935687-49-3Relevant academic research and scientific papers
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus
Pfefferkorn, Jeffrey A.,Guzman-Perez, Angel,Litchfield, John,Aiello, Robert,Treadway, Judith L.,Pettersen, John,Minich, Martha L.,Filipski, Kevin J.,Jones, Christopher S.,Tu, Meihua,Aspnes, Gary,Risley, Hud,Bian, Jianwei,Stevens, Benjamin D.,Bourassa, Patricia,D'Aquila, Theresa,Baker, Levenia,Barucci, Nicole,Robertson, Alan S.,Bourbonais, Francis,Derksen, David R.,MacDougall, Margit,Cabrera, Over,Chen, Jing,Lapworth, Amanda Lee,Landro, James A.,Zavadoski, William J.,Atkinson, Karen,Haddish-Berhane, Nahor,Tan, Beijing,Yao, Lili,Kosa, Rachel E.,Varma, Manthena V.,Feng, Bo,Duignan, David B.,El-Kattan, Ayman,Murdande, Sharad,Liu, Shenping,Ammirati, Mark,Knafels, John,Dasilva-Jardine, Paul,Sweet, Laurel,Liras, Spiros,Rolph, Timothy P.
experimental part, p. 1318 - 1333 (2012/04/18)
Glucokinase is a key regulator of glucose homeostasis, and small molecule allosteric activators of this enzyme represent a promising opportunity for the treatment of type 2 diabetes. Systemically acting glucokinase activators (liver and pancreas) have bee
PRODRUGS OF OPIOIDS AND USES THEREOF
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Page/Page column 53, (2011/08/08)
The present invention concerns prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing more consistent pain relief by increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are provided. The invention also provides for decreasing the adverse GI side effects of opioid analgesics.
Substituted Pyrazinone Amides
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Page/Page column 15, (2010/08/07)
The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. The variables R1, R2
Electrocatalytic carboxylation of 2-amino-5-bromopyridine with CO 2 in ionic liquid 1-butyl-3-methyllimidazoliumtetrafluoborate to 6-aminonicotinic acid
Feng, Qiuju,Huang, Kelong,Liu, Suqin,Wang, Xuanyun
experimental part, p. 5741 - 5745 (2011/01/07)
A new electrochemical procedure for the electrocatalytic carboxylation of 2-amino-5-bromopyridine with CO2 in ionic liquid, 1-butyl-3-methyllimidazolium tetrafluoborate (BMIMBF4), to 6-aminonicotinic acid was investigated for the first time. The experiments were carried out in three electrodes undivided cell under mild conditions, and the use of volatile and toxic solvents and catalysts, as well as any other additional supporting electrolytes, was avoided. The electrochemical reduction behavior of 2-amino-5-bromopyridine in BMIMBF4 had been studied by cyclic voltammetry with a reduction peak at-1.6V (vs. Ag). 6-Aminonicotinic acid was obtained in 75% yield and 100% selectivity, under the optimized condition. Moreover, the ionic liquid was successfully recycled.
HETEROARYLS AMIDE DERIVATIVES AND THEIR USE AS GLUCOKINASE ACTIVATORS
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Page/Page column 65-66, (2010/04/06)
The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.
Substituted Dihydroisoindolones As Allosteric Modulators of Glucokinase
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Page/Page column 48, (2010/11/27)
The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating glucokinase mediated disorders. More particularly, the compounds of the present invention are glucokinase modulators useful for treating disorders including, but not limited to, type II diabetes.
