Search Results - "Labaudiniere, R"

New 4-Point Pharmacophore Method for Molecular Similarity and Diversity Applications:  Overview of the Method and Applications, Including a Novel Approach to the Design of Combinatorial Libraries Containing Privileged Substructures by Mason, Jonathan S, Morize, Isabelle, Menard, Paul R, Cheney, Daniel L, Hulme, Christopher, Labaudiniere, Richard F

“…A new 4-point pharmacophore method for molecular similarity and diversity that rapidly calculates all potential pharmacophores/pharmacophoric shapes for a…”
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Tafamidis for transthyretin familial amyloid polyneuropathy: a randomized, controlled trial by Coelho, Teresa, Maia, Luis F, Martins da Silva, Ana, Waddington Cruz, Marcia, Planté-Bordeneuve, Violaine, Lozeron, Pierre, Suhr, Ole B, Campistol, Josep M, Conceição, Isabel Maria, Schmidt, Hartmut H-J, Trigo, Pedro, Kelly, Jeffery W, Labaudinière, Richard, Chan, Jason, Packman, Jeff, Wilson, Amy, Grogan, Donna R

“…To evaluate the efficacy and safety of 18 months of tafamidis treatment in patients with early-stage V30M transthyretin familial amyloid polyneuropathy…”
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RPR's approach to high-speed parallel synthesis for lead generation by Labaudiniere, Richard F.

“…Rhône-Poulenc Rorer (RPR) is developing high-speed parallel synthesis as an essential tool to produce large libraries for lead generation. Libraries of 5000–10…”
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The Discovery of Tadalafil:  A Novel and Highly Selective PDE5 Inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1‘,2‘:1,6]pyrido[3,4-b]indole-1,4-dione Analogues by Daugan, Alain, Grondin, Pascal, Ruault, Cécile, Le Monnier de Gouville, Anne-Charlotte, Coste, Hervé, Linget, Jean Michel, Kirilovsky, Jorge, Hyafil, François, Labaudinière, Richard

“…Modification of the hydantoin ring in the previously described lead compound 2a has led to the discovery of compound 12a, tadalafil, a highly potent and highly…”
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The Discovery of Tadalafil:  A Novel and Highly Selective PDE5 Inhibitor. 1: 5,6,11,11a-Tetrahydro-1H-imidazo[1‘,5‘:1,6]pyrido[3,4-b]indole-1,3(2H)-dione Analogues by Daugan, Alain, Grondin, Pascal, Ruault, Cécile, Le Monnier de Gouville, Anne-Charlotte, Coste, Hervé, Kirilovsky, Jorge, Hyafil, François, Labaudinière, Richard

“…Starting from ethyl β-carboline-3-carboxylate (β-CCE), 1, a modest inhibitor of type 5 phosphodiesterase (PDE5), a series of functionalized…”
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Synthesis and Binding Affinities of Novel Spirocyclic Lactam Peptidomimetics of Somatostatin by Damour, Dominique, Barreau, Michel, Blanchard, Jean-Charles, Burgevin, Marie-Claude, Doble, Adam, Pantel, Guy, Labaudinière, Richard, Mignani, Serge

“…Synthesis of novel spirocyclic lactam peptidomimetics of the binding domain of somatostatin from commercially available D, L-methionine is described…”
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omega.-[(4-Phenyl-2-quinolyl)oxy]alkanoic acid derivatives: a new family of potent LTB4 antagonists by Labaudiniere, Richard, Hendel, Wolfram, Terlain, Bernard, Cavy, Francoise, Marquis, Olivier, Dereu, Norbert

“…A series of omega-[(4-phenyl-2-quinolyl)oxy]alkanoic acid derivatives was prepared which inhibited the binding of the leukotriene B4 to its receptors on guinea…”
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omega.-[(4,6-Diphenyl-2-pyridyl)oxy]alkanoic acid derivatives: a new family of potent and orally active LTB4 antagonists by Labaudiniere, Richard, Dereu, Norbert, Cavy, Francoise, Guillet, Marie Christine, Marquis, Olivier, Terlain, Bernard

“…A series of omega-[(4,6-diphenyl-2-pyridyl)oxy]alkanoic acid derivatives was prepared which inhibited the binding of leukotriene B4 to its receptors on guinea…”
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Synthesis of vinyl selenides or sulfides and ketene selenoacetals or thioacetals by nickel(II) vinylation of sodium benzeneselenolate or benzenethiolate by Cristau, H. J, Chabaud, B, Labaudiniere, R, Christol, H

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omega.-[(.omega.-Arylalkyl)thienyl]alkanoic acids: from specific LTA4 hydrolase inhibitors to LTB4 receptor antagonists by Labaudiniere, Richard, Hilboll, Gerd, Leon-Lomeli, Alicia, Terlain, Bernard, Cavy, Francoise, Parnham, Michael, Kuhl, Peter, Dereu, Norbert

