Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors
Taylor, Alexander M., Williams, Bret R., Giordanetto, Fabrizio, Kelley, Elizabeth H., Lescarbeau, André, Shortsleeves, Kelley, Tang, Yong, Walters, W. Patrick, Arrazate, Alfonso, Bowman, Christine, Brophy, Erin, Chan, Emily W., Deshmukh, Gauri, Greisman, Jack B., Hunsaker, Thomas L., Kipp, D. Randal, Saenz Lopez-Larrocha, Pablo, Maddalo, Danilo, Martin, Iain J., Maragakis, Paul, Merchant, Mark, Murcko, Mark, Nisonoff, Hunter, Nguyen, Vi, Nguyen, Vy, Orozco, Olivia, Owen, Christopher, Pierce, Levi, Schmidt, Molly, Shaw, David E., Smith, Sherri, Therrien, Eric, Tran, John C., Watters, Jim, Waters, Nigel J., Wilbur, Jeremy, Willmore, Lindsay
Published in Journal of medicinal chemistry (12.10.2023)
Published in Journal of medicinal chemistry (12.10.2023)
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Journal Article
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)‑γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate
Evans, Catherine A, Liu, Tao, Lescarbeau, André, Nair, Somarajan J, Grenier, Louis, Pradeilles, Johan A, Glenadel, Quentin, Tibbitts, Thomas, Rowley, Ann M, DiNitto, Jonathan P, Brophy, Erin E, O’Hearn, Erin L, Ali, Janid A, Winkler, David G, Goldstein, Stanley I, O’Hearn, Patrick, Martin, Christian M, Hoyt, Jennifer G, Soglia, John R, Cheung, Culver, Pink, Melissa M, Proctor, Jennifer L, Palombella, Vito J, Tremblay, Martin R, Castro, Alfredo C
Published in ACS medicinal chemistry letters (08.09.2016)
Published in ACS medicinal chemistry letters (08.09.2016)
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Journal Article
Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2
Schönherr, Heike, Ayaz, Pelin, Taylor, Alexander M, Casaletto, Jessica B, Touré, B Barry, Moustakas, Demetri T, Hudson, Brandi M, Valverde, Roberto, Zhao, Songping, O'Hearn, Patrick J, Foster, Lindsey, Sharon, Dina A, Garfinkle, Sam, Giordanetto, Fabrizio, Lescarbeau, André, Kurukulasuriya, Ravi, Gerami-Moayed, Nastaran, Maglic, Dejan, Bruderek, Kamil, Naik, Gaauri, Gunaydin, Hakan, Mader, Mary M, Boezio, Alessandro A, McLean, Thomas H, Chen, Rongfeng, Wang, Yanxia, Shaw, David E, Watters, James, Bergstrom, Donald A
Published in Proceedings of the National Academy of Sciences - PNAS (06.02.2024)
Published in Proceedings of the National Academy of Sciences - PNAS (06.02.2024)
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Journal Article
Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia
Varkaris, Andreas, Pazolli, Ermira, Gunaydin, Hakan, Wang, Qi, Pierce, Levi, Boezio, Alessandro A, Bulku, Artemisa, DiPietro, Lucian, Fridrich, Cary, Frost, Adam, Giordanetto, Fabrizio, Hamilton, Erika P, Harris, Katherine, Holliday, Michael, Hunter, Tamieka L, Iskandar, Amanda, Ji, Yongli, Larivée, Alexandre, LaRochelle, Jonathan R, Lescarbeau, André, Llambi, Fabien, Lormil, Brenda, Mader, Mary M, Mar, Brenton G, Martin, Iain, McLean, Thomas H, Michelsen, Klaus, Pechersky, Yakov, Puente-Poushnejad, Erika, Raynor, Kevin, Rogala, Dipali, Samadani, Ramin, Schram, Alison M, Shortsleeves, Kelley, Swaminathan, Sweta, Tajmir, Shahein, Tan, Gege, Tang, Yong, Valverde, Roberto, Wehrenberg, Bryan, Wilbur, Jeremy, Williams, Bret R, Zeng, Hongtao, Zhang, Hanmo, Walters, W Patrick, Wolf, Beni B, Shaw, David E, Bergstrom, Donald A, Watters, James, Fraser, James S, Fortin, Pascal D, Kipp, D Randal
Published in Cancer discovery (08.02.2024)
Published in Cancer discovery (08.02.2024)
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Journal Article
Discovery of a Potent and Orally Active Hedgehog Pathway Antagonist (IPI-926)
Tremblay, Martin R, Lescarbeau, André, Grogan, Michael J, Tan, Eddy, Lin, Grace, Austad, Brian C, Yu, Lin-Chen, Behnke, Mark L, Nair, Somarajan J, Hagel, Margit, White, Kerry, Conley, James, Manna, Joseph D, Alvarez-Diez, Teresa M, Hoyt, Jennifer, Woodward, Caroline N, Sydor, Jens R, Pink, Melissa, MacDougall, John, Campbell, Matthew J, Cushing, Jill, Ferguson, Jeanne, Curtis, Michael S, McGovern, Karen, Read, Margaret A, Palombella, Vito J, Adams, Julian, Castro, Alfredo C
Published in Journal of medicinal chemistry (23.07.2009)
Published in Journal of medicinal chemistry (23.07.2009)
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Journal Article
Synthetic Silvestrol Analogues as Potent and Selective Protein Synthesis Inhibitors
