- Therapeutic compounds
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The invention provides a compound of formula I: or a salt thereof, wherein R2-R4 and p have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as ant
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Page/Page column 15; 16
(2021/01/17)
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- Synthesis and photovoltaic properties of two-dimensional copolymers based on novel benzothiadiazole and quinoxaline acceptors with conjugated dithienylbenzothiadiazole pendants
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Two novel acceptors of benzo[c][1,2,5]thiadiazole and quinoxaline with conjugated dithienylbenzothiadiazole pendants were first designed and synthesized for building efficient photovoltaic copolymers. Based on benzo[1,2-b;3,4-b′]dithiophene donors and the
- Huang, Yuanshuai,Ye, Linglong,Wu, Fen,Mei, Suli,Chen, Huajie,Tan, Songting
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p. 668 - 677
(2016/02/09)
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- Optimisation of conoidin A, a peroxiredoxin inhibitor
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Lead optimisation: Interest in the inhibition of peroxiredoxin has been revitalised by their recently identified role in signalling cascades. Here, the synthesis and analysis of novel analogues of the peroxiredoxin inhibitor conoidin A is described. Computational methods are used to rationalise the generated SAR data. These studies lead to a proposed binding mode for this class of compounds that will aid the design of second generation inhibitors. (Figure Presented)
- Liu, Gu,Botting, Catherine H.,Evans, Kathryn M.,Walton, Jeffrey A. G.,Xu, Guogang,Slawin, Alexandra M. Z.,Westwood, Nicholas J.
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scheme or table
p. 41 - 45
(2010/11/02)
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- Multicyclic sulfonamide compounds as inhibitors of histone deacetylase for the treatment of disease
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Disclosed herein are sulfonamide compounds of Formula VII as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
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Page/Page column 17; 24
(2010/11/25)
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- Stereoselectivity in the formation of tris-diimine complexes of Fe(ii), Ru(ii), and Os(ii) with a C2-symmetric chiral derivative of 2,2′-bipyridine
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A C2-symmetric enantiopure 4,5-bis(pinene)-2, 2′-bipyridine ligand (-)-L was used to investigate the diastereoselectivity in the formation of [ML3]2+ coordination species (M = Fe(ii), Ru(ii), Os(ii), Zn(ii), Cd(ii), Cu(ii), Ni(ii)), and [ML2Cl2] (M = Ru(ii), Os(ii)). The X-ray structures of the [ML3]2+ complexes were determined for Δ-[FeL3](PF6)2, Δ-[RuL 3](PF6)2, Λ-[RuL3](PF 6)2, Δ-[OsL3](PF6) 2, and Λ-[OsL3](TfO)2. All of these compounds were also characterized by NMR, CD and UV/VIS absorption spectroscopy. The [FeL3]2+ diastereoisomers were studied in equilibrated solutions at various temperatures and in several solvents. The [RuL3]2+ complexes, which are thermally stable up to 200 °C, were photochemically equilibrated. The Royal Society of Chemistry 2006.
- Drahonovsky, Dusan,Knof, Ulrich,Jungo, Laurence,Belser, Thomas,Neels, Antonia,Labat, Gael Charles,Stoeckli-Evans, Helen,Von Zelewsky, Alex
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p. 1444 - 1454
(2007/10/03)
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- 5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d] pyrimidin-4-ylamine: Structure-activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors
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4-Amino-5,7-disubstituted pyridopyrimidines are potent, non-nucleoside inhibitors of adenosine kinase (AK). We recently identified a potent, orally efficacious analog, 4 containing a 7-pyridylmorpholine substituted ring system as the key structural element of this template. In this report, we disclose the pharmacologic effects of five- and six-membered heterocyclic ring replacements for the pyridine ring in 4. These replacements were found to have interesting effects on in vivo efficacy and genotoxicity as well as in vitro potency. We discovered that the nitrogen in the heterocyclic ring at C(7) is important for the modulation of mutagenic side effects (Ames assay).
- Matulenko, Mark A.,Lee, Chih-Hung,Jiang, Meiqun,Frey, Robin R.,Cowart, Marlon D.,Bayburt, Erol K.,DiDomenico Jr., Stanley,Gfesser, Gregory A.,Gomtsyan, Arthur,Guo, Zhu Zheng,McKie, Jeffery A.,Stewart, Andrew O.,Yu, Haixia,Kohlhaas, Kathy L.,Alexander, Karen M.,McGaraughty, Steve,Wismer, Carol T.,Mikusa, Joseph,Marsh, Kennan C.,Snyder, Ronald D.,Diehl, Marilyn S.,Kowaluk, Elizabeth A.,Jarvis, Michael F.,Bhagwat, Shripad S.
