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The Discovery of C7-Substituted Norbornyl Bisamides as RXFP1 Small Molecule Agonists C7-取代降冰片基双酰胺类化合物作为RXFP1小分子激动剂的发现 Su, Shun; Myers, Michael C.; Bilder, Donna M.; Clarke, Adam; Friends, Todd; Petrone, Thomas V.; Ryan, Carol; Krause, Carol M.; Chen, Ruihua; Li, Yi-xin; Fronheiser, Matthew; Galella, Michael A.; Rose, Anne V.; Generaux, Claudia N.; Zhao, Lei; Bostwick, Jeff; Li, Jianqing; Mathur, Arvind; Duclos, Franck; Madsen, Cort S.; Wexler, Ruth R.; Lawrence, R. Michael 分享 收藏
Development of a Buchwald-Hartwig Amination for an Accelerated Library Synthesis of Cereblon Binders Lejava, Anastasia; Miseo, Giulianna A.; Phan, Thomas; Zhu, Jinyi; Powers, Hannah L.; Li, Jianqing; Mortensen, Deborah S.; Zapf, Christoph W.; Khambatta, Gody; Buenviaje, Jennifer; Holmberg-Douglas, Natalie 分享 收藏
Development of a Safe and Practical Synthesis of Enantiomerically Pure (S)- and (R)-N-Boc-3-(Trifluoromethyl)piperazines Enabled by Aza-Michael Addition of Optically Pure 4-Phenyl-2-Oxazolidinone to 3,3,3-Trifluoro-1-Nitropropene Darne, Chetan Padmakar; Li, Ning; Smith, Daniel; Zhang, Shasha; Neithnadka, Premsai Rai; Silamkoti, Arundutt; Arumugam, Arunachalam; Gupta, Anuradha; Hong, Zhenqiu; Krishnananthan, Subramaniam; Wang, Bei; Zhao, Rulin; Yip, Shiuhang; Wu, Dauh-Rurng; Kempson, James; Mortensen, Deborah S.; Mathur, Arvind; Li, Jianqing 分享 收藏
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Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4 Priestley, E. Scott; Banville, Jacques; Deon, Daniel; Dube, Laurence; Gagnon, Marc; Guy, Julia; Lapointe, Philippe; Lavallee, Jean-Francois; Martel, Alain; Plamondon, Serge; Remillard, Roger; Ruediger, Edward; Tremblay, Francois; Posy, Shana L.; Guarino, Victor R.; Richter, Jeremy M.; Li, Jianqing; Gupta, Anuradha; Vetrichelvan, Muthalagu; Balapragalathan, T. J.; Mathur, Arvind; Hua, Ji; Callejo, Mario; Guay, Jocelyne; Sum, Chi Shing; Cvijic, Mary Ellen; Watson, Carol; Wong, Pancras; Yang, Jing; Bouvier, Michel; Gordon, David A.; Wexler, Ruth R.; Marinier, Anne 分享 收藏
Synthesis Optimization, Scale-Up, and Catalyst Screening Efforts toward the MGAT2 Clinical Candidate, BMS-963272 Kempson, James; Hou, Xiaoping; Sun, Jung-Hui; Wong, Michael; Pawluczyk, Joseph; Li, Jianqing; Krishnananthan, Subramaniam; Simmons, Eric M.; Hsiao, Yi; Li, Yi-Xin; Sun, Dawn; Wu, Dauh-Rurng; Meng, Wei; Ahmad, Saleem; Negash, Lidet; Brigance, Robert; Turdi, Huji; Hangeland, Jon J.; Lawrence, R. Michael; Devasthale, Pratik; Robl, Jeffrey A.; Mathur, Arvind 分享 收藏
Discovery of (S)-1-((2′,6-Bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): AHighly Selective, CNS Penetrable, and Orally Active AdaptorProtein-2 Associated Kinase 1 Inhibitor in Clinical Trials for theTreatment of Neuropathic Pain Luo, Guanglin; Chen, Ling; Kostich, Walter A.; Hamman, Brian; Allen, Jason; Easton, Amy; Bourin, Clotilde; Gulianello, Michael; Lippy, Jonathan; Nara, Susheel; Maishal, Tarun Kumar; Thiyagarajan, Kamalraj; Jalagam, Prasadrao; Pattipati, Sreenivasulu Naidu; Dandapani, Kumaran; Dokania, Manoj; Vattikundala, Pradeep; Sharma, Vivek; Elavazhagan, Saravanan; Verma, Manoj Kumar; Das, Manish Lal; Wagh, Santosh; Balakrishnan, Anand; Johnson, Benjamin M.; Santone, Kenneth S.; Thalody, George; Denton, Rex; Saminathan, Hariharan; Holenarsipur, Vinay K.; Kumar, Anoop; Rao, Abhijith; Putlur, Siva Prasad; Sarvasiddhi, Sarat Kumar; Shankar, Ganesh; Louis, Justin, V; Ramarao, Manjunath; Conway, Charles M.; Li, Yu-Wen; Pieschl, Rick; Tian, Yuan; Hong, Yang; Ditta, Jonathan; Mathur, Arvind; Li, Jianqing; Smith, Daniel; Pawluczyk, Joseph; Sun, Dawn; Yip, Shiuhang; Wu, Dauh-Rurng; Vetrichelvan, Muthalagu; Gupta, Anuradha; Wilson, Alan; Gopinathan, Suma; Wason, Suman; Bristow, Linda; Albright, Charles F.; Bronson, Joanne J.; Macor, John E.; Dzierba, Carolyn D. 分享 收藏
