- SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1
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The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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Page/Page column 1030
(2018/01/20)
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- Robust C-C bonded porous networks with chemically designed functionalities for improved CO2 capture from flue gas
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Effective carbon dioxide (CO2) capture requires solid, porous sorbents with chemically and thermally stable frameworks. Herein, we report two new carbon-carbon bonded porous networks that were synthesized through metal-free Knoevenagel nitrile-aldol condensation, namely the covalent organic polymer, COP-156 and 157. COP-156, due to high specific surface area (650 m2/g) and easily interchangeable nitrile groups, was modified post-synthetically into free amine- or amidoxime-containing networks. The modified COP-156-amine showed fast and increased CO2 uptake under simulated moist flue gas conditions compared to the starting network and usual industrial CO2 solvents, reaching up to 7.8 wt % uptake at 40°C.
- Thirion, Damien,Lee, Joo S.,?zdemir, Ercan,Yavuz, Cafer T.
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supporting information
p. 2274 - 2279
(2016/11/17)
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- Soluble narrow band gap and blue propylenedioxythiophene-cyanovinylene polymers as multifunctional materials for photovoltaic and electrochromic applications
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A family of soluble narrow band gap donor-acceptor conjugated polymers based on dioxythiophenes and cyanovinylenes is reported. The polymers were synthesized using Knoevenagel polycondensation or Yamamoto coupling polymerizations to yield polymers with molecular weights on the order of 10 000-20 000 g/mol, which possess solubility in common organic solvents. Thin film optical measurements revealed narrow band gaps of 1.5-1.8 eV, which gives the polymers a strong overlap of the solar spectrum. The energetic positions of the band edges were determined by cyclic voltammetry and differential pulse voltammetry and demonstrate that the polymers are both air stable and show a strong propensity for photoinduced charge transfer to fullerene acceptors. Such measurements also suggest that the polymers can be both p- and n-type doped, which is supported by spectroelectrochemical results. These polymers have been investigated as electron donors in photovoltaic devices in combination with PCBM ([6,6]-phenyl C61-butyric acid methyl ester) as an electron acceptor based on the near ideal band structures designed into the polymers. Efficiencies as high as 0.2% (AM1.5) with short circuit current densities as high as 1.2-1.3 mA/cm2 have been observed in polymer/PCBM (1:4 by weight) devices and external quantum efficiencies of more than 10% have been observed at wavelengths longer than 600 nm. The electrochromic properties of the narrow band gap polymers are also of interest as the polymers show three accessible color states changing from an absorptive blue or purple in the neutral state to a transmissive sky-blue or gray in the oxidized and reduced forms. The wide electrochemical range of electrochromic activity coupled with the strong observed changes in transmissivity between oxidation states makes these materials potentially interesting for application to electrochromic displays.
- Thompson, Barry C.,Kim, Young-Gi,McCarley, Tracy D.,Reynolds, John R.
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p. 12714 - 12725
(2008/02/05)
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- Ruthenium-catalyzed knoevenagel condensation: A new route toward cyano-substituted poly(p-phenylenevinylene)s
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The ruthenium-catalyzed Knoevenagel reaction was developed for the preparation of cyano-substituted conjugated polymers. The polymerization was quenched by pouring the reaction mixture into methanol. The structures of polymers were confirmed by spectroscopic studies and elemental analysis. The results show that Knoevenagel polycondensation mediated by transition metal complexes enjoys the advantages of neutral and mild reaction conditions.
- Liao, Jian,Wang, Qing
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p. 7061 - 7063
(2007/10/03)
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- Syntheses and Different Chemical Behaviour of Precursors of Putative Dibasic Inhibitors of Human Mast Cell Tryptase
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Choosing the best conditions and pathways for the synthesis of peptidic compounds remains a challenge for the peptide chemist. Our efforts towards the syntheses of two precursors of potential tryptase inhibitors, building block A and B, led to the development of two different synthesis routes. Each of them is successful in the synthesis of only one of the two, structurally nearly identical target compounds.
- Radau, Gregor
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p. 1159 - 1166
(2007/10/03)
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- SYNTHESES AND HOMOPOLYMERIZATION OF 7,8-DIALKOXYCARBONYL-7,8-DICYANOQUINODIMETHANES
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7,8-Dimethoxycarbonyl-7,8-dicyanoquinodimethane and 7,8-diethoxycarbonyl-7,8-dicyaniquinomethane were prepared succesfully as novel compounds.These two compounds homopolymerized readly under thermal, radical, and anionic conditions except for cationic one.Moreover, weak bases such as triethylamine, pyridine, and pyrrolidine were found to induce the homopolymerization.
- Iwatsuki, Shouji,Itoh, Takahito,Nishihara, Katsumi,Furuhashi, Hidehiko
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p. 517 - 520
(2007/10/02)
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