Search Results - "HALLEY, Frank"

Differential Water Thermodynamics Determine PI3K-Beta/Delta Selectivity for Solvent-Exposed Ligand Modifications by Robinson, Daniel, Bertrand, Thomas, Carry, Jean-Christophe, Halley, Frank, Karlsson, Andreas, Mathieu, Magali, Minoux, Hervé, Perrin, Marc-Antoine, Robert, Benoit, Schio, Laurent, Sherman, Woody

“…Phosphoinositide 3-kinases (PI3Ks) are involved in important cellular functions and represent desirable targets for drug discovery efforts, especially related…”
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Preparation and optimization of pyrazolo[1,5-a]pyrimidines as new potent PDE4 inhibitors by Le Roux, Jacques, Leriche, Caroline, Chamiot-Clerc, Philippe, Feutrill, John, Halley, Frank, Papin, David, Derimay, Nathalie, Mugler, Christelle, Grépin, Claudine, Schio, Laurent

“…[Display omitted] A new series of pyrazolo[1,5-a]pyrimidines exemplified by compound 1, has been identified with moderate activity (IC50=165nM), following…”
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SAR439859, a Novel Selective Estrogen Receptor Degrader (SERD), Demonstrates Effective and Broad Antitumor Activity in Wild-Type and Mutant ER-Positive Breast Cancer Models by Shomali, Maysoun, Cheng, Jane, Sun, Fangxian, Koundinya, Malvika, Guo, Zhuyan, Hebert, Andrew T, McManus, Jessica, Levit, Mikhail N, Hoffmann, Dietmar, Courjaud, Albane, Arrebola, Rosalia, Cao, Hui, Pollard, Jack, Lee, Joon Sang, Besret, Laurent, Caron, Anne, Bangari, Dinesh S, Abecassis, Pierre-Yves, Schio, Laurent, El-Ahmad, Youssef, Halley, Frank, Tabart, Michel, Certal, Victor, Thompson, Fabienne, McCort, Gary, Filoche-Rommé, Bruno, Cheng, Hong, Garcia-Echeverria, Carlos, Debussche, Laurent, Bouaboula, Monsif

“…Primary treatment for estrogen receptor-positive (ER+) breast cancer is endocrine therapy. However, substantial evidence indicates a continued role for ER…”
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Discovery of 6‑(2,4-Dichlorophenyl)-5-[4-[(3S)‑1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro‑7H‑benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer by El-Ahmad, Youssef, Tabart, Michel, Halley, Frank, Certal, Victor, Thompson, Fabienne, Filoche-Rommé, Bruno, Gruss-Leleu, Florence, Muller, Claire, Brollo, Maurice, Fabien, Laurence, Loyau, Véronique, Bertin, Luc, Richepin, Patrick, Pilorge, Fabienne, Desmazeau, Pascal, Girardet, Chrystelle, Beccari, Sylvie, Louboutin, Audrey, Lebourg, Gilles, Le-Roux, Jacques, Terrier, Corinne, Vallée, François, Steier, Valérie, Mathieu, Magali, Rak, Alexey, Abecassis, Pierre-Yves, Vicat, Pascale, Benard, Tsiala, Bouaboula, Monsif, Sun, Fangxian, Shomali, Maysoun, Hebert, Andrew, Levit, Mikhail, Cheng, Hong, Courjaud, Albane, Ginesty, Celine, Perrault, Christelle, Garcia-Echeverria, Carlos, McCort, Gary, Schio, Laurent

“…More than 75% of breast cancers are estrogen receptor alpha (ERα) positive (ER+), and resistance to current hormone therapies occurs in one-third of ER+…”
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Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3 S )-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7 H -benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer by El-Ahmad, Youssef, Tabart, Michel, Halley, Frank, Certal, Victor, Thompson, Fabienne, Filoche-Rommé, Bruno, Gruss-Leleu, Florence, Muller, Claire, Brollo, Maurice, Fabien, Laurence, Loyau, Véronique, Bertin, Luc, Richepin, Patrick, Pilorge, Fabienne, Desmazeau, Pascal, Girardet, Chrystelle, Beccari, Sylvie, Louboutin, Audrey, Lebourg, Gilles, Le-Roux, Jacques, Terrier, Corinne, Vallée, François, Steier, Valérie, Mathieu, Magali, Rak, Alexey, Abecassis, Pierre-Yves, Vicat, Pascale, Benard, Tsiala, Bouaboula, Monsif, Sun, Fangxian, Shomali, Maysoun, Hebert, Andrew, Levit, Mikhail, Cheng, Hong, Courjaud, Albane, Ginesty, Celine, Perrault, Christelle, Garcia-Echeverria, Carlos, McCort, Gary, Schio, Laurent

