Bruton's tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care
Gillooly, Kathleen M, Pulicicchio, Claudine, Pattoli, Mark A, Cheng, Lihong, Skala, Stacey, Heimrich, Elizabeth M, McIntyre, Kim W, Taylor, Tracy L, Kukral, Daniel W, Dudhgaonkar, Shailesh, Nagar, Jignesh, Banas, Dana, Watterson, Scott H, Tino, Joseph A, Fura, Aberra, Burke, James R
Published in PloS one (24.07.2017)
Published in PloS one (24.07.2017)
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Enhanced Gastrointestinal Motility with Orally Active Ghrelin Receptor Agonists
Charoenthongtrakul, Soratree, Giuliana, Derek, Longo, Kenneth A, Govek, Elizabeth K, Nolan, Anna, Gagne, Samantha, Morgan, Kristen, Hixon, Jeffrey, Flynn, Neil, Murphy, Brian J, Hernández, Andres S, Li, Jun, Tino, Joseph A, Gordon, David A, DiStefano, Peter S, Geddes, Brad J
Published in The Journal of pharmacology and experimental therapeutics (01.06.2009)
Published in The Journal of pharmacology and experimental therapeutics (01.06.2009)
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Journal Article
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton’s Tyrosine Kinase (BTK)
Watterson, Scott H, Liu, Qingjie, Beaudoin Bertrand, Myra, Batt, Douglas G, Li, Ling, Pattoli, Mark A, Skala, Stacey, Cheng, Lihong, Obermeier, Mary T, Moore, Robin, Yang, Zheng, Vickery, Rodney, Elzinga, Paul A, Discenza, Lorell, D’Arienzo, Celia, Gillooly, Kathleen M, Taylor, Tracy L, Pulicicchio, Claudine, Zhang, Yifan, Heimrich, Elizabeth, McIntyre, Kim W, Ruan, Qian, Westhouse, Richard A, Catlett, Ian M, Zheng, Naiyu, Chaudhry, Charu, Dai, Jun, Galella, Michael A, Tebben, Andrew J, Pokross, Matt, Li, Jianqing, Zhao, Rulin, Smith, Daniel, Rampulla, Richard, Allentoff, Alban, Wallace, Michael A, Mathur, Arvind, Salter-Cid, Luisa, Macor, John E, Carter, Percy H, Fura, Aberra, Burke, James R, Tino, Joseph A
Published in Journal of medicinal chemistry (11.04.2019)
Published in Journal of medicinal chemistry (11.04.2019)
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Discovery of 6‑Fluoro-5‑(R)‑(3‑(S)‑(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)‑yl)-2-methylphenyl)-2‑(S)‑(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro‑1H‑carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers
Watterson, Scott H, De Lucca, George V, Shi, Qing, Langevine, Charles M, Liu, Qingjie, Batt, Douglas G, Beaudoin Bertrand, Myra, Gong, Hua, Dai, Jun, Yip, Shiuhang, Li, Peng, Sun, Dawn, Wu, Dauh-Rurng, Wang, Chunlei, Zhang, Yingru, Traeger, Sarah C, Pattoli, Mark A, Skala, Stacey, Cheng, Lihong, Obermeier, Mary T, Vickery, Rodney, Discenza, Lorell N, D’Arienzo, Celia J, Zhang, Yifan, Heimrich, Elizabeth, Gillooly, Kathleen M, Taylor, Tracy L, Pulicicchio, Claudine, McIntyre, Kim W, Galella, Michael A, Tebben, Andy J, Muckelbauer, Jodi K, Chang, ChiehYing, Rampulla, Richard, Mathur, Arvind, Salter-Cid, Luisa, Barrish, Joel C, Carter, Percy H, Fura, Aberra, Burke, James R, Tino, Joseph A
Published in Journal of medicinal chemistry (13.10.2016)
Published in Journal of medicinal chemistry (13.10.2016)
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Journal Article
Discovery, synthesis, and structure–activity studies of tetrazole based growth hormone secretagogues
Hernández, Andrés S., Cheng, Peter T.W., Musial, Christa M., Swartz, Stephen G., George, Rocco J., Grover, Gary, Slusarchyk, Dorothy, Seethala, R. Krishna, Smith, Mark, Dickinson, Kenneth, Giupponi, Leah, Longhi, Daniel A., Flynn, Neil, Murphy, Brian J., Gordon, David A., Biller, Scott A., Robl, Jeffrey A., Tino, Joseph A.
