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See detailPharmacology Of The Hypoglycaemic Sulphonylurea Gliquidone .3. Conformational Analysis
Lins, Laurence ULg; Brasseur, Robert ULg; Malaisse, Wj.

in Pharmacological Research (1996), 34(1-2), 9-10

The hypoglycaemic sulphonylurea gliquidone was found, by conformation analysis, to display a U-shaped configuration, with hydrophobic cycles placed at the extremity of each branch and a peptidic bond ... [more ▼]

The hypoglycaemic sulphonylurea gliquidone was found, by conformation analysis, to display a U-shaped configuration, with hydrophobic cycles placed at the extremity of each branch and a peptidic bond placed at the bottom of the U. This configuration is similar to that recently observed with the hypoglycaemic sulphonylureas glimepiride and glibenclamide and non-sulphonylurea hypoglycaemic agents of the meglitinide family, such as S3075, repaglinide, A-4166 and KAD-1229. The identification of a conformation common to these various hypoglycaemic drugs may provide an imprint of their binding site at the level of the B-cell sulphonylurea receptor. [less ▲]

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See detailPharmacology of the Thromboxane Receptor Antagonist and Thromboxane Synthase Inhibitor Bm-531
Dogné, J. M.; Rolin, S.; de Leval, X. et al

in Cardiovascular Drug Reviews (2001), 19(2, Summer), 87-96

BM-531 (N-tert-butyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea), a torasemide derivative, is a novel noncarboxylic thromboxane receptor antagonist and thromboxane synthase inhibitor. Indeed, its ... [more ▼]

BM-531 (N-tert-butyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea), a torasemide derivative, is a novel noncarboxylic thromboxane receptor antagonist and thromboxane synthase inhibitor. Indeed, its affinity for human washed platelet TXA2 receptors labeled with [3H]SQ-29548 (IC50 = 0.0078 microM) is higher than sulotroban (IC50 = 0.93 microM) and SQ-29548 (IC50 = 0.021 microM). Moreover, BM-531 is characterized by a potent antiaggregatory property. Indeed, on one hand, in human citrated platelet-rich plasma BM-531 prevents platelet aggregation induced by arachidonic acid (600 microM) (ED100 = 0.125 microM), U-46619, a stable TXA2 agonist (1 microM) (ED50 = 0.482 microM) or collagen (1 microgram/mL) (percentage of inhibition: 42.9% at 10 microM) and inhibits the second wave of ADP (2 microM)-induced aggregation. On the other hand, when BM-531 is incubated in whole blood from healthy donors, the closure time measured by the recently developed platelet function analyser (PFA-100) is significantly prolonged. In addition, at the concentrations of 10 and 1 microM, BM-531 totally prevents the production of TXB2 by human platelets activated by arachidonic acid. Finally, at 10 microM, BM-531 significantly prevents rat fundus contractions induced by U-46619 but not by prostacyclin. These results suggest that BM-531, which is devoid of the diuretic property of torasemide, can be regarded as a promising antiplatelet agent. [less ▲]

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See detailPharmacology of tiludronate in horses
Delguste, Catherine ULg

Conference (2008, November 08)

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See detailPharmacomodulation of torasemide led to original diuretic, neuroprotective, anticonvulsant and antithrombotic drugs
Masereel, B.; Dogne, J. M.; Damas, J. et al

Conference (1997, April)

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See detailPharmacomodulation of torasemide led to original diuretic, neuroprotective, anticonvulsant and antithrombotic drugs
Masereel, B.; Dogne, J.-M.; Damas, J. et al

in Journal de Pharmacie de Belgique (1997), 52

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See detailPHARMACOMODULATIONS DU WAY-100635 : DE NOUVELLES PISTES DANS LA CONCEPTION D’ANTAGONISTES SÉLECTIFS DES RÉCEPTEURS 5-HT1A
Dilly, Sébastien ULg; Mangin, Floriane; Joly, Benoît ULg et al

Poster (2012, May 24)

Le composé WAY-100635 est un outil pharmacologique abondamment utilisé dans l’exploration des récepteurs sérotoninergiques 5-HT1A. Dès lors, cette molécule de référence devrait présenter une sélectivité ... [more ▼]