“…More than 75% of breast cancers are estrogen receptor alpha (ERα) positive (ER+), and resistance to current hormone therapies occurs in one-third of ER+…”
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Discovery and Optimization of Pyrimidone Indoline Amide PI3Kβ Inhibitors for the Treatment of Phosphatase and Tensin Homologue (PTEN)-Deficient Cancers by Certal, Victor, Carry, Jean-Christophe, Halley, Frank, Virone-Oddos, Angela, Thompson, Fabienne, Filoche-Rommé, Bruno, El-Ahmad, Youssef, Karlsson, Andreas, Charrier, Véronique, Delorme, Cécile, Rak, Alexey, Abecassis, Pierre-Yves, Amara, Céline, Vincent, Loïc, Bonnevaux, Hélène, Nicolas, Jean-Paul, Mathieu, Magali, Bertrand, Thomas, Marquette, Jean-Pierre, Michot, Nadine, Benard, Tsiala, Perrin, Marc-Antoine, Lemaitre, Olivier, Guerif, Stephane, Perron, Sébastien, Monget, Sylvie, Gruss-Leleu, Florence, Doerflinger, Gilles, Guizani, Houlfa, Brollo, Maurice, Delbarre, Laurence, Bertin, Luc, Richepin, Patrick, Loyau, Véronique, Garcia-Echeverria, Carlos, Lengauer, Christoph, Schio, Laurent

“…Compelling molecular biology publications have reported the implication of phosphoinositide kinase PI3Kβ in PTEN-deficient cell line growth and proliferation…”
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Abstract 943: SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer by Bouaboula, Monsif, Shomali, Maysoun, Cheng, Jane, Malkova, Natalia, Sun, Fangxian, Koundinya, Malvika, Guo, Zhuyan, Poirier, Stephane, Levit, Mikhail, Hoffman, Dietmar, Cao, Hui, Bestret, Laurent, Adrian, Francisco, Winter, Christoph, El-Ahmad, Youssef, Vincent, Sylvie, Halley, Frank, McCort, Gary, Schio, Laurent, Richon, Vicky, Cheng, Hong, Hsu, Karl, Soria, Chris, Cohen, Patrick, Lager, Joanne, Garcia-Echeverria, Carlos, Debussche, Laurent

“…Abstract Despite resistance to endocrine therapies, estrogen receptor-positive (ER+) breast cancers (BC) still rely on ER. Eliminating ER by inducing its…”
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Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/BRAF-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3Kβ-Selective Inhibitor by Bonnevaux, Hélène, Lemaitre, Olivier, Vincent, Loic, Levit, Mikhail N, Windenberger, Fanny, Halley, Frank, Delorme, Cécile, Lengauer, Christoph, Garcia-Echeverria, Carlos, Virone-Oddos, Angela

“…Class IA PI3K pathway activation resulting from PTEN deficiency has been associated with lack of sensitivity of melanoma to BRAF kinase inhibitors. Although…”
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Discovery and Optimization of New Benzimidazole- and Benzoxazole-Pyrimidone Selective PI3Kβ Inhibitors for the Treatment of Phosphatase and TENsin homologue (PTEN)-Deficient Cancers by Certal, Victor, Halley, Frank, Virone-Oddos, Angela, Delorme, Cécile, Karlsson, Andreas, Rak, Alexey, Thompson, Fabienne, Filoche-Rommé, Bruno, El-Ahmad, Youssef, Carry, Jean-Christophe, Abecassis, Pierre-Yves, Lejeune, Pascale, Vincent, Loic, Bonnevaux, Hélène, Nicolas, Jean-Paul, Bertrand, Thomas, Marquette, Jean-Pierre, Michot, Nadine, Benard, Tsiala, Below, Peter, Vade, Isabelle, Chatreaux, Fabienne, Lebourg, Gilles, Pilorge, Fabienne, Angouillant-Boniface, Odile, Louboutin, Audrey, Lengauer, Christoph, Schio, Laurent

