Valerjans KAUSS
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Dr.chem. Valerjans Kauss
Head of Laboratory of CNS Active Compounds
Latvian Institute of Organic Synthesis
Aizkraukles str. 21
Riga, LV 1006
LatviaPhone: +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.
Recent/Representative Publications:
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. Kalvin, 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. 16851688.)
- 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. 16801684.)
- 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. 16741679.)
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)
Last update 22.11.2010