Development of a Rapid Scale-Up Synthesis of (S)-N-(8-((2-Amino-2,4-dimethylpentyl)oxy)-5H-chromeno[3,4-c]pyridin-2-yl)acetamide, a Potent Adaptor-Associated Kinase 1 Inhibitor Li, Jianqing; Smith, Daniel; Pawluczyk, Joseph; Krishnananthan, Subramaniam; Wang, Bei; Hou, Xiaoping; Zhao, Rulin; Kempson, James; Sun, Dawn; Yip, Shiuhang; Wu, Dauh-Rurng; Maddala, Nageswararao; Vetrichelvan, Muthalagu; Gupta, Anuradha; Macor, John E.; Dzierba, Carolyn D.; Mathur, Arvind 分享 收藏
Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases Cheng, Peter T. W.; Kaltenbach, Robert F.; Zhang, Hao; Shi, Jun; Tao, Shiwei; Li, Jun; Kennedy, Lawrence J.; Walker, Steven J.; Shi, Yan; Wang, Ying; Dhanusu, Suresh; Reddigunta, Ramesh; Kumaravel, Selvakumar; Jusuf, Sutjano; Smith, Daniel; Krishnananthan, Subramaniam; Li, Jianqing; Wang, Tao; Heiry, Rebekah; Sum, Chi Shing; Kalinowski, Stephen S.; Hung, Chen-Pin; Chu, Ching-Hsuen; Azzara, Anthony, V; Ziegler, Milinda; Burns, Lisa; Zinker, Bradley A.; Boehm, Stephanie; Taylor, Joseph; Sapuppo, Julia; Mosure, Kathy; Everlof, Gerry; Guarino, Victor; Zhang, Lisa; Yang, Yanou; Ruan, Qian; Xu, Carrie; Apedo, Atsu; Traeger, Sarah C.; Cvijic, Mary Ellen; Lentz, Kimberley A.; Tirucherai, Giridhar; Sivaraman, Lakshmi; Robl, Jeffrey; Ellsworth, Bruce A.; Rosen, Glenn; Gordon, David A.; Soars, Matthew G.; Gill, Michael; Murphy, Brian J. 分享 收藏
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design Gavai, Ashvinikumar, V; Norris, Derek; Delucca, George; Tortolani, David; Tokarski, John S.; Dodd, Dharmpal; O'Malley, Daniel; Zhao, Yufen; Quesnelle, Claude; Gill, Patrice; Vaccaro, Wayne; Tram Huynh; Ahuja, Vijay; Han, Wen-Ching; Mussari, Christopher; Harikrishnan, Lalgudi; Kamau, Muthoni; Poss, Michael; Sheriff, Steven; Yan, Chunhong; Marsilio, Frank; Menard, Krista; Wen, Mei-Li; Rampulla, Richard; Wu, Dauh-Rurng; Li, Jianqing; Zhang, Huiping; Li, Peng; Sun, Dawn; Yip, Henry; Traeger, Sarah C.; Zhang, Yingru; Mathur, Arvind; Zhang, Haiying; Huang, Christine; Yang, Zheng; Ranasinghe, Asoka; Everlof, Gerry; Raghavan, Nirmala; Tye, Ching Kim; Wee, Susan; Hunt, John T.; Vite, Gregory; Westhouse, Richard; Lee, Francis Y. 分享 收藏
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy Dilger, Andrew K.; Pabbisetty, Kumar B.; Corte, James R.; De Lucca, Indawati; Fang, Tianan; Yang, Wu; Pinto, Donald J. P.; Wang, Yufeng; Zhu, Yeheng; Mathur, Arvind; Li, Jianqing; Hou, Xiaoping; Smith, Daniel; Sun, Dawn; Zhang, Huiping; Krishnananthan, Subramaniam; Wu, Dauh-Rurng; Myers, Joseph E., Jr.; Sheriff, Steven; Rossi, Karen A.; Chacko, Silvi; Zheng, Joanna J.; Galella, Michael A.; Ziemba, Theresa; Dierks, Elizabeth A.; Bozarth, Jeffrey M.; Wu, Yiming; Crain, Earl; Wong, Pancras C.; Luettgen, Joseph M.; Wexler, Ruth R.; Ewing, William R. 分享 收藏
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2 Liu, Chunjian; Lin, James; Langevine, Charles; Smith, Daniel; Li, Jianqing; Tokarski, John S.; Khan, Javed; Ruzanov, Max; Strnad, Joann; Zupa-Fernandez, Adriana; Cheng, Lihong; Gillooly, Kathleen M.; Shuster, David; Zhang, Yifan; Thankappan, Anil; McIntyre, Kim W.; Chaudhry, Charu; Elzinga, Paul A.; Chiney, Manoj; Chimalakonda, Anjaneya; Lombardo, Louis J.; Macor, John E.; Carter, Percy H.; Burke, James R.; Weinstein, David S. 分享 收藏
Synthesis of Differentially Protected Azatryptophan Analogs via Pd2(dba)3/XPhos Catalyzed Negishi Coupling of N-Ts Azaindole Halides with Zinc Derivative from Fmoc-Protected tert-Butyl (R)-2-Amino-3-iodopropanoate Nimje, Roshan Y.; Vytla, Devaiah; Kuppusamy, Prakasam; Velayuthaperumal, Rajeswari; Jarugu, Lokesh Babu; Reddy, China Anki; Chikkananjaiah, Nanjundaswamy Kanikahalli; Rampulla, Richard A.; Cavallaro, Cullen L.; Li, Jianqing; Mathur, Arvind; Gupta, Anuradha; Roy, Amrita 分享 收藏
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; Dhar, T. G. Murali; Cherney, Robert J. 分享 收藏
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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; Bertrand, Myra Beaudoin; 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. 分享 收藏