Search Results - "Ye, Xiaocong M."

Novel cinnoline-based inhibitors of LRRK2 kinase activity by 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

“…Leucine rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson’s disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic…”
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Triazolopyridazine LRRK2 kinase inhibitors by 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

“…Leucine-rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson’s disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic…”
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Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors by 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

“…Mutations in leucine-rich repeat kinase 2 (LRRK2) are associated with familial Parkinson’s disease (PD). The kinase activity of this complex protein is…”
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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro‑2H‑pyrazolo[4,3‑c]quinoline (ELND007): Metabolically Stable γ‑Secretase Inhibitors that Selectively Inhibit the Production of Amyloid‑β over Notch by Probst, Gary, Aubele, Danielle L, Bowers, Simeon, Dressen, Darren, Garofalo, Albert W, Hom, Roy K, Konradi, Andrei W, Marugg, Jennifer L, Mattson, Matthew N, Neitzel, Martin L, Semko, Chris M, Sham, Hing L, Smith, Jenifer, Sun, Minghua, Truong, Anh P, Ye, Xiaocong M, Xu, Ying-zi, Dappen, Michael S, Jagodzinski, Jacek J, Keim, Pamela S, Peterson, Brian, Latimer, Lee H, Quincy, David, Wu, Jing, Goldbach, Erich, Ness, Daniel K, Quinn, Kevin P, Sauer, John-Michael, Wong, Karina, Zhang, Hongbin, Zmolek, Wes, Brigham, Elizabeth F, Kholodenko, Dora, Hu, Kang, Kwong, Grace T, Lee, Michael, Liao, Anna, Motter, Ruth N, Sacayon, Patricia, Santiago, Pamela, Willits, Christopher, Bard, Frédérique, Bova, Michael P, Hemphill, Susanna S, Nguyen, Lam, Ruslim, Lany, Tanaka, Kevin, Tanaka, Pearl, Wallace, William, Yednock, Ted A, Basi, Guriqbal S

“…Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We…”
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Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors by 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.

“…Structure–activity relationship (SAR) of a novel, potent and metabolically stable series of benzo [3.2.1] bicyclic sulfonamide-pyrazoles as γ-secretase…”
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Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious γ-Secretase Inhibitors by Ye, Xiaocong M., Konradi, Andrei W., Smith, Jenifer, Xu, Ying-Zi, Dressen, Darren, Garofalo, Albert W., Marugg, Jennifer, Sham, Hing L., Truong, Anh P., Jagodzinski, Jacek, Pleiss, Michael, Zhang, Hongbin, Goldbach, Erich, Sauer, John-Michael, Brigham, Elizabeth, Bova, Michael, Basi, Guriqbal S.

“…Discovery of a series of pyrazolopiperidine sulfonamide based γ-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency…”
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Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious γ-secretase inhibitors (Part II) by Ye, Xiaocong M., Konradi, Andrei W., Smith, Jenifer, Aubele, Danielle L., Garofalo, Albert W., Marugg, Jennifer, Neitzel, Marty L., Semko, Chris M., Sham, Hing L., Sun, Minghua, Truong, Anh P., Wu, Jing, Zhang, Hongbin, Goldbach, Erich, Sauer, John-Michael, Brigham, Elizabeth F., Bova, Michael, Basi, Guriqbal S.

“…Significant improvement in metabolic stability on the pyrazolopiperidine scaffold over the original series were achieved and this stability improvement…”
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Discovery of ( R )-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1 H -pyrazolo[4,3- c ]quinoline (ELND006) and ( R )-4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2 H -pyrazolo[4,3- c ]quinoline (ELND007): Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch by Probst, Gary, Aubele, Danielle L., Bowers, Simeon, Dressen, Darren, Garofalo, Albert W., Hom, Roy K., Konradi, Andrei W., Marugg, Jennifer L., Mattson, Matthew N., Neitzel, Martin L., Semko, Chris M., Sham, Hing L., Smith, Jenifer, Sun, Minghua, Truong, Anh P., Ye, Xiaocong M., Xu, Ying-zi, Dappen, Michael S., Jagodzinski, Jacek J., Keim, Pamela S., Peterson, Brian, Latimer, Lee H., Quincy, David, Wu, Jing, Goldbach, Erich, Ness, Daniel K., Quinn, Kevin P., Sauer, John-Michael, Wong, Karina, Zhang, Hongbin, Zmolek, Wes, Brigham, Elizabeth F., Kholodenko, Dora, Hu, Kang, Kwong, Grace T., Lee, Michael, Liao, Anna, Motter, Ruth N., Sacayon, Patricia, Santiago, Pamela, Willits, Christopher, Bard, Frédérique, Bova, Michael P., Hemphill, Susanna S., Nguyen, Lam, Ruslim, Lany, Tanaka, Kevin, Tanaka, Pearl, Wallace, William, Yednock, Ted A., Basi, Guriqbal S.

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Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious [gamma]-secretase inhibitors by 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

“…Structure-activity relationship (SAR) of a novel, potent and metabolically stable series of benzo [3.2.1] bicyclic sulfonamide-pyrazoles as [gamma]-secretase…”
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Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious g-Secretase Inhibitors by Ye, Xiaocong M, Konradi, Andrei W, Smith, Jenifer, Xu, Ying-Zi, Dressen, Darren, Garofalo, Albert W, Marugg, Jennifer, Sham, Hing L, Truong, Anh P, Jagodzinski, Jacek, Pleiss, Michael, Zhang, Hongbin, Goldbach, Erich, Sauer, John-Michael, Brigham, Elizabeth, Bova, Michael, Basi, Guriqbal S

“…Discovery of a series of pyrazolopiperidine sulfonamide based g-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency…”
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