- NOVEL SGLT INHIBITORS
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The present invention relates to novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula (I) and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
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Page/Page column 56-57
(2013/02/28)
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- Novel L-xylose derivatives as selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes
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The prevalence of diabetes throughout the world continues to increase and has become a major health issue. Recently there have been several reports of inhibitors directed toward the sodium-dependent glucose cotransporter 2 (SGLT2) as a method of maintaining glucose homeostasis in diabetic patients. Herein we report the discovery of the novel O-xyloside 7c that inhibits SGLT2 in vitro and urinary glucose reabsorption in vivo. 2009 American Chemical Society.
- Goodwin, Nicole C.,Mabon, Ross,Harrison, Bryce A.,Shadoan, Melanie K.,Almstead, Zheng Y.,Xie, Yiling,Healy, Jason,Buhring, Lindsey M.,DaCosta, Christopher M.,Bardenhagen, Jennifer,Mseeh, Faika,Liu, Qingyun,Nouraldeen, Amr,Wilson, Alan G. E.,Kimball, S. David,Powell, David R.,Rawlins, David B.
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supporting information; experimental part
p. 6201 - 6204
(2010/03/31)
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- INHIBITORS OF SODIUM GLUCOSE CO-TRANSPORTER 2 AND METHODS OF THEIR USE
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Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.
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Page/Page column 22
(2008/06/13)
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- Synthesis and biological evaluation of some 4′-C-(hydroxymethyl)- α- and -β-D-arabinofuranosyl pyrimidine and adenine nucleosides
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A series of 4′-C-(hydroxymethyl) analogs of pyrimidine and purine nucleosides have been prepared utilizing standard methodologies, and the α and β anomers were separated. These analogs are part of our continuing efforts to identify new anticancer drugs as well as to explore the substrate specificities of these analogs with the initial activating enzymes in the metabolic pathway leading to nucleoside triphosphates. Although not cytotoxic to CCRF-CEM cells (an acute lymphoblastic leukemia of T-cell origin), many of these compounds were utilized as substrates for the various human nucleoside kinases, including deoxycytidine kinase, thymidine kinase 1, and thymidine kinase 2. Because the 4′-C-(hydroxymethyl) analog of arabinofuranosyl cytosine was identified as a good substrate with deoxycytidine kinase, its metabolism in CEM cells was evaluated. These results indicated that nucleosides with this modification could be activated in human cells without cytotoxicity, which suggested that they should be examined for antiviral activity.
- Griffon, Jean-Francois,Shaddix, Sue C.,Parker, William B.,Al-Madhoun, Ashraf S.,Eriksson, Staffan,Montgomery, John A.,Secrist III, John A.
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p. 1063 - 1087
(2008/02/09)
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- Synthesis and antiproliferative activity of some 4′-C-hydroxymethyl α- and -β-D-arabino-pentofuranosyl pyrimidine nucleosides
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A suitably protected 4-C-hydroxymethyl-arabino-pentofuranose was prepared and condensed with the following nucleobases: uracil, 5-fluorouracil and thymine. The corresponding cytosine and 5-fluorocytosine derivatives have also been obtained respectively from the uracil and 5-fluorouracil nucleosides. Separation of the anomeric mixtures followed by deprotection afforded the target compounds that were found to be non-cytotoxic to CCRF-CEM leukemia cells.
- Griffon,Montgomery,Secrist III
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p. 649 - 652
(2007/10/03)
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