ASCMC'04 Moscow
04/05/2004
13:00

Registration
The registration desk will remain open during the whole symposium.

17:30

Welcome Reception
From 17:30 - 18:30, in the hall of the Mezhdunarodnaya Hotel.

05/05/2004
08:30

Opening

09:20

Perspectives in Total Synthesis

Prof. K.C. NICOLAOU
(THE SCRIPPS RESEARCH INSTITUTE, Houston, United States)
10:20

Coffee break

10:45

Biomimetic Oxidations of Organic Substrates

Prof. Jan-Erling BÄCKVALL
(STOCKHOLM UNIVERSITY, Stockholm, Sweden)
11:35Studies on Bioactive Macrocycles: New Concepts and Spin-offs
Prof. Alois FÜRSTNER
(MAX PLANCK INSTITUT FUR KOHLENFORSCHUNG, Muelheim an der Ruhr, Germany)
12:25

Lunch

13:45"IN SILICO" Design and Focused Synthesis of New Neuroactive Compounds in the Series of Glutamate Receptors Ligands
Prof. Nikolay S. ZEFIROV
(INSTITUTE OF PHYSIOLOGICALLY ACTIVE COMPOUNDS, Moscow, Russia)
14:35Biomimetic Synthesis
Prof. Sir Jack BALDWIN
(UNIVERSITY OF OXFORD, OXFORD, United Kingdom)
15:25

Coffee break

15:50Catalytic Asymmetric Synthesis of Pharmaceuticals
Prof. Masakatsu SHIBASAKI
(UNIVERSITY OF TOKYO, Tokyo, Japan)
16:40Drug Discovery - Back to the Future
Prof. K. Barry SHARPLESS
(THE SCRIPPS RESEARCH INSTITUTE, LA JOLLA,, CA, United States)
19:30

BANQUET
Buffet dinner at the Presidency of the Academy of Science.

06/05/2004
08:30

Challenges in Drug Discovery: Design and Synthesis of Novel Drug Candidates

Prof Magid ABOU-GHARBIA
(TEMPLE UNIVERSITY, Philadelphia, United States)
09:05Application of Enabling Technologies to Expedite Drug Discovery
Dr Mark DUGGAN
(LINK MEDICINE CORPORATION, Cambridge, United States)
09:30Designing Selective Kinase Inhibitors: Tools, Concepts, Challenges and Opportunities
Dr Serge HALAZY
(SERONO INTERNATIONAL S.A., GENEVE, Switzerland)
09:55Electrophilic Fluorodesilylation of Organosilanes a New Synthetic Route to Various Fluorinated Compounds
Prof. Véronique GOUVERNEUR
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
10:05

Coffee break

10:35Design and Synthesis of Enzyme Inhibitors - From Concepts to Practice
Prof. Stephen HANESSIAN
(UNIVERSITY OF MONTREAL, MONTREAL, QC, Canada)
11:25Indoline and Indolenine Intermediates in the Syntheses of Complex Indole Derivatives
Prof. Maria PREOBRAZHENSKAYA
(GAUSE INSTITUTE OF NEW ANTIBIOTICS, MOSCOW, Russia)
11:35Molecular Diversity from Acylnitroso Cycloadditions: Preparation of Novel Scaffolds and Focused Targets
Prof. Marvin MILLER
(UNIVERSITY OF NOTRE DAME, NOTRE DAME, IN, United States)
11:45

ViagraTM & Beyond: Selective PDE5 Inhibitors for Treatment of MED

Dr Mark BUNNAGE
(VERTEX PHARMACEUTICALS, Boston, United States)
12:10Application of Chemogenomic Principles to Library and Template Design
Dr Thomas R. WEBB
(CHEMBRIDGE CORPORATION, SAN DIEGO, United States)
12:35

Lunch

13:45Structure-Based Design of Nonpeptidic Enzyme Inhibitors: Molecular Recognition Studies with Biological Receptors
Prof. François DIEDERICH
(ETH ZURICH, Zürich, Switzerland)
14:35SAR By XRay: A New Approach Combining Screening and Rational Drug Design. Application to the Discovery of Nanomolar Src SH2 Binders
Dr Dominique LESUISSE
(SANOFI AVENTIS, Chilly-Mazarin, France)
15:00Molecular Design, Chemical Synthesis and Biological Evaluation of Quinoxaline-Carbohydrate Hybrids as Novel and Selective Photo-Induced Dna Cleaving and Cytotoxic Agents
Prof. Kazunobu TOSHIMA
(KEIO UNIVERSITY, YOKOHAMA, Japan)
15:10

Coffee break

15:40

From Synthetic Polyelectrolites to Vaccinating Macromolecules

Prof. Viktor A. KABANOV
(RUSSIAN ACADEMY OF SCIENCES, Russia)
16:30Arene-Arene Interactions Between the Substrate and the Organocatalyst as the Driving Force In the Asymmetric Allylation of Aldehydes with Allyltrichlorosilanes.
Dr Andrei MALKOV
(UNIVERSITY OF GLASGOW, Glasgow, United Kingdom)
16:40Asymmetric Approach to Proline-Derived Spiro-Β-Lactams - Staudinger Reaction of N-Protected-4-Methanesulfonyloxy-L-Proline with N-Aryl Imines
Dr Mohan THIRUVAZHI
(CHEMBRIDGE RESEARCH LABORATORIES, SAN DIEGO, United States)
16:50Hit and Lead Generation - Beyond High Throughput Screening
Dr Alexander ALANINE
(INDEPENDANT RESEARCHER, Brinckheim, France)
19:00

