Xiaohui Du
Amgen
42 Papers
328 Citations
Xiaohui Du is an academic researcher from Amgen. The author has contributed to research in topics: Triazole & Chemistry. The author has an hindex of 15, co-authored 42 publications.
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Papers
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles
Yingcai Wang,Jiwen Jim Liu,Paul John Dransfield,Liusheng Zhu,Zhongyu Wang,Xiaohui Du,Xianyun Jiao,Yongli Su,An-Rong Li,Sean P. Brown,Annie Kasparian,Marc Vimolratana,Ming Yu,Vatee Pattaropong,Jonathan B. Houze,Gayathri Swaminath,Thanhvien Tran,Khanh Nguyen,Qi Guo,Jane Zhang,Run Zhuang,Frank Li,Lynn Miao,Michael D. Bartberger,Tiffany L. Correll,David Chow,Simon Wong,Jian Luo,Daniel C.-H. Lin,Julio C. Medina +29 more
TL;DR: The discovery of GPR40 full agonists containing conformationally constrained tricyclic spirocycles and their structure-activity relationships leading to more potent agonists such as AM-5262 with improved rat PK profile and general selectivity profile are presented.
Patent
Aryl nitrile compounds and compositions and their uses in treating inflammatory and related disorders
Philippe Bergeron,Xiaoqi Chen,Xiaohui Du,Jeffrey Deignan,Jason Duquette,Darin J. Gustin,Julio C. Medina,Jeffrey T. Mihalic,George Tonn +8 more
- 26 Jun 2006
TL;DR: In this article, aryl nitrile compounds which modulate the expression and/or function of a chemokine receptor were provided for the treatment of inflammatory and immunoregulatory disorders such as multiple sclerosis, rheumatoid arthritis, type I diabetes, asthma, psoriasis and inflammatory bowel disease.
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Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
An-Rong Li,Michael G. Johnson,Jiwen Liu,Xiaoqi Chen,Xiaohui Du,Jeffrey T. Mihalic,Jeffrey Deignan,Darin J. Gustin,Jason Duquette,Zice Fu,Liusheng Zhu,Andrew P. Marcus,Phillipe Bergeron,Lawrence R. McGee,Jay Danao,Bryan Lemon,Teresa Arazas Carabeo,Tim Sullivan,Ji Ma,Liang Tang,George Tonn,Tassie L. Collins,Julio C. Medina +22 more
TL;DR: A series of six-six and six-five fused heterocyclic CXCR3 antagonists has been synthesized and their activities evaluated in an [(125)I]-IP-10 displacement assay and an ITAC mediated in vitro cell migration assay, leading to the discovery of compounds with increased potency and improved pharmacokinetic properties that could serve as useful tools to study the role of the CX CR3 receptor in vivo.
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Imidazo-pyrazine derivatives as potent CXCR3 antagonists
Xiaohui Du,Darin J. Gustin,Xiaoqi Chen,Jason Duquette,Lawrence R. McGee,Zhulun Wang,Karen Ebsworth,Kirk Henne,Bryan Lemon,Ji Ma,Shichang Miao,Emmanuel Sabalan,Tim Sullivan,George Tonn,Tassie L. Collins,Julio C. Medina +15 more
TL;DR: Optimization efforts led to the discovery of a series of imidazo-pyrazine derivatives with improved pharmacokinetic properties in addition to increased potency of CXCR3 antagonists with fused hetero-bicyclic cores.
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Patent
Substituted biphenyl gpr40 modulators
Yong-Jae Kim,Sean P. Brown,Qiong Cao,Paul John Dransfield,Xiaohui Du,Jonathan B. Houze,Xian Yun Jiao,Todd J. Kohn,Sujen Lai,An-Rong Li,Daniel Lin,Jian Luo,Julio C. Medina,Reagan Jeffrey D,Vatee Pattaropong,Margrit Schwarz,Wang Shen,Yongli Su,Gayathri Swaminath,Marc Vimolratana,Wang Xiang,Yumei Xiong,Li Yang,Ming Yu,Jie Zhang,Liusheng Zhu,Yingcai Wang,Jiwen Liu,Zica Fu +28 more
- 03 Oct 2008
TL;DR: In this paper, a general formula for I: where the definitions of the variables are provided herein is presented. And the present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
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