Search Results - "Tellew, John E"

Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic by Ramurthy, Savithri, Taft, Benjamin R, Aversa, Robert J, Barsanti, Paul A, Burger, Matthew T, Lou, Yan, Nishiguchi, Gisele A, Rico, Alice, Setti, Lina, Smith, Aaron, Subramanian, Sharadha, Tamez, Victoriano, Tanner, Huw, Wan, Lifeng, Hu, Cheng, Appleton, Brent A, Mamo, Mulugeta, Tandeske, Laura, Tellew, John E, Huang, Shenlin, Yue, Qin, Chaudhary, Apurva, Tian, Hung, Iyer, Raman, Hassan, A. Quamrul, Mathews Griner, Lesley A, La Bonte, Laura R, Cooke, Vesselina G, Van Abbema, Anne, Merritt, Hanne, Gampa, Kalyani, Feng, Fei, Yuan, Jing, Mishina, Yuji, Wang, Yingyun, Haling, Jacob R, Vaziri, Sepideh, Hekmat-Nejad, Mohammad, Polyakov, Valery, Zang, Richard, Sethuraman, Vijay, Amiri, Payman, Singh, Mallika, Sellers, William R, Lees, Emma, Shao, Wenlin, Dillon, Michael P, Stuart, Darrin D

“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Stereocontrolled Synthesis of Triazacyclopenta[cd]pentalenes by Intramolecular 1,3-Dipolar Cycloaddition Reactions of Azomethine Imines by Bélanger, Guillaume, Hong, Fang-Tsao, Overman, Larry E, Rogers, Bruce N, Tellew, John E, Trenkle, William C

“…The construction of triazacyclopenta[cd]pentalene diesters 6 by the reaction of dihydropyrrole α-ketoesters 3 with acylated hydrazines was evaluated further as…”
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Discovery of N-Isoxazolyl Biphenylsulfonamides as Potent Dual Angiotensin II and Endothelin A Receptor Antagonists by Murugesan, Natesan, Tellew, John E, Gu, Zhengxiang, Kunst, Bridgette L, Fadnis, Leena, Cornelius, Lyndon A, Baska, Rose Ann F, Yang, Yifan, Beyer, Sophie M, Monshizadegan, Hossain, Dickinson, Kenneth E, Panchal, Balkrushna, Valentine, Maria T, Chong, Saeho, Morrison, Richard A, Carlson, Kenneth E, Powell, James R, Moreland, Suzanne, Barrish, Joel C, Kowala, Mark C, Macor, John E

“…The ETA receptor antagonist (2) (N-(3,4-dimethyl-5-isoxazolyl)-4‘-(2-oxazolyl)-[1,1‘-biphenyl]-2-sulfonamide, BMS-193884) shares the same biphenyl core as a…”
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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers by Nishiguchi, Gisele A, Rico, Alice, Tanner, Huw, Aversa, Robert J, Taft, Benjamin R, Subramanian, Sharadha, Setti, Lina, Burger, Matthew T, Wan, Lifeng, Tamez, Victoriano, Smith, Aaron, Lou, Yan, Barsanti, Paul A, Appleton, Brent A, Mamo, Mulugeta, Tandeske, Laura, Dix, Ina, Tellew, John E, Huang, Shenlin, Mathews Griner, Lesley A, Cooke, Vesselina G, Van Abbema, Anne, Merritt, Hanne, Ma, Sylvia, Gampa, Kalyani, Feng, Fei, Yuan, Jing, Wang, Yingyun, Haling, Jacob R, Vaziri, Sepideh, Hekmat-Nejad, Mohammad, Jansen, Johanna M, Polyakov, Valery, Zang, Richard, Sethuraman, Vijay, Amiri, Payman, Singh, Mallika, Lees, Emma, Shao, Wenlin, Stuart, Darrin D, Dillon, Michael P, Ramurthy, Savithri

“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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Efficacy and Tolerability of Pyrazolo[1,5‑a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma by Mathison, Casey J. N, Chianelli, Donatella, Rucker, Paul V, Nelson, John, Roland, Jason, Huang, Zhihong, Yang, Yang, Jiang, Jiqing, Xie, Yun Feng, Epple, Robert, Bursulaya, Badry, Lee, Christian, Gao, Mu-Yun, Shaffer, Jennifer, Briones, Sergio, Sarkisova, Yelena, Galkin, Anna, Li, Lintong, Li, Nanxin, Li, Chun, Hua, Su, Kasibhatla, Shailaja, Kinyamu-Akunda, Jacqueline, Kikkawa, Rie, Molteni, Valentina, Tellew, John E

