Search Results - "Pickrell, Alexander J."

The optimization of aminooxadiazoles as orally active inhibitors of Cdc7 by Harrington, Paul E., Bourbeau, Matthew P., Fotsch, Christopher, Frohn, Michael, Pickrell, Alexander J., Reichelt, Andreas, Sham, Kelvin, Siegmund, Aaron C., Bailis, Julie M., Bush, Tammy, Escobar, Sonia, Hickman, Dean, Heller, Scott, Hsieh, Faye, Orf, Jessica N., Rong, Minqing, San Miguel, Tisha, Tan, Helming, Zalameda, Leeanne, Allen, John G.

“…A series of aminooxadiazoles was optimized for inhibition of Cdc7. Early lead isoquinoline 1 suffered from modest cell potency (cellular IC50=0.71μM measuring…”
Get full text

Quinolinone-based agonists of S1P1: Use of a N-scan SAR strategy to optimize in vitro and in vivo activity by Pennington, Lewis D., Croghan, Michael D., Sham, Kelvin K.C., Pickrell, Alexander J., Harrington, Paul E., Frohn, Michael J., Lanman, Brian A., Reed, Anthony B., Lee, Matthew R., Xu, Han, McElvain, Michele, Xu, Yang, Zhang, Xuxia, Fiorino, Michael, Horner, Michelle, Morrison, Henry G., Arnett, Heather A., Fotsch, Christopher, Tasker, Andrew S., Wong, Min, Cee, Victor J.

“…We reveal how a N-scan SAR strategy (systematic substitution of each CH group with a N atom) was employed for quinolinone-based S1P1 agonist 5 to modulate…”
Get full text

Discovery of a Covalent Inhibitor of KRAS G12C (AMG 510) for the Treatment of Solid Tumors by Lanman, Brian A, Allen, Jennifer R, Allen, John G, Amegadzie, Albert K, Ashton, Kate S, Booker, Shon K, Chen, Jian Jeffrey, Chen, Ning, Frohn, Michael J, Goodman, Guy, Kopecky, David J, Liu, Longbin, Lopez, Patricia, Low, Jonathan D, Ma, Vu, Minatti, Ana E, Nguyen, Thomas T, Nishimura, Nobuko, Pickrell, Alexander J, Reed, Anthony B, Shin, Youngsook, Siegmund, Aaron C, Tamayo, Nuria A, Tegley, Christopher M, Walton, Mary C, Wang, Hui-Ling, Wurz, Ryan P, Xue, May, Yang, Kevin C, Achanta, Pragathi, Bartberger, Michael D, Canon, Jude, Hollis, L Steven, McCarter, John D, Mohr, Christopher, Rex, Karen, Saiki, Anne Y, San Miguel, Tisha, Volak, Laurie P, Wang, Kevin H, Whittington, Douglas A, Zech, Stephan G, Lipford, J Russell, Cee, Victor J

“…KRAS has emerged as a promising target in the treatment of solid tumors. Covalent inhibitors targeting the mutant cysteine-12 residue have been shown to…”
Get full text

NMR Detection of Intramolecular OH/OH Hydrogen Bond Networks: An Approach Using Isotopic Perturbation and Hydrogen Bond Mediated OH···OH J-Coupling by J. O’Leary, Daniel, E. Anderson, Carolyn, J. Pickrell, Alexander, L. Sperry, Sarah, E. Vasquez, Thomas, G. Custer, Thomas, B. Fierman, Matthew, C. Lazar, Daniel, W. Brown, Zachary, S. Iskenderian, Wendy, D. Hickstein, Daniel

Get full text

Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility by Rzasa, Robert M., Frohn, Michael J., Andrews, Kristin L., Chmait, Samer, Chen, Ning, Clarine, Jeffrey G., Davis, Carl, Eastwood, Heather A., Horne, Daniel B., Hu, Essa, Jones, Adrie D., Kaller, Matthew R., Kunz, Roxanne K., Miller, Silke, Monenschein, Holger, Nguyen, Thomas, Pickrell, Alexander J., Porter, Amy, Reichelt, Andreas, Zhao, Xiaoning, Treanor, James J.S., Allen, Jennifer R.

