153435-84-8Relevant articles and documents
Discovery of TUG-770: A highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist for treatment of type 2 diabetes
Christiansen, Elisabeth,Hansen, Steffen V. F.,Urban, Christian,Hudson, Brian D.,Wargent, Edward T.,Grundmann, Manuel,Jenkins, Laura,Zaibi, Mohamed,Stocker, Claire J.,Ullrich, Susanne,Kostenis, Evi,Kassack, Matthias U.,Milligan, Graeme,Cawthorne, Michael A.,Ulven, Trond
supporting information, p. 441 - 445 (2013/07/11)
Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing.
ORTHO-FLUORO SUBSTITUTED COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES
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Page/Page column 42, (2012/10/18)
There is provided novel fluoro-substituted compounds capable of modulating the G- protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
Synthesis of sulfones by iron-catalyzed decomposition of sulfonylhydrazones
Barluenga, Jose,Tomas-Gamasa, Maria,Aznar, Fernando,Valdes, Carlos
experimental part, p. 1520 - 1526 (2011/04/25)
The Fe-catalyzed decomposition of sulfonylhydrazones gives rise to sulfones. The reaction is quite general and allows the preparation of sulfones from a variety of aryl, alkyl, and α,β-unsaturated aldehydes and ketones. Crossover experiments reveal that the reaction is an intermolecular process, which may proceed by nucleophilic attack of the sulfinate anion on an iron carbene complex. Carbonyl compounds can be easily transformed into sulfones by Fe-catalyzed decomposition of the corresponding sulfonylhydrazones. The process most likely proceeds through an iron carbene complex and opens the door for the design of othernovel Fe-catalyzed reductive couplings. Copyright
TRICYCLIC INHIBITORS OF 5-LIPOXYGENASE
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Page/Page column 88, (2010/11/28)
Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.
COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 27, (2010/10/19)
Compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1 4alkylamino; R2 and R3, which may be the same or different, are
Novel synthesis of sulfones from α,α-dibromomethyl aromatics
Xu, Feng,Savary, Kimberly,Williams, J. Michael,Grabowski, Edward J. J.,Reider, Paul J.
, p. 1283 - 1286 (2007/10/03)
A novel, high yielding preparation of sulfones from α,α-dibromomethyl aromatics through reaction with a sulfinate salt is reported.
Azetidine derivatives, their preparation and medicaments containing them
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, (2008/06/13)
The invention concerns compounds of formula (1) wherein: R represents a chain (A) or (B); R1 is methyl or ethyl; R2 is either an optionally substituted aromatic or an optionally substituted heteroaromatic ring; R3 and R4, identical or different, are either an optionally substituted aromatic or an optionally substituted heteroaromatic ring; R′ represents a hydrogen atom or a —CO—alk radical, their optical isomers, their salts, their preparation and medicines containing them.