Liu, Tao, Nair, Somarajan J, Lescarbeau, André, Belani, Jitendra, Peluso, Stéphane, Conley, James, Tillotson, Bonnie, O’Hearn, Patrick, Smith, Sherri, Slocum, Kelly, West, Kip, Helble, Joseph, Douglas, Mark, Bahadoor, Adilah, Ali, Janid, McGovern, Karen, Fritz, Christian, Palombella, Vito J, Wylie, Andrew, Castro, Alfredo C, Tremblay, Martin R
Published in Journal of medicinal chemistry (25.10.2012)
Published in Journal of medicinal chemistry (25.10.2012)
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Journal Article
Development of a Multi Kilogram-Scale, Tandem Cyclopropanation Ring-Expansion Reaction en Route to Hedgehog Antagonist IPI-926
Austad, Brian C, Hague, Andrew B, White, Priscilla, Peluso, Stéphane, Nair, Somarajan J, Depew, Kristopher M, Grogan, Michael J, Charette, André B, Yu, Lin-Chen, Lory, Caroline D, Grenier, Louis, Lescarbeau, André, Lane, Benjamin S, Lombardy, Richard, Behnke, Mark L, Koney, Nii, Porter, James R, Campbell, Matthew J, Shaffer, Jeanne, Xiong, Jimin, Helble, Joseph C, Foley, Michael A, Adams, Julian, Castro, Alfredo C, Tremblay, Martin R
Published in Organic process research & development (15.04.2016)
Published in Organic process research & development (15.04.2016)
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Journal Article
Abstract P5-16-10: RLY-2608: The first allosteric mutant- and isoform-selective inhibitor of PI3Kα, is efficacious as a single agent and drives regressions in combination with standard of care therapies in PIK3CA mutant breast cancer models
Pazolli, Ermira, Kipp, Randy, Boezio, Alessandro, Gunaydin, Hakan, Iskandar, Amanda, Zubrowski, Matthew, Williams, Bret, Shortsleeves, Kelley, Larivee, Alexandre, McLean, Tom, Michelsen, Klaus, Zeng, Hongtao, LaRochelle, Jonathan, Manna, Joe, DiPietro, Lucian, Lescarbeau, Andre, Mader, Mary, Bennet, Bindu, Wilbur, Jeremy, Wang, Qi, Pierce, Levi, Martin, Iain, Watters, James, Fortin, Pascal, Bergstrom, Donald
Published in Cancer research (Chicago, Ill.) (15.02.2022)
Published in Cancer research (Chicago, Ill.) (15.02.2022)
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Journal Article
FGFR 억제제 및 이의 제조 및 사용 방법
ISAAK ELISABETH, ZHURAKOVSKYI OLEKSANDR, SULEIMAN OSAMA, BEAMISH COOK JETHRO, LESCARBEAU ANDRE, TRINCHERA PIERA, PRENTICE ZOE, DUMAS AARON, KENDALL THOMAS
Year of Publication 21.08.2023
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Year of Publication 21.08.2023
Patent
SHP2 포스파테이스 억제제 및 이의 제조 및 사용 방법
WANG JING, ZHANG YANYAN, TAYLOR ALEXANDER M, LESCARBEAU ANDRE, LIAN GAODENG
Year of Publication 24.05.2022
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Year of Publication 24.05.2022
Patent
PI3K-알파 저해제 그리고 이의 제조 방법 및 사용 방법
WANG XIAOHONG, YIN CHANGBO, HE HONGYAN, CHE QINGLIN, LIN YUAN, CHEN JIAHUI, BOEZIO ALESSANDRO, ZHOU JIAJIA, ZHOU QIUXIANG, LU MIN, ZHOU YUNFEI, GU WEI, SINGH SURENDRA P, JIANG SIYI, LESCARBEAU ANDRE, GONG XIJIAN
Year of Publication 18.07.2024
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Year of Publication 18.07.2024
Patent
CDK 억제제 및 이의 사용 방법
EVANS CATHERINE A, HE JING, FRIDRICH CARY GRIFFIN, KRUEGER ELAINE B, KELLEY BRIAN P, BRIGGS TIMOTHY F, KURUKULASURIYA RAVI, MCLEAN THOMAS H, TAYLOR ALEXANDER M, LESCARBEAU ANDRE, BOEZIO ALESSANDRO, PABON NICOLAS A
Year of Publication 26.12.2023
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Year of Publication 26.12.2023
Patent
A Design of Experiments Approach to a Robust Final Deprotection and Reactive Crystallization of IPI-926, A Novel Hedgehog Pathway Inhibitor
Martinot, Theodore A, Austad, Brian C, Côté, Alexandre, Depew, Kristopher M, Genov, Daniel, Grenier, Louis, Helble, Joseph, Lescarbeau, Andre, Nair, Somarajan, Trudeau, Martin, White, Priscilla, Yu, Lin-Chen
Published in Organic process research & development (20.11.2015)
Published in Organic process research & development (20.11.2015)
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Journal Article
Abstract 3327: Discovery and characterization of the potent, allosteric SHP2 inhibitor GDC-1971 for the treatment of RTK/RAS driven tumors
Williams, Bret, Taylor, Alexander, Orozco, Olivia, Owen, Christopher, Kelley, Elizabeth, Lescarbeau, Andre, Shortsleeves, Kelley, Kipp, Randy, Nguyen, Vy, Brophy, Erin, Wilbur, Jeremy, Tang, Yong, Lanzetta, David, Waters, Nigel, Smith, Sherri, Giordanetto, Fabrizio, Maragakis, Paul, Greismann, Jack, Willmore, Lindsay, Therrien, Eric, Xiao, Yang, Evangelista, Marie, Gerosa, Luca, Lin, Eva, Merchant, Mark, Arrazate, Alfonso, Chan, Emily, Larrocha, Pablo Sáenz-López, Chun, Stefan, Hunsaker, Thomas, Deshmukh, Gauri, Bowman, Christine M., Shaw, David E., Murcko, Mark, Padval, Mahesh, Walters, W Patrick, Watters, James, Bergstrom, Donald A.
