未登录 Discovery of liver-selective glucokinase activators comprising N-(4-alkylthiazol-2-yl)benzamides and N-(3-alkyl-1,2,4-thiadiazol-5-yl) benzamides for the treatment of metabolic disorders 肝选择性葡萄糖激酶激活剂的发现，包括N-(4-烷基硫唑-2-基)苯甲酰胺和N-(3-烷基-1,2,4-噻二唑-5-基)苯甲酰胺，用于治疗代谢紊乱 Yoon, David S.; Wu, Shung; Chen, Sean S.; Smirk, Rebecca A.; Brigance, Robert P.; Meng, Wei; Shi, Yan; Tao, Shiwei; Wang, Ying; Zhang, Hao; Mathur, Arvind; Catanio, Helen Grace; Kalinowski, Stephen; Zebo, Rachel; Zalaznick, Jacob; Taylor, Joseph; Zinker, Bradley; Kopcho, Lisa M.; Behnia, Kamelia; Xu, Carrie; Spronk, Steven A.; Yang, Yanou; Josephs, Jonathan; Janovitz, Evan B.; Marathe, Punit; Whaley, Jean; Barrish, Joel C.; Kirby, Mark; Cheng, Peter T. W. 分享 收藏
SLC6A19 inhibition facilitates urinary neutral amino acid excretion and lowers plasma phenylalanine Wobst, Heike J.; Viader, Andreu; Muncipinto, Giovanni; Hollibaugh, Ryan; van Kalken, Daniel; Burkhart, Christopher T.; Cantin, Susan M.; Bates, Rachel M.; Regimbald-Dumas, Yannik; Gross, Liam; Antalek, Mitchell T.; Zweig, Joshua E.; Wu, Frank; Rettenmaier, T. Justin; Labenski, Matthew T.; Pullen, Nicholas; Blanchette, Heather S.; Henderson, Jaclyn L.; Weng, Haoling H.; Vaughn, Toby A.; Brown, Dean G.; Throup, John P.; Barrish, Joel C. 分享 收藏
Novel Corrector for Variants of SLC6A8: A Therapeutic Opportunity for Creatine Transporter Deficiency Gechijian, Lara N.; Muncipinto, Giovanni; Rettenmaier, T. Justin; Labenski, Matthew T.; Rusu, Victor; Rosskamp, Lea; Conway, Leslie; van Kalken, Daniel; Gross, Liam; Iantosca, Gianna; Crotty, William; Mathis, Robert; Park, Hyejin; Rabin, Benjamin; Westgate, Christina; Lyons, Matthew; Deshusses, Chloe; Brandon, Nicholas; Brown, Dean G.; Blanchette, Heather S.; Pullen, Nicholas; Jones, Lyn H.; Barrish, Joel C. 分享 收藏
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JNT-517, a first-in-class SLC6A19 inhibitor for the treatment of phenylketonuria, enhances urinary excretion of phenylalanine in healthy volunteers Viader, Andreu; Throup, John; Wobst, Heike; Blanchette, Heather; Nix, Darrell; Pullen, Nicholas; Brown, Dean; Barrish, Joel; Vaughn, Tobias; Weng, Haoling; Longo, Nicola; Harding, Cary 分享 收藏
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities Jurica, Elizabeth A.; Wu, Ximao; Williams, Kristin N.; Haque, Lauren E.; Rampulla, Richard A.; Mathur, Arvind; Zhou, Min; Cao, Gary; Cai, Hong; Wang, Tao; Liu, Heng; Xu, Carrie; Kunselman, Lori K.; Antrilli, Thomas M.; Hicks, Michael B.; Sun, Qin; Dierks, Elizabeth A.; Apedo, Atsu; Moore, Douglas B.; Foster, Kimberly A.; Cvijic, Mary Ellen; Panemangalore, Reshma; Khandelwal, Purnima; Wilkes, Jason J.; Zinker, Bradley A.; Robertson, Donald G.; Janovitz, Evan B.; Galella, Michael; Li, Yi-Xin; Li, Julia; Ramar, Thangeswaran; Jalagam, Prasada Rao; Jayaram, Ramya; Whaley, Jean M.; Barrish, Joel C.; Robl, Jeffrey A.; Ewing, William R.; Ellsworth, Bruce A. 分享 收藏
A SMALL MOLECULE SLC6A19 INHIBITOR INCREASES URINARY PHENYLALANINE EXCRETION AND REDUCES ITS PATHOGENIC PLASMA ACCUMULATION IN A PHENYLKETONURIA MOUSE MODEL Wobst, Heike; Hollibaugh, Ryan; Muncipinto, Giovanni; Burkhart, Christopher; van Kalken, Daniel; Viader, Andreu; Blanchette, Heather; Brown, Dean; Pullen, Nick; Throup, John; Barrish, Joel 分享 收藏
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. 分享 收藏
BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate Cherney, Robert J.; Anjanappa, Prakash; Selvakumar, Kumaravel; Batt, Douglas G.; Brown, Gregory D.; Rose, Anne, V; Vuppugalla, Ragini; Chen, Jing; Pang, Jian; Xu, Songmei; Yarde, Melissa; Tebben, Andrew J.; Paidi, Venkatram Reddy; Cvijic, Mary Ellen; Mathur, Arvind; Barrish, Joel C.; Mandlekar, Sandhya; Zhao, Qihong; Carter, Percy H. 分享 收藏
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. 分享 收藏
Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis 烟酰胺作为有效和选择性IRAK4抑制剂的优化，在银屑病小鼠模型中具有疗效 Nair, Satheesh; Kumar, Sreekantha Ratna; Paidi, Venkatram Reddy; Sistla, Ramesh; Kantheti, Durgarao; Polimera, Subba Rao; Thangavel, Soodamani; Mukherjee, Amrita Jha; Das, Mitalee; Bhide, Rajeev S.; Pitts, William J.; Murugesan, Natesan; Dudhgoankar, Shailesh; Nagar, Jignesh; Subramani, Siva; Mazumder, Debarati; Carman, Julie A.; Holloway, Deborah A.; Li, Xin; Fereshteh, Mark P.; Ruepp, Stefan; Palanisamy, Kamalavenkatesh; Mariappan, T. Thanga; Maddi, Srinivas; Saxena, Ajay; Elzinga, Paul; Chimalakonda, Anjaneya; Ruan, Qian; Ghosh, Kaushik; Bose, Sucharita; Sack, John; Yan, Chunhong; Kiefer, Susan E.; Xie, Dianlin; Newitt, John A.; Saravanakumar, S. Pon; Rampulla, Richard A.; Barrish, Joel C.; Carter, Percy H.; Hynes, John, Jr. 分享 收藏
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis Spergel, Steven H.; Mertzman, Michael E.; Kempson, James; Guo, Junqing; Stachura, Syl-Wia; Hague, Lauren; Lippy, Jonathan S.; Zhang, Rosemary F.; Galena, Michael; Pitt, Sidney; Shen, Guoxiang; Fura, Aberra; Gillooly, Kathleen; McIntyre, Kim W.; Tang, Vicky; Tokarski, John; Sack, John S.; Khan, Javed; Carter, Percy H.; Barrish, Joel C.; Nadler, Steven G.; Salter-Cid, Luisa M.; Schieven, Gary L.; Wrobleski, Stephen T.; Pitts, William J. 分享 收藏
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672 Yang, Michael G.; Xiao, Zili; Cherney, Robert J.; Tebben, Andrew J.; Batt, Douglas G.; Brown, Gregory D.; Chen, Jing; Cvijic, Mary Ellen; Dabros, Marta; Duncia, John V.; Galena, Michael; Gardner, Daniel S.; Khandelwal, Purnima; Ko, Soo S.; Malley, Mary F.; Mo, Ruowei; Pang, Jian; Rose, Anne V.; Santella, Joseph B., III; Shi, Hong; Srivastava, Anurag; Traeger, Sarah C.; Wang, Bei; Xu, Songmei; Zhao, Rulin; Barrish, Joel C.; Mandlekar, Sandhya; Zhao, Qihong; Carter, Percy H. 分享 收藏
Evaluation of risk of bacteria-mediated putative bystander hemolysis of PNH red blood cells in vitro: No evidence of significant complement-mediated hemolysis induced by microorganisms Yang, Guangwei; Yuan, Xuan; Galvan, Manuel; Thanassi, Jane A.; Zhao, Yongsen; Patel, Dharaben; Fabrycki, Joanne; Luu, Amanda; Yang, Wengang; Wiles, Jason; Phadke, Avinash; Barrish, Joel; Huang, Mingjun; Brodsky, Robert; Podos, Steven D. 分享 收藏
Evaluation of mechanisms of paroxysm in paroxysmal nocturnal hemoglobinuria: In vitro explorations of bystander hemolysis and of perturbations of soluble regulators Thanassi, Jane A.; Galvan, Manuel D.; Yuan, Xuan; Yang, Guangwei; Zhao, Yongsen; Patel, Dharaben; Fabrycki, Joanne; Luu, Amanda; Yang, Wengang; Wiles, Jason; Phadke, Avinash; Barrish, Joel; Podos, Steven D.; Huang, Mingjun; Brodsky, Robert 分享 收藏
