- A compound containing a 2,5-benzofuran group, a liquid crystal composition containing same, and a display unit having specific characteristics like light and heat stability and UV stability after curing by a light
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A kind of 2,5 compound containing a 2,5-benzofuran group has the structure represented by the following chemical formula 1, wherein R1, R2, L1 to L7 Z1, Z2, and n in the chemical formula are as defined in the specification and the scope of the patent, respectively. The present invention further provides a liquid crystal composition comprising at least one compound containing a 2,5-benzofuran group, and a display unit containing the liquid crystal composition. The compound containing the 2,5-benzofuran group of the present invention has good liquid crystal properties such as a wide liquid crystal state temperature range, good low temperature miscibility, higher birefringence, lower viscosity, larger K value, and light and heat stability, and can enhance the performance of liquid crystal composition like Tni, [Delta]n and UV stability.
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Paragraph 0030
(2018/03/09)
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- COMPOUNDS USEFUL FOR THE TREATMENT OF METABOLIC DISORDERS AND SYNTHESIS OF THE SAME
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The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
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Page/Page column 58-59; 106
(2014/10/18)
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- Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4H-chromene-3-carboxylate (sHA 14-1) and its analogues
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Rapid development of multiple drug resistance against current therapies is a major barrier in the treatment of cancer. Therefore, anticancer agents that can overcome acquired drug resistance in cancer cells are of great importance. Previously, we have demonstrated that ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6- phenyl-4H-chromene-3-carboxylate (5a, sHA 14-1), a stable analogue of ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (6, HA 14-1), mitigates drug resistance and synergizes with a variety of cancer therapies in leukemia cells. Structure-activity relationship (SAR) studies of 5a guided the development of ethyl 2-amino-6-(3′,5′-dimethoxyphenyl)- 4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (5q, CXL017), a compound with low micromolar cytotoxicity against a wide-range of hematologic and solid tumor cells. More excitingly, our studies of 5q in camptothecin (CCRF-CEM/C2) and mitoxantrone (HL-60/MX2) resistant cancer cells highlight its ability to selectively kill drug-resistant cells over parent cancer cells. 5q inhibits tumor cell growth through the induction of apoptosis, with detailed mechanism of its selectivity toward drug-resistant cancer cells under investigation. These results suggest that 5q is a promising candidate for treatment of cancers with multiple drug resistance. 2009 American Chemical Society.
- Das, Sonia G.,Doshi, Jignesh M.,Tian, Defeng,Addo, Sadiya N.,Srinivasan, Balasubramanian,Hermanson, David L.,Xing, Chengguo
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scheme or table
p. 5937 - 5949
(2010/03/24)
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- Structure-activity relationship studies of ethyl 2-amino-6-bromo-4-(1- cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (HA 14-1), an antagonist for antiapoptotic Bcl-2 proteins to overcome drug resistance in cancer
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The structure-activity relationship studies of ethyl 2-amino-6-cyclopentyl- 4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (1, HA 14-1), an antagonist of the antiapoptotic Bcl-2 proteins, are reported. A series of analogues of 1 with varied functional groups at the 6-position of the chromene ring were synthesized. These candidates were evaluated for their binding interactions with three antiapoptotic proteins: Bcl-2, Bcl-XL, and Bcl-w. They were also assayed for their in vitro cytotoxicities against a set of Jurkat cells with varied levels of Bcl-2 and Bcl-XL proteins and a non-small-cell lung carcinoma cell line (NCI-H460). It was found that the 6-bromo of 1 was not essential for its bioactivity and the 6-position can accommodate a variety of alkyl groups. 1 and its analogues bind to all of the three antiapoptotic Bcl-2 proteins tested. Positive correlations were observed between the binding affinities of these candidates to the antiapoptotic Bcl-2 proteins and their in vitro cytotoxicities, suggesting that the antiapoptotic Bcl-2 proteins are likely to be the cellular targets of 1 and its analogues. (In this study, the binding interactions of the small molecules to antiapoptotic Bcl-2 proteins were studied by assaying their abilities to compete against a Bak peptide binding to the antiapoptotic Bcl-2 proteins. Inhibitory constants, instead of dissociation constants, were obtained in such assays. The term "binding affinity" is used in this article for simplicity.) The most active compound, 3g, had a > 3-fold increase of binding affinity to the antiapoptotic Bcl-2 proteins and a > 13-fold increase of in vitro cytotoxicity over 1. Though Jurkat cells with transgenic overexpression of Bcl-2 or Bcl-XL protein can develop resistance to standard cancer therapies, such cells failed to develop resistance to 1 based candidates. 1 also sensitizes Jurkat cells to cisplatin. These studies provide further support that 1 and its analogues function as antagonists for antiapoptotic Bcl-2 proteins and that they have the potential, either as a single agent or as a combination therapy with other anticancer agents, to treat cancers with the overexpression of antiapoptotic Bcl-2 proteins.