Published in Cancer research (Chicago, Ill.) (15.06.2022)
Published in Cancer research (Chicago, Ill.) (15.06.2022)
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Journal Article
SHP2 포스파타제 억제제 및 그의 사용 방법
WALTERS W. PATRICK, GUNAYDIN HAKAN, GIORDANETTO FABRIZIO, KELLEY ELIZABETH H, SHORTSLEEVES KELLEY C, MCLEAN THOMAS H, MURCKO MARK ANDREW, TAYLOR ALEXANDER M, LESCARBEAU ANDRE, THERRIEN ERIC
Year of Publication 10.02.2021
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Year of Publication 10.02.2021
Patent
Abstract A192: The potent and selective phosphoinositide-3-kinase-γ inhibitor, IPI-549, inhibits tumor growth in murine syngeneic solid tumor models through alterations in the immune suppressive microenvironment
McGovern, Karen, Ali, Janid, Brophy, Erin, Castro, Alfredo, DiNitto, Jonathan, Evans, Catherine, Faia, Kerrie, Goldstein, Stanley, Kosmider, Nicole, Lescarbeau, Andre, Liu, Tao, Martin, Christian, Nair, Somarajan, Pink, Melissa, Proctor, Jennifer, Rausch, Matthew, Sharma, Sujata, Soglia, John, Tchaicha, Jeremy, Tremblay, Martin, Villegas, Vivian, White, Kerry, Winkler, David, Palombella, Vito, Kutok, Jeffery
Published in Molecular cancer therapeutics (01.12.2015)
Published in Molecular cancer therapeutics (01.12.2015)
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Journal Article
PI3Kα 억제제 및 이의 사용 방법
WALTERS W. PATRICK, GELOZIA SHORENA, DENINNO MICHAEL PAUL, KURUKULASURIYA RAVI, LEE JESSICA, LEPITRE THOMAS, TAYLOR ALEXANDER M, BOEZIO ALESSANDRO, BURNIE ANDREW J, STURINO CLAUDIO, PIERCE LEVI CHARLES THOMAS, MOHAMED TAREK, THORAT RAKESH, KRUEGER ELAINE B, GIGUERE JEAN BENOIT, RAYNOR KEVIN DAVID, LARIVEE ALEXANDRE, LANDAGARAY ELODIE, CHEN FEI, PAL MOHAN, FRIDRICH CARY GRIFFIN, GUNAYDIN HAKAN, MAERTENS GAETAN, SHORTSLEEVES KELLEY C, MCLEAN THOMAS H, WANG QI, JOBIN DES LAURIERS ANTOINE, DIPIETRO LUCIAN V, PAN YUE, GIORDANETTO FABRIZIO, OUTIN JOHANNE, MADER MARY M, ATIENZA BREN JORDAN, BERTRAND LAPERLE MEGAN, VEMULA NARESH, TANVEER KASHIF, ZHANG HANMO, BOUSQUET YVES, LESCARBEAU ANDRE, TANG YONG, PECHERSKY YAKOV, CHITALE SAMPADA
Year of Publication 15.02.2023
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Year of Publication 15.02.2023
Patent
HETEROCYCLIC COMPOUNDS AND USES THEREOF
EVANS CATHERINE A, JANARDANANNAIR SOMARAJANNAIR, TREMBLAY MARTIN R, CASTRO ALFREDO C, LESCARBEAU ANDRE, LIU TAO
Year of Publication 15.06.2016
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Year of Publication 15.06.2016
Patent
COMPOUNDS FOR PREPARING IMMUNOLOGICAL ADJUVANT
NIU XIANG, WU KUO-MING, FANG FRANCIS G, FOY JAMES E, LESCARBEAU ANDRE, HAWKINS LYNN, LEMELIN CHARLES
Year of Publication 19.03.2015
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Year of Publication 19.03.2015
Patent