15th RSC-SCI Medicinal Chemistry Symposium
26/02/09 13:07 Filed in: Medicinal
Chemistry
15th RSC- SCI
Medicinal Chemistry Symposium
6-9 September 2009
Churchill College, Cambridge, UK
FINAL CIRCULAR and APPLICATION FORM
Medicinal Chemistry Symposium
6-9 September 2009
Churchill College, Cambridge, UK
FINAL CIRCULAR and APPLICATION FORM
15th
RSC-
SCI
Medicinal Chemistry Symposium
6-9 September 2009
Churchill College, Cambridge, UK
FINAL CIRCULAR and APPLICATION FORM
Introduction
The organisers cordially invite you to participate in the 15th RSC-SCI Medicinal Chemistry
Symposium, a major biennial event in the field of Medicinal Chemistry. This year, reflecting the
present climate in pharmaceutical research, the theme of the conference will be Refining
Drug Discovery: Evolution or Revolution! Held at Churchill College Cambridge, UK, this
meeting has become synonymous with excellent scientific discussion and enjoyable social
discourse. The organisers hope you will accept their invitation to participate in this
international symposium.
Programme
Sunday 6 September
15.00 Registration Desk open until 18.30
17.00 Tea
18.30 Welcome Barbecue and Reception (College residents and ticket holders)
Monday 7 September
08.55 Welcome and Opening Remarks
David Witty, GlaxoSmithKline (Chair of the Organising Committee)
Enzyme Inhibitors
Chair: Chris Swain, Cambridge Medchem Consulting
09.00 The identification of selective p38 inhibitors with high blood potency suitable for
clinical development
Vipul Patel, GlaxoSmithKline, UK
09.45 Progressing carboxylic acid leads as PDE7 inhibitors
Nigel Swain, Pfizer GRD, UK
10.30 Coffee
11.00 Calcilytics – A treatment for established osteoporosis
Leo Wilder, Novartis Institutes for BioMedical Research , Switzerland
11.45 Potent, non-peptidic, orally-active Renin inhibitors
Olivier Bezençon, Actelion , Switzerland
12.30 Poster talk 1
12.45 Lunch
Chair: Urs Baettig, Novartis Institutes for BioMedical Research
14.00 Non-nucleoside inhibitors for the treatment of hepatitis C vi rus infection
Frank Narjes, Merck Sharp & Dohme, Italy
14.45 Discovery of polymerase inhibitors for the treatment of Dengue Fever: A showcase
of modern drug discovery in tropical diseases
Zheng Yin, Novartis Institute for Tropical Diseases, Singapore
15.30 Tea
16.00 A multivalent approach to drug discovery for novel antibiotics: Clinical compound
TD-1792
Daniel D Long, Theravance, USA
16.45 Inhibitors of GSK-3 kinase for the treatment of neurodegenerative diseases
Juan-Miguel Jimenez, Vertex, UK
17.30 Poster talk 2
17.45 Poster Session 1 and Wine Reception
19.00 Dinner for College residents and ticket holders
Tuesday 8 September
Receptor / Ion Channels
Chair: Andrew Williams, Eli Lilly and Company
09.00 Medicinal chemistry and biology of E2007, an orally active AMPA receptor
antagonist for neurological disorders
Koichi Ito, Eisai, Japan
09.45 MC4 agonists for the treatment of sexual dysfunction
Mark Lansdell, Pfizer GRD, UK
10.30 Coffee
11.00 Presentation, RSC BMCS 2009 Malcolm Ca mpbell Award
11.15 Next generation NK1 antagonists for next generation applications
Robert DeVita, Merck & Co, USA
12.00 Discovery of potent and selective non-steroidal glucocorticoid receptor agonists
David House, GlaxoSmithKline, UK
12.45 Lunch
Chair: Alan Stobie, Pfizer GRD
14.00 Antitussive profile of the NOP agonist SCH 486757
Deen Tulshian, Schering-Plough, USA
14.45 Identification and optimisation of triazole oxytocin antagonists, leading to a clinical
candidate
Alan Brown, Pfizer GRD, UK
15.30 Tea
16.00 Synthesis and pharmacological evaluation of novel GABAb receptor agonists as
gastroesophageal reflux inhibitors
Thomas Elebring, AstraZeneca, Sweden
16.45 The discovery of novel muscarinic M1 receptor agonists for treatment of CNS
disorders
Vincenzo Garzya, GlaxoSmithKline, UK
17.30 Poster talk 3
17.45 Poster Session 2
19.30 Reception
20.00 Conference Dinner and Entertainment for College residents and ticket holders
Wednesday 9 September
Refining Drug Discovery: Evolution or Revolution!
