and oligomers
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Novel pyrrolidine monomers bearing various functional groups are used to prepare oligomeric structures. The pyrrolidine monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.
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