Second-Generation Antibacterial Benzimidazole Ureas: Discovery of a Preclinical Candidate with Reduced Metabolic Liability
Grillot, Anne-Laure, Tiran, Arnaud Le, Shannon, Dean, Krueger, Elaine, Liao, Yusheng, O’Dowd, Hardwin, Tang, Qing, Ronkin, Steve, Wang, Tiansheng, Waal, Nathan, Li, Pan, Lauffer, David, Sizensky, Emmanuelle, Tanoury, Jerry, Perola, Emanuele, Grossman, Trudy H, Doyle, Tim, Hanzelka, Brian, Jones, Steven, Dixit, Vaishali, Ewing, Nigel, Liao, Shengkai, Boucher, Brian, Jacobs, Marc, Bennani, Youssef, Charifson, Paul S
Published in Journal of medicinal chemistry (13.11.2014)
Published in Journal of medicinal chemistry (13.11.2014)
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Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3‑Kinase γ (PI3Kγ) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS)
Come, Jon H, Collier, Philip N, Henderson, James A, Pierce, Albert C, Davies, Robert J, Le Tiran, Arnaud, O’Dowd, Hardwin, Bandarage, Upul K, Cao, Jingrong, Deininger, David, Grey, Ron, Krueger, Elaine B, Lowe, Derek B, Liang, Jianglin, Liao, Yusheng, Messersmith, David, Nanthakumar, Suganthi, Sizensky, Emmanuelle, Wang, Jian, Xu, Jinwang, Chin, Elaine Y, Damagnez, Veronique, Doran, John D, Dworakowski, Wojciech, Griffith, James P, Jacobs, Marc D, Khare-Pandit, Suvarna, Mahajan, Sudipta, Moody, Cameron S, Aronov, Alex M
Published in Journal of medicinal chemistry (28.06.2018)
Published in Journal of medicinal chemistry (28.06.2018)
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Abstract 1276: Identification of S65487/VOB560 as a potent and selective intravenous 2nd-generation BCL-2 inhibitor active in wild-type and clinical mutants resistant to Venetoclax
Tiran, Arnaud Le, Claperon, Audrey, Davidson, James, Starck, Jérôme-Benoit, Diguarher, Thierry Le, Chanrion, Maïa, Mistry, Prakash, Wang, Youzhen, Monceau, Elodie, Bernhardt, Fabienne, Rocchetti, Francesca, Lysiak-Auvity, Gaelle, Chen, Ijen, Daniels, Zoe, Pedder, Chris, Fallowfield, Mandy, Henlin, Jean-Michel, Fejes, Imre, Tatai, Janos, Nyerges, Miklos, Durand, Didier, Zarka, Marion, Sanghavi, Sneha, Girard, Anne-Marie, Schoumacher, Marie, Kraus-Berthier, Laurence, Newcombe, Rick, Halilovic, Ensar, Banquet, Sébastien, Rupin, Alain, Maacke, Heiko, Murray, James, Morris, Erick, Hofmann, Francesco, Colland, Frédéric, Geneste, Olivier
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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Design and synthesis of bridged piperidine and piperazine isosteres
Maertens, Gaëtan, Saavedra, Oscar M., Vece, Vito, Reyes, Miguel A. Vilchis, Hocine, Sofiane, Öney, Esat, Goument, Bertrand, Mirguet, Olivier, Le Tiran, Arnaud, Gloanec, Philippe, Hanessian, Stephen
Published in Bioorganic & medicinal chemistry letters (15.08.2018)
Published in Bioorganic & medicinal chemistry letters (15.08.2018)
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Journal Article
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3‑Kinase γ
Collier, Philip N., Messersmith, David, Le Tiran, Arnaud, Bandarage, Upul K., Boucher, Christina, Come, Jon, Cottrell, Kevin M., Damagnez, Veronique, Doran, John D., Griffith, James P., Khare-Pandit, Suvarna, Krueger, Elaine B., Ledeboer, Mark W., Ledford, Brian, Liao, Yusheng, Mahajan, Sudipta, Moody, Cameron S., Roday, Setu, Wang, Tiansheng, Xu, Jinwang, Aronov, Alex M.