Chair: Steve Swallow, AstraZeneca
09.00 Biophysical techniques in drug design – A medicinal chemistry perspective
Mark Bunnage, Pfizer GRD, UK
09.35 Privileged structures in drug discovery
Klaus Müller, F Hoffmann-La Roche, Switzerland
10.10 Lean thinking in medicinal chemistry
Craig Johnstone, AstraZeneca, UK
10.45 Coffee
11.15 CarboCarrier ™: A novel technology to extend the half-life of small proteins and
peptides
Martin de Kort, Schering-Plough, The Netherlands
11.50 An analysis of physicochemical drug properties associated with in vivo
toxicological outcomes
Simon Bailey, Pfizer GRD, USA
12.25 Lunch
New Topics in Drug Research
Chair: Phil Jones, Schering-Plough
14.00 Indole-carboxylic acid amides as novel CETP inhibitors: From hit to clinical
candidate
Philippe Pflieger, F Hoffmann-La Roche, Switzerland
14.30 Design, synthesis and discovery of the first NO- and Haem-independent sGC
activator BAY 58-2667 for the treatment of acute decompensated heart failure
Michael G Hahn, Bayer Healthcare, Germany
15.00 Targeting the metabolic syndrome through inhibitors of 11beta-hydroxysteroid
dehydrogenase Type 1
Eric Valeur, Merck-Serono, France
15.30 Optimization of hydroxamate based HDAC inhibitors
Michael Shultz, Novartis, USA
16.00 Closing remarks
David Witty, GlaxoSmithKline
Medicinal Chemistry Symposium
6-9 September 2009
Churchill College, Cambridge, UK
FINAL CIRCULAR and APPLICATION FORM
Introduction
The organisers cordially invite you to participate in the 15th RSC-SCI Medicinal Chemistry
Symposium, a major biennial event in the field of Medicinal Chemistry. This year, reflecting the
present climate in pharmaceutical research, the theme of the conference will be Refining
Drug Discovery: Evolution or Revolution! Held at Churchill College Cambridge, UK, this
meeting has become synonymous with excellent scientific discussion and enjoyable social
discourse. The organisers hope you will accept their invitation to participate in this
international symposium.