“…A series of omega-[(omega-arylalkyl)thienyl]alkanoic acid isomers was prepared and a structure-activity relationship was investigated. These compounds have…”
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Novel safety-catch linker and its application with a Ugi/De-BOC/Cyclization (UDC) strategy to access carboxylic acids, 1,4-benzodiazepines, diketopiperazines, ketopiperazines and dihydroquinoxalinones by Hulme, Christopher, Peng, John, Morton, George, Salvino, Joseph M., Herpin, Tim, Labaudiniere, Richard

“…This communication reveals the synthesis and application of a novel resin bound isonitrile. The resin is an example of a novel safety-catch linker which upon…”
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Synthesis of aryl phenyl and heteroaryl phenyl selenides by nickel(II)-catalyzed arylation of sodium benzeneselenolate by Cristau, H. J, Chabaud, B, Labaudiniere, R, Christol, H

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Long-term effects of tafamidis for the treatment of transthyretin familial amyloid polyneuropathy by Coelho, Teresa, Maia, Luis F., da Silva, Ana Martins, Cruz, Márcia W., Planté-Bordeneuve, Violaine, Suhr, Ole B., Conceiçao, Isabel, Schmidt, Hartmut H.-J., Trigo, Pedro, Kelly, Jeffery W., Labaudinière, Richard, Chan, Jason, Packman, Jeff, Grogan, Donna R.

“…Tafamidis, a transthyretin (TTR) kinetic stabilizer, delayed neuropathic progression in patients with Val30Met TTR familial amyloid polyneuropathy (TTR-FAP) in…”
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Improved Procedure for the Solution Phase Preparation of 1,4-Benzodiazepine-2,5-dione Libraries via Armstrong's Convertible Isonitrile and the Ugi Reaction by Hulme, Christopher, Peng, John, Tang, Sheng-Yuh, Burns, Christopher J, Morize, Isabelle, Labaudiniere, Richard

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Rhone-Poulenc Rorer's approach to high-speed parallel synthesis for lead generation by Labaudiniere, R F

“…Rhone-Poulenc Rorer (RPR) is developing high-speed parallel synthesis as an essential tool to produce large libraries for lead generation. Libraries of…”
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Novel applications of resin bound α-amino acids for the synthesis of benzodiazepines (via Wang resin) and ketopiperazines (via hydroxymethyl resin) by Hulme, Christopher, Ma, Liang, Kumar, N.Vasant, Krolikowski, Paul H, Allen, Andrew C, Labaudiniere, Richard

“…This communication reveals a novel application of resin bound α-amino acids coupled with the UDC (Ugi/DeBOC/cyclize) strategy. Reaction with either…”
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Novel applications of convertible isonitriles for the synthesis of mono and bicyclic γ-lactams via a UDC strategy by Hulme, Christopher, Ma, Liang, Cherrier, Marie-Pierre, Romano, Joseph J, Morton, George, Duquenne, Celine, Salvino, Joseph, Labaudiniere, Richard

“…This communication reveals a novel application of the so-called convertible isonitriles for the solution/solid phase generation of γ-lactam analogues. Use of…”
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Synthesis and diversity analysis of lead discovery piperazine-2-carboxamide libraries by Herpin, T F, Morton, G C, Dunn, A K, Fillon, C, Menard, P R, Tang, S Y, Salvino, J M, Labaudinière, R F

“…A Lead Discovery Library of piperazine-2-carboxamide derivatives was produced for general screening. This paper discloses two novel solid phase synthetic…”
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Novel applications of carbon dioxide/MeOH for the synthesis of hydantoins and cyclic ureas via the Ugi reaction by Hulme, Christopher, Ma, Liang, Romano, Joseph J, Morton, George, Tang, Sheng-Yuh, Cherrier, Marie-Pierre, Choi, Steve, Salvino, Joseph, Labaudiniere, Richard

“…This communication reveals novel applications of the CO 2/MeOH reagent combination coupled with the UDC (Ugi/DeBOC/Cyclize) strategy. The Ugi five component…”
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Mechanism of Action and Clinical Application of Tafamidis in Hereditary Transthyretin Amyloidosis by Coelho, Teresa, Merlini, Giampaolo, Bulawa, Christine E., Fleming, James A., Judge, Daniel P., Kelly, Jeffery W., Maurer, Mathew S., Planté-Bordeneuve, Violaine, Labaudinière, Richard, Mundayat, Rajiv, Riley, Steve, Lombardo, Ilise, Huertas, Pedro

“…Transthyretin (TTR) transports the retinol-binding protein–vitamin A complex and is a minor transporter of thyroxine in blood. Its tetrameric structure…”
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