Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis
Himmelbauer, Martin K., Bajrami, Bekim, Basile, Rebecca, Capacci, Andrew, Chen, TeYu, Choi, Colin K., Gilfillan, Rab, Gonzalez-Lopez de Turiso, Felix, Gu, Chungang, Hoemberger, Marc, Johnson, Douglas S., Jones, J. Howard, Kadakia, Ekta, Kirkland, Melissa, Lin, Edward Y., Liu, Ying, Ma, Bin, Magee, Tom, Mantena, Srinivasa, Marx, Isaac E., Metrick, Claire M., Mingueneau, Michael, Murugan, Paramasivam, Muste, Cathy A., Nadella, Prasad, Nevalainen, Marta, Parker Harp, Chelsea R., Pattaropong, Vatee, Pietrasiewicz, Alicia, Prince, Robin J., Purgett, Thomas J., Santoro, Joseph C., Schulz, Jurgen, Sciabola, Simone, Tang, Hao, Vandeveer, H. George, Wang, Ti, Yousaf, Zain, Helal, Christopher J., Hopkins, Brian T.
Published in Journal of medicinal chemistry (23.05.2024)
Published in Journal of medicinal chemistry (23.05.2024)
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Journal Article
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity
Graceffa, Russell F, Boezio, Alessandro A, Able, Jessica, Altmann, Steven, Berry, Loren M, Boezio, Christiane, Butler, John R, Chu-Moyer, Margaret, Cooke, Melanie, DiMauro, Erin F, Dineen, Thomas A, Feric Bojic, Elma, Foti, Robert S, Fremeau, Robert T, Guzman-Perez, Angel, Gao, Hua, Gunaydin, Hakan, Huang, Hongbing, Huang, Liyue, Ilch, Christopher, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Milgram, Benjamin C, Lin, Min-Hwa Jasmine, Marx, Isaac E, Nguyen, Hanh N, Peterson, Emily A, Rescourio, Gwen, Roberts, John, Schenkel, Laurie, Shimanovich, Roman, Sparling, Brian A, Stellwagen, John, Taborn, Kristin, Vaida, Karina R, Wang, Jean, Yeoman, John, Yu, Violeta, Zhu, Dawn, Moyer, Bryan D, Weiss, Matthew M
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Inhibitors of β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE1): Identification of (S)‑7-(2-Fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5′H‑spiro[chromeno[2,3‑b]pyridine-5,4′-oxazol]-2′-amine (AMG-8718)
Dineen, Thomas A, Chen, Kui, Cheng, Alan C, Derakhchan, Katayoun, Epstein, Oleg, Esmay, Joel, Hickman, Dean, Kreiman, Chuck E, Marx, Isaac E, Wahl, Robert C, Wen, Paul H, Weiss, Matthew M, Whittington, Douglas A, Wood, Stephen, Fremeau, Robert T, White, Ryan D, Patel, Vinod F
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
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Journal Article
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities
Weiss, Matthew M, Dineen, Thomas A, Marx, Isaac E, Altmann, Steven, Boezio, Alessandro, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Feric Bojic, Elma, Foti, Robert S, Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Huang, Hongbing, Huang, Liyue, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, Ligutti, Joseph, La, Daniel S, Lin, Min-Hwa Jasmine, Liu, Dong, Moyer, Bryan D, Nguyen, Hanh N, Peterson, Emily A, Rose, Paul E, Taborn, Kristin, Youngblood, Beth D, Yu, Violeta, Fremeau, Robert T
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Lead Optimization and Modulation of hERG Activity in a Series of Aminooxazoline Xanthene β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors
Epstein, Oleg, Bryan, Marian C, Cheng, Alan C, Derakhchan, Katayoun, Dineen, Thomas A, Hickman, Dean, Hua, Zihao, Human, Jason B, Kreiman, Charles, Marx, Isaac E, Weiss, Matthew M, Wahl, Robert C, Wen, Paul H, Whittington, Douglas A, Wood, Stephen, Zheng, Xiao Mei, Fremeau, Robert T, White, Ryan D, Patel, Vinod F
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
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Journal Article
