6320-39-4Relevant academic research and scientific papers
Kinase inhibitor, and preparation and application of kinase inhibitor
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Paragraph 0390-0394, (2018/09/11)
The invention provides a compound shown as a formula (I), or a stereoisomer, a tautomer, nitrogen oxide, metabolite, a prodrug, pharmaceutically acceptable salt or solvate of the compound, and application of the compound to preparing drugs or drug compositions for treating Pim kinase-mediated diseases.
Comprehensive Analysis of Structure-Activity Relationships of α-Ketoheterocycles as sn-1-Diacylglycerol Lipase α Inhibitors
Janssen, Freek J.,Baggelaar, Marc P.,Hummel, Jessica J. A.,Overkleeft, Herman S.,Cravatt, Benjamin F.,Boger, Dale L.,Van Der Stelt, Mario
, p. 9742 - 9753 (2016/01/12)
Diacylglycerol lipase α (DAGLα) is responsible for the formation of the endocannabinoid 2-arachidonoylglycerol (2-AG) in the central nervous system. DAGLα inhibitors are required to study the physiological role of 2-AG. Previously, we identified the α-ketoheterocycles as potent and highly selective DAGLα inhibitors. Here, we present the first comprehensive structure-activity relationship study of α-ketoheterocycles as DAGLα inhibitors. Our findings indicate that the active site of DAGLα is remarkably sensitive to the type of heterocyclic scaffold with oxazolo-4N-pyridines as the most active framework. We uncovered a fundamental substituent effect in which electron-withdrawing meta-oxazole substituents increased inhibitor potency. (C6-C9)-acyl chains with a distal phenyl group proved to be the most potent inhibitors. The integrated SAR data was consistent with the proposed binding pose in a DAGLα homology model. Altogether, our results may guide the design of future DAGLα inhibitors as leads for molecular therapies to treat neuroinflammation, obesity, and related metabolic disorders.
HETEROCYCLIC DERIVATIVES
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Page/Page column 15, (2011/02/25)
The present invention relates to heterocyclic derivatives, and more particularly, to novel heterocyclic derivatives useful for the preparation of medicaments for treating diseases related to uric acid.
Thiazole[4,5-C]pyridine derivatives
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Page/Page column 10, (2008/06/13)
The invention relates to compounds of general formula I: wherein R1, R2 and R3 are as defined in the description such compounds are metabotropic glutamate receptor antagonists and are useful in the treatment or prevention of mGluR5 receptor mediated disorders.
CETP INHIBITORS
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Page/Page column 93, (2008/06/13)
Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. I
Oxazolo, thiazolo and selenazolo [4,5-c]-quinolin-4-amines and analogs thereof
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, (2008/06/13)
Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
New Compounds with Possible Pharmacological Activity
Moffett, Robert Bruce
, p. 176 - 183 (2007/10/02)
Sixty-two new organic compounds are reported.These were prepared for testing in a variety of pharmacological screens or as chemical intermediates.None was found to be more active or less toxic than known medicinals.