Optional:
Swan Lake Ballet at the Bolshoï Theater

21:30

Moscow by night guided tour (First departure)

22:00

Moscow by night guided tour (Second departure)

07/05/2004
08:30Synthesis and Pharmacological Characterization of Novel Epothilone Derivatives
Dr Rainer METTERNICH
(CAPROTEC BIOANALYTICS, Basel, Switzerland)
09:05The Discovery of BIBN4096, a Novel CGRP Antagonist for the Treatment of Migraine
Prof. Dr. Gerd SCHNORRENBERG
(BOEHRINGER INGELHEIM PHARMA KG, Biberach an der Riss, Germany)
09:30The Synthesis of Biarylthioether derivatives as GlyT1 Inhibitors
Dr Garrick SMITH
(H. LUNDBECK A/S, VALBY, Denmark)
09:55Catalytic Synthesis of Azoles, or Teaching an Old Dog New Tricks
Prof. Valery FOKIN
(THE SCRIPPS RESEARCH INSTITUTE, LA JOLLA, United States)
10:05

Coffee break

10:35New Multicomponent Reactions
Prof. Nicos A. PETASIS
(UNIVERSITY OF SOUTHERN CALIFORNIA, LOS ANGELES, United States)
11:25Computer-Aided Discovery of New Pharmacological Agents With Multiple Mechanisms Of Action
Prof. Vladimir POROIKOV
(INSTITUTE OF BIOMEDICAL CHEMISTRY OF RUS. ACAD. MED. SCI., Moscow, Russia)
11:35Dysinosins B – D, Inhibitors Of Factor Viia And Thrombin From The Australian Sponge Lamellodysidea Chlorea
Dr Malcolm BUCHANAN
(GRIFFITH UNIVERSITY, BRISBANE, QUEENSLAND, Australia)
11:45LMW Agonists for the Human LH Receptor: Identification, Optimisation and Mechanism of Action
Dr Marco TIMMERS
(ORGANON, OSS, The Netherlands)
12:10Solution Phase Combinatorial Chemistry: Enabling Technologies for Heterocyclic Synthesis
Dr Larry TRUESDALE
(PFIZER, LA JOLLA, United States)
12:35

Lunch

13:45Research Collaborations and Technology Integration
Dr Michael T. CLARK
(PFIZER, NEW LONDON, United States)
14:10Compound Collection Enhancement Activities in AstraZeneca
Dr Mike T. COX
(, HOLMES CHAPEL, Cheshire, United Kingdom)
14:35Developing and Managing Discovery Chemistry Collaborations
Mr Steven HUTCHINS
(MERCK & CO., RAHWAY, United States)
15:00

Coffee break

15:15The Impact of Out-sourcing on R&D Productivity
Dr Jay MCGILL
(LILLY, INDIANAPOLIS IN, United States)
15:40Chemical Outsourcing: Beyond Routine Work
Dr. Patrice TALAGA
(UCB, Braine-L'Alleud, Belgium)
16:0510 Years of Discovery Chemistry Outsourcing in Russia: From Compound Acquisition to Strategic Research Collaborations
Dr Gene VAISBERG
(CHEMBRIDGE CORPORATION, San Diego, United States)
19:30

OPERA PERFORMANCE at NEW OPERA THEATER

08/05/2004
08:30Progress in the Total Synthesis of Polycyclic Natural Products
Prof. Johann MULZER
(UNIVERSITY OF VIENNA, Vienna, Austria)
09:20The Construction of the Chiral Quaternary Carbon in Drug Discovery Directed towards the Novel Neuroprotective Agent E2050
Dr Teiji KIMURA
(EISAI CO. LTD, IBARAKI, Japan)
09:45Fluorinated Azaheterocycles in Medicinal Chemistry
Prof. Valeri Nikolaevich CHARUSHIN
(URAL TECHNICAL UNIVERSITY, EKATERINBURG, Russia)
10:35

Coffee break

11:05Polycycles from Polyenes, Seeking Opportunities for Organic Synthesis
Prof. Erik SORENSEN
(PRINCETON UNIVERSITY, Princeton, United States)
11:55Tris-(2-Hydroxyethyl) Ammonium Salts of Aryl Heteroacetic Acids – New Class of Drugs And Biologically Active Compounds
Prof. Anna MIRSKOVA
(FAVORSKII INSTITUTE OF CHEMISTRY, IRKUTSK, Russia)
12:05Practical Considerations in Predicting ADMET Properties from Chemical Stucture
Dr Scott BOYER
(ASTRAZENECA, Södertälje, Sweden)
13:00

Lunch

14:00

KREMLIN GUIDED TOUR

19:00

Optional:
Evgeny Onegin at the Bolchoï Theater

09/05/2004
09:00

Optional:
TOUR 1 Tretiakov Galery + Cathedral of Christ the Saviour

09:00

Optional:
TOUR 2 Pushkin Museum + Cathedral of Christ the Saviour

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Under the auspices of the European Federation for Medicinal Chemistry

EFMC

Organized by ChemBridge Corporation


and the Medicinal Chemistry Section of the D.I. Mendeleev Russian Chemical Society