Syntheses of 1-substituted-3-aminopyrazoles
Ji, Nan, Meredith, Erik, Liu, Donglei, Adams, Christopher M., Artman, Gerald D., Jendza, Keith C., Ma, Fupeng, Mainolfi, Nello, Powers, James J., Zhang, Chun
Published in Tetrahedron letters (29.12.2010)
Published in Tetrahedron letters (29.12.2010)
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Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases
Mainolfi, Nello, Ehara, Takeru, Karki, Rajeshri G., Anderson, Karen, Mac Sweeney, Aengus, Liao, Sha-Mei, Argikar, Upendra A., Jendza, Keith, Zhang, Chun, Powers, James, Klosowski, Daniel W., Crowley, Maura, Kawanami, Toshio, Ding, Jian, April, Myriam, Forster, Cornelia, Serrano-Wu, Michael, Capparelli, Michael, Ramqaj, Rrezarta, Solovay, Catherine, Cumin, Frederic, Smith, Thomas M., Ferrara, Luciana, Lee, Wendy, Long, Debby, Prentiss, Melissa, De Erkenez, Andrea, Yang, Louis, Liu, Fang, Sellner, Holger, Sirockin, Finton, Valeur, Eric, Erbel, Paulus, Ostermeier, Daniela, Ramage, Paul, Gerhartz, Bernd, Schubart, Anna, Flohr, Stefanie, Gradoux, Nathalie, Feifel, Roland, Vogg, Barbara, Wiesmann, Christian, Maibaum, Juergen, Eder, Joerg, Sedrani, Richard, Harrison, Richard A., Mogi, Muneto, Jaffee, Bruce D., Adams, Christopher M.
Published in Journal of medicinal chemistry (11.06.2020)
Published in Journal of medicinal chemistry (11.06.2020)
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The Discovery of N‑(1-Methyl-5-(trifluoromethyl)‑1H‑pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)‑1H‑indole-1-carboxamide (Acrizanib), a VEGFR‑2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration
Adams, Christopher M, Anderson, Karen, Artman, Gerald, Bizec, Jean-Claude, Cepeda, Rosemarie, Elliott, Jason, Fassbender, Elizabeth, Ghosh, Malay, Hanks, Shawn, Hardegger, Leo A, Hosagrahara, Vinayak P, Jaffee, Bruce, Jendza, Keith, Ji, Nan, Johnson, Leland, Lee, Wendy, Liu, Donglei, Liu, Fang, Long, Debby, Ma, Fupeng, Mainolfi, Nello, Meredith, Erik L, Miranda, Karl, Peng, Yao, Poor, Stephen, Powers, James, Qiu, Yubin, Rao, Chang, Shen, Siyuan, Sivak, Jeremy M, Solovay, Catherine, Tarsa, Peter, Woolfenden, Amber, Zhang, Chun, Zhang, Yiqin
Published in Journal of medicinal chemistry (22.02.2018)
Published in Journal of medicinal chemistry (22.02.2018)
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A small-molecule inhibitor of C5 complement protein
Jendza, Keith, Kato, Mitsunori, Salcius, Michael, Srinivas, Honnappa, De Erkenez, Andrea, Nguyen, Anh, McLaughlin, Doug, Be, Celine, Wiesmann, Christian, Murphy, Jason, Bolduc, Philippe, Mogi, Muneto, Duca, Jose, Namil, Abdel, Capparelli, Michael, Darsigny, Veronique, Meredith, Erik, Tichkule, Ritesh, Ferrara, Luciana, Heyder, Jessica, Liu, Fang, Horton, Patricia A, Romanowski, Michael J, Schirle, Markus, Mainolfi, Nello, Anderson, Karen, Michaud, Gregory A
Published in Nature chemical biology (01.07.2019)
Published in Nature chemical biology (01.07.2019)
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Journal Article
Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway
Karki, Rajeshri G, Powers, James, Mainolfi, Nello, Anderson, Karen, Belanger, David B, Liu, Donglei, Ji, Nan, Jendza, Keith, Gelin, Christine F, Mac Sweeney, Aengus, Solovay, Catherine, Delgado, Omar, Crowley, Maura, Liao, Sha-Mei, Argikar, Upendra A, Flohr, Stefanie, La Bonte, Laura R, Lorthiois, Edwige L, Vulpetti, Anna, Brown, Ann, Long, Debby, Prentiss, Melissa, Gradoux, Nathalie, de Erkenez, Andrea, Cumin, Frederic, Adams, Christopher, Jaffee, Bruce, Mogi, Muneto