Published in Journal of medicinal chemistry (23.07.2015)
Published in Journal of medicinal chemistry (23.07.2015)
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Synthesis of a 6‑Aza-Isoindolinone-Based Inhibitor of Phosphoinositide 3‑Kinase γ via Ruthenium-Catalyzed [2 + 2 + 2] Cyclotrimerization
Collier, Philip N, Panchagnula, Advaita, O’Dowd, Hardwin, Le Tiran, Arnaud, Aronov, Alex M
Published in ACS medicinal chemistry letters (10.01.2019)
Published in ACS medicinal chemistry letters (10.01.2019)
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Journal Article
Discovery and Characterization of a Water-Soluble Prodrug of a Dual Inhibitor of Bacterial DNA Gyrase and Topoisomerase IV
O’Dowd, Hardwin, Shannon, Dean E, Chandupatla, Kishan R, Dixit, Vaishali, Engtrakul, Juntyma J, Ye, Zhengqi, Jones, Steven M, O’Brien, Colleen F, Nicolau, David P, Tessier, Pamela R, Crandon, Jared L, Song, Bin, Macikenas, Dainius, Hanzelka, Brian L, Le Tiran, Arnaud, Bennani, Youssef L, Charifson, Paul S, Grillot, Anne-Laure
Published in ACS medicinal chemistry letters (09.07.2015)
Published in ACS medicinal chemistry letters (09.07.2015)
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Pyrrole compounds, a process for their preparation and pharmaceutical
Le Diguarher, Thierry, Geneste, Olivier, Fejes, Imre, Davidson, James Edward Paul, Nyerges, Miklós, Chen, I-Jen, Starck, Jérôme-Benoît, Le Tiran, Arnaud, De Nanteuil, Guillaume, Murray, James Brooke, Henlin, Jean-Michel, Durand, Didier, Tatai, János, Guillouzic, Anne-Françoise
Year of Publication 13.07.2021
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Year of Publication 13.07.2021
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Indolizine compounds, a process for their preparation and pharmaceutical compositions containing them
Le Diguarher, Thierry, Geneste, Olivier, Davidson, James Edward Paul, De Nanteuil, Guillaume, Murray, James Brooke, Chen, I-Jen, Henlin, Jean-Michel, Starck, Jérôme-Benoît, Le Tiran, Arnaud
Year of Publication 17.09.2019
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Year of Publication 17.09.2019
Patent
Pyrrole compounds, a process for their preparation and pharmaceutical compositions containing them
Le Diguarher, Thierry, Geneste, Olivier, Fejes, Imre, Davidson, James Edward Paul, Nyerges, Miklós, Chen, I-Jen, Starck, Jérôme-Benoît, Le Tiran, Arnaud, De Nanteuil, Guillaume, Murray, James Brooke, Henlin, Jean-Michel, Durand, Didier, Tatai, János, Guillouzic, Anne-Françoise
Year of Publication 23.06.2020
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Year of Publication 23.06.2020
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Isoindoline or isoquinoline compounds, a process for their preparation and pharmaceutical compositions containing them
Geneste, Olivier, Le Diguarher, Thierry, Fejes, Imre, Davidson, James Edward Paul, Kotschy, András, Dodsworth, Mark, Nyerges, Miklós, Chen, I-Jen, Starck, Jérôme-Benoît, Le Tiran, Arnaud, Szlávik, Zoltán, Brough, Paul, De Nanteuil, Guillaume, Murray, James Brooke, Walmsley, Claire, Meissner, Johannes W. G, Henlin, Jean-Michel, Tatai, János, Guillouzic, Anne-Françoise
Year of Publication 08.06.2021
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Year of Publication 08.06.2021
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Indole and pyrrole compounds, a process for their preparation and pharmaceutical compositions containing them
