Valerjans KAUSS

Dr.chem. Valerjans Kauss Head of Laboratory of CNS Active Compounds Latvian Institute of Organic Synthesis Aizkraukles str. 21 Riga, LV 1006 Latvia Phone: +371 67543503 Fax:     +371 67541408 E-mail: valerjan@osi.lv

Born: August 28, 1954, Aluksne, Latvia

Interests:

• Development of new modulators of ionotropic and metabotropic glutamate receptors.
• Stereoselective synthesis of aminocycloalkanes and nitrogen heterocycles.
• Aminoalkane sp3 CH functionalization reactions.

Languages: Latvian, Russian, English

Education:

• The Latvian State University, Faculty of Chemistry. Riga, Latvia, 1977.
• Dr. Chem. Institute of Organic Synthesis, Riga, Latvia, 1990. Thesis:

„The Addition Reaction of Thiosemicarbazides to Acetylenecarboxylic Acids and their Esters„ Supervisor: Professor I. Kalvinsh.

Experience:

Latvian Institute of Organic Synthesis

• Junior research associate, 1977 - 1985
• Research scientist, 1986 1993
• Senior research scientist, head of group, 1994 – 2001
• Head of laboratory, CNS active compounds, 2001

Honors and Awards:

• Corresponding Member, Latvian Academy of Sciences, 2007
• Testimonial writing from Prime Minister of the Latvian Republic „For contribution in the development of medicinal chemistry and preparing of new specialists”, February 2007.
• Award of academician Solomon Hiller, 2006.

Professional Activities:

Member of Scientific Council, Latvian Institute of Organic Synthesis.

Total number of scientific publications – more than100 (including patents and theses at conferences) 

• T.Noeske, D.Trifanova, V.Kauss, S.Renner, C.G.Parsons, G.Schneider, T.Weil. Synergism of virtual screening and medicinal chemistry: Identification of allosteric antagonists of metabotropic glutamate receptor 1. - Bioorg.Med.Chem, 2009, 17 (15), 5708-5715.
• 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.
• K. Gilling, C. Jatzke, C. Wollenburg, M. Vanejevs, V. Kauss, A. Jirgensons, C. G. Parsons. A novel class of amino-alkylcyclohexanes as uncompetitive, fast, voltage-dependent, N-methyl-D-aspartate (NMDA) receptor antagonists – in vitro characterization. J. Neural Transm. 2007, publ. online 31 August 2007.
• M. Vanejevs, C. Jatzke, S. Renner, M. Hechenberger, T. Bauer, A. Klochkova, I. Pyatkin , D. Kazyulkin , E. Aksenova , S. Shulepin, O. Timonina, A. Gutcaits, M. Henrich, V. Kauss, C. G. Parsons, T. Weil. Positive and Negative Modulation of Group I Metabotropic Glutamate Receptors. J. Med. Chem. 2007, publ. online October 2007.
• T. Noeske, A. Jirgensons, I. Stachenkovs, S. Renner, I. Jaunzeme, D. Trifanova, M. Hechenberger, T. Bauer, V. Kauss, C. G. Parsons, G. Schneider, T. Weil. Virtual Screening for Selective Allosteric mGluR1 Antagonists and Structure-Activity Relationship Investigations for Coumarine Derivatives. ChemMedChem. 2007, publ. online 17 September 2007.
• I. Jaunzeme, A. Jirgensons, V. Kauss and E. Liepins. Diastereoselectivity in the Overman rearrangement of O-cyclohexylideneethylimidates. Tetrahedron Lett. 2006, 3885-3887.
• D. Trifanova, M. Trifonova, A. Jirgensons, V. Kauss, O. Pugovich, I. Kalvinsh and G. Quack. The synthesis of potential Neramexane metabolites: cis- and trans-3-amino-1,3,5,5-tetramethylcyclohexanecarboxylic acids. Tetrahedron Lett. 2004, 8145-8147.
• W. Danysz, C.G. Parsons, A. Jirgensons, V. Kauss, J. Tillner. Amino-Alkyl-Cyclohexanes as a Novel Class of Uncompetitive NMDA Receptor Antagonists. Curr. Pharm. Design, 2002, 8, 835-843.
• A. Jirgensons, V. Kauss, I. Kalvinsh, M. R. Gold, W. Danysz, C. G. Parsons, G. Quack. Synthesis and structure - affinity relationships of 1,3,5-alkylsubstituted cyclohexylamines binding at NMDA receptor PCP site. Eur. J. Med. Chem., 2000, 35, 555-565.
• A. Jirgensons, V. Kauss, I. Kalvinsh, M. R. Gold. A practical synthesis of tert-carbinamines via the Ritter reaction with chloroacetonitrile. Synthesis, 2000, 1709-1712.
• I. Starchenkov, P. Trapencieris, V. Kauss, G. Jas, I. Kalvinsh. A convenient synthesis of 5b -cholestan-26-oic and 5b -cholestan-26,27-dioic acids. Steroids, 2000, 65, 143-147.
• A. Jirgensons, V. Kauss, A. F. Mishnev, I. Kalvinsh. The synthesis of 3-amino-3-methylbicyclo[3.3.1]nonanes. Endo-selectivity in the Ritter reaction of 1,3,5,7a -tetramethylbicyclo[3.3.1]nonan-3-ol. J. Chem. Soc. PT 1, 1999, 3527-3530.
• O. Pugovics, V. Kauss, I. Kalvinsh, M. R. Gold, G. Quack. Convenient synthesis of 2,6-di-tert-butyl-4-(5-(3-pyridyl)-4-oxapentyl)phenols and their thia analogues. J. Chem. Res. (M), 1998, 1885-1894.
• O. Pugovics, V. Kauss, I. Kalvinsh, M. R. Gold. The synthesis of (3,5-di-tert-butyl-4-hydroxyphenyl)methyl-(3-pyridylalkyl)ethers via 1-(3,5-di-tert-butyl-4-hydroxyphenyl)-methyl pyridinium salts. Synth. Commun., 1998, 28, 2227-2236.
• A. Jirgensons, I. Kums, V. Kauss, I. Kalvinsh. A convenient reagent for N-hydroxyguanylation. Synth. Commun., 1997, 27, 315-322.
• P. Trapencieris, I. Kalvinš, L. Kaulina, V. Kauss . Unnatural amino acids. 1. A facile synthesis of methyl ester of aziridine-2-carboxylic acid. Organic Process Research & Development, 1997, 1, 259-263.
• V. Ya. Kauss and I. Ya. Kalvin'sh. 2-Amino-4,4-disubstituted- 5-carboxymethyl-? ²-1,3,4-oxadiazolin-4-ium chlorides and their recyclization in acetic anhydride. Chemistry of Heterocyclic Compounds, 1992, 28 (12) 1449-1452. (Translated from Khimiya Geterotsiklicheskikh Soedinenii, 1992, No. 12, pp. 1685–1688.)
• V. Ya. Kauss, E. Kh. Grinberga and I. Ya. Kalvin'sh. Recyclization of 2-amino-4,4-dimethyl-?²-1,3,4-thiadiazolin-4-io-5-acetates into 2-dimethyl-hydrazono-2,3-dihydro-4h-1,3-thiazin-4-ones, Chemistry of Heterocyclic Compounds, 1992, 28 (12) 1445-1448. (Translated from Khimiya Geterotsiklicheskikh Soedinenii, 1992, No. 12, pp. 1680–1684.)
• V. Ya. Kauss, A. F. Mishnev and I. Ya. Kalvin'sh. Reactions of 1,1-dialkylthiosemicarbazides with propiolic acid and its esters. Chemistry of Heterocyclic Compounds, 1992, 28 (12) 1439-1444. (Translated from Khimiya Geterotsiklicheskikh Soedinenii, 1992, No. 12, pp. 1674–1679.)