Published in Bioorganic & medicinal chemistry letters (01.11.2007)
Published in Bioorganic & medicinal chemistry letters (01.11.2007)
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Journal Article
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγtIdentification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy
Marcoux, David, Duan, James J.-W, Shi, Qing, Cherney, Robert J, Srivastava, Anurag S, Cornelius, Lyndon, Batt, Douglas G, Liu, Qingjie, Beaudoin-Bertrand, Myra, Weigelt, Carolyn A, Khandelwal, Purnima, Vishwakrishnan, Sureshbabu, Selvakumar, Kumaravel, Karmakar, Ananta, Gupta, Arun Kumar, Basha, Mushkin, Ramlingam, Sridharan, Manjunath, Naveen, Vanteru, Sridhar, Karmakar, Sukhen, Maddala, Nageswara, Vetrichelvan, Muthalagu, Gupta, Anuradha, Rampulla, Richard A, Mathur, Arvind, Yip, Shiuhang, Li, Peng, Wu, Dauh-Rurng, Khan, Javed, Ruzanov, Max, Sack, John S, Wang, Jinhong, Yarde, Melissa, Cvijic, Mary Ellen, Li, Sha, Shuster, David J, Borowski, Virna, Xie, Jenny H, McIntyre, Kim W, Obermeier, Mary T, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Hynes, John, Tino, Joseph A, Macor, John E, Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Carter, Percy H, Dhar, T. G. Murali
Published in Journal of medicinal chemistry (14.11.2019)
Published in Journal of medicinal chemistry (14.11.2019)
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Annulation reaction enables the identification of an exocyclic amide tricyclic chemotype as retinoic acid Receptor-Related orphan receptor gamma (RORγ/RORc) inverse agonists
Marcoux, David, Bertrand, Myra Beaudoin, Weigelt, Carolyn A., Yip, Shiuhang, Galella, Michael, Park, Hyunsoo, Wu, Dauh-Rurng, Wang, Jinhong, Yarde, Melissa, Cvijic, Mary Ellen, Li, Sha, Hynes, John, Tino, Joseph A., Zhao, Qihong, Dhar, T.G. Murali
Published in Bioorganic & medicinal chemistry letters (01.10.2020)
Published in Bioorganic & medicinal chemistry letters (01.10.2020)
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Synthesis of 1‑(tert-Butyl) 4‑Methyl (1R,2S,4R)‑2-Methylcyclohexane-1,4-dicarboxylate from Hagemann’s tert-Butyl Ester for an Improved Synthesis of BMS-986251
Cornelius, Lyndon A. M, Li, Jianqing, Smith, Daniel, Krishnananthan, Subramaniam, Yip, Shiuhang, Wu, Dauh-Rurng, Pawluczyk, Joseph, Aulakh, Darpandeep, Sarjeant, Amy A, Kempson, James, Tino, Joseph A, Mathur, Arvind, Murali Dhar, T. G, Cherney, Robert J
Published in Journal of organic chemistry (21.08.2020)
Published in Journal of organic chemistry (21.08.2020)
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Small Molecule Reversible Inhibitors of Bruton’s Tyrosine Kinase (BTK): Structure–Activity Relationships Leading to the Identification of 7‑(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]‑9H‑carbazole-1-carboxamide (BMS-935177)
De Lucca, George V, Shi, Qing, Liu, Qingjie, Batt, Douglas G, Beaudoin Bertrand, Myra, Rampulla, Rick, Mathur, Arvind, Discenza, Lorell, D’Arienzo, Celia, Dai, Jun, Obermeier, Mary, Vickery, Rodney, Zhang, Yingru, Yang, Zheng, Marathe, Punit, Tebben, Andrew J, Muckelbauer, Jodi K, Chang, ChiehYing J, Zhang, Huiping, Gillooly, Kathleen, Taylor, Tracy, Pattoli, Mark A, Skala, Stacey, Kukral, Daniel W, McIntyre, Kim W, Salter-Cid, Luisa, Fura, Aberra, Burke, James R, Barrish, Joel C, Carter, Percy H, Tino, Joseph A
