Search Results - "Hungate, Randall"

Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σS–X) Interaction for Conformational Constraint by Pennington, Lewis D, Bartberger, Michael D, Croghan, Michael D, Andrews, Kristin L, Ashton, Kate S, Bourbeau, Matthew P, Chen, Jie, Chmait, Samer, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Hong, Fang-Tsao, Hungate, Randall W, Jordan, Steven R, Kong, Ke, Liu, Longbin, Michelsen, Klaus, Moyer, Carolyn, Nishimura, Nobuko, Norman, Mark H, Reichelt, Andreas, Siegmund, Aaron C, Sivits, Glenn, Tadesse, Seifu, Tegley, Christopher M, Van, Gwyneth, Yang, Kevin C, Yao, Guomin, Zhang, Jiandong, Lloyd, David J, Hale, Clarence, St. Jean, David J

“…The HTS-based discovery and structure-guided optimization of a novel series of GKRP-selective GK–GKRP disrupters are revealed. Diarylmethane­sulfonamide hit 6…”
Get full text

Discovery of Clinical Candidate 1‑(4-(3-(4-(1H‑Benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), A Potent, Selective, and Efficacious Inhibitor of Phosphodiesterase 10A (PDE10A) by Hu, Essa, Chen, Ning, Bourbeau, Matthew P, Harrington, Paul E, Biswas, Kaustav, Kunz, Roxanne K, Andrews, Kristin L, Chmait, Samer, Zhao, Xiaoning, Davis, Carl, Ma, Ji, Shi, Jianxia, Lester-Zeiner, Dianna, Danao, Jean, Able, Jessica, Cueva, Madelyn, Talreja, Santosh, Kornecook, Thomas, Chen, Hang, Porter, Amy, Hungate, Randall, Treanor, James, Allen, Jennifer R

“…We report the identification of a PDE10A clinical candidate by optimizing potency and in vivo efficacy of promising keto-benzimidazole leads 1 and 2…”
Get full text

Discovery of a Potent, Orally Active 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor for Clinical Study: Identification of (S)-2-((1S,2S,4R)-Bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221) by Véniant, Murielle M, Hale, Clarence, Hungate, Randall W, Gahm, Kyung, Emery, Maurice G, Jona, Janan, Joseph, Smriti, Adams, Jeffrey, Hague, Andrew, Moniz, George, Zhang, Jiandong, Bartberger, Michael D, Li, Vivian, Syed, Rashid, Jordan, Steven, Komorowski, Renée, Chen, Michelle M, Cupples, Rod, Kim, Ki Won, St. Jean, David J, Johansson, Lars, Henriksson, Martin A, Williams, Meredith, Vallgårda, Jerk, Fotsch, Christopher, Wang, Minghan

“…Thiazolones with an exo-norbornylamine at the 2-position and an isopropyl group on the 5-position are potent 11β-HSD1 inhibitors. However, the C-5 center was…”
Get full text

2-(S)-Phenethylaminothiazolones as Potent, Orally Efficacious Inhibitors of 11β-Hydroxysteriod Dehydrogenase Type 1 by St. Jean, David J, Yuan, Chester, Bercot, Eric A, Cupples, Rod, Chen, Michelle, Fretland, Jenne, Hale, Clarence, Hungate, Randall W, Komorowski, Renee, Veniant, Murielle, Wang, Minghan, Zhang, Xiping, Fotsch, Christopher

“…11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is the enzyme that converts cortisone to cortisol. A growing body of evidence suggests that selective…”
Get full text

Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists by Chen, Jian Jeffrey, Qian, Wenyuan, Biswas, Kaustav, Viswanadhan, Vellarkad N., Askew, Benny C., Hitchcock, Stephen, Hungate, Randall W., Arik, Leyla, Johnson, Eileen

“…Novel dihydroquinoxalinone acetamides containing bicyclic aminotetralins or chromans were found to be potent Bradykinin B1 receptor antagonists. Replacement of…”
Get full text

Discovery of Novel, Potent Benzamide Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Exhibiting Oral Activity in an Enzyme Inhibition ex Vivo Model by Julian, Lisa D, Wang, Zhulun, Bostick, Tracy, Caille, Seb, Choi, Rebekah, DeGraffenreid, Michael, Di, Yongmei, He, Xiao, Hungate, Randall W, Jaen, Juan C, Liu, Jinsong, Monshouwer, Mario, McMinn, Dustin, Rew, Yosup, Sudom, Athena, Sun, Daqing, Tu, Hua, Ursu, Stefania, Walker, Nigel, Yan, Xuelei, Ye, Qiuping, Powers, Jay P