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement
Marx, Isaac E, Dineen, Thomas A, Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Du, Bingfan, Foti, Robert S, Fremeau, Robert T, Gao, Hua, Gunaydin, Hakan, Hall, Brian E, Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S, Moyer, Bryan D, Peterson, Emily A, Roberts, Jonathan T, Rose, Paul, Wang, Jean, Youngblood, Beth D, Yu, Violeta, Weiss, Matthew M
Published in ACS medicinal chemistry letters (08.12.2016)
Published in ACS medicinal chemistry letters (08.12.2016)
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Journal Article
Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities
Weiss, Matthew M, Dineen, Thomas A, Marx, Isaac E, Altmann, Steven, Boezio, Alessandro, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Feric Bojic, Elma, Foti, Robert S, Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Huang, Hongbing, Huang, Liyue, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, Ligutti, Joseph, La, Daniel S, Lin, Min-Hwa Jasmine, Liu, Dong, Moyer, Bryan D, Nguyen, Hanh N, Peterson, Emily A, Rose, Paul E, Taborn, Kristin, Youngblood, Beth D, Yu, Violeta, Fremeau, Jr, Robert T
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity
Graceffa, Russell F, Boezio, Alessandro A, Able, Jessica, Altmann, Steven, Berry, Loren M, Boezio, Christiane, Butler, John R, Chu-Moyer, Margaret, Cooke, Melanie, DiMauro, Erin F, Dineen, Thomas A, Feric Bojic, Elma, Foti, Robert S, Fremeau, Jr, Robert T, Guzman-Perez, Angel, Gao, Hua, Gunaydin, Hakan, Huang, Hongbing, Huang, Liyue, Ilch, Christopher, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Milgram, Benjamin C, Lin, Min-Hwa Jasmine, Marx, Isaac E, Nguyen, Hanh N, Peterson, Emily A, Rescourio, Gwen, Roberts, John, Schenkel, Laurie, Shimanovich, Roman, Sparling, Brian A, Stellwagen, John, Taborn, Kristin, Vaida, Karina R, Wang, Jean, Yeoman, John, Yu, Violeta, Zhu, Dawn, Moyer, Bryan D, Weiss, Matthew M
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement
Marx, Isaac E, Dineen, Thomas A, Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Du, Bingfan, Foti, Robert S, Fremeau, Jr, Robert T, Gao, Hua, Gunaydin, Hakan, Hall, Brian E, Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S, Moyer, Bryan D, Peterson, Emily A, Roberts, Jonathan T, Rose, Paul, Wang, Jean, Youngblood, Beth D, Yu, Violeta, Weiss, Matthew M
Published in ACS medicinal chemistry letters (08.12.2016)
Published in ACS medicinal chemistry letters (08.12.2016)
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Journal Article
Correction to “Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement”
Marx, Isaac E, Dineen, Thomas A, Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Du, Bingfan, Foti, Robert S, Fremeau, Robert T, Gao, Hua, Gunaydin, Hakan, Hall, Brian E, Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S, Moyer, Bryan D, Nguyen, Hanh N, Peterson, Emily A, Roberts, Jonathan T, Rose, Paul, Wang, Jean, Youngblood, Beth D, Yu, Violeta, Weiss, Matthew M
Published in ACS medicinal chemistry letters (09.03.2017)
Published in ACS medicinal chemistry letters (09.03.2017)
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Journal Article
Correction to "Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement"
Marx, Isaac E, Dineen, Thomas A, Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Du, Bingfan, Foti, Robert S, Fremeau, Jr, Robert T, Gao, Hua, Gunaydin, Hakan, Hall, Brian E, Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S, Moyer, Bryan D, Nguyen, Hanh N, Peterson, Emily A, Roberts, Jonathan T, Rose, Paul, Wang, Jean, Youngblood, Beth D, Yu, Violeta, Weiss, Matthew M