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p. 3705 - 3720
(2007/10/03)
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- Efficient synthesis of novel dipyridoimidazoles and pyrido[1′,2′;1,2]imidazo[4,5-d]pyridazine derivatives
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Novel dipyrido[1,2-a;3′,4′-d]imidazoles 7a-d, dipyrido[1,2-a;4′,3′-d]imidazoles 8a,c and pyrido[1′,2′;1,2]imidazo[4,5-d]pyridazine derivatives 9a-d were synthesized by two pathways: thermal electrocyclic reaction of 3-alkenylimidazopyridine-2-oximes 10 and direct condensation of ethyl glycinate (or hydrazine) with 2,3-dicarbonylimidazo[1,2-a]pyridines 11.
- Chezal, Jean M.,Moreau, Emmanuel,Chavignon, Olivier,Lartigue, Claire,Blache, Yves,Teulade, Jean C.
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p. 5869 - 5878
(2007/10/03)
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- Identification and quantitation of key aroma compounds formed in Maillard-type reactions of fructose with cysteamine or isothiaproline (1,3-thiazolidine-2-carboxylic acid)
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Fructose was reacted in the presence of either cysteamine (model A) or isothiaproline (model B) in aqueous buffer at 145 °C and pH 7.0. Application of an aroma extract dilution analysis on the bulk of the volatile compounds formed in model A revealed 5-acetyl-3,4-dihydro-2H-1,4-thiazine (19), N-(2- mercaptoethyl)-1,3-thiazolidine (16), 4-hydroxy-2,5-dimethyl-3(2H)-furanone (15), and 2-acetyl-2- thiazoline (11) as the key aroma compounds among the 10 odorants detected. A similar set of aroma compounds was formed when isothiaproline was reacted (model B), but the flavor dilution factors were generally lower. Substitution of the buffer by silica gel/water (9 + 1 w/w) in both models and application of 150 °C for 10 min also gave the same key odorants from both thio compounds; however, under these conditions isothiaproline was the better precursor of, in particular, 19 and 11. Quantitative measurements performed by means of stable isotope dilution assays revealed a significant effect of the pH on odorant formation. For example, in model A, formation of 19 as well as of 11 was suppressed at pH values 5.0. A clear maximum was, however, found for 19 at pH 7.0 (~1 mol % yield), whereas 11 increased with increasing pH from 7.0 to 9.0.
- Engel, Wolfgang,Schieberle, Peter
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p. 5394 - 5399
(2007/10/03)
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- Platinum(II) compounds with enantiomerically pure bis(pinene)-fused bipyridine ligands - Diimine-dichloro complexes and their substitution reactions
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The synthesis of chiral square-planar PtII complexes using symmetrical and unsymmetrical bis(pinene)-fused 2,2′-bipyridine is described. The neutral diimine dichloro complexes show a strong deviation of the coordination sphere from planarity if the pinene groups are attached at the 5-and 6-positions of the pyridine rings. However, this distortion does not occur in parallel with the chiral configuration at the diimine ligands. The substitution of the two cis-chloro ligands with diamines to form five-membered chelate rings shows little diastereoselectivity when racemic mixtures of chiral diamines are used. Also, ligands that are prochiral at the ligating centers show little selectivity upon coordination.
- Kolp, Brunhilde,Abeln, Dirk,Stoeckli-Evans, Helen,Von Zelewsky, Alexander
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p. 1207 - 1220
(2007/10/03)
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- A C3-symmetric chiral hexadentate podand ligand based on a tris(pyrazolyl)borate core
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A hexadentate podand ligand having C3 symmetry has been prepared, consisting of a tris(pyrazolyl)borate core bearing pinene-functionalised 2-pyridyl units attached to the C3 position of each pyrazolyl ring such that each arm is a chiral bidentate chelate; complexes with Tl(I) and Tb(III) have been prepared and structurally characterised.
- Motson,Mamula,Jeffery,McCleverty,Ward,Von Zelewsky
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p. 1389 - 1391
(2007/10/03)
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- Phenylsulphonyloxiranes as Functional Acyl Anion Equivalents in Organic Synthesis
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Phenylsulphonyloxiranes can be lithiated with butyllithium α to the phenylsulphonyl group at low temperature.The anions formed are unstable, but sufficiently reactive to allow the isolation of adducts in good yield following treatment with a variety of el
- Ashwell, Mark,Clegg, William,Jackson, Richard F. W.
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p. 897 - 908
(2007/10/02)
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- Phenylsulphonyl Oxirane: a Versatile Reagent for Organic Synthesis
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Phenylsulphonyl oxirane (1) reacts as the synthetic equivalent of the acetaldehyde dipolar synthon (2).
- Ashwell, Mark,Jackson, Richard F. W.
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p. 645 - 647
(2007/10/02)
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- The Synthesis of 2-Heteroarylimidazopyridin-3-ols and Related Compounds
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A reaction between pyridin-2-amine 1-oxides and phenalcyl bromides has been extended to some bromoacetyl heteroaromatic compounds to form the title compounds.The reaction of some 2-aminodiazine 1-oxides with phenacyl bromides has also been studied.The imidazopyrimidne and imidazophthalazine systems have been prepared but reaction of pyrazin-2-amine 1-oxide did not give the desired cyclization.
- Deady, Leslie W.,Stanborough, Mark S.
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p. 1295 - 1302
(2007/10/02)
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