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Leenders R.,Mercachem BV | Heeres J.,Janssen Research Foundation | Vandenput D.,Mercachem BV | Guillemont J.,Johnson and Johnson Pharmaceutical Research and Development | Lewi P.,Janssen Research Foundation
Synthetic Communications | Year: 2011

Sterically hindered electron-deficient anilines are coupled to the 6-position of the purine core only when activated as their corresponding TFA-amide. The free anilines did not react under all conditions tested. After aqueous work-up, the TFA-group is lost. This procedure provides a new tool in the construction of purines functionalized with a sterically hindered electron-deficient aniline in the 6-position. Copyright © 2011 Taylor & Francis Group, LLC.

Leenders R.,Mercachem BV | Heeres J.,Janssen Research Foundation | Vandenput D.,Mercachem BV | Zijlmans R.,Mercachem BV | And 2 more authors.
European Journal of Organic Chemistry | Year: 2010

An optimized procedure is given for the synthesis of novel 3-(arylamino)-1,2,4-triazin-5-one building blocks from commercially available material. By employing these building blocks, a practical protocol is described for the functionalization of the 5-position of the triazine core with anilines or phenols. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.

Leenders R.,Mercachem BV | Heeres J.,Janssen Research Foundation | Guillemont J.,Johnson and Johnson Pharmaceutical Research and Development | Lewi P.,Janssen Research Foundation
Tetrahedron Letters | Year: 2010

A method is described to couple sterically-hindered electron-poor anilines to the 4-position of the pyrimidine core using a pyrimidine-2,4-bis(trifluoromethanesulfonate). © 2009 Elsevier Ltd. All rights reserved.

Kaido T.,Johannes Gutenberg University Mainz | Kempski O.,Johannes Gutenberg University Mainz | Heimann A.,Johannes Gutenberg University Mainz | Heers C.,Janssen Research Foundation | Bartsch D.,Janssen Research Foundation
Turkish Neurosurgery | Year: 2012

AIM: The purpose of this study is to detect gene expression patterns following focal cerebral ischemia. MATERIAL and METHODS: 25 male Wistar rats were divided into control (n = 8) and ischemic (n = 17) groups. In the ischemic group, slowly progressing focal ischemia was simulated by two-vein occlusion with spreading depression (SD) a cortical microinjection of KCI induced. Ischemic tissue was removed at 2, 8, 24, or 72 h postischemia. Using semiquantitative reverse transcription polymerase chain reaction, we investigated mRNA expression levels of 13 representative genes related to cerebral ischemia. Cluster analysis of the gene expression levels was done. RESULTS: In the ischemic group, the expression levels of c-fos, cyclin D1, and COX-2 were significantly higher at 2 h postischemia, and those of bcl-2, bcl-xL, and HO-1 at 72 h. Based on the cluster analysis, we statistically divided examined genes into three groups: group A, early expression (COX-2, c-fos, and bd-2); group B, s expression (c-jun, SOD-1, bad, p53, SOD-2, bd-xL, and bax); and group C, late expression (cyclin D1,c-myc, and HO-1). CONCLUSION: We statistically classified the genes into three groups after focal ischemia. The genes of the early- and late-expression groups can be possible therapeutic targets for the treatment of cerebral ischemia.

Van Poucke S.,Critical Care | Haeghen Y.V.,Ghent University | Vissers K.,Radboud University Nijmegen | Meert T.,Janssen Research Foundation | Jorens P.,University of Antwerp
BMC Medical Imaging | Year: 2010

Background: Recently, digital photography in medicine is considered an acceptable tool in many clinical domains, e.g. wound care. Although ever higher resolutions are available, reproducibility is still poor and visual comparison of images remains difficult. This is even more the case for measurements performed on such images (colour, area, etc.). This problem is often neglected and images are freely compared and exchanged without further thought.Methods: The first experiment checked whether camera settings or lighting conditions could negatively affect the quality of colorimetric calibration. Digital images plus a calibration chart were exposed to a variety of conditions. Precision and accuracy of colours after calibration were quantitatively assessed with a probability distribution for perceptual colour differences (dE_ab). The second experiment was designed to assess the impact of the automatic calibration procedure (i.e. chart detection) on real-world measurements. 40 Different images of real wounds were acquired and a region of interest was selected in each image. 3 Rotated versions of each image were automatically calibrated and colour differences were calculated.Results: 1stExperiment: Colour differences between the measurements and real spectrophotometric measurements reveal median dE_ab values respectively 6.40 for the proper patches of calibrated normal images and 17.75 for uncalibrated images demonstrating an important improvement in accuracy after calibration. The reproducibility, visualized by the probability distribution of the dE_ab errors between 2 measurements of the patches of the images has a median of 3.43 dE* for all calibrated images, 23.26 dE_ab for all uncalibrated images. If we restrict ourselves to the proper patches of normal calibrated images the median is only 2.58 dE_ab! Wilcoxon sum-rank testing (p < 0.05) between uncalibrated normal images and calibrated normal images with proper squares were equal to 0 demonstrating a highly significant improvement of reproducibility. In the second experiment, the reproducibility of the chart detection during automatic calibration is presented using a probability distribution of dE_ab errors between 2 measurements of the same ROI.Conclusion: The investigators proposed an automatic colour calibration algorithm that ensures reproducible colour content of digital images. Evidence was provided that images taken with commercially available digital cameras can be calibrated independently of any camera settings and illumination features. © 2010 Van Poucke et al; licensee BioMed Central Ltd.

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