Inhibition of complement alternative pathway by ACH-4471, the first clinical investigational orally-administered inhibitor of complement factor D Huang, Mingjun; Yang, Wengang; Podos, Steven D.; Yang, Guangwei; Zhao, Yongsen; Thanassi, Jane A.; Patel, Dharaben; Fabrycki, Joanne; Luu, Amanda; Galvan, Manuel; Yuan, Xuan; Brodsky, Robert; Ajari, Ifode; Lahey, John; Kocinsky, Hetal; Geffner, Michael; Phadke, Avinash; Wiles, Jason; Barrish, Joel 分享 收藏
Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3′-hydroxyazetidin-1-yl)ethanone [BMS-8163361, an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor Ye, Xiang-Yang; Chen, Stephanie Y.; Wu, Shung; Yoon, David S.; Wang, Haixia; Hong, Zhenqiu; O'Connor, Stephen P.; Li, Jun; Li, James J.; Kennedy, Lawrence J.; Walker, Steven J.; Nayeem, Akbar; Sheriff, Steven; Camac, Daniel M.; Ramamurthy, Vidyhashankar; Morin, Paul E.; Zebo, Rachel; Taylor, Joseph R.; Morgan, Nathan N.; Ponticiello, Randolph P.; Harrity, Thomas; Apedo, Atsu; Golla, Rajasree; Seethala, Ramakrishna; Wang, Mengmeng; Harper, Timothy W.; Sleczka, Bogdan G.; He, Bin; Kirby, Mark; Leahy, David K.; Li, Jianqing; Hanson, Ronald L.; Guo, Zhiwei; Li, Yi-Xin; DiMarco, John D.; Scaringe, Raymond; Maxwell, Brad; Moulin, Frederick; Barrish, Joel C.; Gordon, David A.; Robl, Jeffrey A. 分享 收藏
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode Jurica, Elizabeth A.; Wu, Ximao; Williams, Kristin N.; Hernandez, Andres S.; Nirschl, David S.; Rampulla, Richard A.; Mathur, Arvind; Zhou, Min; Cao, Gary; Xie, Chunshan; Jacob, Biji; Cai, Hong; Wang, Tao; Murphy, Brian J.; Liu, Heng; Xu, Carrie; Kunselman, Lori K.; Hicks, Michael B.; Sun, Qin; Schnur, Dora M.; Sitkoff, Doree F.; Dierks, Elizabeth A.; Apedo, Atsu; Moore, Douglas B.; Foster, Kimberly A.; Cvijic, Mary Ellen; Panemangalore, Reshma; Flynn, Neil A.; Maxwell, Brad D.; Hong, Yang; Tian, Yuan; Wilkes, Jason J.; Zinker, Bradley A.; Whaley, Jean M.; Barrish, Joel C.; Robl, Jeffrey A.; Ewing, William R.; Ellsworth, Bruce A. 分享 收藏
Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-34(R)-6-hexy1-5,6,7,8-tetrahydronaphthalen-2yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P1 Receptor Modulator Yang, Michael G.; Xiao, Zili; Dhar, T. G. Murali; Xiao, Hai-Yun; Gilmore, John L.; Marcoux, David; Xie, Jenny H.; McIntyre, Kim W.; Taylor, Tracy L.; Borowski, Virna; Heimrich, Elizabeth; Li, Yu-Wen; Feng, Jianlin; Fernandes, Alda; Yang, Zheng; Balimane, Praveen; Marino, Anthony M.; Cornelius, Georgia; Warrack, Bethanne M.; Mathur, Arvind; Wu, Dauh-Rurng; Li, Peng; Gupta, Anuradha; Pragalathan, Bala; Shen, Ding Ren; Cvijic, Mary Ellen; Lehman-McKeeman, Lois D.; Salter-Cid, Luisa; Barrish, Joel C.; Carter, Percy H.; Dyckman, Alaric J. 分享 收藏
Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design Xiao, Hai-Yun; Watterson, Scott H.; Langevine, Charles M.; Srivastava, Anurag S.; Ko, Soo S.; Zhang, Yanlei; Cherney, Robert J.; Guo, Wei-Wei; Gilmore, John L.; II, James E. Sheppeck; Wu, Dauh-Rurng; Li, Peng; Ramasamy, Duraisamy; Arunachalam, Piramanayagam; Mathur, Arvind; Taylor, Tracy L.; Shuster, David J.; McIntyre, Kim W.; Shen, Ding-Ren; Yarde, Melissa; Cvijic, Mary Ellen; Marino, Anthony M.; Balimane, Praveen V.; Yang, Zheng; Banas, Dana M.; Cornelius, Georgia; D'Arienzo, Celia J.; Warrack, Bethanne M.; Lehman-McKeeman, Lois; Salter-Cid, Luisa M.; Xie, Jenny; Barrish, Joel C.; Carter, Percy H.; Dyckman, Alaric J.; Dhar, T. G. Murali 分享 收藏
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