Search Results - "Talaga, Patrice"

SV2A protein is a broad-spectrum anticonvulsant target: Functional correlation between protein binding and seizure protection in models of both partial and generalized epilepsy by Kaminski, Rafal M., Matagne, Alain, Leclercq, Karine, Gillard, Michel, Michel, Philippe, Kenda, Benoit, Talaga, Patrice, Klitgaard, Henrik

“…SV2A, a synaptic vesicle protein, has been recently identified as a binding target for levetiracetam (Keppra ®). The specific mechanism by which SV2A binding…”
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Discovery of 4-Substituted Pyrrolidone Butanamides as New Agents with Significant Antiepileptic Activity by Kenda, Benoit M, Matagne, Alain C, Talaga, Patrice E, Pasau, Patrick M, Differding, Edmond, Lallemand, Bénédicte I, Frycia, Anne M, Moureau, Florence G, Klitgaard, Henrik V, Gillard, Michel R, Fuks, Bruno, Michel, Philippe

“…(S)-α-ethyl-2-oxopyrrolidine acetamide 2 (levetiracetam, Keppra, UCB S.A.), a structural analogue of piracetam, has recently been approved as an add-on…”
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4-Benzyl-1H-imidazoles with Oxazoline Termini as Histamine H3 Receptor Agonists by Wijtmans, Maikel, Celanire, Sylvain, Snip, Erwin, Gillard, Michel R, Gelens, Edith, Collart, Philippe P, Venhuis, Bastiaan J, Christophe, Bernard, Hulscher, Saskia, Goot, Henk van der, Lebon, Florence, Timmerman, Henk, Bakker, Remko A, Lallemand, Bénédicte I. L. F, Leurs, Rob, Talaga, Patrice E, Esch, Iwan J. P. de

“…Research on the therapeutic applications of the histamine H3 receptor (H3R) has traditionally focused on antagonists/inverse agonists. In contrast, H3R…”
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Open Innovation: share or die by Talaga, Patrice

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Opinion: The future of pharmaceutical R&D: somewhere between open and reverse innovation? by Talaga, Patrice

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Keynote review: Histamine H3 receptor antagonists reach out for the clinic by Celanire, Sylvain, Wijtmans, Maikel, Talaga, Patrice, Leurs, Rob, de Esch, Iwan J.P.

“…Histamine receptors represent a tried and tested target for the treatments of various conditions including allergic responses, gastric ulcers and dyspepsia…”
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Pyrazolo[4,3-c]isoquinolines as potential inhibitors of NF-κB activation by Mortier, Jérémie, Frederick, Raphaël, Ganeff, Corinne, Remouchamps, Caroline, Talaga, Patrice, Pochet, Lionel, Wouters, Johan, Piette, Jacques, Dejardin, Emmanuel, Masereel, Bernard

“…Docking of a new inhibitor of TAK1 (IC 50 = 0.56 μM) and identification of potential interactions with the hinge region: In this work, we aimed to build a…”
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Compound decomposition: a new drug discovery tool? by Talaga, Patrice

“…Chemical decomposition reactions might represent an unexplored and exciting research tool potentially leading to the discovery of completely new molecular…”
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Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H3 Receptor Agonist by Kitbunnadaj, Ruengwit, Zuiderveld, Obbe P, Christophe, Bernard, Hulscher, Saskia, Menge, Wiro M. P. B, Gelens, Edith, Snip, Erwin, Bakker, Remko A, Celanire, Sylvain, Gillard, Michel, Talaga, Patrice, Timmerman, Henk, Leurs, Rob

“…In this study, the piperidine ring of immepip and its analogues was replaced by a rigid heterocyclic pyridine ring. Many compounds in the series exhibit high…”
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Identification of 4-(1 H -Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H 3 Receptor Agonist by Kitbunnadaj, Ruengwit, Zuiderveld, Obbe P., Christophe, Bernard, Hulscher, Saskia, Menge, Wiro M. P. B., Gelens, Edith, Snip, Erwin, Bakker, Remko A., Celanire, Sylvain, Gillard, Michel, Talaga, Patrice, Timmerman, Henk, Leurs, Rob

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First dual NK1 antagonists-serotonin reuptake inhibitors: Synthesis and SAR of a new class of potential antidepressants by RYCKMANS, Thomas, BALANCON, Laurent, BERTON, Olivier, GENICOT, Christophe, LAMBERTY, Yves, LALLEMAND, Benedicte, PASAU, Patrick, PIRLOT, Nathalie, QUERE, Luc, TALAGA, Patrice

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Alkyne–quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD by Starck, Jean-Philippe, Provins, Laurent, Christophe, Bernard, Gillard, Michel, Jadot, Sophie, Lo Brutto, Patrick, Quéré, Luc, Talaga, Patrice, Guyaux, Michel

