Search Results - "Sakwa, Samuel A."

Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators by Rynearson, Kevin D., Buckle, Ronald N., Herr, R. Jason, Mayhew, Nicholas J., Chen, Xinchao, Paquette, William D., Sakwa, Samuel A., Yang, Jinhai, Barnes, Keith D., Nguyen, Phuong, Mobley, William C., Johnson, Graham, Lin, Juinn H., Tanzi, Rudolph E., Wagner, Steven L.

“…[Display omitted] The evolution of gamma-secretase modulators (GSMs) through the introduction of novel heterocycles with the goal of aligning activity for…”
Get full text

Synthesis and Biological Evaluation of N‑((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter‑1 by Cioffi, Christopher L, Liu, Shuang, Wolf, Mark A, Guzzo, Peter R, Sadalapure, Kashinath, Parthasarathy, Visweswaran, Loong, David T. J, Maeng, Jun-Ho, Carulli, Edmund, Fang, Xiao, Karunakaran, Kalesh, Matta, Lakshman, Choo, Sok Hui, Panduga, Shailijia, Buckle, Ronald N, Davis, Randall N, Sakwa, Samuel A, Gupta, Priya, Sargent, Bruce J, Moore, Nicholas A, Luche, Michele M, Carr, Grant J, Khmelnitsky, Yuri L, Ismail, Jiffry, Chung, Mark, Bai, Mei, Leong, Wei Yee, Sachdev, Nidhi, Swaminathan, Srividya, Mhyre, Andrew J

“…We previously disclosed the discovery of rationally designed N-((1-(4-(propylsulfonyl)­piperazin-1-yl)­cycloalkyl)­methyl)­benzamide inhibitors of glycine…”
Get full text

Design and synthesis of aminothiazole modulators of the gamma-secretase enzyme by Rynearson, Kevin D., Buckle, Ronald N., Barnes, Keith D., Herr, R. Jason, Mayhew, Nicholas J., Paquette, William D., Sakwa, Samuel A., Nguyen, Phuong D., Johnson, Graham, Tanzi, Rudolph E., Wagner, Steven L.

“…[Display omitted] The design and construction of a series of novel aminothiazole-derived γ-secretase modulators is described. The incorporation of heterocyclic…”
Get full text

Bioavailable pyrrolo-benzo-1,4-diazines as Na(v)1.7 sodium channel blockers for the treatment of pain by Yang, Shu-Wei, Ho, Ginny D, Tulshian, Deen, Bercovici, Ana, Tan, Zheng, Hanisak, Jennifer, Brumfield, Stephanie, Matasi, Julius, Sun, Xianfeng, Sakwa, Samuel A, Herr, R Jason, Zhou, Xiaoping, Bridal, Terry, Urban, Mark, Vivian, Jeffrey, Rindgen, Diane, Sorota, Steve

“…A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized to improve the profile of the previous lead compound 1. The syntheses, structure-activity…”
Get full text

A Concise Palladium-Catalyzed Carboamination Route to (±)-Tylophorine by Rossiter, Lana M, Slater, Meagan L, Giessert, Rachel E, Sakwa, Samuel A, Herr, R. Jason

“…A total synthesis of the racemic natural product tylophorine [(±)-1] has been demonstrated using the palladium-catalyzed carboamination method developed by…”
Get full text

Synthesis and Suzuki–Miyaura reactions of 5-halo-3,4-dihydropyrimidin-2(1 H)-ones by Zych, Andrew J., Wang, Hong-Jun, Sakwa, Samuel A.

“…A novel synthesis of 6-methyl-4-phenyl-5-substituted-3,4-dihydropyrimidin-2(1 H)-ones from 6-methyl-4-phenyl-5-halo-3,4-dihydropyrimidin-2(1 H)-ones via the…”
Get full text

The optimization of pyridazinone series of glucan synthase inhibitors by Kuang, Rongze, Wu, Heping, Ting, Pauline C., Aslanian, Robert G., Cao, Jianhua, Kim, David W., Lee, Joe F., Schwerdt, John, Zhou, Gang, Jason Herr, R., Zych, Andrew J., Yang, Jinhai, Lam, Sang Q., Jenkins, David M., Sakwa, Samuel A., Wainhaus, Samuel, Black, Todd A., Cacciapuoti, Anthony, McNicholas, Paul M., Xu, Yiming, Walker, Scott S.

“…A detailed structure–activity relationship study of a novel series of pyridazine-based small molecule glucan synthase inhibitors is described. The optimization…”
Get full text

Bioavailable pyrrolo-benzo-1,4-diazines as Nav1.7 sodium channel blockers for the treatment of pain by Yang, Shu-Wei, Ho, Ginny D., Tulshian, Deen, Bercovici, Ana, Tan, Zheng, Hanisak, Jennifer, Brumfield, Stephanie, Matasi, Julius, Sun, Xianfeng, Sakwa, Samuel A., Herr, R. Jason, Zhou, Xiaoping, Bridal, Terry, Urban, Mark, Vivian, Jeffrey, Rindgen, Diane, Sorota, Steve

“…A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5…”
Get full text

Bioavailable pyrrolo-benzo-1,4-diazines as Na sub(v)1.7 sodium channel blockers for the treatment of pain by Yang, Shu-Wei, Ho, Ginny D, Tulshian, Deen, Bercovici, Ana, Tan, Zheng, Hanisak, Jennifer, Brumfield, Stephanie, Matasi, Julius, Sun, Xianfeng, Sakwa, Samuel A, Herr, RJason, Zhou, Xiaoping, Bridal, Terry, Urban, Mark, Vivian, Jeffrey, Rindgen, Diane, Sorota, Steve

“…A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized to improve the profile of the previous lead compound 1. The syntheses, structure-activity…”
Get full text