Published in Journal of medicinal chemistry (09.05.2019)
Published in Journal of medicinal chemistry (09.05.2019)
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Journal Article
A Reliable Synthesis of 3-Amino-5-Alkyl and 5-Amino-3-Alkyl Isoxazoles
Johnson, Leland, Powers, James, Ma, Fupeng, Jendza, Keith, Wang, Bing, Meredith, Erik, Mainolfi, Nello
Published in Synthesis (Stuttgart) (01.01.2013)
Published in Synthesis (Stuttgart) (01.01.2013)
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Journal Article
Transaminases Provide Key Chiral Building Blocks for the Synthesis of Selective M1/M4 Agonists
Thomson, Christopher G., Boss, Kelly, Calhoun, Amy, Fridrich, Cary, Gardinier, Kevin M., Hall, Edward C., Jendza, Keith, Kirman, Louise, Labbé-Giguere, Nancy, Laumen, Kurt, Qian, Ming, Sanyal, Sanjit, Shultz, Michael D., Snajdrova, Radka, Tan, Kian, Wang, Kate Yaping, Yang, Fan, Gao, Feng, Hong, Tao, Dale, Elena, Kuzmiski, Brent, Ortuno, Danny, Palacios, Daniel S.
Published in ACS medicinal chemistry letters (14.12.2023)
Published in ACS medicinal chemistry letters (14.12.2023)
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Journal Article
Discovery of TD-0212, an Orally Active Dual Pharmacology AT(1) Antagonist and Neprilysin Inhibitor (ARNI)
McKinnell, R. Murray, Fatheree, Paul, Choi, Seok-Ki, Gendron, Roland, Jendza, Keith, Blair, Brooke Olson, Budman, Joe, Hill, Craig M., Hegde, Laxminarayan G., Yu, Cecile, McConn, Donavon, Hegde, Sharath S., Marquess, Daniel G., Klein, Uwe
Published in ACS medicinal chemistry letters (01.01.2019)
Published in ACS medicinal chemistry letters (01.01.2019)
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The Discovery of N -(1-Methyl-5-(trifluoromethyl)-1 H -pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1 H -indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration
Adams, Christopher M., Anderson, Karen, Artman, Gerald, Bizec, Jean-Claude, Cepeda, Rosemarie, Elliott, Jason, Fassbender, Elizabeth, Ghosh, Malay, Hanks, Shawn, Hardegger, Leo A., Hosagrahara, Vinayak P., Jaffee, Bruce, Jendza, Keith, Ji, Nan, Johnson, Leland, Lee, Wendy, Liu, Donglei, Liu, Fang, Long, Debby, Ma, Fupeng, Mainolfi, Nello, Meredith, Erik L., Miranda, Karl, Peng, Yao, Poor, Stephen, Powers, James, Qiu, Yubin, Rao, Chang, Shen, Siyuan, Sivak, Jeremy M., Solovay, Catherine, Tarsa, Peter, Woolfenden, Amber, Zhang, Chun, Zhang, Yiqin
Published in Journal of medicinal chemistry (22.02.2018)
Published in Journal of medicinal chemistry (22.02.2018)
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Journal Article
Discovery of TD-0212, an Orally Active Dual Pharmacology AT 1 Antagonist and Neprilysin Inhibitor (ARNI)
McKinnell, R Murray, Fatheree, Paul, Choi, Seok-Ki, Gendron, Roland, Jendza, Keith, Olson Blair, Brooke, Budman, Joe, Hill, Craig M, Hegde, Laxminarayan G, Yu, Cecile, McConn, Donavon, Hegde, Sharath S, Marquess, Daniel G, Klein, Uwe
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 of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI)