“…RET (REarranged during Transfection) kinase gain-of-function aberrancies have been identified as potential oncogenic drivers in lung adenocarcinoma, along with…”
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Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3‑d]pyrimidine RET Inhibitors by Mathison, Casey J. N, Yang, Yang, Nelson, John, Huang, Zhihong, Jiang, Jiqing, Chianelli, Donatella, Rucker, Paul V, Roland, Jason, Xie, Yun Feng, Epple, Robert, Bursulaya, Badry, Lee, Christian, Gao, Mu-Yun, Shaffer, Jennifer, Briones, Sergio, Sarkisova, Yelena, Galkin, Anna, Li, Lintong, Li, Nanxin, Li, Chun, Hua, Su, Kasibhatla, Shailaja, Kinyamu-Akunda, Jacqueline, Kikkawa, Rie, Molteni, Valentina, Tellew, John E

“…The selective inhibition of RET kinase as a treatment for relevant cancer types including lung adenocarcinoma has garnered considerable interest in recent…”
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Stereocontrolled Synthesis of the Tetracyclic Core of the Bisguanidine Alkaloids Palau'amine and Styloguanidine by Overman, Larry E, Rogers, Bruce N, Tellew, John E, Trenkle, William C

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Discovery of 4′-[(Imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/Angiotensin II receptor antagonists by Tellew, John E, Baska, Rose Ann F, Beyer, Sophie M, Carlson, Kenneth E, Cornelius, Lyndon A, Fadnis, Leena, Gu, Zhengxiang, Kunst, Bridgette L, Kowala, Mark C, Monshizadegan, Hossain, Murugesan, Natesan, Ryan, Carol S, Valentine, Maria T, Yang, Yifan, Macor, John E

“…A series of 4′-[(imidazol-1-yl)methyl]biphenylsulfonamides has potent antagonist activity against both angiotensin II AT 1 and endothelin ET A receptors. Such…”
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Small molecule antagonists of the corticotropin releasing factor (CRF) receptor: recent medicinal chemistry developments by Tellew, John E, Luo, Zhiyong

“…Antagonists of the corticotropin releasing factor (CRF or CRH) receptor have shown promise for the treatment of anxiety, depression, and irritable bowel…”
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Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF 1) receptor antagonist with improved pharmacokinetic properties by Tellew, John E., Lanier, Marion, Moorjani, Manisha, Lin, Emily, Luo, Zhiyong, Slee, Deborah H., Zhang, Xiaohu, Hoare, Sam R.J., Grigoriadis, Dimitri E., Denis, Yves St, Fabio, Romano Di, Modugno, Enza Di, Saunders, John, Williams, John P.

“…Antagonists of the corticotropin-releasing factor (CRF) neuropeptide may prove effective in treating stress and anxiety related disorders. In an effort to…”
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Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson’s Disease by Zhang, Xiaohu, Tellew, John E, Luo, Zhiyong, Moorjani, Manisha, Lin, Emily, Lanier, Marion C, Chen, Yongsheng, Williams, John P, Saunders, John, Lechner, Sandra M, Markison, Stacy, Joswig, Tanya, Petroski, Robert, Piercey, Jaime, Kargo, William, Malany, Siobhan, Santos, Mark, Gross, Raymond S, Wen, Jenny, Jalali, Kayvon, O’Brien, Zhihong, Stotz, Carol E, Crespo, María I, Díaz, José-Luis, Slee, Deborah H

“…4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-pyrimidines bearing substituted pyridyl groups as C-6 substituents were prepared as selective adenosine hA2A…”
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Dual Angiotensin II and Endothelin A Receptor Antagonists:  Synthesis of 2‘-Substituted N-3-Isoxazolyl Biphenylsulfonamides with Improved Potency and Pharmacokinetics by Murugesan, Natesan, Gu, Zhengxiang, Fadnis, Leena, Tellew, John E, Baska, Rose Ann F, Yang, Yifan, Beyer, Sophie M, Monshizadegan, Hossain, Dickinson, Kenneth E, Valentine, Maria T, Humphreys, W. Griffith, Lan, Shih-Jung, Ewing, William R, Carlson, Kenneth E, Kowala, Mark C, Zahler, Robert, Macor, John E

