Search Results - "Duan, James" :: K.UTB vyhledávací portál | TBU Library Retrieval Portal

Rationally Designed, Conformationally Constrained Inverse Agonists of RORγtIdentification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy

Rationally Designed, Conformationally Constrained Inverse Agonists of RORγtIdentification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy

by 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)

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Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists

by Duan, James J.-W, Lu, Zhonghui, Jiang, Bin, Stachura, Sylwia, Weigelt, Carolyn A, Sack, John S, Khan, Javed, Ruzanov, Max, Galella, Michael A, Wu, Dauh-Rurng, Yarde, Melissa, Shen, Ding-Ren, Shuster, David J, Borowski, Virna, Xie, Jenny H, Zhang, Lisa, Vanteru, Sridhar, Gupta, Arun Kumar, Mathur, Arvind, Zhao, Qihong, Foster, William, Salter-Cid, Luisa M, Carter, Percy H, Dhar, T. G. Murali
Published in ACS medicinal chemistry letters (14.03.2019)

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Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches

Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches

by Xiao, Hai-Yun, Li, Ning, Duan, James J.-W, Jiang, Bin, Lu, Zhonghui, Ngu, Khehyong, Tino, Joseph, Kopcho, Lisa M, Lu, Hao, Chen, Jing, Tebben, Andrew J, Sheriff, Steven, Chang, ChiehYing Y, Yanchunas, Joseph, Calambur, Deepa, Gao, Mian, Shuster, David J, Susulic, Vojkan, Xie, Jenny H, Guarino, Victor R, Wu, Dauh-Rurng, Gregor, Kurt R, Goldstine, Christine B, Hynes, John, Macor, John E, Salter-Cid, Luisa, Burke, James R, Shaw, Patrick J, Dhar, T. G. Murali
Published in Journal of medicinal chemistry (10.12.2020)

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Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity

Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity

by Gong, Hua, Weinstein, David S., Lu, Zhonghui, Duan, James J.-W., Stachura, Sylwia, Haque, Lauren, Karmakar, Ananta, Hemagiri, Hemalatha, Raut, Dhanya Kumar, Gupta, Arun Kumar, Khan, Javed, Camac, Dan, Sack, John S., Pudzianowski, Andrew, Wu, Dauh-Rurng, Yarde, Melissa, Shen, Ding-Ren, Borowski, Virna, Xie, Jenny H., Sun, Huadong, D'Arienzo, Celia, Dabros, Marta, Galella, Michael A., Wang, Faye, Weigelt, Carolyn A., Zhao, Qihong, Foster, William, Somerville, John E., Salter-Cid, Luisa M., Barrish, Joel C., Carter, Percy H., Dhar, T.G. Murali
Published in Bioorganic & medicinal chemistry letters (15.01.2018)

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Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists

Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists

by Jiang, Bin, Duan, James J.-W., Stachura, Sylwia, Karmakar, Ananta, Hemagiri, Hemalatha, Raut, Dhanya Kumar, Gupta, Arun Kumar, Weigelt, Carolyn A., Khan, Javed, Sack, John S., Wu, Dauh-Rurng, Yarde, Melissa, Shen, Ding-Ren, Galella, Michael A., Mathur, Arvind, Zhao, Qihong, Salter-Cid, Luisa M., Carter, Percy H., Dhar, T.G. Murali
Published in Bioorganic & medicinal chemistry letters (01.09.2020)

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Discovery of highly potent, selective, covalent inhibitors of JAK3

Discovery of highly potent, selective, covalent inhibitors of JAK3

by Kempson, James, Ovalle, Damaso, Guo, Junqing, Wrobleski, Stephen T., Lin, Shuqun, Spergel, Steven H., Duan, James J.-W., Jiang, Bin, Lu, Zhonghui, Das, Jagabandhu, Yang, Bingwei V., Hynes, John, Wu, Hong, Tokarski, John, Sack, John S., Khan, Javed, Schieven, Gary, Blatt, Yuval, Chaudhry, Charu, Salter-Cid, Luisa M., Fura, Aberra, Barrish, Joel C., Carter, Percy H., Pitts, William J.
Published in Bioorganic & medicinal chemistry letters (15.10.2017)

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Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists

Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists

by Harikrishnan, Lalgudi S., Gill, Patrice, Kamau, Muthoni G., Qin, Lan-Ying, Ruan, Zheming, O'Malley, Daniel, Huynh, Tram, Stachura, Sylwia, Cavallaro, Cullen L., Lu, Zhonghui, J.-W. Duan, James, Weigelt, Carolyn A., Sack, John S., Ruzanov, Max, Khan, Javed, Gururajan, Murali, Wong, Jessica J., Huang, Yanling, Yarde, Melissa, Li, Zhuyin, Chen, Cliff, Sun, Huadong, Borowski, Virna, Murtaza, Anwar, Fink, Brian E.
Published in Bioorganic & medicinal chemistry letters (15.06.2020)

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Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists

Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists

by Lu, Zhonghui, Duan, James J.-W., Xiao, Haiyun, Neels, James, Wu, Dauh-Rurng, Weigelt, Carolyn A., Sack, John S., Khan, Javed, Ruzanov, Max, An, Yongmi, Yarde, Melissa, Karmakar, Ananta, Vishwakrishnan, Sureshbabu, Baratam, Venkata, Shankarappa, Harisha, Vanteru, Sridhar, Babu, Venkatesh, Basha, Mushkin, Kumar Gupta, Arun, Kumaravel, Selvakumar, Mathur, Arvind, Zhao, Qihong, Salter-Cid, Luisa M., Carter, Percy H., Murali Dhar, T.G.
Published in Bioorganic & medicinal chemistry letters (15.08.2019)

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Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors

Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors

by Hynes, John, Wu, Hong, Kempson, James, Duan, James J.-W., Lu, Zhonghui, Jiang, Bin, Stachura, Sylwia, Tokarski, John S., Sack, John S., Khan, Javed A., Lippy, Jonathan S., Zhang, Rosemary F., Pitt, Sidney, Shen, Guoxiang, Gillooly, Kate, McIntyre, Kim, Carter, Percy H., Barrish, Joel C., Nadler, Steven G., Salter-Cid, Luisa M., Fura, Aberra, Schieven, Gary L., Pitts, William J., Wrobleski, Stephen T.
Published in Bioorganic & medicinal chemistry letters (15.07.2017)

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Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR gamma t Inverse Agonist

Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR gamma t Inverse Agonist

by 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)

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Discovery of 2,6–difluorobenzyl ether series of phenyl ((R)–3–phenylpyrrolidin–3–yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists

Discovery of 2,6–difluorobenzyl ether series of phenyl ((R)–3–phenylpyrrolidin–3–yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists

by Duan, James J.-W., Jiang, Bin, Lu, Zhonghui, Stachura, Sylwia, Weigelt, Carolyn A., Sack, John S., Khan, Javed, Ruzanov, Max, Wu, Dauh–Rurng, Yarde, Melissa, Shen, Ding–Ren, Zhao, Qihong, Salter–Cid, Luisa M., Carter, Percy H., Murali Dhar, T.G.
Published in Bioorganic & medicinal chemistry letters (01.10.2020)

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Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors

Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors

by Duan, James J. -W., Lu, Zhonghui, Jiang, Bin, Yang, Bingwei V., Doweyko, Lidia M., Nirschl, David S., Haque, Lauren E., Lin, Shuqun, Brown, Gregory, Hynes, John, Tokarski, John S., Sack, John S., Khan, Javed, Lippy, Jonathan S., Zhang, Rosemary F., Pitt, Sidney, Shen, Guoxiang, Pitts, William J., Carter, Percy H., Barrish, Joel C., Nadler, Steven G., Salter-Cid, Luisa M., McKinnon, Murray, Fura, Aberra, Schieven, Gary L., Wrobleski, Stephen T.
Published in Bioorganic & medicinal chemistry letters (15.12.2014)

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Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE): Discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1′ substituents

Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE): Discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1′ substituents

by Lu, Zhonghui, Ott, Gregory R., Anand, Rajan, Liu, Rui-Qin, Covington, Maryanne B., Vaddi, Krishna, Qian, Mingxin, Newton, Robert C., Christ, David D., Trzaskos, James, Duan, James J.-W.
Published in Bioorganic & medicinal chemistry (15.03.2008)

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Pharmacologic and Genetic Manipulation of MMP-2 and -9 Affects Retinal Neovascularization in Rodent Models of OIR

