475480-98-9Relevant academic research and scientific papers
SUBSTITUTED ARYLOXAZOLES AND THEIR USE
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Page/Page column 25-26, (2011/06/23)
The present application relates to novel substituted aryloxazole derivatives, a method for the production thereof, the use thereof for the treatment and/or prophylaxis of diseases and the use thereof for the production of drugs for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.
Aleglitazar, a new, potent, and balanced dual PPARα/γ agonist for the treatment of type II diabetes
Benardeau, Agnes,Benz, Joerg,Binggeli, Alfred,Blum, Denise,Boehringer, Markus,Grether, Uwe,Hilpert, Hans,Kuhn, Bernd,Maerki, Hans Peter,Meyer, Markus,Puentener, Kurt,Raab, Susanne,Ruf, Armin,Schlatter, Daniel,Mohr, Peter
scheme or table, p. 2468 - 2473 (2010/03/24)
Design, synthesis, and SAR of novel α-alkoxy-β-arylpropionic acids as potent and balanced PPARαγ coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical development. Its X-ray structure in complex with both receptors as well as its high efficacy in animal models of T2D and dyslipidemia are also presented.
Compounds, pharmaceutical compositions and methods for use in treating metabolic disorders
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Page/Page column 37, (2010/02/15)
The present invention provides compounds useful, for example, for modulating insulin levels in a subject and that have the general formula [in-line-formulae]Q-L1-P-L2-M-X-L3-A [/in-line-formulae] wherein the definitions of
Structure-based design of indole propionic acids as novel PPARα/γ co-agonists
Kuhn, Bernd,Hilpert, Hans,Benz, Joerg,Binggeli, Alfred,Grether, Uwe,Humm, Roland,Maerki, Hans Peter,Meyer, Markus,Mohr, Peter
, p. 4016 - 4020 (2007/10/03)
In the quest for novel PPARα/γ co-agonists as putative drugs for the treatment of type 2 diabetes and dyslipidemia, we have used a structure-based design approach to identify propionic acids with a 1,5-disubstituted indole scaffold as potent PPARα/γ activ
Oxazole derivatives
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, (2008/06/13)
The present invention relates to novel oxazole compounds which act as PPARα and PPARγ agonists and are accordingly useful for the treatment of diseases modulated by PPARα and PPARγ such as diabetes.
New azolidinediones as inhibitors of protein tyrosine phosphatase lb with antihyperglycemic properties
Malamas, Michael S.,Sredy, Janet,Gunawan, Iwan,Mihan, Brenda,Sawicki, Diane R.,Seestaller, Laura,Sullivan, Donald,Flam, Brenda R.
, p. 995 - 1010 (2007/10/03)
Insulin resistance in the liver and peripheral tissues together with a pancreatic cell defect are the common causes of type 2 diabetes. It is now appreciated that insulin resistance can result from a defect in the insulin receptor signaling system, at a site post binding of insulin to its receptor. Protein tyrosine phosphatases (PTPases) have been shown to be negative regulators of the insulin receptor. Inhibiton of PTPases may be an effective method in the treatment of type 2 diabetes. A series of azolidinediones has been prepared as protein tyrosine phosphatase 1B (PTP1B) inhibitors. Several compounds were Potent inhibitors against the recombinant rat and human PTP1B enzymes with submicromolar IC50 values. Elongated spacers between the azolidinedione moiety and the central aromatic portion of the molecule as well as hydrophobic groups at the vicinity of this aromatic region were very important to the inhibitory activity. Oxadiazolidinediones 87 and 88 and the corresponding acetic acid analogues 119 and 120 were the best h-PTP1B inhibitors with IC50 values in the range of 0.12-0.3 μM. Several compounds normalized plasma glucose and insulin levels in the ob/ob and db/db diabetic mouse models.
Azole phenoxy hydroxyureas as selective and orally active inhibitors of 5- lipoxygenase
Malamas,Carlson,Grimes,Howell,Glaser,Gunawan,Nelson,Kanzelberger,Shah,Hartman
, p. 237 - 245 (2007/10/03)
Azole phenoxy hydroxyureas are a new class of 5-lipoxygenase (5-LO) inhibitors. Structure-activity relationship studies have demonstrated that electronegative substituents on the 2-phenyl portion of the oxazole tail increased the ex vivo potency of these
