Medicinal Chemistry Symposium 2013


Speakers: 9 September 2013

Laurent Sanière
Galapagos
GLPG0974, a FFA2 antagonist from hit to clinic

John Cumming
AstraZeneca
CCR2 antagonists for the treatment of neuropathic pain - the discovery and development of AZD2423

Miles Congreve
Heptares
Identification of orexin antagonists for the treatment of insomnia and addiction using structure based drug design

Daniel Long
Theravance Inc
A multivalent approach to peripherally restricted m-opioid receptor antagonists (PmMA) for opioid-induced bowel dysfunction (OBD)

Jorg Benningshof
Mercachem
Orally active CK1d inhibitors: novel treatment modality for insomnia and Alzheimer’s disease

Roger Butlin
AstraZeneca
Discovery of pyrazine carboxamide-basedDGAT1 inhibitors leading to clinical candidate AZD7687

Ramatoulie Camara
School of Life & Medical Sciences
Rational design of S100P/RAGE inhibitors: in search of a therapeutic agent in the fight against pancreatic cancer

Al Dossetter
MedChemica Limited
Multiparameter optimization of pharmaceuticals: the big-data way

Rebecca Deprez-Poulain
Pasteur Institute Lille
Discovery and optimization of Insulin-Degrading Enzyme inhibitors by screening and target-guided synthesis: from structure to cellular activity

Guido Furlotti
ACRAF Spa – Angelini Research Cente
Novel 3,4-dihydropyrazino[1,2-b]indazol-1(2H)-one derivatives targeting serotonin 2A and adrenergic alpha1 receptors as ocular antihypertensive agents

Nigel Greene
Pfizer Worldwide
Selecting safer chemical space using in vitro assays and chemical properties

Stijn Gremmen
Mercachem
CDK8 INHIBITORS with long residence time emerging from a retro-design approach: new opportunities for cancer treatment

Simon Hodgson
Hodgson Pharma Consulting/GlaxoSmithKline
Enhancing molecule quality by combining fragment approaches with early pharmacy input – an example with PGD2 synthase

John Link
Gilead Sciences
The discovery and development of GS-5885, a potent NS5A targeted antiviral agent for the treatment of HCV infection

Frederic Berst
Novartis
Non-ATP-site-directed kinase inhibitors: the IGF1R case

Stuart Onions
Sygnature Discovery
The discovery and profile of narrow spectrum kinase inhibitors as novel treatments for inflammatory pulmonary disease

Duncan Hay
University of Oxford
Reader’s block: discovery of an epigenetic chemical probe for CREBBP/p300 bromodomains

Jennie Hickin
Imperial College London
Aminoacylpyrrolidines as Leishmanial N-myristoyltranferase inhibitors

Rhian Holvey
University of Cambridge
Fragment-Based approach towards inhibitors of the TPX2 – Importin-a Interaction

Gu Liu
University of Oxford
Development of chemical tools for promoting iPS cell self renewal

William McCoull
AstraZeneca
Designing safer aminopyrazoles through simple quantum mechanical predictions for Ames activity

Oscar Méndez-Lucio
University of Cambridge
Proteochemometrics modelling: a technique for the design of GPCR ligands, kinase inhibitors and personalizing HIV treatment

Dale Mitchell
BioFocus
The identification of potential PET ligands for Alpha-Synuclein

Speakers: 10 September 2013

Jamie Scott
AstraZeneca
Discovery of novel agonists of GPR119 for the treatment of Type II Diabetes

Robert Owen
Pfizer
TRPM8 blockade and its role in cold pain signalling

Sanjeev Redkar
Astex Pharmaceuticals
Development of SGI-110, a potent hypomethylating agent, as epigenetic therapy in cancer

Paul Barsanti
Novartis Institutes for Biomedical Research
New approaches to traditional anti-mitotic chemotherapy: structure based drug design of the Eg5 inhibitor NVP-BQS481, from computer to clinic

Scott Webster
University of Edinburgh
Discovery of 11ß-HSD1 inhibitors for the treatment of Alzheimer’s dementia

Chas Bountra
University of Oxford and SGC
Medicinal chemistry experts in pharma are helping us to generate freely available probes for target discovery

Trevor Perrior
Domainex Inc
A novel approach to asthma therapy: inhibitors of the allergenic house dust mite peptidases

Tim Ritchie 
TJR Chem
Molecule properties and compound developability – what’s new?