Pharmacologic and Genetic Manipulation of MMP-2 and -9 Affects Retinal Neovascularization in Rodent Models of OIR

by Barnett, Joshua M, McCollum, Gary W, Fowler, Jessica A, Duan, James J.-W, Kay, Jesse D, Liu, Rui-Qin, Bingaman, David P, Penn, John S
Published in Investigative ophthalmology & visual science (01.02.2007)

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Improving the Pharmacokinetic and CYP Inhibition Profiles of Azaxanthene-Based Glucocorticoid Receptor ModulatorsIdentification of (S)‑5-(2-(9-Fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)‑5H‑chromeno[2,3‑b]pyridin-5-yl)-2-methylpropanamido)‑N‑(tetrahydro‑2H‑pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide (BMS-341)

Improving the Pharmacokinetic and CYP Inhibition Profiles of Azaxanthene-Based Glucocorticoid Receptor ModulatorsIdentification of (S)‑5-(2-(9-Fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)‑5H‑chromeno[2,3‑b]pyridin-5-yl)-2-methylpropanamido)‑N‑(tetrahydro‑2H‑pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide (BMS-341)

by Yang, Michael G, Dhar, T. G. Murali, Xiao, Zili, Xiao, Hai-Yun, Duan, James J.-W, Jiang, Bin, Galella, Michael A, Cunningham, Mark, Wang, Jinhong, Habte, Sium, Shuster, David, McIntyre, Kim W, Carman, Julie, Holloway, Deborah A, Somerville, John E, Nadler, Steven G, Salter-Cid, Luisa, Barrish, Joel C, Weinstein, David S
Published in Journal of medicinal chemistry (28.05.2015)

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Pharmacokinetics and pharmacodynamics of DPC 333 (2R)-2-((3R)-3 -amino -3{4 -[2 -methyl -4 -quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl -n -hydroxy -4 -methylpentanamide , a potent and selective inhibitor of tumor necrosis factor α-Converting enzyme in rodents, dogs, chimpanzees, and humans

Pharmacokinetics and pharmacodynamics of DPC 333 (2R)-2-((3R)-3 -amino -3{4 -[2 -methyl -4 -quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl -n -hydroxy -4 -methylpentanamide , a potent and selective inhibitor of tumor necrosis factor α-Converting enzyme in rodents, dogs, chimpanzees, and humans

by MINGXIN QIAN, BAI, Stephen A, YUZHONG DENG, MADUSKUIE, Thomas, TRZASKOS, James, DUAN, James J.-W, DECICCO, Carl P, CHRIST, David D, BROGDON, Bernice, WU, Jing-Tao, LIU, Rui-Qin, COVINGTON, Maryanne B, VADDI, Kris, NEWTON, Robert C, FOSSLER, Michael J, GARNER, C. Edwin
Published in Drug metabolism and disposition (01.10.2007)

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Discovery of β-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors

Discovery of β-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors

by Duan, James J.-W., Chen, Lihua, Lu, Zhonghui, Xue, Chu-Biao, Liu, Rui-Qin, Covington, Maryanne B., Qian, Mingxin, Wasserman, Zelda R., Vaddi, Krishna, Christ, David D., Trzaskos, James M., Newton, Robert C., Decicco, Carl P.
Published in Bioorganic & medicinal chemistry (2008)

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Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents

Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents

by Ott, Gregory R, Asakawa, Naoyuki, Lu, Zhonghui, Anand, Rajan, Liu, Rui-Qin, Covington, Maryanne B, Vaddi, Krishna, Qian, Mingxin, Newton, Robert C, Christ, David D, Trzaskos, James M, Duan, James J-W
Published in Bioorganic & medicinal chemistry (01.03.2008)

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Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-α converting enzyme (TACE)

by Duan, James J.-W., Chen, Lihua, Lu, Zhonghui, Jiang, Bin, Asakawa, Naoyuki, Sheppeck, James E., Liu, Rui-Qin, Covington, Maryanne B., Pitts, William, Kim, Soong-Hoon, Decicco, Carl P.
Published in Bioorganic & medicinal chemistry letters (2007)

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Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-α converting enzyme (TACE)

by Sheppeck, James E., Gilmore, John L., Tebben, Andrew, Xue, Chu-Biao, Liu, Rui-Qin, Decicco, Carl P., Duan, James J.-W.
Published in Bioorganic & medicinal chemistry letters (15.05.2007)

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