“…We report the discovery of potent benzamide inhibitors of 11β-hydroxysteroid dehydrogenase (11β-HSD1). The optimization and correlation of in vitro and in vivo…”
Get full text

The discovery of 2-anilinothiazolones as 11β-HSD1 inhibitors by Yuan, Chester, St. Jean, David J., Liu, Qingyian, Cai, Lynn, Li, Aiwen, Han, Nianhe, Moniz, George, Askew, Ben, Hungate, Randall W., Johansson, Lars, Tedenborg, Lars, Pyring, David, Williams, Meredith, Hale, Clarence, Chen, Michelle, Cupples, Rod, Zhang, Jiandong, Jordan, Steven, Bartberger, Michael D., Sun, Yaxiong, Emery, Maurice, Wang, Minghan, Fotsch, Christopher

“…A series of 2-anilinothiazolones were prepared as inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The most potent compounds contained a…”
Get full text

Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5- a]pyrimidines: A New Class of KDR Kinase Inhibitors by Fraley, Mark E., Hoffman, William F., Rubino, Robert S., Hungate, Randall W., Tebben, Andrew J., Rutledge, Ruth Z., McFall, Rosemary C., Huckle, William R., Kendall, Richard L., Coll, Kathleen E., Thomas, Kenneth A.

“…Graphic We have synthesized and evaluated the activity of 3,6-disubstituted pyrazolo[1,5- a]pyrimidines as a new class of KDR kinase inhibitors. Starting with…”
Get full text

Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit by Hu, Essa, Tasker, Andrew, White, Ryan D, Kunz, Roxanne K, Human, Jason, Chen, Ning, Bürli, Roland, Hungate, Randall, Novak, Perry, Itano, Andrea, Zhang, Xuxia, Yu, Violeta, Nguyen, Yen, Tudor, Yanyan, Plant, Matthew, Flynn, Shaun, Xu, Yang, Meagher, Kristin L, Whittington, Douglas A, Ng, Gordon Y

“…Inhibition of c-Kit has the potential to treat mast cell associated fibrotic diseases. We report the discovery of several aminoquinazoline pyridones that are…”
Get full text

Discovery of novel hydroxy-thiazoles as HIF-α prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation by Tegley, Christopher M., Viswanadhan, Vellarkad N., Biswas, Kaustav, Frohn, Michael J., Peterkin, Tanya A.N., Chang, Catherine, Bürli, Roland W., Dao, Jennifer H., Veith, Henrike, Rogers, Norma, Yoder, Sean C., Biddlecome, Gloria, Tagari, Philip, Allen, Jennifer R., Hungate, Randall W.

“…Inhibition of the PHD2 enzyme has been associated with increased red blood cell levels. From a screening hit, a series of novel hydroxyl-thiazoles were…”
Get full text

Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors by Rew, Yosup, McMinn, Dustin L., Wang, Zhulun, He, Xiao, Hungate, Randall W., Jaen, Juan C., Sudom, Athena, Sun, Daqing, Tu, Hua, Ursu, Stefania, Villemure, Elisia, Walker, Nigel P.C., Yan, Xuelei, Ye, Qiuping, Powers, Jay P.

“…The discovery and optimization of a piperidyl benzamide series of 11β-HSD1 inhibitors is reported. Discovery and optimization of a piperidyl benzamide series…”
Get full text

2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics by Zeng, Qingping, Bourbeau, Matthew P., Wohlhieter, G. Erich, Yao, Guomin, Monenschein, Holger, Rider, James T., Lee, Matthew R., Zhang, Shiwen, Lofgren, Julie, Freeman, Daniel, Li, Chun, Tominey, Elizabeth, Huang, Xin, Hoffman, Douglas, Yamane, Harvey, Tasker, Andrew S., Dominguez, Celia, Viswanadhan, Vellarkad N., Hungate, Randall, Zhang, Xiaoling

“…The development of a series of potent AKT1 inhibitors is reported. A series of 2-aminothiadiazole of inhibitors of AKT1 is described. SAR relationships are…”
Get full text

Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency by Qian, Wenyuan, Chen, Jian Jeffrey, Human, Jason, Aya, Toshihiro, Zhu, Jiawang, Biswas, Kaustav, Peterkin, Tanya, Hungate, Randall W., Arik, Leyla, Johnson, Eileen, Kumar, Gondi, Joseph, Smriti, Jona, Janan, Guo, Hong-Xun, Wu, Zufan

“…In a series of bradykinin B1 antagonists, we discovered that replacement of oxopiperazine acetamides with dehydro-oxopiperazine acetamides provided compounds…”
Get full text

New ‘chemical probes’ to examine the role of the hFPRL1 (or ALXR) receptor in inflammation by Frohn, Mike, Xu, Han, Zou, Xiaoming, Chang, Catherine, McElvaine, Michele, Plant, Matthew H., Wong, Min, Tagari, Philip, Hungate, Randall, Bürli, Roland W.