“…[Display omitted] We report the discovery of a novel series of 2-(3-alkoxy-1-azetidinyl) quinolines as potent and selective PDE10A inhibitors…”
Get full text

Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1α prolyl hydroxylase-2 inhibitors by Frohn, Mike, Viswanadhan, Vellarkad, Pickrell, Alexander J., Golden, Jennifer E., Muller, Kristine M., Bürli, Roland W., Biddlecome, Gloria, Yoder, Sean C., Rogers, Norma, Dao, Jennifer H., Hungate, Randall, Allen, Jennifer R.

“…We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which…”
Get full text

Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups by Reed, Anthony B., Lanman, Brian A., Neira, Susana, Harrington, Paul E., Sham, Kelvin K.C., Frohn, Mike, Pickrell, Alexander J., Tasker, Andrew S., Gore, Anu, Fiorino, Mike, Itano, Andrea, McElvain, Michele, Middleton, Scot, Morrison, Henry, Xu, Han, Xu, Yang, Wong, Min, Cee, Victor J.

“…Replacement of the azetidine carboxylate of an S1P1 agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a…”
Get full text

Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: Potent S1P1 agonists with in vivo lymphocyte-depleting activity by Frohn, Mike, Cee, Victor J., Lanman, Brian A., Pickrell, Alexander J., Golden, Jennifer, Rivenzon-Segal, Dalia, Middleton, Scot, Fiorino, Mike, Xu, Han, Schrag, Michael, Xu, Yang, McElvain, Michele, Muller, Kristine, Siu, Jerry, Bürli, Roland

“…An SAR campaign designed to increase polarity in the ‘tail’ region of benzothiazole 1 resulted in two series of structurally novel 5-and 6-substituted S1P1…”
Get full text

Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core by Harrington, Paul E, Croghan, Michael D, Fotsch, Christopher, Frohn, Mike, Lanman, Brian A, Pennington, Lewis D, Pickrell, Alexander J, Reed, Anthony B, Sham, Kelvin K. C, Tasker, Andrew, Arnett, Heather A, Fiorino, Michael, Lee, Matthew R, McElvain, Michele, Morrison, Henry G, Xu, Han, Xu, Yang, Zhang, Xuxia, Wong, Min, Cee, Victor J

“…The optimization of a series of S1P1 agonists with limited activity against S1P3 is reported. A polar headgroup was used to improve the physicochemical and…”
Get full text

Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1) by Lanman, Brian A, Cee, Victor J, Cheruku, Srinivasa R, Frohn, Mike, Golden, Jennifer, Lin, Jian, Lobera, Mercedes, Marantz, Yael, Muller, Kristine M, Neira, Susana C, Pickrell, Alexander J, Rivenzon-Segal, Dalia, Schutz, Nili, Sharadendu, Anurag, Yu, Xiang, Zhang, Zhaoda, Buys, Janet, Fiorino, Mike, Gore, Anu, Horner, Michelle, Itano, Andrea, McElvain, Michele, Middleton, Scot, Schrag, Michael, Vargas, Hugo M, Xu, Han, Xu, Yang, Zhang, Xuxia, Siu, Jerry, Bürli, Roland W

“…Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of…”
Get full text

4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1 by Pennington, Lewis D, Sham, Kelvin K. C, Pickrell, Alexander J, Harrington, Paul E, Frohn, Michael J, Lanman, Brian A, Reed, Anthony B, Croghan, Michael D, Lee, Matthew R, Xu, Han, McElvain, Michele, Xu, Yang, Zhang, Xuxia, Fiorino, Michael, Horner, Michelle, Morrison, Henry G, Arnett, Heather A, Fotsch, Christopher, Wong, Min, Cee, Victor J

“…The sphingosine-1-phosphate-1 receptor (S1P1) and its endogenous ligand sphingosine-1-phosphate (S1P) cooperatively regulate lymphocyte trafficking from the…”
Get full text

Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors by Lanman, Brian A., Chen, Jian Jeffrey, Liu, Longbin, Lopez, Patricia, Pickrell, Alexander J., Reed, Anthony B., Wang, Hui-Ling, Achanta, Pragathi, Canon, Jude, Erlanson, Daniel A., Fucini, Raymond V., Jeong, Joon Won, Mohr, Christopher, Saiki, Anne Y., Cee, Victor J., Lipford, J. Russell, Rex, Karen, Volak, Laurie P.

