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THE SECOND EUROPEAN SYMPOSIUM ON

COMBINATORIAL SCIENCES

COPENHAGEN 29 JUNE - 3 JULY, 2003

Program for EUROCOMBI-2

June 29th –July 3rd, Bella Center, Copenhagen, Denmark

Organised by the European Society of Combinatorial Sciences (ESCS)

 

 

Monday, June 30

 

Opening Remarks

Chair: Morten Meldal

08:45: By the Chairman

08:50: Bodil Norild, The Danish National Research Foundation

08:55: Ferenc Darvas, Secretary of ESCS

Supports and Solid Phase Chemistry

Chair: Morten Meldal

09:00 – IN1: Mark Bradley, University of Southampton

"High-Throughput Methods of Library Synthesis and Screening"

 

09:25 - O1: Andreas Marzinzik, Novartis Pharma AG

"Combinatorial Chemistry on Macrobeads: Single Compounds from Individual Carriers"

 

09:45 – O2: Roice Michael, Carlsberg Biosector

"Synthesis and characterization of ULTRAMINE: a high capacity polyethylenamine-based polymer and its application as a scavenger resin"

 

10:05 - O3: Jörg Rademann

“Reagent linkers for diversity-oriented preparation of compound libraries”

 

 

10:25: Coffee Break

Supports and Solid Phase Chemistry

Chair: Mark Bradley

10:55 – O4: Morten Meldal, Carlsberg Laboratory, SPOCC Centre

"Single bead structure analysis, progress in MAS NMR spectroscopy and MS/MS fragmentation analysis by ES-mass spectrometry."

 

11:15 – O5: Jamart-Gregoire Brigitte, ENSIC-INPL

"Solid phase synthesis of chiral a -hydrazinoacids"

 

11:35 – O6: Knud Jensen, Dept. of Chemistry, KVL

"A highly Acid-Labile Thiophene Backbone Amide Linker: T-BAL"

 

11:55: Lunch/Poster/Exhibition

 

Combinatorial Synthesis and Technology

Chair: Mats Larhed

13:25 – IN2: Oliver Kappe, Karl-Franzens University

"Rapid generation and scaffold decoration of dihydropyrimidine libraries"

 

13:50 – O7: Árpád Furka, Eötvös Loránd University

"Application of string synthesis for preparation of cherry-picked combinatorial libraries"

 

14:10 – O8: Jin Ku Cho, University of Southampton

"Sensor Beads and in situ Reaction Monitoring"

 

14:30 – O9: Pino Pilotti, Personal Chemistry AB,

"Solid phase synthesis of aminopropenones and aminopropenoates as efficient and versatile synthons for combinatorial synthesis of heterocycles"

 

 

14:50: Break

Combinatorial Synthesis and Technology

Chair: Rob Liskamp

15:20 – IN3: Günther Jung, University of Tübingen

"Combinatorial Microelectrochemistry and Fast Capillary Chromatography on Monolithic Silica Coupled to ESI-FTICR-MS"

 

15:45 – O10: A. Ganesan, University of Southampton

"New vistas in the Pictet-Spengler reaction"

 

16:05 – O11: Thomas E. Nielsen, Carlsberg Laboratory, SPOCC Centre

"Novel Applications of the Picket-Spengler to Solid-Phase Combinatorial Chemistry"

 

16:25 – O12: Fernando Albericio, University of Barcelona

"Solid-phase and solution strategies for the preparation of a -Amido Ketone-based libraries"

 

 

16:45: Break

Combinatorial Synthesis and Technology

Chair: Günther Jung

17:05 – IN4: Rob Liskamp, Utrecht University

"From synthetic receptors towards synthetic antibodies using combinatorial chemistry"

 

17:30 – O13: Chaim Gilon, The Hebrew University, Jerusalem

"Discovery of SEB superantigen antagonists using backbone cyclic peptide libraries"

 

17:50 – O14: Koichi Fukase, University of Osaka

"Synthesis based on affinity separation : rapid synthesis using affinity tag"

 

 

Tuesday, June 31

Nanoscale Synthesis, Assays and Analysis

Chair: Lars Baltzer

09:00 – IN5: Manfred Auer,  Novartis, Austria

“CONA-HTS (Confocal Nanoscanning - Bead-Picking - AIDA-Technology),Redefining the lead discovery process by a joint combinatorial chemistry-, confocal fluorescence- and dye chemistry approach”

 

09:25 – O15: György Dormán, ComGenex, Inc.