McKinnell, R. Murray, Fatheree, Paul, Choi, Seok-Ki, Gendron, Roland, Jendza, Keith, Olson Blair, Brooke, Budman, Joe, Hill, Craig M, Hegde, Laxminarayan G, Yu, Cecile, McConn, Donavon, Hegde, Sharath S, Marquess, Daniel G, Klein, Uwe
Published in ACS medicinal chemistry letters (10.01.2019)
Published in ACS medicinal chemistry letters (10.01.2019)
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"Cyclopenta[c]pyrrol Negative Allosteric Modulators of NR2B"
WANG, Kate Yaping, GARDINIER, Kevin Matthew, PAN, Yue, HEALY, Mark Patrick, YANG, Fan, JENDZA, Keith
Year of Publication 27.06.2024
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Year of Publication 27.06.2024
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NOVEL CYCLOPENTAL[C]PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B
WANG, Kate Yaping, GARDINIER, Kevin Matthew, PAN, Yue, HEALY, Mark Patrick, YANG, Fan, JENDZA, Keith
Year of Publication 07.02.2024
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Year of Publication 07.02.2024
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NOVEL CYCLOPENTAL[C]PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B
WANG, Kate Yaping, GARDINIER, Kevin Matthew, PAN, Yue, HEALY, Mark Patrick, YANG, Fan, JENDZA, Keith
Year of Publication 07.09.2023
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Year of Publication 07.09.2023
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NOVEL CYCLOPENTA[C]PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B
GARDINIER, KEVIN MATTHEW, HEALY, MARK PATRICK, YANG, FAN, PAN, YUE, WANG, KATE YAPING, JENDZA, KEITH
Year of Publication 29.09.2022
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Year of Publication 29.09.2022
Patent
NOVEL CYCLOPENTAL[C]PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B
WANG, Kate Yaping, GARDINIER, Kevin Matthew, PAN, Yue, HEALY, Mark Patrick, YANG, Fan, JENDZA, Keith
Year of Publication 29.09.2022
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Year of Publication 29.09.2022
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2-AZASPIRO[3.4]OCTANE DERIVATIVES AS M4 AGONISTS
CALHOUN, Amy, GARDINIER, Kevin Matthew, THOMSON, Christopher G, PALACIOS, Daniel Steven, QIAN, Ming, YANG, Fan, JENDZA, Keith, NEEF, James Anthony, WANG, Kate Yaping, CHEN, Xin, LABBE-GIGUERE, Nancy, HALL, Edward Charles, SHULTZ, Michael David
Year of Publication 02.05.2024
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Year of Publication 02.05.2024
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2-azaspiro(3.4)octane derivatives as M4 agonists
CALHOUN, Amy, GARDINIER, Kevin Matthew, NEEF, James, THOMSON, Christopher G, PALACIOS, Daniel Steven, QIAN, Ming, YANG, Fan, JENDZA, Keith, WANG, Kate Yaping, CHEN, Xin, LABBE-GIGUERE, Nancy, HALL, Edward Charles, SHULTZ, Michael David
Year of Publication 18.04.2024
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Year of Publication 18.04.2024
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5-oxa-2-azaspiro(3.4)octane derivatives as M4 agonists
CALHOUN, Amy, GARDINIER, Kevin Matthew, NEEF, James, THOMSON, Christopher G, PALACIOS, Daniel Steven, QIAN, Ming, YANG, Fan, JENDZA, Keith, WANG, Kate Yaping, CHEN, Xin, LABBE-GIGUERE, Nancy, HALL, Edward Charles, SHULTZ, Michael David
Year of Publication 30.11.2023
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Year of Publication 30.11.2023
Patent