217811-63-7Relevant academic research and scientific papers
THIOETHER-PIPERIDINYL OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 36, (2015/07/07)
The present invention is directed to thioether-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the thioether-piperidinyl compounds described herein in the potential treatment or prevention
MITOCHONDRIAL ALDEHYDE DEHYDROGENASE-2 MODULATORS AND METHODS OF USE THEREOF
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Paragraph 00324, (2014/10/15)
The present disclosure provides compounds that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds.
Novel small molecule bradykinin B2 receptor antagonists
Gibson, Christoph,Schnatbaum, Karsten,Pfeifer, Jochen R.,Locardi, Elsa,Paschke, Matthias,Reimer, Ulf,Richter, Uwe,Scharn, Dirk,Faussner, Alexander,Tradler, Thomas
supporting information; experimental part, p. 4370 - 4379 (2010/02/28)
Blockade of the bradykinin B2 receptor provides therapeutic benefit in hereditary angioedema (HAE) and potentially in many other diseases. Herein, we describe the development of highly potent B2 receptor antagonists with a molecular weight of approximately 500 g/mol. First, known quinoline-based B2 receptor antagonists were stripped down to their shared core motif 53, which turned out to be the minimum pharmacophore. Targeted modifications of 53 resulted in the highly water-soluble lead compound 8a. Extensive exploration of its structure-activity relationship resulted in a series of highly potent B2 receptor antagonists, featuring a hydrogen bond accepting functionality, which presumably interacts with the side chain of Asn-107 of the B2 receptor. Optimization of the microsomal stability and cytochrome P450 inhibition eventually led to the discovery of the highly potent and orally available B2 receptor antagonist 52e (JSM10292), which showed the best overall properties.
8-OXY-QUINOLINE DERIVATIVES AS BRADYKININ B2 RECEPTOR MODULATORS
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, (2008/12/04)
The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.
