Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-( N, N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor
Zhang, Penglie, Huang, Wenrong, Wang, Lingyan, Bao, Liang, Jia, Zhaozhong J., Bauer, Shawn M., Goldman, Erick A., Probst, Gary D., Song, Yonghong, Su, Ting, Fan, Jingmei, Wu, Yanhong, Li, Wenhao, Woolfrey, John, Sinha, Uma, Wong, Paul W., Edwards, Susan T., Arfsten, Ann E., Clizbe, Lane A., Kanter, James, Pandey, Anjali, Park, Gary, Hutchaleelaha, Athiwat, Lambing, Joseph L., Hollenbach, Stanley J., Scarborough, Robert M., Zhu, Bing-Yan
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
Get full text
Journal Article
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model
Truong, Anh P., Tóth, Gergley, Probst, Gary D., Sealy, Jennifer M., Bowers, Simeon, Wone, David W.G., Dressen, Darren, Hom, Roy K., Konradi, Andrei W., Sham, Hing L., Wu, Jing, Peterson, Brian T., Ruslim, Lany, Bova, Michael P., Kholodenko, Dora, Motter, Ruth N., Bard, Frédérique, Santiago, Pamela, Ni, Huifang, Chian, David, Soriano, Ferdie, Cole, Tracy, Brigham, Elizabeth F., Wong, Karina, Zmolek, Wes, Goldbach, Erich, Samant, Bhushan, Chen, Linda, Zhang, Hongbing, Nakamura, David F., Quinn, Kevin P., Yednock, Ted A., Sauer, John-Michael
Published in Bioorganic & medicinal chemistry letters (01.11.2010)
Published in Bioorganic & medicinal chemistry letters (01.11.2010)
Get full text
Journal Article
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor
Bowers, Simeon, Truong, Anh P., Neitz, R. Jeffrey, Neitzel, Martin, Probst, Gary D., Hom, Roy K., Peterson, Brian, Galemmo, Robert A., Konradi, Andrei W., Sham, Hing L., Tóth, Gergley, Pan, Hu, Yao, Nanhua, Artis, Dean R., Brigham, Elizabeth F., Quinn, Kevin P., Sauer, John-Michael, Powell, Kyle, Ruslim, Lany, Ren, Zhao, Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene
Published in Bioorganic & medicinal chemistry letters (15.03.2011)
Published in Bioorganic & medicinal chemistry letters (15.03.2011)
Get full text
Journal Article
Design and synthesis of cell potent BACE-1 inhibitors: Structure–activity relationship of P1′ substituents
Sealy, Jennifer M., Truong, Anh P., Tso, Luke, Probst, Gary D., Aquino, Jose, Hom, Roy K., Jagodzinska, Barbara M., Dressen, Darren, Wone, David W.G., Brogley, Louis, John, Varghese, Tung, Jay S., Pleiss, Michael A., Tucker, John A., Konradi, Andrei W., Dappen, Michael S., Toth, Gergely, Pan, Hu, Ruslim, Lany, Miller, Jim, Bova, Michael P., Sinha, Sukanto, Quinn, Kevin P., Sauer, John-Michael
Published in Bioorganic & medicinal chemistry letters (15.11.2009)
Published in Bioorganic & medicinal chemistry letters (15.11.2009)
Get full text
Journal Article
Ruthenium-Catalyzed Alder Ene Type Reactions. A Formal Synthesis of Alternaric Acid
Trost, Barry M, Probst, Gary D, Schoop, Andreas
Published in Journal of the American Chemical Society (16.09.1998)
Published in Journal of the American Chemical Society (16.09.1998)
Get full text
Journal Article
Novel cinnoline-based inhibitors of LRRK2 kinase activity
Garofalo, Albert W., Adler, Marc, Aubele, Danielle L., Bowers, Simeon, Franzini, Maurizio, Goldbach, Erich, Lorentzen, Colin, Neitz, R. Jeffrey, Probst, Gary D., Quinn, Kevin P., Santiago, Pam, Sham, Hing L., Tam, Danny, Truong, Anh P., Ye, Xiaocong M., Ren, Zhao
Published in Bioorganic & medicinal chemistry letters (01.01.2013)
Published in Bioorganic & medicinal chemistry letters (01.01.2013)
Get full text
Journal Article
Triazolopyridazine LRRK2 kinase inhibitors
Franzini, Maurizio, Ye, Xiaocong M., Adler, Marc, Aubele, Danielle L., Garofalo, Albert W., Gauby, Shawn, Goldbach, Erich, Probst, Gary D., Quinn, Kevin P., Santiago, Pam, Sham, Hing L., Tam, Danny, Truong, Anh, Ren, Zhao
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
Get full text
Journal Article
Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors
