References of "Delarge, Jacques"
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See detailWATER SOLUBLE CURCUMIN COMPOSITIONS FOR USE IN ANTI-CANCER AND ANTI-INFLAMMATORY THERAPY
Neven, Philippe; Serteyn, Didier ULg; Delarge, Jacques et al

Patent (2011)

The present invention relates to the medical field. In a first aspect the present invention relates to novel water soluble cyclodextrin-curcumin complexes having a pharmacological activity, in particular ... [more ▼]

The present invention relates to the medical field. In a first aspect the present invention relates to novel water soluble cyclodextrin-curcumin complexes having a pharmacological activity, in particular an anti-tumour and/or anti-inflammatory activity, and improved physico-chemical properties. In a second aspect, the present invention relates to a method for preparation of said water soluble curcumin derivatives. The invention further relates in a third aspect to a pharmaceutical composition comprising an effective amount of said water soluble curcumin derivatives. In a fourth aspect, the present invention concerns the use of said water soluble cucumin derivatives as a medicament and the use of said water soluble curcumin derivatives for the preparation of a medicament for the treatment of cancer and inflammatory diseases. In a fifth aspect, the present invention relates to the use of a pharmaceutical composition comprising said water soluble curcumin derivatives in the treatment of cancer and inflammatory diseases and to a new pharmaceutical composition comprising said water soluble curcumin derivatives. [less ▲]

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See detail8-Chloro-6-(3-dimethylaminopropylamino)-11H-pyrido[2,3-b][1,4]benzodiazepine
Dupont, Léon ULg; Eyrolles, Laurence; Evrard, Guy et al

in Acta Crystallographica Section E-Structure Reports Online (2002), 58(Part 1), 69-71

The crystal structure determination of the title compound, C17H20ClN5, has been undertaken as part of studies on antipsychotic drugs. Its structure is compared with that of clozapine (C18H19ClN4), a well ... [more ▼]

The crystal structure determination of the title compound, C17H20ClN5, has been undertaken as part of studies on antipsychotic drugs. Its structure is compared with that of clozapine (C18H19ClN4), a well known atypical antipsychotic drug. The side chain is more flexible than in the N-methylpiperazine analogues, but its folding is influenced by an intramolecular N-H . . .N hydrogen bond. The distances between the N-distal atom, a possible pharmacophore, and the centres of the two aromatic rings are significantly shorter than in clozapine. The crystal packing involves one N-H . . .N intermolecular hydrogen bond. The title compound showed no affinity for the receptors tested. [less ▲]

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See detailThe behavioral effects of acute and chronic JL 13, a putative antipsychotic, in Cebus non-human primates
Casey, Daniel; Bruhwyler, Jacques; Delarge, Jacques et al

in Psychopharmacology (2001), 157

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See detailAntiinflammatory and chonroprotective activity of prodelphinidins isolated from Ribes nigrum leaves
Tits, Monique ULg; de Leval Xavier; Dierckxsens, Yvan et al

Poster (2000, July)

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See detailAnti-inflammatory and chondroprotective activity of prodelphinidins isolated from Ribes nigrum leaves.
Tits, Monique ULg; de Leval, Xavier; Diercksens, Yves et al

Poster (2000)

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See detailStudy of the Influence of Both Cyclodextrins and L-Lysine on the Aqueous Solubility of Nimesulide; Isolation and Characterization of Nimesulide-L-Lysine-Cyclodextrin Complexes
Piel, Géraldine ULg; Pirotte, Bernard ULg; Delneuville, Isabelle et al

in Journal of Pharmaceutical Sciences (1997), 86(4), 475-80

Nimesulide is a nonsteroidal antiinflammatory drug that exhibits a very poor water solubility (0.01 mg.mL-1). A nimesulide-beta-cyclodextrin complex prepared according to patent application WO 94/ 02177 ... [more ▼]

Nimesulide is a nonsteroidal antiinflammatory drug that exhibits a very poor water solubility (0.01 mg.mL-1). A nimesulide-beta-cyclodextrin complex prepared according to patent application WO 94/ 02177 has an aqueous solubility of approximately 16 mg.mL-1 of nimesulide. A nimesulide-L-lysine salt has also been prepared and increases the aqueous solubility of nimesulide to approximately 5.0-7.5 mg.mL-1. The purpose of the present study was to investigate the interaction of both cyclodextrins and L-lysine on the aqueous solubility of nimesulide. Nimesulide-L-lysine-beta- or gamma-cyclodextrin complexes were prepared by spray-drying. The inclusion of the nimesulide-L-lysine salt into the cyclodextrin cavity was confirmed by differential scanning calorimetry and proton nuclear magnetic resonance spectroscopy. These complexes offered remarkable aqueous solubility. The incorporation of nimesulide in a nimesulide-L-lysine-beta-cyclodextrin complex increased its water solubility by a factor of 10 at pH 1.5 (0.050 mg.mL-1 for the complex versus 0.005 mg.mL-1 for nimesulide), 160 at pH 6.8 (2.373 mg.mL-1 for the complex versus 0.015 mg.mL-1 for nimesulide), and 3600 in purified water (36.400 mg.mL-1 for the complex versus 0.01 mg.mL-1 for nimesulide). [less ▲]

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See detailStudy of the influence of g-cyclodextrin on the molsidomine photostability
Piel, Géraldine ULg; Pochet, Lionel; Delattre, Luc ULg et al

Poster (1996, April)

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See detailPhotostability studies of molsidomine-cyclodextrin complexes
Piel, Géraldine ULg; Pochet, Lionel; Delattre, Luc ULg et al

Poster (1995, June)

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See detailLes activateurs de canaux potassiques: étude structurale comparative du pinacidil, du diazoxide et du cromakalim
Dupont, Léon ULg; Pirotte, Bernard ULg; De Tullio, Pascal ULg et al

in Annales Pharmaceutiques Françaises (1995), 53(5), 201-208

A conformational analysis has been performed with SYBYL starting from the energy optimized (Tripos force field) X-ray conformation of (R,S)-pinacidil. The geometry of four selected low energy conformers ... [more ▼]

A conformational analysis has been performed with SYBYL starting from the energy optimized (Tripos force field) X-ray conformation of (R,S)-pinacidil. The geometry of four selected low energy conformers has been reoptimized using the AM1 semiempirical Molecular Orbital method (MOPAC 5.0), and the total energy of the optimized conformers has been compared. In spite of an apparent structural dissimilarity, a good analogy has been found between the calculated isopotential map of diazoxide and that of at least one selected low energy conformer of pinacidil. It has been suggested that, unlike cromakalim, the low but observable activity of pinacidil on pancreatic B-cells could be explained by adoption for this compound of a conformation having a diazoxide-like stereoelectronical imprint which could assume a similar interaction on the same biological receptor. [less ▲]

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See detailSynthèse, étude théorique et évaluation biologique de dérivés du 4-amino-4H-1,2,4-triazole analogues des antibiotiques b-lactamiques
Pirotte, Bernard ULg; Dive, Georges ULg; Delarge, Jacques et al

in European Journal of Medicinal Chemistry (1992), 27(3), 193-205

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See detailNew alkoxypyridine Sulfonamides: Synthesis, Biological Evaluation and Physicochemical Properties
Liégeois, Jean-François ULg; Dive, Georges ULg; Dupont, Léon et al

in Helvetica Chimica Acta (1991), 74(8), 1764-1772

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