Programme
Sunday 6 September
15.00 Registration Desk open until 18.30
17.00 Tea
18.30 Welcome Barbecue and Reception (College residents and ticket holders)
Monday 7 September
08.55 Welcome and Opening Remarks
David Witty, GlaxoSmithKline (Chair of the Organising Committee)
Enzyme Inhibitors
Chair: Chris Swain, Cambridge Medchem Consulting
09.00 The identification of selective p38 inhibitors with high blood potency suitable for
clinical development
Vipul Patel, GlaxoSmithKline, UK
09.45 Progressing carboxylic acid leads as PDE7 inhibitors
Nigel Swain, Pfizer GRD, UK
10.30 Coffee
11.00 Calcilytics – A treatment for established osteoporosis
Leo Wilder, Novartis Institutes for BioMedical Research , Switzerland
11.45 Potent, non-peptidic, orally-active Renin inhibitors
Olivier Bezençon, Actelion , Switzerland
12.30 Poster talk 1
12.45 Lunch
Chair: Urs Baettig, Novartis Institutes for BioMedical Research
14.00 Non-nucleoside inhibitors for the treatment of hepatitis C vi rus infection
Frank Narjes, Merck Sharp & Dohme, Italy
14.45 Discovery of polymerase inhibitors for the treatment of Dengue Fever: A showcase
of modern drug discovery in tropical diseases
Zheng Yin, Novartis Institute for Tropical Diseases, Singapore
15.30 Tea
16.00 A multivalent approach to drug discovery for novel antibiotics: Clinical compound
TD-1792
Daniel D Long, Theravance, USA
16.45 Inhibitors of GSK-3 kinase for the treatment of neurodegenerative diseases
Juan-Miguel Jimenez, Vertex, UK
17.30 Poster talk 2
17.45 Poster Session 1 and Wine Reception
19.00 Dinner for College residents and ticket holders
Tuesday 8 September
Receptor / Ion Channels
Chair: Andrew Williams, Eli Lilly and Company
09.00 Medicinal chemistry and biology of E2007, an orally active AMPA receptor
antagonist for neurological disorders
Koichi Ito, Eisai, Japan
09.45 MC4 agonists for the treatment of sexual dysfunction
Mark Lansdell, Pfizer GRD, UK
10.30 Coffee
11.00 Presentation, RSC BMCS 2009 Malcolm Ca mpbell Award
11.15 Next generation NK1 antagonists for next generation applications
Robert DeVita, Merck & Co, USA
12.00 Discovery of potent and selective non-steroidal glucocorticoid receptor agonists
David House, GlaxoSmithKline, UK
12.45 Lunch
Chair: Alan Stobie, Pfizer GRD
14.00 Antitussive profile of the NOP agonist SCH 486757
Deen Tulshian, Schering-Plough, USA
14.45 Identification and optimisation of triazole oxytocin antagonists, leading to a clinical
candidate
Alan Brown, Pfizer GRD, UK
15.30 Tea
16.00 Synthesis and pharmacological evaluation of novel GABAb receptor agonists as
gastroesophageal reflux inhibitors
Thomas Elebring, AstraZeneca, Sweden
16.45 The discovery of novel muscarinic M1 receptor agonists for treatment of CNS
disorders
Vincenzo Garzya, GlaxoSmithKline, UK
17.30 Poster talk 3
17.45 Poster Session 2
19.30 Reception
20.00 Conference Dinner and Entertainment for College residents and ticket holders
Wednesday 9 September
Refining Drug Discovery: Evolution or Revolution!
Chair: Steve Swallow, AstraZeneca
09.00 Biophysical techniques in drug design – A medicinal chemistry perspective
Mark Bunnage, Pfizer GRD, UK
09.35 Privileged structures in drug discovery
Klaus Müller, F Hoffmann-La Roche, Switzerland
10.10 Lean thinking in medicinal chemistry
Craig Johnstone, AstraZeneca, UK
10.45 Coffee
11.15 CarboCarrier ™: A novel technology to extend the half-life of small proteins and
peptides
Martin de Kort, Schering-Plough, The Netherlands
11.50 An analysis of physicochemical drug properties associated with in vivo
toxicological outcomes
Simon Bailey, Pfizer GRD, USA
12.25 Lunch
New Topics in Drug Research
Chair: Phil Jones, Schering-Plough
14.00 Indole-carboxylic acid amides as novel CETP inhibitors: From hit to clinical
candidate
Philippe Pflieger, F Hoffmann-La Roche, Switzerland
14.30 Design, synthesis and discovery of the first NO- and Haem-independent sGC
activator BAY 58-2667 for the treatment of acute decompensated heart failure
Michael G Hahn, Bayer Healthcare, Germany
15.00 Targeting the metabolic syndrome through inhibitors of 11beta-hydroxysteroid
dehydrogenase Type 1
Eric Valeur, Merck-Serono, France
15.30 Optimization of hydroxamate based HDAC inhibitors
Michael Shultz, Novartis, USA
16.00 Closing remarks
David Witty, GlaxoSmithKline