Liestal, Switzerland
Liestal, Switzerland

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Caronna T.,University of Bergamo | Mele A.,Polytechnic of Milan | Famulari A.,Polytechnic of Milan | Mendola D.,Polytechnic of Milan | And 5 more authors.
Chemistry - A European Journal | Year: 2015

Helicenes and heterohelicenes are attractive compounds with great potential in materials sciences to be used in optoelectronics as ligand backbones in enantioselective catalysis and as chiral sensors. The properties of these materials are related to the stereodynamics of these helical chiral compounds. However, little is known about features controlling stereodynamics in helicenes; in particular, for heterohelicenes the position of the heteroatom could be relevant in this respect. Herein the complete stereodynamic characterization of monoaza[5]helicenes is shown by enantioselective dynamic HPLC and DFT calculations. At variance with previous theoretical calculations, 1-aza[5]helicene shows a surprisingly high enantiomerization barrier, which is triggered by specific solvent interactions. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


PubMed | University of Bergamo, Polytechnic of Milan, University of Heidelberg and Corden Pharma Switzerland LLC
Type: Journal Article | Journal: Chemistry (Weinheim an der Bergstrasse, Germany) | Year: 2015

Helicenes and heterohelicenes are attractive compounds with great potential in materials sciences to be used in optoelectronics as ligand backbones in enantioselective catalysis and as chiral sensors. The properties of these materials are related to the stereodynamics of these helical chiral compounds. However, little is known about features controlling stereodynamics in helicenes; in particular, for heterohelicenes the position of the heteroatom could be relevant in this respect. Herein the complete stereodynamic characterization of monoaza[5]helicenes is shown by enantioselective dynamic HPLC and DFT calculations. At variance with previous theoretical calculations, 1-aza[5]helicene shows a surprisingly high enantiomerization barrier, which is triggered by specific solvent interactions.


Grant
Agency: European Commission | Branch: FP7 | Program: BSG-SME | Phase: SME-2012-1 | Award Amount: 1.81M | Year: 2012

Helicobacter pylori infection is highly prevalent worldwide and is an important cause of gastritis, peptic ulcer disease, and significantly gastric cancer. Because eradication requires treatment with multidrug regimens, there exists a very strong need for a vaccine to prevent initial infection. Immunization with H pylori protein subunits in humans has shown adjuvant-related adverse effects and only moderate effectiveness. However, with much greater knowledge of the molecular basis of infection and having learnt lessons from previous vaccine developments, the current consortium have drawn together three strand that are considered critical to the development of an effective vaccine: - Powerful, safe and multivalent antigens - Powerful, safe and multi-acting adjuvants - Powerful, modular and flexible oral vaccine delivery system All three of the above innovative technologies have been proven to be effective in doing what they are required to do, namely: - Antigens produce antibodies against a number of key H pylori bacterial components - Adjuvants stimulate the immune cells to produce significant numbers of long lasting antibodies - Delivery formulate antigens and adjuvants together and target the stomach and intestine This consortium (HELICOVAXOR) uniquely converges all three into a true vaccine with real potential to protect from H pylori infection. The vaccine is being designed for oral administration, efficacy, safety and temperature stability. This consortium has assembled leading academic, industrial and regulatory groups, the activities of which will be coordinated to perform analysis of the formulations, efficacy and safety testing of the vaccines and the preparation of a regulatory dossier, all required before the product can enter human clinical studies. If successful in pre-clinical studies, the consortium will work with vaccine companies to progress human studies and launch the product as a vaccine to confer protection from H pylori infection.


PubMed | University of Vienna, Corden Pharma Switzerland LLC and University of Pavia
Type: Journal Article | Journal: Molecules (Basel, Switzerland) | Year: 2016

The identification of novel pan-sigma receptor (SR) modulators, potentially useful in cancer treatment, represents a new goal of our research. Here, we report on the preparation of novel chiral compounds characterized by a 3-C alkyl chain bridging an aromatic portion to a 4-benzyl-piperidine moiety. All of the studied compounds have been prepared both in racemic and enantiomerically-pure form, with the final aim to address the role of chirality in the SR interaction. To isolate and characterize enantiomeric compounds, high-performance liquid chromatography (HPLC) procedures were set up. A systematic analytical screening, involving several combinations of chiral stationary and mobile phases, allowed us to optimize the analytical resolution and to set up the (semi-)preparative chromatographic conditions. Applying the optimized procedure, the enantiomeric resolution of the studied compounds was successfully achieved, obtaining all of the compounds with an enantiomeric excess higher than 95%. Lastly, the absolute configuration has been empirically assigned to enantiopure compounds, combining the electronic circular dichroism (ECD) technique to the elution order study.


Rossi D.,University of Pavia | Marra A.,NicOx | Rui M.,University of Pavia | Brambilla S.,NicOx | And 2 more authors.
Journal of Pharmaceutical and Biomedical Analysis | Year: 2016

A rapid and straightforward screening protocol of chiral stationary phases (CSPs) in HPLC and SFC resulted in three different methods "fit-for-purpose", i.e. analysis and scale-up to semi-preparative enantioselective chromatography. The efficient use of these three methods allowed expedited preparation of an important drug discovery target, (R/S)-1, a potent new sigma 1 (σ1) receptor agonist. The approach taken resulted in significant savings of both time and labor for the isolation of enantiomers compared to the development of a stereo-selective synthesis.The enantiomers of 1 have been isolated allowing studies of their chirooptical properties and an in-deep comparative examination of the pharmacological profile for the individual enantiomers. © 2015 Elsevier B.V.


PubMed | Corden Pharma Switzerland LLC, University of Pavia and NicOx
Type: | Journal: Journal of pharmaceutical and biomedical analysis | Year: 2015

A rapid and straightforward screening protocol of chiral stationary phases (CSPs) in HPLC and SFC resulted in three different methods fit-for-purpose, i.e. analysis and scale-up to semi-preparative enantioselective chromatography. The efficient use of these three methods allowed expedited preparation of an important drug discovery target, (R/S)-1, a potent new sigma 1 (1) receptor agonist. The approach taken resulted in significant savings of both time and labor for the isolation of enantiomers compared to the development of a stereo-selective synthesis. The enantiomers of 1 have been isolated allowing studies of their chirooptical properties and an in-deep comparative examination of the pharmacological profile for the individual enantiomers.


Schmidli E.,Corden Pharma Switzerland LLC | Middleditch M.,Corden Pharma Switzerland LLC | Heckhoff S.,Corden Pharma Switzerland LLC
Lipid Technology | Year: 2014

Phospholipids derived from fatty acids are increasingly used by the pharmaceutical industry as excipients and also as active pharmaceutical ingredients (API) themselves. Newly developed HPLC-CAD (charged aerosol detection) methods allow the resolution of phospholipids with the same headgroup but different fatty acid chains. A new manufacturing process has been established on multi-Kg scale, which enables the manufacture of phospholipids meeting the quality requirements for use as excipients or APIs. Such products can now be obtained in significantly higher chemical purities than previously possible, with no unqualified impurity exceeding the International Conference on Harmonisation (ICH) limit of 0.15%. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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