Published in ACS medicinal chemistry letters (09.03.2017)
Published in ACS medicinal chemistry letters (09.03.2017)
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Journal Article
Discovery of α-amidosulfones as potent and selective agonists of CB2 : Synthesis, SAR, and pharmacokinetic properties
MARX, Isaac E, DIMAURO, Erin F, MARTIN, Matthew W, WHITE, Ryan D, FREMEAU, Robert T, PATEL, Vinod F, CHENG, Alan, EMKEY, Renee, HITCHCOCK, Stephen A, LIYUE HUANG, HUANG, Ming Y, HUMAN, Jason, LEE, Josie H, XINGWEN LI
Published in Bioorganic & medicinal chemistry letters (2009)
Published in Bioorganic & medicinal chemistry letters (2009)
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Journal Article
비시클릭 케톤 술폰아마이드 화합물
MILGRAM BENJAMIN C, STELLWAGEN JOHN, GUZMAN PEREZ ANGEL, WEISS MATTHEW, BOEZIO ALESSANDRO, MARX ISAAC E, DINEEN THOMAS
Year of Publication 06.12.2017
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Year of Publication 06.12.2017
Patent
Sulfonamides as Selective Na(V)1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities
Weiss, Matthew M., Dineen, Thomas A., Marx, Isaac E., Altmann, Steven, Boezio, Alessandro, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F., Bojic, Elma Feric, Foti, Robert S., Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Huang, Hongbing, Huang, Liyue, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R., Ligutti, Joseph, La, Daniel S., Lin, Min-Hwa Jasmine, Liu, Dong, Moyer, Bryan D., Nguyen, Hanh N., Peterson, Emily A., Rose, Paul E., Taborn, Kristin, Youngblood, Beth D., Yu, Violeta, Fremeau, Robert T.
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Sulfonamides as Selective Na(v)1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement
Marx, Isaac E., Dineen, Thomas A., Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F., Du, Bingfan, Foti, Robert S., Fremeau, Robert T., Gao, Hua, Gunaydin, Hakan, Hall, Brian E., Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R., La, Daniel S., Ligutti, Joseph, Ling, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S., Moyer, Bryan D., Peterson, Emily A., Roberts, Jonathan T., Rose, Paul, Wang, Jean, Youngblood, Beth D., Yu, Violeta, Weiss, Matthew M.
Published in ACS medicinal chemistry letters (01.12.2016)
Published in ACS medicinal chemistry letters (01.12.2016)
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Journal Article
Discovery of alpha -amidosulfones as potent and selective agonists of CB sub(2): Synthesis, SAR, and pharmacokinetic properties
Marx, Isaac E, DiMauro, Erin F, Cheng, Alan, Emkey, Renee, Hitchcock, Stephen A, Huang, Liyue, Huang, Ming Y, Human, Jason, Lee, Josie H, Li, Xingwen, Martin, Matthew W, White, Ryan D, Fremeau, Robert T, Patel, Vinod F
Published in Bioorganic & medicinal chemistry letters (01.01.2009)
Published in Bioorganic & medicinal chemistry letters (01.01.2009)
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Journal Article
Discovery of α-amidosulfones as potent and selective agonists of CB 2: Synthesis, SAR, and pharmacokinetic properties
Marx, Isaac E., DiMauro, Erin F., Cheng, Alan, Emkey, Renee, Hitchcock, Stephen A., Huang, Liyue, Huang, Ming Y., Human, Jason, Lee, Josie H., Li, Xingwen, Martin, Matthew W., White, Ryan D., Fremeau, Robert T., Patel, Vinod F.
Published in Bioorganic & medicinal chemistry letters (2009)
Published in Bioorganic & medicinal chemistry letters (2009)
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Journal Article