Le Diguarher, Thierry, Geneste, Olivier, Davidson, James Edward Paul, Ray, Stuart, Graham, Christopher John, Chen, I-Jen, Starck, Jérôme-Benoît, Bedford, Simon, Le Tiran, Arnaud, Maddox, Daniel, De Nanteuil, Guillaume, Murray, James Brooke, Walmsley, Claire, Casara, Patrick, Henlin, Jean-Michel
Year of Publication 26.05.2020
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Year of Publication 26.05.2020
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Novel indolizine derivatives useful as bcl-2 inhibitors, method for the production thereof and pharmaceutical compositions containing same
Le Diguarher, Thierry, Geneste, Olivier, Davidson, James Edward Paul, De Nanteuil, Guillaume, Murray, James Brooke, Chen, I-Jen, Henlin, Jean-Michel, Starck, Jérôme-Benoît, Le Tiran, Arnaud
Year of Publication 31.05.2019
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Year of Publication 31.05.2019
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Combination therapy to treat mycobacterium diseases
Le Tiran Arnaud, O'Dowd Hardwin, Bennani Youssef Laafiret, Grillot Anne-Laure, Locher Christopher Phillip, Charifson Paul S, Perola Emanuele
Year of Publication 10.04.2018
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Year of Publication 10.04.2018
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Pyrimidine gyrase and topoisomerase IV inhibitors
O'dowd, Hardwin, Perola, Emanuele, Bennani, Youssef Laafiret, Grillot, Anne-Laure, Charifson, Paul S, Le Tiran, Arnaud
Year of Publication 02.02.2017
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Year of Publication 02.02.2017
Patent
Novel indolizine derivatives, method for the production thereof and pharmaceutical compositions containing same
Le Diguarher, Thierry, Geneste, Olivier, Davidson, James Edward Paul, Starck, Jerome-Benoit, De Nanteuil, Guillaume, Murray, James Brooke, Chen, I-Jen, Henlin, Jean-Michel, Le Tiran, Arnaud
Year of Publication 04.10.2018
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Year of Publication 04.10.2018
Patent
New indole and pyrrole derivatives useful as bcl-2 inhibitors, a process for their preparation and pharmaceutical compositions containing them
Le Diguarher, Thierry, Geneste, Olivier, Davidson, James Edward Paul, Ray, Stuart, Graham, Christopher John, Chen, I-Jen, Starck, Jérôme-Benoît, Bedford, Simon, Le Tiran, Arnaud, Maddox, Daniel, De Nanteuil, Guillaume, Murray, James Brooke, Walmsley, Claire, Casara, Patrick, Henlin, Jean-Michel
Year of Publication 28.06.2019
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Year of Publication 28.06.2019
Patent
Isoindoline or isoquinoline compounds, a process for their preparation and pharmaceutical compositions containing them
Geneste, Olivier, Le Diguarher, Thierry, Fejes, Imre, Davidson, James Edward Paul, Kotschy, András, Dodsworth, Mark, Nyerges, Miklós, Chen, I-Jen, Starck, Jérôme-Benoît, Le Tiran, Arnaud, Szlávik, Zoltán, Brough, Paul, De Nanteuil, Guillaume, Murray, James Brooke, Walmsley, Claire, Meissner, Johannes W. G, Henlin, Jean-Michel, Tatai, János, Guillouzic, Anne-Françoise
Year of Publication 23.06.2020
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Year of Publication 23.06.2020
Patent
COMBINATION THERAPY TO TREAT MYCOBACTERIUM DISEASES
Le Tiran Arnaud, O'Dowd Hardwin, Bennani Youssef Laafiret, Grillot Anne-Laure, Locher Christopher Phillip, Charifson Paul S, Perola Emanuele
Year of Publication 11.05.2017
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Year of Publication 11.05.2017
Patent