Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Qingyian Liu"'
Autor:
Michael D. Bartberger, Vijay Keshav Gore, Mark R. Fielden, Ryan White, Qingyian Liu, E. Allen Sickmier, Stephen J. Wood, Jonathan D. Low, Jonathan Werner, Yuan Cheng, Dean Hickman, Hugo M. Vargas, Douglas A. Whittington, Ana Elena Minatti, Kui Chen
Publikováno v:
MedChemComm. 8:1196-1206
As part of an ongoing effort at Amgen to develop a disease-modifying therapy for Alzheimer's disease, we have previously used the aminooxazoline xanthene (AOX) scaffold to generate potent and orally efficacious BACE1 inhibitors. While AOX-BACE1 inhib
Autor:
Paul H. Wen, Stephen J. Wood, Qingyian Liu, Aaron C. Siegmund, Liping H. Pettus, Adrian Nanez, Matthew P. Bourbeau, Jennifer R. Allen, Michael D. Bartberger, Douglas A. Whittington, Jodi Bradley, James R. Manning, Kui Chen, Dean Hickman, Michael E. Johnson
Publikováno v:
Journal of medicinal chemistry. 63(5)
β-Site amyloid precursor protein cleaving enzyme 1 (BACE1) is an aspartyl protease that plays a key role in the production of amyloid β (Aβ) in the brain and has been extensively pursued as a target for the treatment of Alzheimer's disease (AD). B
Autor:
Jeffrey Clarine, Qingyian Liu, Beth D. Youngblood, Chester Chenguang Yuan, Michelle Horner, James Brown, Jian J. Chen, Michael D. Bartberger, Vu Van Ma, Matthew R. Kaller, Carl D. Davis, Maosheng Zhang, Thomas T. Nguyen, Narender R. Gavva, Scott Harried, Sonya G. Lehto, Jennifer R. Allen, Holger Monenschein, Daniel B. Horne, Vijay Keshav Gore, Wenge Zhong, Kaustav Biswas
Publikováno v:
Journal of medicinal chemistry. 61(18)
Transient-receptor-potential melastatin 8 (TRPM8), the predominant mammalian cold-temperature thermosensor, is a nonselective cation channel expressed in a subpopulation of sensory neurons in the peripheral nervous system, including nerve circuitry i
Autor:
Qingyian Liu, Kaustav Biswas, Frank Koegler, Tiffany L. Correll, Toni Williamson, Jodi Bradley, Jennifer R. Allen, Leeanne Zalameda, Darren L. Reid, Michael D. Bartberger, Joe Zhu, Stephen J. Wood, Randy Hungate, Yichin Liu, Frank Chavez, Robert M. Rzasa, Jianhua Zhang, John D. McCarter, Thomas Nixey, Paul H. Wen, Li Zhu, Shannon Rumfelt, Yi Luo, Safura Babu-Khan, Stephen Hitchcock, Ning Chen, Mqhele Ncube, Wenyuan Qian, Frenel Fils Demorin, Dean Hickman, Christopher M. Tegley, Jian J. Chen, Albert Amegadzie, Charles W. Dean, Chester Chenguang Yuan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6447-6454
γ-Secretase modulators (GSMs) are potentially disease-modifying treatments for Alzheimer's disease. They selectively lower pathogenic Aβ42 levels by shifting the enzyme cleavage sites without inhibiting γ-secretase activity, possibly avoiding know
Autor:
Maurice Emery, Rod Cupples, David J. St. Jean, George A. Moniz, David Pyring, Randall W. Hungate, Chester Chenguang Yuan, Lars Johansson, Aiwen Li, Michelle Chen, Qingyian Liu, Meredith Williams, Steven R. Jordan, Lynn Cai, Lars Tedenborg, Minghan Wang, Christopher H. Fotsch, Nianhe Han, Michael D. Bartberger, Jiandong Zhang, Clarence Hale, Yaxiong Sun, Ben C. Askew
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6056-6061
A series of 2-anilinothiazolones were prepared as inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). The most potent compounds contained a 2-chloro or 2-fluoro group on the aniline ring with an isopropyl substituent on the 5-posi