Published in Journal of medicinal chemistry (08.09.2016)
Published in Journal of medicinal chemistry (08.09.2016)
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Journal Article
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1 H -pyrazol-1-yl)methyl)phosphonate (BMS-820132)
Shi, Yan, Wang, Ying, Meng, Wei, Brigance, Robert P, Ryono, Denis E, Bolton, Scott, Zhang, Hao, Chen, Sean, Smirk, Rebecca, Tao, Shiwei, Tino, Joseph A, Williams, Kristin N, Sulsky, Richard, Nielsen, Laura, Ellsworth, Bruce, Wong, Michael K Y, Sun, Jung-Hui, Leith, Leslie W, Sun, Dawn, Wu, Dauh-Rurng, Gupta, Anuradha, Rampulla, Richard, Mathur, Arvind, Chen, Bang-Chi, Wang, Aiying, Fuentes-Catanio, Helen G, Kunselman, Lori, Cap, Michael, Zalaznick, Jacob, Ma, Xiaohui, Liu, Heng, Taylor, Joseph R, Zebo, Rachel, Jones, Beverly, Kalinowski, Stephen, Swartz, Joann, Staal, Ada, O'Malley, Kevin, Kopcho, Lisa, Muckelbauer, Jodi K, Krystek, Jr, Stanley R, Spronk, Steven A, Marcinkeviciene, Jovita, Everlof, Gerry, Chen, Xue-Qing, Xu, Carrie, Li, Yi-Xin, Langish, Robert A, Yang, Yanou, Wang, Qi, Behnia, Kamelia, Fura, Aberra, Janovitz, Evan B, Pannacciulli, Nicola, Griffen, Steven, Zinker, Bradley A, Krupinski, John, Kirby, Mark, Whaley, Jean, Zahler, Robert, Barrish, Joel C, Robl, Jeffrey A, Cheng, Peter T W
Published in Journal of medicinal chemistry (10.03.2022)
Published in Journal of medicinal chemistry (10.03.2022)
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Journal Article
Conversion of carbazole carboxamide based reversible inhibitors of Bruton’s tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series
Liu, Qingjie, Batt, Douglas G., Chaudhry, Charu, Lippy, Jonathan S., Pattoli, Mark A., Surti, Neha, Xu, Songmei, Carter, Percy H., Burke, James R., Tino, Joseph A.
Published in Bioorganic & medicinal chemistry letters (01.10.2018)
Published in Bioorganic & medicinal chemistry letters (01.10.2018)
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Journal Article
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR gamma t Inverse Agonist
Cherney, Robert J., Cornelius, Lyndon A. M., Srivastava, Anurag, Weigelt, Carolyn A., Marcoux, David, Duan, James J-W, Shi, Qing, Batt, Douglas G., Liu, Qingjie, Yip, Shiuhang, Wu, Dauh-Rurng, Ruzanov, Max, Sack, John, Khan, Javed, Wang, Jinhong, Yarde, Melissa, Cvijic, Mary Ellen, Mathur, Arvind, Li, Sha, Shuster, David, Khandelwal, Purnima, Borowski, Virna, Xie, Jenny, Obermeier, Mary, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Tino, Joseph A., Macor, John E., Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Carter, Percy H., Dhar, T. G. Murali
Published in ACS medicinal chemistry letters (11.06.2020)
Published in ACS medicinal chemistry letters (11.06.2020)
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Journal Article
Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists – Exploring C6 and C8 SAR using late-stage functionalization
Shi, Qing, Xiao, Zili, Yang, Michael G., Marcoux, David, Cherney, Robert J., Yip, Shiuhang, Li, Peng, Wu, Dauh-Rurng, Weigelt, Carolyn A., Sack, John, Khan, Javed, Ruzanov, Max, Wang, Jinhong, Yarde, Melissa, Ellen Cvijic, Mary, Li, Sha, Shuster, David J., Xie, Jenny, Sherry, Tara, Obermeier, Mary, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Chacko, Silvi, Shu, Yue-Zhong, Khandelwal, Purnima, Hynes, John, Tino, Joseph A., Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Dhar, T.G. Murali