“…Most of the phosphoinositide-3 kinase (PI3K) kinase inhibitors currently in clinical trials for cancer treatment exhibit pan PI3K isoform profiles. Single PI3K…”
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Abstract 5775: Identification of SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that has strong anti-tumor activity in wild-type and mutant ER+ breast cancer models by Shomali, Maysoun, El-Ahmad, Youssef, Halley, Frank, Cheng, Jane, Weinstein, Michael, Wang, Muchun, Sun, Fangxian, Malkova, Natalia, Levit, Mikhail, Koundinya, Malvika, Gou, Zhuyan, Hebert, Andrew, McManus, Jessica, Hoffman, Dietmar, Cao, Hui, Jung, Joonil, Pollard, Jack, Vincent, Sylvie, Ackerson, Timothy, Adrian, Francisco, Winter, Chris, Richon, Victoria, Chen, Hong, Hsu, Karl, Lager, Joanne, Courjaud, Albane, Arrebola, Rosalia, Besret, Laurent, Abecassis, Pierre-Yves, Schio, Laurent, McCort, Gary, Tabart, Michel, Certal, Victor, Thompson, Fabienne, Filoche-Rommé, Bruno, Debussche, Laurent, Cohen, Patrick, Garcia-Echeverria, Carlos, Bouaboula, Monsif

“…Abstract Nearly 70% or more of newly diagnosed cases of breast cancer (BC) are estrogen receptor positive (ER+) where endocrine therapy is a primary treatment…”
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Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kβ inhibitors by Certal, Victor, Halley, Frank, Virone-Oddos, Angela, Thompson, Fabienne, Filoche-Rommé, Bruno, El-Ahmad, Youssef, Carry, Jean-Christophe, Delorme, Cécile, Karlsson, Andreas, Abecassis, Pierre-Yves, Vincent, Loic, Bonnevaux, Hélène, Nicolas, Jean-Paul, Morales, Renaud, Michot, Nadine, Vade, Isabelle, Louboutin, Audrey, Perron, Sébastien, Doerflinger, Gilles, Tric, Bernadette, Monget, Sylvie, Lengauer, Christoph, Schio, Laurent

“…From a HTS campaign, a new series of pyrimidone anilides exemplified by compound 1 has been identified with good inhibitory activity for the PI3Kβ isoform. The…”
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Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kβ inhibitors by Certal, Victor, Halley, Frank, Virone-Oddos, Angela, Filoche-Rommé, Bruno, Carry, Jean-Christophe, Gruss-Leleu, Florence, Bertin, Luc, Guizani, Houlfa, Pilorge, Fabienne, Richepin, Patrick, Karlsson, Andreas, Charrier, Véronique, Abecassis, Pierre-Yves, Vincent, Loic, Nicolas, Jean-Paul, Lengauer, Christoph, Garcia-Echeverria, Carlos, Schio, Laurent

“…In our continuous efforts to identify and develop novel targeted cancer treatments, a new morpholino-thiazole scaffold active against PI3Kβ has been…”
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Rational design of potent GSK3β inhibitors with selectivity for Cdk1 and Cdk2 by Lesuisse, Dominique, Dutruc-Rosset, Gilles, Tiraboschi, Gilles, Dreyer, Matthias K., Maignan, Sébastien, Chevalier, Alain, Halley, Frank, Bertrand, Philippe, Burgevin, Marie-Claude, Quarteronet, Dominique, Rooney, Thomas

“…From an HTS hit, a series of potent and selective inhibitors of GSK3β have been designed based on a Cdk2-homology model and with the help of several crystal…”
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Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3K[beta] inhibitors by Certal, Victor, Halley, Frank, Virone-Oddos, Angela, Thompson, Fabienne, Filoche-Romme, Bruno, El-Ahmad, Youssef, Carry, Jean-Christophe, Delorme, Cecile, Karlsson, Andreas, Abecassis, Pierre-Yves, Vincent, Loic, Bonnevaux, Helene, Nicolas, Jean-Paul, Morales, Renaud, Michot, Nadine, Vade, Isabelle, Louboutin, Audrey, Perron, Sebastien, Doerflinger, Gilles, Tric, Bernadette, Monget, Sylvie, Lengauer, Christoph, Schio, Laurent