“…In a previous report we demonstrated that merging together key structural elements present in an AT1 receptor antagonist (1, irbesartan) with key structural…”
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Dehydroamino acid derivatives from D-arabinose and L-serine: synthesis of models for the azinomycin antitumor antibiotics by Moran, Edmund J, Tellew, John E, Zhao, Zuchun, Armstrong, Robert W

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Practical Synthesis of 3-Amino-4,5-dimethylisoxazole from 2-Methyl-2-butenenitrile and Acetohydroxamic Acid by Tellew, John E, Leith, Leslie, Mathur, Arvind

“…3-Amino-4,5-dimethylisoxazole was prepared from technical-grade 2-methyl-2-butenenitrile and acetohydroxamic acid in a 62% overall yield on a multimole scale…”
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Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists by XIAOHU ZHANG, RUETER, Jaimie K, MARKISON, Stacy, JOSWIG, Tanya, MALANY, Siobhan, SANTOS, Mark, CASTRO-PALOMINO, Julio C, CRESPO, Maria I, PRAT, Maria, GUAL, Silvia, DIAZ, José-Luis, SAUNDERS, John, YONGSHENG CHEN, SLEE, Deborah H, MOORJANI, Manisha, LANIER, Marion C, LIN, Emily, GROSS, Raymond S, TELLEW, John E, WILLIAMS, John P, LECHNER, Sandra M

“…A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A(2A) antagonists is described. SAR studies led to compound 14 with excellent potency (K(i) = 0.4 nM),…”
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2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability by Moorjani, Manisha, Luo, Zhiyong, Lin, Emily, Vong, Binh G, Chen, Yongsheng, Zhang, Xiaohu, Rueter, Jaimie K, Gross, Raymond S, Lanier, Marion C, Tellew, John E, Williams, John P, Lechner, Sandra M, Malany, Siobhan, Santos, Mark, Crespo, María I, Díaz, José-Luis, Saunders, John, Slee, Deborah H

“…In this report, the strategy and outcome of expanding SAR exploration to improve solubility and metabolic stability are discussed. Compound 35 exhibited…”
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2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A2A antagonists with improved solubility and metabolic stability by MOORJANI, Manisha, ZHIYONG LUO, WILLIAMS, John P, LECHNER, Sandra M, MALANY, Siobhan, SANTOS, Mark, CRESPO, Maria I, DIAZ, José-Luis, SAUNDERS, John, SLEE, Deborah H, LIN, Emily, VONG, Binh G, YONGSHENG CHEN, XIAOHU ZHANG, RUETER, Jaimie K, GROSS, Raymond S, LANIER, Marion C, TELLEW, John E

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Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists by Cole, Andrew G., Stroke, Ilana L., Qin, Lan-Ying, Hussain, Zahid, Simhadri, Srilatha, Brescia, Marc-Raleigh, Waksmunski, Frank S., Strohl, Barbara, Tellew, John E., Williams, John P., Saunders, John, Appell, Kenneth C., Henderson, Ian, Webb, Maria L.

“…The synthesis and evaluation of (dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists are reported. The discovery and synthesis of a series…”
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Stereoselective synthesis of (E)- and (Z)-1-azabicyclo[3.1.0]hex-2-ylidene dehydroamino acid derivatives by Armstrong, Robert W, Tellew, John E, Moran, Edmund J

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2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability by Moorjani, Manisha, Zhang, Xiaohu, Chen, Yongsheng, Lin, Emily, Rueter, Jaimie K, Gross, Raymond S, Lanier, Marion C, Tellew, John E, Williams, John P, Lechner, Sandra M, Malany, Siobhan, Santos, Mark, Ekhlassi, Paddi, Castro-Palomino, Julio C, Crespo, María I, Prat, Maria, Gual, Silvia, Díaz, José-Luis, Saunders, John, Slee, Deborah H

“…In this report, the design and synthesis of a series of pyrimidine based adenosine A(2A) antagonists are described. The strategy and outcome of expanding SAR…”
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