“…Abstract The RAS gene family encodes the small GTPase proteins NRAS, HRAS, and KRAS, which play an essential role in cellular growth and proliferation. KRAS is…”
Get full text

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors by Lanman, Brian A, Allen, Jennifer R, Allen, John G, Amegadzie, Albert K, Ashton, Kate S, Booker, Shon K, Chen, Jian Jeffrey, Chen, Ning, Frohn, Michael J, Goodman, Guy, Kopecky, David J, Liu, Longbin, Lopez, Patricia, Low, Jonathan D, Ma, Vu, Minatti, Ana E, Nguyen, Thomas T, Nishimura, Nobuko, Pickrell, Alexander J, Reed, Anthony B, Shin, Youngsook, Siegmund, Aaron C, Tamayo, Nuria A, Tegley, Christopher M, Walton, Mary C, Wang, Hui-Ling, Wurz, Ryan P, Xue, May, Yang, Kevin C, Achanta, Pragathi, Bartberger, Michael D, Canon, Jude, Hollis, L. Steven, McCarter, John D, Mohr, Christopher, Rex, Karen, Saiki, Anne Y, San Miguel, Tisha, Volak, Laurie P, Wang, Kevin H, Whittington, Douglas A, Zech, Stephan G, Lipford, J. Russell, Cee, Victor J

“…KRASG12C has emerged as a promising target in the treatment of solid tumors. Covalent inhibitors targeting the mutant cysteine-12 residue have been shown to…”
Get full text

4-Methoxy- N -[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P 1 by Pennington, Lewis D., Sham, Kelvin K. C., Pickrell, Alexander J., Harrington, Paul E., Frohn, Michael J., Lanman, Brian A., Reed, Anthony B., Croghan, Michael D., Lee, Matthew R., Xu, Han, McElvain, Michele, Xu, Yang, Zhang, Xuxia, Fiorino, Michael, Horner, Michelle, Morrison, Henry G., Arnett, Heather A., Fotsch, Christopher, Wong, Min, Cee, Victor J.

Get full text

Optimization of a Potent, Orally Active S1P 1 Agonist Containing a Quinolinone Core by Harrington, Paul E., Croghan, Michael D., Fotsch, Christopher, Frohn, Mike, Lanman, Brian A., Pennington, Lewis D., Pickrell, Alexander J., Reed, Anthony B., Sham, Kelvin K. C., Tasker, Andrew, Arnett, Heather A., Fiorino, Michael, Lee, Matthew R., McElvain, Michele, Morrison, Henry G., Xu, Han, Xu, Yang, Zhang, Xuxia, Wong, Min, Cee, Victor J.

Get full text

Discovery of a Potent, S1P 3 -Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P 1 ) by Lanman, Brian A., Cee, Victor J., Cheruku, Srinivasa R., Frohn, Mike, Golden, Jennifer, Lin, Jian, Lobera, Mercedes, Marantz, Yael, Muller, Kristine M., Neira, Susana C., Pickrell, Alexander J., Rivenzon-Segal, Dalia, Schutz, Nili, Sharadendu, Anurag, Yu, Xiang, Zhang, Zhaoda, Buys, Janet, Fiorino, Mike, Gore, Anu, Horner, Michelle, Itano, Andrea, McElvain, Michele, Middleton, Scot, Schrag, Michael, Vargas, Hugo M., Xu, Han, Xu, Yang, Zhang, Xuxia, Siu, Jerry, Bürli, Roland W.

Get full text

Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors by Frohn, Mike, Viswanadhan, Vellarkad, Pickrell, Alexander J, Golden, Jennifer E, Muller, Kristine M, Bürli, Roland W, Biddlecome, Gloria, Yoder, Sean C, Rogers, Norma, Dao, Jennifer H, Hungate, Randall, Allen, Jennifer R

“…We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which…”
Get full text