67475-56-3Relevant articles and documents
Metal-Free Twofold Electrochemical C?H Amination of Activated Arenes: Application to Medicinally Relevant Precursor Synthesis
D?rr, Carolin,Diehl, Erika,Hellmich, Ute A.,Schollmeyer, Dieter,Shimizu, Akihiro,Waldvogel, Siegfried R.,Wesenberg, Lars J.,Yoshida, Jun-ichi,Z?hringer, Till J. B.
supporting information, p. 17574 - 17580 (2020/12/07)
The efficient production of many medicinally or synthetically important starting materials suffers from wasteful or toxic precursors for the synthesis. In particular, the aromatic non-protected primary amine function represents a versatile synthetic precu
Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor
Pinkerton, Anthony B.,Sergienko, Eduard,Bravo, Yalda,Dahl, Russell,Ma, Chen-Ting,Sun, Qing,Jackson, Michael R.,Cosford, Nicholas D.P.,Millán, José Luis
, p. 31 - 34 (2017/11/27)
Tissue-nonspecific alkaline phosphatase (TNAP) is an ectoenzyme crucial for bone matrix mineralization via its ability to hydrolyze extracellular inorganic pyrophosphate (ePPi), a potent mineralization inhibitor, to phosphate (Pi). B
A novel, flexible strategy to construct privileged dibenzo[b,f][1,4,5]oxathiazepine 5,5-dioxides and their heterocyclic isosteres
Sapegin, Alexander,Panova, Valeria,Reutskaya, Elena,Smirnov, Alexey V.,Krasavin, Mikhail
, p. 7570 - 7578 (2016/11/11)
Secondary o-hydroxybenzene sulfonamides have been explored as bis-electrophilic partners in a practically simple, atom-economical approach to dibenzo[b,f][1,4,5]oxathiazepine-5,5-dioxides and their heterocyclic analogs, which is an underexplored version o
Design and synthesis of new potassium channel activators derived from the ring opening of diazoxide: Study of their vasodilatory effect, stimulation of elastin synthesis and inhibitory effect on insulin release
Bouider, Nafila,Fhayli, Wassim,Ghandour, Zeinab,Boyer, Marjorie,Harrouche, Kamel,Florence, Xavier,Pirotte, Bernard,Lebrun, Philippe,Faury, Gilles,Khelili, Smail
, p. 1735 - 1746 (2015/03/30)
Benzenesulfonylureas and benzenesulfonylthioureas, as well as benzenecarbonylureas and benzenecarbonylthioureas, were prepared and evaluated as myorelaxants on 30 mM KCl-precontracted rat aortic rings. The most active compounds were further examined as stimulators of elastin synthesis by vascular smooth muscle cells and as inhibitors of insulin release from pancreaticβ-cells. The drugs were also characterized for their effects on glycaemia in rats. Benzenesulfonylureas and benzenesulfonylthioureas did not display any myorelaxant activity on precontracted rat aortic rings. Such an effect could be attributed to their ionization at physiological pH. By contrast, almost all benzenecarbonylureas and benzenecarbonylthioureas displayed a myorelaxant activity, in particular the benzenecarbonylureas with an oxybenzyl group linked to the ortho position of the phenyl ring. The vasodilatory activity of the most active compounds was reduced when measured in the presence of 80 mM KCl or in the presence of 30 mM KCl and 10 μM glibenclamide. Such results suggested the involvement, at least in part, of KATP channels. Preservation of a vasodilatory activity in rat aortic rings without endothelium indicated that the site of action of such molecules was located on the vascular smooth muscle cells and not on the endothelial cells. Some of the most active compounds also stimulated elastin synthesis by vascular smooth muscle cells. Lastly, most of the active vasorelaxant drugs, except 15k and 15t at high concentrations, did not exhibit marked inhibitory effects on the insulin releasing process and on glycaemia, suggesting a relative tissue selectivity of some of these compounds for the vascular smooth muscle.
SULFONAMIDE COMPOUNDS AND USES AS TNAP INHIBITORS
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Paragraph 00812, (2013/09/12)
Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper- mineralization.
IMIDAZOPYRIMIDINONES AND USES THEREOF
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Page/Page column 86, (2010/04/03)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.
PHENOXIACETIC ACID DERIVATIVES
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Page/Page column 54, (2008/06/13)
The invention relates to certain 2-substituted phenoxyacetic acid derivatives of formula (I), in which the variables are as defined in the claims, useful in the treatment of diseases or conditions in which modulation of the CRTh2 receptor is beneficial, s