Garofalo, Albert W., Adler, Marc, Aubele, Danielle L., Brigham, Elizabeth F., Chian, David, Franzini, Maurizio, Goldbach, Erich, Kwong, Grace T., Motter, Ruth, Probst, Gary D., Quinn, Kevin P., Ruslim, Lany, Sham, Hing L., Tam, Danny, Tanaka, Pearl, Truong, Anh P., Ye, Xiaocong M., Ren, Zhao
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
Get full text
Journal Article
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration
Bowers, Simeon, Truong, Anh P., Jeffrey Neitz, R., Hom, Roy K., Sealy, Jennifer M., Probst, Gary D., Quincy, David, Peterson, Brian, Chan, Wayman, Galemmo, Robert A., Konradi, Andrei W., Sham, Hing L., Tóth, Gergely, Pan, Hu, Lin, May, Yao, Nanhua, Artis, Dean R., Zhang, Heather, Chen, Linda, Dryer, Mark, Samant, Bhushan, Zmolek, Wes, Wong, Karina, Lorentzen, Colin, Goldbach, Erich, Tonn, George, Quinn, Kevin P., Sauer, John-Michael, Wright, Sarah, Powell, Kyle, Ruslim, Lany, Ren, Zhao, Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Get full text
Journal Article
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration
Probst, Gary D., Bowers, Simeon, Sealy, Jennifer M., Truong, Anh P., Hom, Roy K., Galemmo, Robert A., Konradi, Andrei W., Sham, Hing L., Quincy, David A., Pan, Hu, Yao, Nanhua, Lin, May, Tóth, Gergley, Artis, Dean R., Zmolek, Wes, Wong, Karina, Qin, Ann, Lorentzen, Colin, Nakamura, David F., Quinn, Kevin P., Sauer, John-Michael, Powell, Kyle, Ruslim, Lany, Wright, Sarah, Chereau, David, Ren, Zhao, Anderson, John P., Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene
Published in Bioorganic & medicinal chemistry letters (01.01.2011)
Published in Bioorganic & medicinal chemistry letters (01.01.2011)
Get full text
Journal Article
Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates
Bowers, Simeon, Xu, Ying-zi, Yuan, Shendong, Probst, Gary D., Hom, Roy K., Chan, Wayman, Konradi, Andrei W., Sham, Hing L., Zhu, Yong L., Beroza, Paul, Pan, Hu, Brecht, Eric, Yao, Nanhua, Lougheed, Julie, Tam, Danny, Ren, Zhao, Ruslim, Lany, Bova, Michael P., Artis, Dean R.
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
Get full text
Journal Article
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors
Ye, Xiaocong M., Konradi, Andrei W., Sun, Minghua, Yuan, Shendong, Aubele, Danielle L., Dappen, Michael, Dressen, Darren, Garofalo, Albert W., Jagodzinski, Jacek J., Latimer, Lee, Probst, Gary D., Sham, Hing L., Wone, David, Xu, Ying-zi, Ness, Daniel, Brigham, Elizabeth, Kwong, Grace T., Willtis, Chris, Tonn, George, Goldbach, Erich, Quinn, Kevin P., Zhang, Hongbin H., Sauer, John-Michael, Bova, Michael, Basi, Guriqbal S.
Published in Bioorganic & medicinal chemistry letters (15.02.2013)
Published in Bioorganic & medicinal chemistry letters (15.02.2013)
Get full text
Journal Article
Design, synthesis, and structure–activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline γ-secretase inhibitors
Truong, Anh P., Aubele, Danielle L., Probst, Gary D., Neitzel, Martin L., Semko, Chris M., Bowers, Simeon, Dressen, Darren, Hom, Roy K., Konradi, Andrei W., Sham, Hing L., Garofalo, Albert W., Keim, Pamela S., Wu, Jing, Dappen, Michael S., Wong, Karina, Goldbach, Erich, Quinn, Kevin P., Sauer, John-Michael, Brigham, Elizabeth F., Wallace, William, Nguyen, Lan, Hemphill, Susanna S., Bova, Michael P., Basi, Guriqbal
Published in Bioorganic & medicinal chemistry letters (01.09.2009)
Published in Bioorganic & medicinal chemistry letters (01.09.2009)
Get full text
Journal Article
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Prime side chromane-containing inhibitors
Ng, Raymond A., Sun, Minghua, Bowers, Simeon, Hom, Roy K., Probst, Gary D., John, Varghese, Fang, Lawrence Y., Maillard, Michel, Gailunas, Andrea, Brogley, Louis, Neitz, R. Jeffrey, Tung, Jay S., Pleiss, Michael A., Konradi, Andrei W., Sham, Hing L., Dappen, Michael S., Adler, Marc, Yao, Nanhua, Zmolek, Wes, Nakamura, David, Quinn, Kevin P., Sauer, John-Michael, Bova, Michael P., Ruslim, Lany, Artis, Dean R., Yednock, Ted A.