Le composé WAY-100635 est un outil pharmacologique abondamment utilisé dans l’exploration des récepteurs sérotoninergiques 5-HT1A. Dès lors, cette molécule de référence devrait présenter une sélectivité importante pour sa cible. Cependant, des travaux récents ont démontré que, à côté de son activité antagoniste des récepteurs 5-HT1A, le WAY-100635 possédait également une affinité et activité conséquentes vis-à-vis des récepteurs dopaminergiques D4, ce qui pourrait limiter son utilisation comme outil pharmacologique. Dans ce contexte, nous avons entrepris diverses modulations structurales de cette molécule de manière à augmenter sa sélectivité vis-à-vis des récepteurs 5-HT1A. Cette sélectivité a été augmentée de manière significative lors du remplacement de la chaîne latérale basique par un groupement 4-phénylpipérazine ou 4-phényl-1,2,3,6-tétrahydropyridine. Une évaluation biologique plus approfondie des deux composés comprenant un profil d’affinité élargi à d’autres récepteurs a confirmé leur sélectivité vis-à-vis des récepteurs 5-HT1A. De plus, des expériences électrophysiologiques sur tranches de cerveau. [less ▲]

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See detailPharmacophore generation to design new leads for selective cyclooxygenase-2 (COX-2) inhibition
Michaux, C.; De Leval, X.; Julemont, F. et al

Poster (2003, May)

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See detailPharmacophore generation to design new leads for selective cyclooxygenase-2 inhibition
Michaux, C.; Julemont, F.; De Leval, X. et al

Poster (2004, October 07)

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See detailPharmacopoea Aegyptia et Graeco-Aegyptia : bibliographie générale
Marganne, Marie-Hélène ULg; Koemoth, Pierre ULg

Textual, factual or bibliographical database (2003)

Bibliographical references to identify animal, plant and mineral products used in the pharmacopoeias of Pharaonic, Greco-Roman and Byzantine Egypt

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See detailPharmacotherapie du sujet agee: primum non nocere!
Scheen, André ULg

in Revue medicale de Liege (2014), 69(5-6), 282-6

Elderly patients, having various chronic diseases, are generally exposed to polypharmacy that may lead to potential adverse events. The latter may be explained by pharmacokinetic and pharmacodynamic ... [more ▼]

Elderly patients, having various chronic diseases, are generally exposed to polypharmacy that may lead to potential adverse events. The latter may be explained by pharmacokinetic and pharmacodynamic particularities that render elderly individuals more vulnerable when exposed to certain medications. Recruitment of elderly patients in clinical trials is often limited, so that it is not always easy to determine the real benefit/risk ratio of pharmacotherapy in this population. Obviously, iatrogenicity is quite frequent. Therefore, in front of unexplained alterations of health status in an elderly individual, the physician should consider the possibility of a drug adverse effect. Because of this situation, the physician should envisage a reasonable drug prescription in an elderly patient. Especially, not only the initiation of drug therapy should be carefully analyzed, but also the opportunity to eventually stop a medication that may be useless or even dangerous. Rather polypharmacy per se, it is the inappropriate prescription that should be avoided in the elderly. [less ▲]

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See detailPharmacotherapy of onychomycosis
Baran, R.; Gupta, A. K.; Pierard, Gérald ULg

in Expert Opinion on Pharmacotherapy (2005), 6(4), 609-624

Fungal infections of the nails are frequent in some segments of the population. Dermatophytes, yeasts and moulds are potential pathogens. A series of antifungal treatments are available to the clinician ... [more ▼]

Fungal infections of the nails are frequent in some segments of the population. Dermatophytes, yeasts and moulds are potential pathogens. A series of antifungal treatments are available to the clinician, differing by both their mechanistic nature and mode of administration. The pharmacodynamic and pharmacokinetic properties of each antifungal agent are distinct. This review focuses on the characteristics of amorolfine, bifonazole, ciclopirox, fluconazole, griseofulvin, itraconazole, ketoconazole, ravuconazole, R126638 and terbinafine. Single drug treatments and combined therapies are presented. None of the current drug regimens have demonstrated reliable efficacy against all cases of onychomycosis. Treatment failures, relapses and reinfections remain stubborn problems in the management of onychomycosis. [less ▲]

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See detailA phase 1-2, prospective, double blind, randomized study of the safety and efficacy of Sulfasalazine for the treatment of progressing malignant gliomas: study protocol of [ISRCTN45828668].
Robe, Pierre ULg; Martin, Didier ULg; Albert, Adelin ULg et al

in BMC Cancer (2006), 6

BACKGROUND: The prognosis of patients suffering from WHO grade 3 and 4 astrocytic glioma remains poor despite surgery, radiation therapy and the use of current chemotherapy regimen. Indeed, the median ... [more ▼]

