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Your search keyword '"Xing, Charles"' showing total 2 results
Start Over Author "Xing, Charles" Publisher elsevier b.v.
2 results on '"Xing, Charles"'

1. Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P1 agonists

Author

Buzard, Daniel, Han, Sangdon, Thoresen, Lars, Moody, Jeanne, Lopez, Luis, Kawasaki, Andrew, Schrader, Thomas, Sage, Carleton, Gao, Yinghong, Edwards, Jeff, Barden, Jeremy, Thatte, Jayant, Fu, Lixia, Solomon, Michelle, Liu, Ling, Al-Shamma, Hussien, Gatlin, Joel, Le, Minh, Xing, Charles, and Espinola, Sheryll

Subjects
*PHARMACEUTICAL research, *DRUG synergism, *BUTYRIC acid, *LYMPHOPENIA, *AUTOIMMUNE disease treatment, *SPHINGOSINE, *PHOSPHATES, *DRUG receptors
Abstract

Abstract: S1P1 receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P1 receptor agonists, we have identified a novel chemical series of 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acid S1P1 receptor agonists. [Copyright &y& Elsevier]

Published
2011
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2. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control

Author

Semple, Graeme, Ren, Albert, Fioravanti, Beatriz, Pereira, Guillherme, Calderon, Imelda, Choi, Karoline, Xiong, Yifeng, Shin, Young-Jun, Gharbaoui, Tawfik, Sage, Carleton R., Morgan, Michael, Xing, Charles, Chu, Zhi-Liang, Leonard, James N., Grottick, Andrew J., Al-Shamma, Hussein, Liang, Yin, Demarest, Keith T., and Jones, Robert M.

Subjects
*DRUG development, *CELL receptors, *G proteins, *TREATMENT of diabetes, *LABORATORY rats, *BLOOD sugar, *PYRIMIDINES, *METABOLISM
Abstract

Abstract: We herein outline the design of a new series of agonists of the pancreatic and GI-expressed orphan G-protein coupled receptor GPR119, a target that has been of significant recent interest in the field of metabolism, starting from our prototypical agonist AR231453. A number of key parameters were improved first by incorporation of a pyrazolopyrimidine core to create a new structural series and secondly by the introduction of a piperidine ether group capped with a carbamate. Chronic treatment with one compound from the series, 3k, showed for the first time that blood glucose and glycated hemoglobin (HbA1c) levels could be significantly reduced in Zucker Diabetic Fatty (ZDF) rats over several weeks of dosing. As a result of these and other data described here, 3k (APD668, JNJ-28630368) was the first compound with this mechanism of action to be progressed into clinical development for the treatment of diabetes. [Copyright &y& Elsevier]

Published
2011
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