Published in Bioorganic & medicinal chemistry letters (15.08.2013)
Published in Bioorganic & medicinal chemistry letters (15.08.2013)
Get full text
Journal Article
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK
Hom, Roy K., Bowers, Simeon, Sealy, Jennifer M., Truong, Anh P., Probst, Gary D., Neitzel, Martin L., Neitz, R. Jeffrey, Fang, Larry, Brogley, Louis, Wu, Jing, Konradi, Andrei W., Sham, Hing L., Tóth, Gergely, Pan, Hu, Yao, Nanhua, Artis, Dean R., Quinn, Kevin, Sauer, John-Michael, Powell, Kyle, Ren, Zhao, Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene
Published in Bioorganic & medicinal chemistry letters (15.12.2010)
Published in Bioorganic & medicinal chemistry letters (15.12.2010)
Get full text
Journal Article
A Formal Synthesis of (−)-Mycalamide A
Trost, Barry M, Yang, Hanbiao, Probst, Gary D
Published in Journal of the American Chemical Society (14.01.2004)
Published in Journal of the American Chemical Society (14.01.2004)
Get full text
Journal Article
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: Structure–activity relationship of P2′ substituents
Truong, Anh P., Probst, Gary D., Aquino, Jose, Fang, Larry, Brogley, Louis, Sealy, Jennifer M., Hom, Roy K., Tucker, John A., John, Varghese, Tung, Jay S., Pleiss, Michael A., Konradi, Andrei W., Sham, Hing L., Dappen, Michael S., Tóth, Gergley, Yao, Nanhua, Brecht, Eric, Pan, Hu, Artis, Dean R., Ruslim, Lany, Bova, Michael P., Sinha, Sukanto, Yednock, Ted A., Zmolek, Wes, Quinn, Kevin P., Sauer, John-Michael
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
Get full text
Journal Article
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Structure–activity relationship of the aryl region
Probst, Gary D., Bowers, Simeon, Sealy, Jennifer M., Stupi, Brian, Dressen, Darren, Jagodzinska, Barbara M., Aquino, Jose, Gailunas, Andrea, Truong, Anh P., Tso, Luke, Xu, Ying-Zi, Hom, Roy K., John, Varghese, Tung, Jay S., Pleiss, Michael A., Tucker, John A., Konradi, Andrei W., Sham, Hing L., Jagodzinski, Jacek, Toth, Gergely, Brecht, Eric, Yao, Nanhua, Pan, Hu, Lin, May, Artis, Dean R., Ruslim, Lany, Bova, Michael P., Sinha, Sukanto, Yednock, Ted A., Gauby, Shawn, Zmolek, Wes, Quinn, Kevin P., Sauer, John-Michael
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
Get full text
Journal Article
Design, synthesis and structure–activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors
Aubele, Danielle L., Truong, Anh P., Dressen, Darren B., Probst, Gary D., Bowers, Simeon, Mattson, Matthew N., Semko, Chris M., Sun, Minghua, Garofalo, Albert W., Konradi, Andrei W., Sham, Hing L., Zmolek, Wes, Wong, Karina, Goldbach, Erich, Quinn, Kevin P., Sauer, John-Michael, Brigham, Elizabeth F., Wallace, William, Nguyen, Lan, Bova, Michael P., Hemphill, Susanna S., Basi, Guriqbal
Published in Bioorganic & medicinal chemistry letters (01.10.2011)
Published in Bioorganic & medicinal chemistry letters (01.10.2011)
Get full text
Journal Article
N-Bridged bicyclic sulfonamides as inhibitors of γ-secretase
Bowers, Simeon, Probst, Gary D., Truong, Anh P., Hom, Roy K., Konradi, Andrei W., Sham, Hing L., Garofalo, Albert W., Wong, Karina, Goldbach, Erich, Quinn, Kevin P., Sauer, John-Michael, Wallace, William, Nguyen, Lan, Hemphill, Susanna S., Bova, Michael P., Basi, Guriqbal S.
Published in Bioorganic & medicinal chemistry letters (15.12.2009)
Published in Bioorganic & medicinal chemistry letters (15.12.2009)
Get full text
Journal Article