BACKGROUND: The prognosis of patients suffering from WHO grade 3 and 4 astrocytic glioma remains poor despite surgery, radiation therapy and the use of current chemotherapy regimen. Indeed, the median survival of glioblastoma multiforme (WHO grade 4) patients is at best 14.6 month with only 26.5 percent of the patients still alive after 2 years and the median survival of anaplastic astrocytomas (WHO grade 3) is 19.2 month. Recent evidence suggests that the transcription factor NF-kappaB is constitutively expressed in malignant gliomas and that its inhibition by drugs like Sulfasalazine may block the growth of astrocytic tumors in vitro and in experimental models of malignant gliomas. DESIGN: ULg_GBM_04/1 is a prospective, randomized, double blind single-center phase 1-2 study. A total of twenty patients with progressive malignant glioma despite surgery, radiation therapy and a first line of chemotherapy will be recruited and assigned to four dosage regimen of Sulfasalazine. This medication will be taken orally t.i.d. at a daily dose of 1.5-3-4 or 6 g, continuously until complete remission, evidence of progression or drug intolerance. Primary endpoints are drug safety in the setting of malignant gliomas and tumor response as measured according to MacDonald's criteria. An interim analysis of drug safety will be conducted after the inclusion of ten patients. The complete evaluation of primary endpoints will be conducted two years after the enrollment of the last patient or after the death of the last patient should this occur prematurely. DISCUSSION: The aim of this study is to evaluate the safety and efficacy of Sulfasalazine as a treatment for recurring malignant gliomas. The safety and efficacy of this drug are analyzed as primary endpoints. Overall survival and progression-free survival are secondary endpoint. [less ▲]

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See detailPhase 2 Results of XL184 in a Cohort of Patients with Advanced Melanoma
Nechushtan, Hovav; Edelman, Gerald; JERUSALEM, Guy ULg et al

in EJC Supplements (2010, November), 8(7), 126-127

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See detailA phase 3 study of the efficacy and safety of Denosumab in men with low bone mineral density : design of the ADAMO
Orwoll, E.; Stubbe Teglbjaerg, Ch; Langdahl, B. et al

in Journal of Bone and Mineral Research (2011), 26(S1), 511

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See detailPhase And Amplitude Of Ecosystem Carbon Release And Uptake Potentials As Derived From Fluxnet Measurements
Falge, Eva; Tenhunen, John; Baldocchi, Dennis et al

in Agricultural and Forest Meteorology (2002), 113(1-4),

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See detailPhase behavior of diblock copolymers between styrene and n-alkyl methacrylates
Ruzette, A. V. G.; Banerjee, P.; Mayes, A. M. et al

in Macromolecules (1998), 31(24), 8509-8516

In contrast to most diblock copolymers which exhibit the classical upper critical ordering transition (UCOT), polystyrene-b-poly n-butyl methacrylatePS-b-PBMAhas been shown to undergo ordering upon ... [more ▼]

In contrast to most diblock copolymers which exhibit the classical upper critical ordering transition (UCOT), polystyrene-b-poly n-butyl methacrylatePS-b-PBMAhas been shown to undergo ordering upon heating through a lower critical ordering transition (LCOT). Here we report the phase behavior of a family of diblock copolymers formed from styrene and a homologous series of n-alkyl methacrylates, as determined by combined dynamic rheological testing and small-angle neutron scattering (SANS). It is shown that the shortest side chain methacrylates, with the exception of methyl methacrylate, exhibit the LCOT, while for side chains longer than n-butyl, the copolymers exhibit the classical UCOT behavior. Combined group contribution/lattice fluid model calculations of the solubility parameter and specific volume of the corresponding homopolymers qualitatively support these observations. The same calculations were further employed to molecularly design LCOT behavior into a new diblock material consisting of styrene and a random copolymer of methyl and lauryl methacrylate, denoted PS-b-P(MMA-r-LMA). The success of this approach suggests a simple semiquantitative method for predicting and designing the phase behavior of weakly interacting polymer pairs. [less ▲]

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See detailPhase Change Memories challenges: A material and process perspective
Maitrejean, S.; Ghezzi, G.; Gourvest, E. et al

in 2012 IEEE International Interconnect Technology Conference, IITC 2012 (2012)

