138731-14-3Relevant academic research and scientific papers
5-Hydroxyindole-2-carboxylic acid amides: Novel histamine-3 receptor inverse agonists for the treatment of obesity
Pierson, Pascale David,Fettes, Alec,Freichel, Christian,Gatti-McArthur, Silvia,Hertel, Cornelia,Huwyler, J?rg,Mohr, Peter,Nakagawa, Toshito,Nettekoven, Matthias,Plancher, Jean-Marc,Raab, Susanne,Richter, Hans,Roche, Olivier,Sarmiento, Rosa María Rodríguez,Schmitt, Monique,Schuler, Franz,Takahashi, Tadakatsu,Taylor, Sven,Ullmer, Christoph,Wiegand, Ruby
supporting information; experimental part, p. 3855 - 3868 (2010/02/28)
Obesity is a major risk factor in the development of conditions such as hypertension, hyperglycemia, dyslipidemia, coronary artery disease, and cancer. Several pieces of evidence across different species, including primates, underscore the implication of the histamine 3 receptor (H3R) in the regulation of food intake and body weight and the potential therapeutic effect of H3R inverse agonists. A pharmacophore model, based on public information and validated by previous investigations, was used to design several potential scaffolds. Out of these scaffolds, the 5-hydroxyindole-2-carboxylic acid amide appeared to be of great potential as a novel series of H3R inverse agonist. Extensive structure-activity relationships revealed the interconnectivity of microsomal clearance and hERG (human ether-a-go-go-related gene) affinity with lipophilicity, artificial membrane permeation, and basicity. This effort led to the identification of compounds reversing the (R)-R-methylhistamine-induced water intake increase in Wistar rats and, further, reducing food intake in diet-induced obese Sprague-Dawley rats. Of these, the biochemical, pharmacokinetic, and pharmacodynamic characteristics of (4,4-difluoropiperidin- 1-yl)[1-isopropyl-5-(1-isopropylpiperidin-4-yloxy)-1H-indol-2-yl]-methanone 36 are detailed.
New indole derivatives as factor xa inhibitors
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Page 51, (2010/02/09)
The present invention relates to compounds of the formula I, in which R0 ; R1 ; R2 ; R3 ; R4 ; R5 ; R6 ; R7 ; Q; V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Synthesis of Novel DNA Binding Agents: Indole-Containing Analogues of Bis-Netropsin
Khalaf, Abedawn I.,Pitt, Andrew R.,Suckling, Colin J.,Scobie, Martin,Urwin, John,Waigh, Roger D.,Fishleigh, Robert V.,Young, Stephen C.
, p. 751 - 770 (2007/10/03)
Molecular modelling studies showed that indole dicarboxylic acids are potential linkers for the synthesis of bis-netropsin analogues with a good fit to the minor groove of DNA. To test this hypothesis, 2-carboxyindole-6-acetic acid, indole-2,6-dicarboxyli
