400-92-0Relevant academic research and scientific papers
GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Page/Page column 176, (2017/03/17)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula II.
GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Page/Page column 191, (2017/03/08)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I), as follows: wherein R1, R2, R4, W, X, Y, and G, are defined herein.
GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Page/Page column 187, (2017/03/08)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (III); wherein R1c, R2C, R4C, Wc, Yc, Zc and Gc, are defined herein.
Optimization of thiazole analogues of resveratrol for induction of NAD(P)H:quinone reductase 1 (QR1)
Mayhoub, Abdelrahman S.,Marler, Laura,Kondratyuk, Tamara P.,Park, Eun-Jung,Pezzuto, John M.,Cushman, Mark
, p. 7030 - 7039 (2013/01/15)
NAD(P)H:quinone reductase 1 (QR1) belongs to a class of enzymes called cytoprotective enzymes. It exhibits its cancer protective activity mainly by inhibiting the formation of intracellular semiquinone radicals, and by generating α-tocopherolhydroquinone, which acts as a free radical scavenger. It is therefore believed that QR1 inducers can act as cancer chemopreventive agents. Resveratrol (1) is a naturally occurring stilbene derivative that requires a concentration of 21 μM to double QR1 activity (CD = 21 μM). The stilbene double bond of resveratrol was replaced with a thiadiazole ring and the phenols were eliminated to provide a more potent and selective derivative 2 (CD = 2.1 μM). Optimizing the substitution pattern of the two phenyl rings and the central heterocyclic linker led to a highly potent and selective QR1 inducer 9o with a CD value of 0.087 μM.
CHROMAN DERIVATIVES
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, (2008/06/13)
3-amino-5-carbamoylchromans and 8-fluoro-3-amino-5-carbamoylchromans, as well as enantiomers and salts thereof, are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.