“…SAR around alkyne–quinuclidine derivatives allowed the discovery of highly potent muscarinic antagonists displaying interesting preferential slow off-rates…”
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In vitro properties of 5-(benzylsulfonyl)-4-bromo-2-methyl-3(2H)-pyridazinone: A novel permeability transition pore inhibitor by Fuks, Bruno, Talaga, Patrice, Huart, Catherine, Hénichart, Jean-Pierre, Bertrand, Karine, Grimée, Renée, Lorent, Geneviève

“…Despite the increasing implication of the permeability transition pore (PTP) in the pathophysiology of neurodegenerative diseases, few selective PTP inhibitors…”
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Discovery of a New Class of Non‐imidazole Oxazoline‐Based Histamine H 3 Receptor (H 3 R) Inverse Agonists by Célanire, Sylvain, Wijtmans, Maikel, Christophe, Bernard, Collart, Philippe, de Esch, Iwan, Dassesse, Donald, Delaunoy, Christel, Denonne, Frédéric, Durieu, Véronique, Gelens, Edith, Gillard, Michel, Lallemand, Bénédicte, Lamberty, Yves, Lebon, Florence, Nicolas, Jean‐Marie, Quéré, Luc, Snip, Erwin, Vanbellinghen, Alain, Van houtvin, Nathalie, Verbois, Valérie, Timmerman, Henk, Talaga, Patrice, Leurs, Rob, Provins, Laurent

“…H 3 R inverse agonists based on an aminopropoxy‐phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse…”
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4-Benzyl-1 H -imidazoles with Oxazoline Termini as Histamine H 3 Receptor Agonists by Wijtmans, Maikel, Celanire, Sylvain, Snip, Erwin, Gillard, Michel R., Gelens, Edith, Collart, Philippe P., Venhuis, Bastiaan J., Christophe, Bernard, Hulscher, Saskia, Goot, Henk van der, Lebon, Florence, Timmerman, Henk, Bakker, Remko A., Lallemand, Bénédicte I. L. F., Leurs, Rob, Talaga, Patrice E., Esch, Iwan J. P. de

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Histamine H3 receptor antagonists reach out for the clinic by CELANIRE, Sylvain, WIJTMANS, Maikel, TALAGA, Patrice, LEURS, Rob, DE ESCH, Iwan J. P

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4-Benzyl-lH-imidazoles with Oxazoline Termini as Histamine H3 Receptor Agonists by WIJTMANS, Maikel, CELANIRE, Sylvain, LEBON, Florence, TIMMERMAN, Henk, BAKKER, Remko A, LALLEMAND, Bénédicte I. L. F, LEURS, Rob, TALAGA, Patrice E, DE ESCH, Iwan J. P, SNIP, Erwin, GILLARD, Michel R, GELENS, Edith, COLLART, Philippe P, VENHUIS, Bastiaan J, CHRISTOPHE, Bernard, HULSCHER, Saskia, VAN DER GOOT, Henk

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Dual NK1 antagonists: Serotonin reuptake inhibitors as potential antidepressants. Part 2: Sar and activity of benzyloxyphenethyl piperazine derivatives by RYCKMANS, Thomas, BERTON, Olivier, GRIMEE, Renée, KOGEJ, Thierry, LAMBERTY, Yves, PASAU, Patrick, TALAGA, Patrice, GENICOT, Christophe

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Discovery of a New Class of Non-imidazole Oxazoline-Based Histamine H3 Receptor (H3R) Inverse Agonists by Célanire, Sylvain, Wijtmans, Maikel, Christophe, Bernard, Collart, Philippe, de Esch, Iwan, Dassesse, Donald, Delaunoy, Christel, Denonne, Frédéric, Durieu, Véronique, Gelens, Edith, Gillard, Michel, Lallemand, Bénédicte, Lamberty, Yves, Lebon, Florence, Nicolas, Jean-Marie, Quéré, Luc, Snip, Erwin, Vanbellinghen, Alain, Van houtvin, Nathalie, Verbois, Valérie, Timmerman, Henk, Talaga, Patrice, Leurs, Rob, Provins, Laurent

“…H3R inverse agonists based on an aminopropoxy‐phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse…”
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Efficient and regioselective 4-amino-de-chlorination of 2,4,6-trichloropyrimidine with N-sodium carbamates by Zanda, Matteo, Talaga, Patrice, Wagner, Alain, Mioskowski, Charles

“…4- N-Alkoxycarbonyl-2,6-dichloropyrimidines have been synthesized with good to excellent regioselectivity and yields from 2,4,6-trichloropyrimidine and…”
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