Published in Bioorganic & medicinal chemistry letters (01.12.2020)
Published in Bioorganic & medicinal chemistry letters (01.12.2020)
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Journal Article
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)‑1H‑pyrazol-1-yl)methyl)phosphonate (BMS-820132)
Shi, Yan, Wang, Ying, Meng, Wei, Brigance, Robert P, Ryono, Denis E, Bolton, Scott, Zhang, Hao, Chen, Sean, Smirk, Rebecca, Tao, Shiwei, Tino, Joseph A, Williams, Kristin N, Sulsky, Richard, Nielsen, Laura, Ellsworth, Bruce, Wong, Michael K. Y, Sun, Jung-Hui, Leith, Leslie W, Sun, Dawn, Wu, Dauh-Rurng, Gupta, Anuradha, Rampulla, Richard, Mathur, Arvind, Chen, Bang-Chi, Wang, Aiying, Fuentes-Catanio, Helen G, Kunselman, Lori, Cap, Michael, Zalaznick, Jacob, Ma, Xiaohui, Liu, Heng, Taylor, Joseph R, Zebo, Rachel, Jones, Beverly, Kalinowski, Stephen, Swartz, Joann, Staal, Ada, O’Malley, Kevin, Kopcho, Lisa, Muckelbauer, Jodi K, Krystek, Stanley R, Spronk, Steven A, Marcinkeviciene, Jovita, Everlof, Gerry, Chen, Xue-Qing, Xu, Carrie, Li, Yi-Xin, Langish, Robert A, Yang, Yanou, Wang, Qi, Behnia, Kamelia, Fura, Aberra, Janovitz, Evan B, Pannacciulli, Nicola, Griffen, Steven, Zinker, Bradley A, Krupinski, John, Kirby, Mark, Whaley, Jean, Zahler, Robert, Barrish, Joel C, Robl, Jeffrey A, Cheng, Peter T. W
Published in Journal of medicinal chemistry (10.03.2022)
Published in Journal of medicinal chemistry (10.03.2022)
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Journal Article
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton’s tyrosine kinase (BTK) and Janus kinase 2 (JAK2)
Liu, Qingjie, Batt, Douglas G., Lippy, Jonathan S., Surti, Neha, Tebben, Andrew J., Muckelbauer, Jodi K., Chen, Lin, An, Yongmi, Chang, Chiehying, Pokross, Matt, Yang, Zheng, Wang, Haiqing, Burke, James R., Carter, Percy H., Tino, Joseph A.
Published in Bioorganic & medicinal chemistry letters (01.10.2015)
Published in Bioorganic & medicinal chemistry letters (01.10.2015)
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Journal Article
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach
Liu, Qingjie, Batt, Douglas G, Weigelt, Carolyn A, Yip, Shiuhang, Wu, Dauh-Rurng, Ruzanov, Max, Sack, John S, Wang, Jinhong, Yarde, Melissa, Li, Sha, Shuster, David J, Xie, Jenny H, Sherry, Tara, Obermeier, Mary T, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Khandelwal, Purnima, Tino, Joseph A, Macor, John E, Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Dhar, T. G. Murali
Published in ACS medicinal chemistry letters (10.12.2020)
Published in ACS medicinal chemistry letters (10.12.2020)
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Journal Article
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors
Qin, Lan-Ying, Ruan, Zheming, Cherney, Robert J., Dhar, T.G. Murali, Neels, James, Weigelt, Carolyn A., Sack, John S., Srivastava, Anurag S., Cornelius, Lyndon A.M., Tino, Joseph A., Stefanski, Kevin, Gu, Xiaomei, Xie, Jenny, Susulic, Vojkan, Yang, Xiaoxia, Yarde-Chinn, Melissa, Skala, Stacey, Bosnius, Ruth, Goldstein, Christine, Davies, Paul, Ruepp, Stefan, Salter-Cid, Luisa, Bhide, Rajeev S., Poss, Michael A.