“…We report the development of the novel N-substituted benzimidazole 11 as a potent and selective human formyl peptide receptor-like 1 (hFPRL1) agonist. This…”
Get full text

Further Studies with the 2-Amino-1,3-thiazol-4(5H)-one Class of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Reducing Pregnane X Receptor Activity and Exploring Activity in a Monkey Pharmacodynamic Model by Fotsch, Christopher, Bartberger, Michael D, Bercot, Eric A, Chen, Michelle, Cupples, Rod, Emery, Maury, Fretland, Jenne, Guram, Anil, Hale, Clarence, Han, Nianhe, Hickman, Dean, Hungate, Randall W, Hayashi, Michael, Komorowski, Renee, Liu, Qingyian, Matsumoto, Guy, St. Jean, David J, Ursu, Stefania, Véniant, Murielle, Xu, Guifen, Ye, Qiuping, Yuan, Chester, Zhang, Jiandong, Zhang, Xiping, Tu, Hua, Wang, Minghan

“…A series of compounds containing the 2-amino-1,3-thiazol-4(5H)-one core were found to be potent inhibitors of the enzyme 11β-hydroxysteroid dehydrogenase type…”
Get full text

Effect of microwave heating on Ullmann-type heterocycle-aryl ether synthesis using chloro-heterocycles by D’Angelo, Noel D., Peterson, Joseph J., Booker, Shon K., Fellows, Ingrid, Dominguez, Celia, Hungate, Randall, Reider, Paul J., Kim, Tae-Seong

“…Ullmann ether synthesis was conducted on a variety of chloro-heterocycles with different phenols using optimized conditions involving copper powder and cesium…”
Get full text

3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation by Chen, Jian Jeffrey, Nguyen, Thomas, D’Amico, Derin C., Qian, Wenyuan, Human, Jason, Aya, Toshihiro, Biswas, Kaustav, Fotsch, Christopher, Han, Nianhe, Liu, Qingyian, Nishimura, Nobuko, Peterkin, Tanya A.N., Yang, Kevin, Zhu, Jiawang, Riahi, Babak Bobby, Hungate, Randall W., Andersen, Neil G., Colyer, John T., Faul, Margaret M., Kamassah, Augustus, Wang, Judy, Jona, Janan, Kumar, Gondi, Johnson, Eileen, Askew, Benny C.

“…The discovery of novel and highly potent oxopiperazine based B1 receptor antagonists is described. Compared to the previously described arylsulfonylated (…”
Get full text

An Efficient and Scalable One-Pot Double Michael Addition-Dieckmann Condensation for the Synthesis of 4,4-Disubstituted Cyclohexane β-Keto Esters by DeGraffenreid, Michael R, Bennett, Sarah, Caille, Sebastien, Gonzalez-Lopez de Turiso, Felix, Hungate, Randall W, Julian, Lisa D, Kaizerman, Jacob A, McMinn, Dustin L, Rew, Yosup, Sun, Daqing, Yan, Xuelei, Powers, Jay P

“…A simple, scalable, and efficient one-pot methodology for the synthesis of 4,4-disubstituted cyclohexane β-keto esters from benzylic nitriles or esters and…”
Get full text

Azole-based inhibitors of AKT/PKB for the treatment of cancer by Zeng, Qingping, Allen, John G., Bourbeau, Matthew P., Wang, Xianghong, Yao, Guomin, Tadesse, Seifu, Rider, James T., Yuan, Chester C., Hong, Fang-Tsao, Lee, Matthew R., Zhang, Shiwen, Lofgren, Julie A., Freeman, Daniel J., Yang, Suijin, Li, Chun, Tominey, Elizabeth, Huang, Xin, Hoffman, Douglas, Yamane, Harvey K., Fotsch, Christopher, Dominguez, Celia, Hungate, Randall, Zhang, Xiaoling

“…Through a combination of screening and structure-based rational design, we have discovered a series of N…”
Get full text

Aryl sulfones as novel Bradykinin B1 receptor antagonists for treatment of chronic pain by Biswas, Kaustav, Aya, Toshihiro, Qian, Wenyuan, Peterkin, Tanya A.N., Chen, Jian Jeffrey, Human, Jason, Hungate, Randall W., Kumar, Gondi, Arik, Leyla, Lester-Zeiner, Dianna, Biddlecome, Gloria, Manning, Barton H., Sun, Hong, Dong, Hong, Huang, Ming, Loeloff, Richard, Johnson, Eileen J., Askew, Benny C.

“…We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist,…”
Get full text