Autor:
Burgess Laurence E, Leyla Arik, Chester Chenguang Yuan, Nianhe Han, Randall W. Hungate, Derin C. D'amico, David A. Mareska, Feng-Yin Hsieh, Eileen Johnson, Hong Sun, Qingyian Liu, Barton H. Manning, Bobby Riahi, Christopher H. Fotsch, Gloria Biddlecome, Mark H. Norman, Augustus Kamassah, Ming Huang, Richard Loeloff, Gondi N. Kumar, Andras Toro, Jian J. Chen, Jason Brooks Human, Hideo Suzuki, Robert D. Groneberg, Benny C. Askew, Aiwen Li, Gordon Ng, James Zhan, Kaustav Biswas, Dianna Lester-Zeiner, Hong Dong, David E. Clarke
Publikováno v:
Journal of Medicinal Chemistry. 50:2200-2212
The bradykinin B1 receptor is induced following tissue injury and/or inflammation. Antagonists of this receptor have been studied as promising candidates for treatment of chronic pain. We have identified aryl sulfonamides containing a chiral chroman
Autor:
Qingyian Liu, Randall W. Hungate, Rami Tamir, Shimin Xu, Elizabeth M. Doherty, James J. S. Treanor, Christopher H. Fotsch, Mark H. Norman, Lana Klionsky, Yunxin Bo, Nianhe Han, Ning Xi, Narender R. Gavva
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5211-5217
A thiazole derivative, 2-(2,6-dichlorobenzyl)-N-(4-isopropylphenyl) thiazole-4-carboxamide (1), was identified as a TRPV1 antagonist. We synthesized various thiazole analogs and evaluated them for their ability to block capsaicin- or acid-induced cal
Autor:
Nuria A. Tamayo, Shimin Xu, Michael G. Kelly, Duncan M. Smith, Ning Chen, Michelle Carmouche, Mark H. Norman, Martin H. Goldberg, James Davis, Christopher H. Fotsch, Clarence Hale, Ning Xi, Markian Stec, James W. Baumgartner, Premilla Arasasingham, Nianhe Han, Feng-Yin Hsieh, Qingyian Liu, Yunxin Bo, Anthony W. Bannon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1623-1627
The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. Compounds from this set had binding and functional activities at MC4R less than 30 nM.
Autor:
Yuelie Lu, Ling Wang, Michael Handley, Ning Xi, Stephen Arvedson, Andrew Tasker, Jiandong Zhang, Tingjian Xiang, Osslund Timothy D, Celia Dominguez, Qi Huang, Liang Huang, David Powers, Nianhe Han, Gladys Nunez, Qingyian Liu, Jiawang Zhu, Shawn Eisenberg, Shimin Xu, Alexander S. Kiselyov, Richard Kendall
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2905-2909
Novel αvβ3 antagonists based on the N-aryl-γ-lactam scaffold were prepared. SAR studies led to the identification of potent antagonists for αvβ3 receptor with excellent selectivity against the structurally related αIIbβ3 receptor. Additional i
Autor:
Vinod F. Patel, Timothy Powers, Michael D. Bartberger, Ted Judd, Ryan White, Stephen J. Wood, Ana Elena Minatti, Stephen Hitchcock, Vijay Keshav Gore, Wenge Zhong, Hugo M. Vargas, Jason Brooks Human, Kui Chen, Steven Vonderfecht, Robert T. Fremeau, Robert T. Dunn, James Brown, Patricia Lopez, Qingyian Liu, Vu Van Ma, Nancy E. Everds, Matthew Weiss, Charles Kreiman, Oleg Epstein, May Xue, Chester Chenguang Yuan, Jonathan Werner, Alan C. Cheng, Jian J. Chen, Albert Amegadzie, Paul H. Wen, Yuan Cheng, Douglas A. Whittington, Wenyuan Qian, Isaac E. Marx, Thomas Dineen, Dean Hickman
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(4)
The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer’s disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-aza