Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3‑(5-Fluoro‑1H‑indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate
Crosignani, Stefano, Bingham, Patrick, Bottemanne, Pauline, Cannelle, Hélène, Cauwenberghs, Sandra, Cordonnier, Marie, Dalvie, Deepak, Deroose, Frederik, Feng, Jun Li, Gomes, Bruno, Greasley, Samantha, Kaiser, Stephen E, Kraus, Manfred, Négrerie, Michel, Maegley, Karen, Miller, Nichol, Murray, Brion W, Schneider, Manfred, Soloweij, James, Stewart, Albert E, Tumang, Joseph, Torti, Vince R, Van Den Eynde, Benoit, Wythes, Martin
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
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Journal Article
Inhibition of Tryptophan-Dioxygenase Activity Increases the Antitumor Efficacy of Immune Checkpoint Inhibitors
Schramme, Florence, Crosignani, Stefano, Frederix, Kim, Hoffmann, Delia, Pilotte, Luc, Stroobant, Vincent, Preillon, Julie, Driessens, Gregory, Van den Eynde, Benoit J
Published in Cancer immunology research (01.01.2020)
Published in Cancer immunology research (01.01.2020)
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Journal Article
Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy
Gomes, Bruno, Driessens, Gregory, Bartlett, Derek, Cai, Danying, Cauwenberghs, Sandra, Crosignani, Stefano, Dalvie, Deepak, Denies, Sofie, Dillon, Christopher P, Fantin, Valeria R, Guo, Jie, Letellier, Marie-Claire, Li, Wenlin, Maegley, Karen, Marillier, Reece, Miller, Nichol, Pirson, Romain, Rabolli, Virginie, Ray, Chad, Streiner, Nicole, Torti, Vince R, Tsaparikos, Konstantinos, Van den Eynde, Benoit J, Wythes, Martin, Yao, Li-Chin, Zheng, Xianxian, Tumang, Joseph, Kraus, Manfred
Published in Molecular cancer therapeutics (01.12.2018)
Published in Molecular cancer therapeutics (01.12.2018)
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Journal Article
Discovery of a New Class of Potent, Selective, and Orally Bioavailable CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases
Crosignani, Stefano, Page, Patrick, Missotten, Marc, Colovray, Véronique, Cleva, Christophe, Arrighi, Jean-François, Atherall, John, Macritchie, Jackie, Martin, Thierry, Humbert, Yves, Gaudet, Marilène, Pupowicz, Doris, Maio, Maurizio, Pittet, Pierre-André, Golzio, Lucia, Giachetti, Claudio, Rocha, Cynthia, Bernardinelli, Gérald, Filinchuk, Yaroslav, Scheer, Alexander, Schwarz, Matthias K, Chollet, André
Published in Journal of medicinal chemistry (10.04.2008)
Published in Journal of medicinal chemistry (10.04.2008)
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Journal Article
Optimization of the Central Core of Indolinone–Acetic Acid-Based CRTH2 (DP2) Receptor Antagonists
Crosignani, Stefano, Jorand-Lebrun, Catherine, Page, Patrick, Campbell, Gordon, Colovray, Véronique, Missotten, Marc, Humbert, Yves, Cleva, Christophe, Arrighi, Jean-François, Gaudet, Marilène, Johnson, Zoe, Ferro, Pamela, Chollet, André
Published in ACS medicinal chemistry letters (11.08.2011)
Published in ACS medicinal chemistry letters (11.08.2011)
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Journal Article
Discovery of Potent, Selective, and Orally Bioavailable Alkynylphenoxyacetic Acid CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases
Crosignani, Stefano, Prêtre, Adeline, Jorand-Lebrun, Catherine, Fraboulet, Gaële, Seenisamy, Jeyaprakashnarayanan, Augustine, John Kallikat, Missotten, Marc, Humbert, Yves, Cleva, Christophe, Abla, Nada, Daff, Hamina, Schott, Olivier, Schneider, Manfred, Burgat-Charvillon, Fabienne, Rivron, Delphine, Hamernig, Ingrid, Arrighi, Jean-François, Gaudet, Marilène, Zimmerli, Simone C, Juillard, Pierre, Johnson, Zoe
Published in Journal of medicinal chemistry (27.10.2011)
Published in Journal of medicinal chemistry (27.10.2011)
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Journal Article
Discovery of a novel series of CXCR3 antagonists
Crosignani, Stefano, Missotten, Marc, Cleva, Christophe, Dondi, Ruggero, Ratinaud, Yann, Humbert, Yves, Mandal, Ashis Baran, Bombrun, Agnès, Power, Christine, Chollet, André, Proudfoot, Amanda
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