"Immobilized surrogate compound libraries for rapid affinity profiling"

 

09:45 – O16: Ronald Frank, GBF, Germany

"Highly parallel micro-scale synthesis of structurally diverse compound repertoires: chemical recombination of natural product fragments"

 

10:05 – IN6: Ferenc Darvas, ComGenex, Inc.

"Combinatorial Chemistry: Facing the Challenge of Micro- and Nanochemistry"

 

 

10:30: Coffee Break

New Scaffolds and Natural Product Synthesis

Chair: Dennis Hall

11:00 – IN7: Ole Hindsgaul, University of Alberta

"Screening of Mixtures Using Frontal Affinity Chromatography Coupled to Mass Spectrometry (FAC/MS): Emphasis on Oligosaccharide Ligands"

 

11:25 – O17: Mercedes Alvarez, University of Barcelona

"Solid Phase Synthesis of Lamellarins"

 

11:45 – O18: Takayuki Doi, Tokyo Inst. Of Technology

"A library synthesis of cyclic depsipeptides Aurilide and its derivatives on solid-support"

 

 

12:05: Lunch/Poster/Exhibition

Combinatorial Biochemistry and Biology

Chair: Arpad Furka

13:35 – PL1: Jim Wells, Sunesis Pharmaceuticals, Inc.

"Drug Discovery at Signaling Interfaces"

 

14:15 – O19: Phaedria St.Hilaire, Carlsberg Biosector

"Protein affinity profiling"

 

14:35 – O20: Lars Baltzer, University of Linköbing

"The combinatorial approach to receptors, screens and sensors in designed folded polypeptides that catalyze their own functionalization site-selectively"

 

14:55 – O21: Michael Pirrung, Duke University

"Analysis of combinatorial mRNA splicing using Arrayed Primer Extension (APEX)"

 

15:15 – IN8: Renata Pasqualini and Wadih Arap, UT M. D. Anderson Cancer Center

"Mapping Vascular Diversity by Screening Peptide Libraries" 

 

 

15:45: Break

 
 

 

16:10 – 19:00 Posters

 

Wednesday, July 2

Drug Discovery and Lead Optimisation

Chair: Steve Maginn

09:00 – IN9: Hossain Saneii, President & CEO, Advanced SynTech

"Ugi-Type Multi-Component Condensation Reactions on Solid Support"

 

09:25 – O22: Hans Emtenas, Umea University

"Design and Synthesis of 2-Pyridiones; Inhibition of Pili Assembly in Pathogenic Bacteria"

 

09:45 – O23: László Ürge, ComGenex, Inc.

"Novel method for calculating the absolute diversity index (ADI) for drug candidate libraries"

 

10:05 – O24: Lieven Meerpoel, Johnson & Johnson Pharmaceutical Research and Development

"Design, parallel Synthesis, and Structure-Activity Relationship of Novel Microsomal Triglyceride Transfer Protein Inhibitors"

 

 

10:25: Coffee Break

Drug Discovery and Lead Optimisation

Chair: Ferenc Darvas

10:55 – IN10: Takashi Takahashi, Tokyo Institute of Technology

"Solution- and solid-phase synthesis for a library of oligosaccharides"

 

11:20 – O25: Mats Larhed,

"High-Speed Optimization of Malarial Plasmepsin I and II Inhibitors"

 

11:40 – O26: Rubén Ventura, University of Barcelona

"Functionally diverse purine libraries as Chemical Inductors of dimerization (CID)