- Doshi, Jignesh M.,Tian, Defeng,Xing, Chengguo
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p. 7731 - 7739
(2007/10/03)
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- Non-metallocene compounds, method for the production thereof and use of the same for the polymerisation of olefins
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The invention relates to a method for producing special transition metal compounds, to novel transition metal compounds and to the use of the same for the polymerisation of olefins.
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- N-(4- carbamimidoyl-phenyl) -glycine derivatives
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The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
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- 3-Benzo[b]furyl- and 3-benzo[b]thienylaminobutyric acids as GABA(B) ligands. Synthesis and structure-activity relationship studies
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Baclofen (β-p-chlorophenyl GABA) is one of the selective agonists for the bicuculline-insensitive GABA(B) receptors. In the search for new compounds that bind to GABA(B) receptors it is very important to clarify the structural requirements. We report the syntheses of and binding studies on various 3- heteroaromatic (benzo[b]furan and benzo[b]thiophen)aminobutyric acids. The 4- amino-3-(7-methyl-benzo[b]furan-2-yl)butanoic acid 8g is a potent and specific ligand for GABA(B) receptors, with an IC50 value of 5.4 μM in the displacement of [3H]GABA.
- Ansar,Al Akoum Ebrik,Mouhoub,Berthelot,Vaccher,Vaccher,Flouquet,Caignard,Renard,Pirard,Rettori,Evrard,Durant,Debaert
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p. 449 - 460
(2007/10/03)
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- Selective Functionalisation. Part 11. Selective Hydrogenation by a Novel Palladium Salicylidene-ethylenediamine Complex and the Properties of Derivatives of some Square Planar Homogenous Hydrogenation Catalysts.
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Analogues of two reported homogenous hydrogenation catalysts based upon square planar palladium complexes have been prepared with a view to modifying the structures to permit the control of selectivity by micellar interactions.Derivatives of bisacetylacetonatopalladium(II) in which the diketone was alkylated at C-3 or C-5 were prepared but no useful catalytic activity was observed for the reduction of nitrobenzene to aniline in the presence of pyridine.Complexes were also prepared from bisacetylacetonatopalladium(II) with 4-substituted pyridines as ligands; 4-tridecylpyridine afforded an unstable complex but 4-decylaminopyridine afforded a stable complex with low catalytic activity.A series of salicylidene imine palladium(II) complexes was prepared.Contrary to previous reports, the well-known salicylidene-ethylenediaminepalladium(II) complex was not a catalyst for homogenous hydrogenation but a new oligomeric green heterogenous complex with selective hydrogenation properties was discovered.This green complex was selective for the hydrogenation of alkynes, especially terminal alkynes, and reduced few other functional groups (ArNO2, ArCHO).Many variations on this structure were investigated in an attempt to discover a soluble or crystalline analogue of the green complex but no complexes with improved properties were isolated.
- Kerr, James M.,Suckling, Colin J.,Bamfield, Peter
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p. 887 - 895
(2007/10/02)
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