- FLT3 RECEPTOR ANTAGONISTS
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The invention pertains to novel FLT3receptor antagonists of general formula (1). The compounds are useful for the treatment or the prevention of pain disorders, cancer and autoimmune diseases.
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Page/Page column 52
(2016/03/29)
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- Synthesis and anticandidal activity of azole-containing sulfonamides
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Twenty five benzenesulfonamides containing one imidazole or triazole ring, or two imidazole or triazole rings have been synthesized and evaluated as anticandidal agents. The most active compounds were 5c, 6b, 6c, 6e, and 17b, which exhibited MIC values of 4.55-24.39 mM depending on the clinical isolate. Comparing imidazole to triazole derivatives did not show a clear effect on activity. Compounds containing a N-benzyl group also showed no clear evidence on activity given the fact that they have an extra aromatic ring. Secondary sulfonamides, 5l, 5m, and 5n showed activities that were proportional to their lipophilicity. The activities of N-aryl-substituted derivatives 5j, 5k, 5l, 5m, 5n, and 6j were also proportional to their lipophilicity. Halogenation enhanced the activity as a result of improvement of lipophilicity. The presence of two imidazole or triazole rings in the same compound did not show a clear enhancement of activity.
- Qandil, Amjad M.,Hassan, Mohammad A.,Al-Shar'i, Nizar A.
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experimental part
p. 99 - 112
(2009/04/03)
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- GLUCAGON ANTAGONISTS/INVERSE AGONISTS
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A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-
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Page/Page column 153
(2010/02/14)
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- Direct Synthesis of Sulfonamides and Activated Sulfonate Esters from Sulfonic Acids
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A general new method for the preparation of sulfonamides and activated sulfonate esters by the direct coupling of sulfonic acid salts with amines and alcohols using the reagent triphenylphosphine ditriflate is described. A new reusable polymer-supported reagent for these transformations under heterogeneous conditions is also described. These methods provide a fundamentally new approach to making small molecules containing the sulfonamide functional group. Copyright
- Caddick, Stephen,Wilden, Jonathan D.,Judd, Duncan B.
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p. 1024 - 1025
(2007/10/03)
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