Laboratory of CNS Active Compounds

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Dr. chem. Valerjans Kauss  
Head of Laboratory
e-mail:
Phone: (+371) 67014815

Laboratory of CNS active compounds, established in 2001, an experienced team of 15 chemists familiar with modern organic synthesis and medicinal chemistry approaches in drug discovery and development. Senior researchers have R&D experience in wide area of medchem projects, including medicines for CNS and peripheral regulation. Chemists have an experience in project oriented team work, networking with molecular modeling. Long term research in medicinal chemistry projects has been done in collaboration with Merz Pharmaceuticals, Germany. Research in organic chemistry – total synthesis of natural products and development of new synthetic methods – is organized by involving students from Riga Technical University and University of Latvia.

 

Selected publications:

  1. G. Smits, R. Zemribo. Total Synthesis of Deoxypumiliotoxin 193H Putative Structure via Ireland – Claisen Rearrangement. Eur. J. Org. Chem. 2015, 3152-3156.
  2. H. Kubas, U. Meyer, B. Kruger, M. Hechenberger, M. Vanejevs, R. Zemribo, V. Kauss, K. Ambartsumova, I. Pyatkin , A. Polosukhin, U. Abel. Discovery, synthesis and structure-activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators. Bioorg. Med. Chem. Lett. 2013, 23 (16), 4493-4500.
  3. G. Smits, R. Zemribo. The Exocyclic Olefin Geometry Control via Ireland-Claisen Rearrangement: Stereoselective Total Syntheses of Barmumycin and Limazepine E. Org. Lett. 2013, 15, 4406-4409.
  4. M. Vanejevs, C. Jatzke, S. Renner, S. Müller, M. Hechenberger, T. Bauer, A. Klochkova, I. Pyatkin, D. Kazyulkin , E. Aksenova , S. Shulepin, O. Timonina, A. Haasis, A. Gutcaits, C. G. Parsons, M. Henrich, V. Kauss, T. Weil. Positive and Negative Modulation of Group I Metabotropic Glutamate Receptors. J. Med. Chem. 2008, 51 (3), 634–647.

 

 

Selected patent applications:

  1. Abel, U.; Hansen, A.; Wolter, F.; Krueger, B.; Kauss, V.; Rozhkovs, J.; Piskunova, I.; Zvagulis, A.; Trifanova, D.; Grunsteine, G.; Ture, A. Glycine B antagonists. WO 2013/030358 (A1) (07.03.2013).
  2. Abel, U.; Hansen, A.; Wolter, F.; Krueger, B.; Kauss, V.; Rozhkovs, J.; Semenihina, V.; Piskunova, I.; Pelss, J. Glycine B antagonists. WO 2012/164085 (A1) (06.12.2012).
  3. Henrich, M.; Abel, U.; Mueller, S.; Kubas, H.; Meyer, U.; Hechenberger, M.; Kauss, V.; Zemribo, R.. Metabotropic glutamate receptor modulators. WO 2012/052451 A1, (26.04.2012).
  4. Abel, U.; Krueger, B.; Kubas, H.; Meyer, U.; Zemribo, R.; Smits, G. Metabotropic glutamate receptor modulators. WO 2012/085167 A1, (28.06.2012).