Representative patents:

• WO 2009/09524. Pyrazolopyridines, a process for their preparation and their use as medicine/  Henrich M., Weil T., Mueller S., Nagel J., Gravius A., Kauss V., Zemribo R., Erdmane E.
• US 2009/0227582. Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors / Kauss V., Jaunzeme I., Jirgensons A., Kalvinsh I., Vanejevs M., Henrich M., Danysz W., Jatzke C., Parsons Ch.G.R., Weil T.
• WO 2008/035049. Adamantanyl-(cyclopropyl)-ketones as metabotropic glutamate receptor modulators / Parsons Ch.G.R., Kalvinsh I., Trifanova D., Jirgensons A., Kauss V., Danysz W., Henrich M .
• WO 2007/023245. Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors / Parsons Ch.G.R., Jirgensons A., Jaunzeme I., Kalvinsh I., Henrich M., Vanejevs M., Weil T., Kauss V., Danysz W., Jatzke C.
• WO 2007/023290. Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors / Parsons Ch.G.R., Jirgensons A., Jaunzeme I., Kalvinsh I., Henrich M., Vanejevs M., Weil T., Kauss V., Danysz W., Jatzke C.
• WO 2007/023242. Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors / Parsons Ch.G.R., Jirgensons A., Jaunzeme I., Kalvinsh I., Henrich M., Vanejevs M., Weil T., Kauss V., Danysz W., Jatzke C.
• WO 2007/045876. Chromenones and their use as modulators of metabotropic glutamate receptors / Parsons Ch.G.R., Jirgensons A., Trifanova D., Kalvinsh I., Starchenkovs I., Henrich M., Noeske T., Weil T., Kauss V., Danysz W.
• WO 2006/037996. Novel cyclic and acyclic propenones for treating CNS disorders / Parsons Ch.G.R., Kalvinsh I., Kauss V., Trifanova D., Zemribo R., Danysz W., Henrich M., Weil T.
• WO 2003/080046. Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT3 and neuronal nicotinic receptor antagonists / Parsons Ch.G.R., Henrich M., Danysz W., Kalvinsh I., Kauss V., Jirgensons A., Gold M., Vanejevs M.
• WO 2002/24186. 1-Amino-alkylcyclohexanes as trypanocidal agents / Kelly M., Kalvinsh I., Kauss V., Jirgensons A., Gold M.
• WO 2001/32640. 1-Cyclic amino-alkylcyclohexane compounds, pharmaceutical compositions thereof, and their use as anticonvulsants./ Gold M., Danysz W., Parsons C. G. R., Kalvinsh I., Kauss V., Jirgensons A.
• WO 99/01416. 1-Amino-alkylcyclohexane NMDA receptor antagonists./ Gold M., Danysz W., Parsons C. G. R., Kalvinsh I., Kauss V., Jirgensons A.

Current research projects:

• Modulators of metabotropic glutamate receptors (Collaboration with Merz Pharmaceuticals, Germany)

   

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  Last update 22.11.2010