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Potsdam, Germany

Neda I.,Institutul National Of Cercetare | Fodor E.,TU Braunschweig | Maftei C.V.,TU Braunschweig | Mihorianu M.,TU Braunschweig | And 2 more authors.
European Journal of Organic Chemistry | Year: 2013

This paper reports the synthesis of the new enantiopure amino aldehydes, 9-aminoquincorine-10-aldehyde (1) and 9-aminoquincoridine-10-aldehyde (2). These alkaloid-like compounds are derivatives of the Cinchona alkaloids quinine and quinidine. Their application as chiral building blocks in the synthesis of novel compounds is demonstrated by the reduction and reductive amidation of the aldehyde moiety. Furthermore, their use in early drug discovery and supramolecular chemistry is described. The synthesis and selected reactions for two new quincorine/quincoridine (QCI/QCD) motifs, N-protected 9-aminoquincorine-10-aldehyde and N-protected 9-aminoquincoridine-10-aldehyde, are presented. As unprecedented motifs with an alkaloid-like nature, they are of interest for the pharmaceutical industry. Reduction of these aldehydes gave C-10 alcohols, which can be used in supramolecular chemistry. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Source


Kueper T.,Symrise GmbH and Co. KG | Krohn M.,BRAIN AG | Haustedt L.O.,AnalytiCon Discovery GmbH | Hatt H.,Ruhr University Bochum | And 2 more authors.
Experimental Dermatology | Year: 2010

During the past years the topic sensitive skin became one of the most important fields in dermatology. The tremendous interest is based on several studies showing that about 50% of the population declares to have sensitive skin. The human thermoreceptor hTRPV1 was previously identified to contribute to this skin condition while facilitating neurogenic inflammation leading to hyperalgesia. Furthermore, skin sensitivity towards capsaicin, a natural activator of TRPV1, was shown to correlate with sensitive skin. In a screening campaign based on recombinant HEK293-cells stably transfected with hTRPV1, the selective antagonist trans-4-tert-butylcyclohexanol was identified. This antagonist is able to inhibit capsaicin-induced hTRPV1 activation with an IC50 value of 34±5μm tested in HEK293-cells as well as in electrophysiological recordings performed in oocytes expressing hTRPV1. Strikingly, in a clinical study with 30 women using topical treatment with o/w emulsions containing 31.6 ppm capsaicin, we were able to show that 0.4% of this inhibitor significantly reduces capsaicin-induced burning (P<0.0001) in vivo. Thus trans-4-tert-butylcyclohexanol has the potential as a novel bioactive for the treatment of sensitive skin. © 2010 John Wiley & Sons A/S. Source


Patent
AnalytiCon Discovery GmbH and Sloan Kettering Institute For Cancer Research | Date: 2010-12-01

In one aspect, the instant invention provides novel compounds and pharmaceutical compositions useful for treating proliferative diseases such as cancer. In another aspect, the invention provides methods of using certain compounds in the treatment of proliferative diseases such as cancer. In particular, the instant invention provides methods of treating ocular cancer (e.g., retinoblastoma) using intraarterial infusion to administer inventive compounds locally to the eye of a subject with an ocular cancer.


Patent
AnalytiCon Discovery GmbH and A+ Network | Date: 2013-09-06

The present invention relates to an anti-dandruff composition comprising 1-acetoxychavicol acetate (I). Furthermore, the present invention relates to a method for preparing said anti-dandruff composition and the use of said anti-dandruff composition for treating or preventing


Healthspan (the life period when one is generally healthy and free from serious disease) depends on nature (genetic make-up) and nurture (environmental influences, from the earliest stages of development throughout life). Genetic studies increasingly reveal mutations and polymorphisms that may affect healthspan. Similarly, claims abound about lifestyle modifications or treatments improving healthspan. In both cases, rigorous testing is hampered by the long lifespan of model organisms like mice (let alone humans) and the difficulty of introducing genetic changes to examine the phenotype of the altered genome. We will develop C. elegans as a healthspan model. Already validated extensively as an ageing model, this organism can be readily modified genetically, and effects of environmental manipulations on healthspan can be measured in days or weeks. Once validated as a healthspan model, it can be used for an initial assessment of preventive and therapeutic measures for humans, as well as for risk identification and the initial evaluation of potential biomarkers. It will also prove useful to study interactions between genetic and various environmental factors.

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