Among all the new memories concepts, Phase Change Memories (PCM) is one of the most promising. However, various challenges remain. This paper reviews the materials and processes required to face these ... [more ▼]

Among all the new memories concepts, Phase Change Memories (PCM) is one of the most promising. However, various challenges remain. This paper reviews the materials and processes required to face these challenges. As an example, attention will be made on the effect of Phase change material composition on stability of the amorphous phase i.e. on the retention of the information. Additionally, it is showed how specific processes such as CVD or ALD can be developed in order to minimize the current required to amorphize the phase change material i.e. to reset the device. Finally, with the perspectives of the advanced integration nodes, experimental results on the effect of scaling on phase transformation are presented and discussed. © 2012 IEEE. [less ▲]

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See detailPhase closure image reconstruction for future VLTI instrumentation
Filho, Mercedes E; Renard, Stephanie; Garcia, Paulo et al

in Schöller, Markus; Danchi, William; Delplancke, Françoise (Eds.) Optical and Infrared Interferometry (2008, July 01)

Classically, optical and near-infrared interferometry have relied on closure phase techniques to produce images. Such techniques allow us to achieve modest dynamic ranges. In order to test the feasibility ... [more ▼]

Classically, optical and near-infrared interferometry have relied on closure phase techniques to produce images. Such techniques allow us to achieve modest dynamic ranges. In order to test the feasibility of next generation optical interferometers in the context of the VLTI-spectro-imager (VSI), we have embarked on a study of image reconstruction and analysis. Our main aim was to test the influence of the number of telescopes, observing nights and distribution of the visibility points on the quality of the reconstructed images. Our results show that observations using six Auxiliary Telescopes (ATs) during one complete night yield the best results in general and is critical in most science cases; the number of telescopes is the determining factor in the image reconstruction outcome. In terms of imaging capabilities, an optical, six telescope VLTI-type configuration and ~200 meter baseline will achieve 4 mas spatial resolution, which is comparable to ALMA and almost 50 times better than JWST will achieve at 2.2 microns. Our results show that such an instrument will be capable of imaging, with unprecedented detail, a plethora of sources, ranging from complex stellar surfaces to microlensing events. [less ▲]

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See detailPhase control for the stabilization of a photorefractive holographic camera in perturbed environments
Thizy, Cédric ULg; Georges, Marc ULg; Lemaire, philippe

in Hesselink, Lambertus; Feinberg, Jack (Eds.) Controlling Light with Light: Photorefractive Effects, Photosensitivity, Fiber Gratings, Photonic Materials and More (2007, October)

The holographic interferometer developed by CSL, and which uses a BSO crystal, exhibits a response time of a few seconds. This prevents us to properly record holograms under perturbated environmental ... [more ▼]

The holographic interferometer developed by CSL, and which uses a BSO crystal, exhibits a response time of a few seconds. This prevents us to properly record holograms under perturbated environmental conditions due to optical phase variations between reference and object beams. We present hereafter several active phase control strategies to overcome this problem [less ▲]

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See detailPhase control strategies for stabilization of photorefractive holographic interferometer
Thizy, Cédric ULg; Georges, Marc ULg; Lemaire, Philippe ULg et al

in Slangen, P.; Cerruti, C. (Eds.) Speckle06 : Speckles, From Grains to Flowers (2006, September)

A current problem encountered in holographic interferometry systems is the phase variations that arise from vibrations, from the use of optical fiber in one arm, by air convection or by unwanted movement ... [more ▼]

A current problem encountered in holographic interferometry systems is the phase variations that arise from vibrations, from the use of optical fiber in one arm, by air convection or by unwanted movement between the object and the measurement device. The holographic device developed by CSL based on photorefractive BSO crystals has the advantage of high resolution fringes with the capability of self-processing and indefinite reusability. The weakness of the technique is a response time that is often slow compared to external perturbations. For applications outside the laboratory, we decided to find solutions adapted to the holographic camera and which tend to limit or to eliminate the effect of such phase variations. An error signal is measured from one or another technique which measure the phase variations and which counteracts on an active element in the interferometer to stabilize the phase during recording. Different solutions have been analysed and are presented here. Interferograms were obtained with and without implementation of the phase control system that show the interest of such approach. Some of the system presented are only adapted to photorefractive holographic interferometry, making use of some crystal diffraction properties. Other systems can be used with other kind of interferometers. [less ▲]

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