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Journal Article
A practical synthesis of a high-loading solid-supported IBX amide for the oxidation of alcohols
Lecarpentier, Patrick, Crosignani, Stefano, Linclau, Bruno
Published in Molecular diversity (01.11.2005)
Published in Molecular diversity (01.11.2005)
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Journal Article
Chiral amplification in Diels-Alder and 1,3-dipolar cycloadditions catalyzed by bis(oxazoline)-Zn(II)-based chiral complexes
Crosignani, Stefano, Desimoni, Giovanni, Faita, Giuseppe, Filippone, Salvatore, Mortoni, Annalisa, Righetti, PierPaolo, Zema, Michele
Published in Tetrahedron letters (17.09.1999)
Published in Tetrahedron letters (17.09.1999)
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Journal Article
Abstract 4154: EOS100850 inhibits A2A receptor signaling in human whole blood: Two pharmacodynamic assays to monitor EOS100850 activity in clinical studies
Martinoli, Chiara, Brouwer, Margreet, Houthuys, Erica, Mercier, Marjorie, Wald, Noemie, Gomes, Bruno, Crosignani, Stefano, Bodo, Veronique
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Discovery of a novel series of selective macrocyclic PKCTheta inhibitors
Crosignani, Stefano, Campos, Sebastien, Bouix-Peter, Claire, Harris, Craig, Talbot, Eric, Hu, Haiyang, Wang, Shun, Maclean, John, Zanelli, Ugo, Taylor, Simon, Foote, Kevin, Hacini-Rachinel, Feriel, Nicodeme, Edwige, Julia, Valerie
Published in Bioorganic & medicinal chemistry letters (01.03.2024)
Published in Bioorganic & medicinal chemistry letters (01.03.2024)
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Journal Article
Abstract 4149: Extensive characterization of the adenosine pathway in human solid tumors gives a hint on cancer indication selection for the A2A receptor antagonist EOS100850
Wald, Noemie, Martinoli, Chiara, Mercier, Marjorie, Hermant, Annelise, Nyawouame, Florence, Marchante, Joao, Moulin, Charlotte, Bol, Vanesa, Crosignani, Stefano, Bodo, Veronique
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i)
Klein, Markus, Busch, Michael, Friese-Hamim, Manja, Crosignani, Stefano, Fuchss, Thomas, Musil, Djordje, Rohdich, Felix, Sanderson, Michael P, Seenisamy, Jeyaprakashnarayanan, Walter-Bausch, Gina, Zanelli, Ugo, Hewitt, Philip, Esdar, Christina, Schadt, Oliver
Published in Journal of medicinal chemistry (22.07.2021)
Published in Journal of medicinal chemistry (22.07.2021)
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Journal Article
암의 치료를 위한 ENT 저해제로서의 거대환식 다이아민 유도체 및 이와 아데노신 수용체 길항제와의 조합물
CROSIGNANI STEFANO, HOUTHUYS ERICA JOKE KATELIJNE HELEEN, DELIGNY MICHAEL
Year of Publication 12.01.2023
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Year of Publication 12.01.2023
Patent
Abstract 3261: EOS100850, a non-brain penetrant highly selective A2Areceptor antagonist, uniquely maintains high potency within the adenosine rich tumor microenvironment
Houthuys, Erica, Basilico, Paola, Brouwer, Margreet, Deregnaucourt, Theo, Detheux, Michel, Driessens, Gregory, Gomes, Bruno, Leroy, Xavier, Marchante, Joao, Marillier, Reece, Swiercz, Jakub, Crosignani, Stefano
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Abstract 4147: EOS100850, an A2Areceptor antagonist with prolonged pharmacodynamic activity, mediates the generation ofspecific durable immune responses in a murine breast cancer model
Pirson, Romain, Michaux, Anne-Catherine, Jamart, Diane, Preillon, Julie, Frederix, Kim, Basilico, Paola, Martinoli, Chiara, Leroy, Xavier, Driessens, Gregory, Houthuys, Erica, Chappel, Scott, Crosignani, Stefano, Marillier, Reece
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Novel Application of α-Azido Aldehydes in Multicomponent Reactions: Synthesis of Triazolo-Fused Dihydrooxazinones via a Passerini Reaction–Dipolar Cycloaddition Strategy
De Moliner, Fabio, Crosignani, Stefano, Galatini, Andrea, Riva, Renata, Basso, Andrea
Published in ACS combinatorial science (12.09.2011)
Published in ACS combinatorial science (12.09.2011)
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Journal Article