- Original electroactive and fluorescent bichromophores based on non-conjugated tetrazine and triphenylamine derivatives: Towards more efficient fluorescent switches
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The synthesis, photophysical and electrochemical properties and their interplay as well as theoretical calculations studies of newly designed fluorescent and electroactive derivatives are described. These molecules are composed of two fluorophores: one triphenylamine, electron-rich unit, and one tetrazine, electron-poor unit, connected by two different links. While in the neutral state the bichromophores are not fluorescent, due to a photoinduced electron transfer from the triphenylamine unit to the tetrazine unit, the fluorescence is restored in the oxidative state (oxidation of the triphenylamine moiety).
- Quinton, Cassandre,Alain-Rizzo, Valérie,Dumas-Verdes, Cécile,Clavier, Gilles,Audebert, Pierre
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p. 49728 - 49738
(2015/06/16)
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- ANTIFUNGAL 5,6-DIHYDRO-4H-PYRROLO[1,2-A][1,4]-BENZODIAZEPINES AND 6H-PYRROLO[1,2-A][1,4]BENZODIAZEPINES SUBSTITUTED WITH PHENYL DERIVATIVES
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The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines of Formula (I) wherein R1, R2, R3, R4, R5 and Rsu
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Page/Page column 45
(2012/06/15)
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- Benzophenone-containing fatty acids and their related photosensitive fluorescent new probes: Design, physico-chemical properties and preliminary functional investigations
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Hydrophobic photoaffinity labeling is a powerful strategy to identify hydrophobic segments within molecules, in particular membrane proteins. Here we report the design and synthesis of a novel family of fluorescent and photosensitive lipid tools, which have a common amino acid scaffold functionalized by three groups: (i) a first fatty acid chain grafted with a photoactivatable benzophenone moiety (Fatty Acid BenzoPhenone, FABP), (ii) a second fatty acid chain to ensure anchoring into a half-bilayer or hydrophobic environment, and (iii) a fluorescent carboxytetramethylrhodamine headgroup (CTMR) to detect the photolabeled compound. We present data of the synthesis and characterization of three lipid tools whose benzophenone ring is situated at various distances from the central scaffold. We could therefore establish structure/properties relationships dependent upon the depth of insertion of benzophenone into the membrane. Our lipid tools were extensively characterized both physico- and bio-chemically, and we assessed their functionality in vitro using bacterioRhodopsin (bR). We thus provide the scientific community with novel and reliable tools for the identification and study of hydrophobic regions in proteins.
- Hilbold, Beno?t,Perrault, Marie,Ehret, Christophe,Niu, Song-Lin,Frisch, Beno?t,Pécheur, Eve-Isabelle,Bourel-Bonnet, Line
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scheme or table
p. 7464 - 7473
(2012/01/06)
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- FLUOROPHORE AND FLUORESCENT SENSOR COMPOUND CONTAINING SAME
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The invention provides fluorophores of formulae (I) and (II) and also fluorescent sensor compounds comprising fluorophore moieties based on such fluorophores in combination with a receptor moiety. There is further provided a method of sensing the presence of a target analyte using the fluorescent sensor compound, as well as the use of the fluorescent sensor compounds to sense a target analyte.
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Page/Page column 70
(2010/11/03)
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- Silicon-derivates for PET-Imaging
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This invention relates to silicon-derivated compounds suitable for labelling or already labelled with 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging, preferably positron emission tomography (PET).
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Page/Page column 14
(2008/06/13)
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- Silicon derivatives for PET imaging
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This invention relates to silicon-derivated compounds suitable for labelling or already labelled with 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of
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Page/Page column 11-12
(2010/11/30)
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- New carboxamide compounds having melanin concentrating hormone antagonistic activity, pharmaceutical preparations comprising these compounds and process for their manufacture
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The present invention relates to carboxamide compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1, R2, R3 and k have the meanings given in claim 1. Moreover the invention relates to process for preparing the above mentioned carboxamides as well as pharmaceutical compositions containing at least one carboxamide according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
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Page/Page column 52
(2010/02/09)
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- Oxime compounds, their use, and intermediates for their production
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Oxime compounds of formula (1) wherein R1, R2, and R3 are independently halogen, C1-C3 alkyl, C1-C3 halolalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, nitro, or cyano; R4 is 3,3-dihalogeno-2-propenyl; a is an integer of 0 to 2; Y is oxygen, sulfur, or NH; Z is oxygen, sulfur, or NR5wherein R5 is hydrogen, acetyl, or C1-C3 alkyl; and X is of formula (2) insecticidal/acaricidal agents containing them as active ingredients; and intermediates for their production.
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- A Novel Approach to Dual-Acting Thromboxane Receptor Antagonist/Synthase Inhibitors Based on the Link of 1,3-Dioxane-Thromboxane Receptor Antagonists and -Thromboxane Synthase Inhibitors
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A new class of dual-acting racemic thromboxane receptor antagonist/thromboxane synthase inhibitors is reported, based on the novel approach of linking the known thromboxane synthase inhibitors (TXSI) dazoxiben (2) or isbogrel (11) (separately) to thromboxane receptor antagonists (TXRA) from the 1,3-dioxane series, such as ICI 192605 (10).Dual activity was observed in vitro with inhibition of human microsomal thromboxane synthase in the range IC50 = 0.01-1.0 μM and receptor antagonist activity by inhibition of U46619-induced human platelet aggregation in the range pA2 = 5.5-7.0.The in vitro results also showed that very large groups could be tolerated at the selected substitution positions of the TXRA and TXSI components.Oral activity was observed in ex vivo tests in both rats and dogs at a dose of 10 mg/kg.Thus, (E)-7--4-(2-hydroxyphenyl)-1,3-dioxan-2-yl>benzyl>oxy>phenyl>-7-(3-pyridyl)hept-6-enoic acid (110) was both an antagonist (pA2 = 6.7) and a synthase inhibitor (IC50 = 0.02 μM)).On oral dosing (10 mg/kg) to rats and dogs, 110 showed significant TXRA activity 64 (rat, 3 h) and >59 +/- 11.3 (dog, 2 h) vs ex vivo U46619-induced platelet aggregation>.Inhibition of thromboxane synthase at the respective time points in these experiments was 81 +/- 4.4percent (rat) and 69 +/- 4.8percent (dog).
- Ackerley, Norman,Brewster, Andrew G.,Brown, George R.,Clarke, David S.,Foubister, Alan J.,et al.
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p. 1608 - 1628
(2007/10/02)
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- Aminopyrimidine derivatives and their production and use
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There is disclosed a novel 4-aminopyrimidine derivative containing an optionally esterified carboxyl group at the 5-position which has potent fungicidal activity as well as insecticidal and miticidal activity. The compound is useful as agricultural fungic
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- Anti-asthmatic, anti-allergic, anti-cholinergic, bronchodilator and anti-inflammatory 1-[(benzoylphenyl)-lower-alkyl]piperidines and analogs thereof
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1-[(3- or 4-Benzoylphenyl)-lower-alkyl]-[(CH2)n --N=B]-substituted-piperidines, useful as anti-asthmatic, anti-allergic, anti-cholinergic, bronchodilator and anti-inflammatory agents, are prepared by alkylation of an appropriate subs
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- Benzoylphenyl lower alkanoyl piperidines
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1-[(3- or 4-Benzoylphenyl)-lower-alkyl]-[(CH2)n -N=B]-substituted-piperidines, useful as anti-asthmatic, anti-allergic, anti-cholinergic, bronchodilator and anti-inflammatory agents, are prepared by alkylation of an appropriate subst
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