“…From a HTS campaign, a new series of pyrimidone anilides exemplified by compound 1 has been identified with good inhibitory activity for the PI3K[beta]…”
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An Algorithm-Directed Two-Component Library Synthesized Via Solid-Phase Methodology Yielding Potent and Orally Bioavailable p38 MAP Kinase Inhibitors by McKenna, Jeffrey M, Halley, Frank, Souness, John E, McLay, Iain M, Pickett, Stephen D, Collis, Alan J, Page, Kenneth, Ahmed, Imtiaz

“…Previously we reported the identification of RPR200765A, a potent orally bioavailable pyridine−imidazole inhibitor of p38 mitogen-activated protein (MAP)…”
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Rational design of potent GSK3b inhibitors with selectivity for Cdk1 and Cdk2 by Lesuisse, Dominique, Dutruc-Rosset, Gilles, Tiraboschi, Gilles, Dreyer, Matthias K, Maignan, Sebastien, Chevalier, Alain, Halley, Frank, Bertrand, Philippe, Burgevin, Marie-Claude, Quarteronet, Dominique, Rooney, Thomas

“…From an HTS hit, a series of potent and selective inhibitors of GSK3b have been designed based on a Cdk2-homology model and with the help of several crystal…”
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Design of potent and selective GSK3β inhibitors with acceptable safety profile and pharmacokinetics by Lesuisse, Dominique, Tiraboschi, Gilles, Krick, Alain, Abecassis, Pierre-Yves, Dutruc-Rosset, Gilles, Babin, Didier, Halley, Frank, Châtreau, Fabienne, Lachaud, Sylvette, Chevalier, Alain, Quarteronet, Dominique, Burgevin, Marie-Claude, Amara, Céline, Bertrand, Philippe, Rooney, Thomas

“…From potent and selective inhibitors of GSK3β displaying CYP1A2 inhibition and poor PK properties mostly linked to metabolic instability and in vivo hydrolysis…”
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Design of potent and selective GSK3b inhibitors with acceptable safety profile and pharmacokinetics by Lesuisse, Dominique, Tiraboschi, Gilles, Krick, Alain, Abecassis, Pierre-Yves, Dutruc-Rosset, Gilles, Babin, Didier, Halley, Frank, Chatreau, Fabienne, Lachaud, Sylvette, Chevalier, Alain, Quarteronet, Dominique, Burgevin, Marie-Claude, Amara, Celine, Bertrand, Philippe, Rooney, Thomas

“…From potent and selective inhibitors of GSK3b displaying CYP1A2 inhibition and poor PK properties, mostly linked to metabolic instability and in vivo…”
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The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy by MCLAY, Lain M, HALLEY, Frank, FOSTER, Martyn, HELE, David, JAYYOSI, Zaid, KELLEY, Mike, MASLEN, Chris, MILLER, Glen, OULDELHKIM, Marie-Claude, PAGE, Kenneth, PHIPPS, Simon, POLLOCK, Kenneth, SOUNESS, John E, PORTER, Barry, RATCLIFFE, Andrew J, REDFORD, Elisabeth J, WEBBER, Stephen, SLATER, Bryan, THYBAUD, Veronique, WILSHER, Nicola, MCKENNA, Jeffrey, BENNING, Veronique, BIRRELL, Mark, BURTON, Brenda, BELVISI, Maria, COLLIS, Alan, CONSTAN, Alex

“…RPR132331, a 2-(2-dioxanyl)imidazole, was identified as an inhibitor of tumour necrosis factor (TNF)alpha release from lipopolysaccharide (LPS)-stimulated…”
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RPR203494 a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency by Collis, Alan J, Foster, Martyn L, Halley, Frank, Maslen, Christopher, McLay, Iain M, Page, Kenneth M, Redford, E.Jane, Souness, John E, Wilsher, Nicola E

“…Following the discovery of RPR200765, a series of pyrimidine analogues have been prepared as backups. Amongst them, RPR203494 was identified with a better in…”
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