 

 

12:25: Lunch/Poster/Exhibition

Material Science and Catalysts

Chair: Hubert Gstach

13:55 – PL2: Manfred Baerns,

"Combinatorial heterogeneous catalysis - design of experiments and data analysis"

 

14:35 – O27: Helma Wennemers, University of Basel

"A New Method for the Discovery of Catalysts in Split-and-mix Libraries"

 

14:55 – O28: Stephen Boppart, Symyx Technologies AG

"High Throughput Exploration of the Physical and Chemical Properties of Materials and Drug Candidates"

 

 

15:15: Break

Material Science and Catalysts

Chair: Manfred Baerns

15:45 – O29: Johannes G. de Vries, DSM Research, Life Sciences - Advanced Synthesis & Catalysis  

"Use of High Throughput Experimentation in Homogeneous Catalysis for Fine Chemicals"

 

16:05 – O30: Yasuhiro Uozumi, Institute for Molecular Science, Okazaki

“Development of Amphiphilic Polymer-Supported Palladium-Phosphine Complexes: Catalysts for Green, Safe and High-Throughput Processes”

 

16:25 – O31: Eicke Kunst, University of Hanover

"Pd-Catalysed transfer hydrogenations and C-C cross coupling reactions in flowthrough reactors"

 

 

17:15 – 1900 Posters

 

 

19:15: Galla Dinner

 

Thursday July 3

Dynamic Libraries and Molecular Recognition

Chair: Fernando Albericio

09:00 – PL3: Jeremy Sanders, University Chemical Laboratory, Cambridge

"Dynamic combinatorial chemistry: New opportunities for molecular recognition and catalysis"

 

09:40 – O32: Christina Chamorro, Utrecht University

"Combinatorial Synthesis and Screening of a CTV-based Tripodal Artificial Receptor Library"

 

10:00 – O33: Thomas Hoeg-Jensen, Novo Nordisk A/S

"Preparation and screening of diboronate libraries for identification of new carbohydrate sensors"

 

10:20 – O34: Juan M. Benito, Carlsberg Laboratory, SPOCC Centre

"Design and Synthesis of Cyclic Peptides as Small Molecule Receptors: A Solid-Phase Combinatorial Approach"

 

 

10:40: Coffee Break

Multicomponent Reactions in Combinatorial Chemistry

Chair: Jean Martinez

11:10 – IN11: Alexander Dömling, Morphochem

"Three themes in drug discovery using multicomponent reaction chemistry"

 

11:35 – O35: Andras Lukács, ComGenex, Inc.

"Novel applications of Biginelli reaction. Solution phase parallel synthesis of dihydropyrimidinone, dihydropyrimidinthione, dihydropyrimidothiazine libraries"

 

11:55 – O36: Dennis Hall, University of Alberta

"A three-component reaction for the diversity-oriented combinatorial synthesis of polysubstituted piperidines"

 

12:15 – O37: Gerardo Byk, Bar Ilan University

"Anomalous regioselective MCR4 Biginelli reaction: One pot synthesis of spiro heterobicyclic aliphatic rings"

 

 

12:35: Lunch/Poster/Exhibition

Multicomponent Reactions in Combinatorial Chemistry

Chair: Jörg Rademann

14:05 – O38: Jefferson Revell, University of Southampton

"Polymer Bound 9-Borabicyclo[3.3.1]nonane: A Novel and Selective Hydroborating Reagent"

 

14:25 – O39: Michael Barth, University of Tübingen

"High loaded ULTRA-resins: An evaluation of different supports and their application in polymer-supported chemistry"

 

14:45 – O40: Birgitte Gundersen, Acadia Pharmaceuticals A/S

"A Combinatorial Scaffold Approach Based Upon a Multicomponent Reaction"

 

 

15:05: Break

 

 

15:30: Awards and Closing Ceremony

 

 O = Oral Presentation

IN = Invited Lecture

PL = Plenary Lecture

 

Overview