Published in Bioorganic & medicinal chemistry letters (15.02.2017)
Published in Bioorganic & medicinal chemistry letters (15.02.2017)
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Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3‑Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders
Liu, Qingjie, Shi, Qing, Marcoux, David, Batt, Douglas G, Cornelius, Lyndon, Qin, Lan-Ying, Ruan, Zheming, Neels, James, Beaudoin-Bertrand, Myra, Srivastava, Anurag S, Li, Ling, Cherney, Robert J, Gong, Hua, Watterson, Scott H, Weigelt, Carolyn, Gillooly, Kathleen M, McIntyre, Kim W, Xie, Jenny H, Obermeier, Mary T, Fura, Aberra, Sleczka, Bogdan, Stefanski, Kevin, Fancher, R. M, Padmanabhan, Shweta, RP, Thatipamula, Kundu, Ipsit, Rajareddy, Kallem, Smith, Rodney, Hennan, James K, Xing, Dezhi, Fan, Jingsong, Levesque, Paul C, Ruan, Qian, Pitt, Sidney, Zhang, Rosemary, Pedicord, Donna, Pan, Jie, Yarde, Melissa, Lu, Hao, Lippy, Jonathan, Goldstine, Christine, Skala, Stacey, Rampulla, Richard A, Mathur, Arvind, Gupta, Anuradha, Arunachalam, Pirama Nayagam, Sack, John S, Muckelbauer, Jodi K, Cvijic, Mary Ellen, Salter-Cid, Luisa M, Bhide, Rajeev S, Poss, Michael A, Hynes, John, Carter, Percy H, Macor, John E, Ruepp, Stefan, Schieven, Gary L, Tino, Joseph A
Published in Journal of medicinal chemistry (22.06.2017)
Published in Journal of medicinal chemistry (22.06.2017)
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Journal Article
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK
Srivastava, Anurag S, Ko, Soo, Watterson, Scott H, Pattoli, Mark A, Skala, Stacey, Cheng, Lihong, Obermeier, Mary T, Vickery, Rodney, Discenza, Lorell N, D’Arienzo, Celia J, Gillooly, Kathleen M, Taylor, Tracy L, Pulicicchio, Claudine, McIntyre, Kim W, Yip, Shiuhang, Li, Peng, Sun, Dawn, Wu, Dauh-Rurng, Dai, Jun, Wang, Chunlei, Zhang, Yingru, Wang, Bei, Pawluczyk, Joseph, Kempson, James, Zhao, Rulin, Hou, Xiaoping, Rampulla, Richard, Mathur, Arvind, Galella, Michael A, Salter-Cid, Luisa, Barrish, Joel C, Carter, Percy H, Fura, Aberra, Burke, James R, Tino, Joseph A
Published in ACS medicinal chemistry letters (12.11.2020)
Published in ACS medicinal chemistry letters (12.11.2020)
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Journal Article
2-Hydroxy- N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors
Li, James J., Wang, Haixia, Tino, Joseph A., Robl, Jeffrey A., Herpin, Timothy F., Lawrence, R. Michael, Biller, Scott, Jamil, Haris, Ponticiello, Randy, Chen, Luping, Chu, Ching-hsuen, Flynn, Neil, Cheng, Dong, Zhao, Rulin, Chen, Bangchi, Schnur, Dora, Obermeier, Mary T., Sasseville, Vito, Padmanabha, Ramesh, Pike, Kristen, Harrity, Thomas
Published in Bioorganic & medicinal chemistry letters (01.06.2007)
Published in Bioorganic & medicinal chemistry letters (01.06.2007)
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