David Norton
Astex Pharmaceuticals
176 compound fragment screen to preclinical candidates novel allosteric protease-helicase inhibitors for HCV

Thorsten Nowak
Conformetrix
Free ligand conformational populations in solution – a powerful drug discovery tool

Mark Pickworth
Heptares Therapeutics
Structure based drug design utilising stabilised receptors (StaRs): Identification of a selective muscarinic M1 pre-clinical candidate

Margarita Puente
GlaxoSmithKline
Advances on the discovery of potential antimalarial therapies derived from phenotypic screening

Mark Rackham 
Imperial College London
Design and synthesis of N-myristoyltranferase inhibitors: a promising treatment for malaria

Kate Smith
Paterson Institute for Cancer Research
The discovery and optimisation of the first reported small-molecule inhibitors of human 5’- tyrosyl DNA phosphodiesterase (Tdp2)

Anna-Karin Tiden
AstraZeneca
A potent, stable cathepsin C inhibitor with a step change in properties achieved through lead hopping

Steve Watson
H Lundbeck
Identification of the first small molecule inhibitors of the VPS10P family sorting receptor Sortilin

Speakers: 11 September 2013

Timothy Chapman
MRC Technology
Inhibitors of plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1), a novel target for the potential treatment of malaria

Juan-Miguel Jimenez
Vertex Pharmaceuticals Ltd
The design and optimisation of selective Protein Kinase C theta (PKC?) inhibitors for the treatment of autoimmune diseases

Martine Keenan
Epichem
Analogues of fenarimol as potential new treatments for Chagas Disease

Giuseppe Cecere
F Hoffmann-La Roche
Discovery of novel imidazolines and imidazoles as selective TAAR1 partial agonists for the treatment of psychiatric disorders

Adam Gilbert
Pfizer
Rational design of covalent enzyme inhibitors

Rick Roberts
Almirall
CRTh2: Can Residence Time help?

Alex Pasternak
Merck & Co
From screening impurity to potent and selective ROMK inhibitors - the path to new mechanism diuretics

Elizabeth Beck
Pfizer
Improving success in the development of novel PET ligands for CNS indications


Downloadable Files

CCR2 antagonists for the treatment of neuropathic pain - the discovery and development of AZD2423
John Cumming
PDF iconPDF (1312k)  

Orally active CK1d inhibitors: novel treatment modality for insomnia and Alzheimer’s disease
Jorg Benningshof
PDF iconPDF (217k)  

Discovery of pyrazine carboxamide-basedDGAT1 inhibitors leading to clinical candidate AZD7687
Roger Butlin
PDF iconPDF (18k)  

Rational design of S100P/RAGE inhibitors: in search of a therapeutic agent in the fight against pancreatic cancer
Ramatoulie Camara
PDF iconPDF (93k)  

Multiparameter optimization of pharmaceuticals: the big-data way
Al Dossetter
PDF iconPDF (57k)  

Rational design of S100P/RAGE inhibitors: in search of a therapeutic agent in the fight against pancreatic cancer
Rebecca Deprez-Poulain
PDF iconPDF (98k)  

Novel 3,4-dihydropyrazino[1,2-b]indazol-1(2H)-one derivatives targeting serotonin 2A and adrenergic alpha1 receptors as ocular antihypertensive agents
Guido Furlotti
PDF iconPDF (158k)  

Selecting safer chemical space using in vitro assays and chemical properties
Nigel Greene
PDF iconPDF (86k)  

CDK8 INHIBITORS with long residence time emerging from a retro-design approach: new opportunities for cancer treatment
Stijn Gremmen
PDF iconPDF (91k)  

Enhancing molecule quality by combining fragment approaches with early pharmacy input – an example with PGD2 synthase
Simon Hodgson
PDF iconPDF (752k)  

Reader’s block: discovery of an epigenetic chemical probe for CREBBP/p300 bromodomains
Duncan Hay
PDF iconPDF (244k)  

Aminoacylpyrrolidines as Leishmanial N-myristoyltranferase inhibitors
Jennie Hickin
PDF iconPDF (163k)  

Fragment-Based approach towards inhibitors of the TPX2 – Importin-a Interaction
Rhian Holvey
PDF iconPDF (210k)  

Development of chemical tools for promoting iPS cell self renewal
Gu Liu
PDF iconPDF (418k)  

Designing safer aminopyrazoles through simple quantum mechanical predictions for Ames activity
William McCoull
PDF iconPDF (25k)  

Proteochemometrics modelling: a technique for the design of GPCR ligands, kinase inhibitors and personalizing HIV treatment
Oscar Méndez-Lucio
PDF iconPDF (59k)  

The identification of potential PET ligands for Alpha-Synuclein
Dale Mitchell
PDF iconPDF (85k)  

Discovery of novel agonists of GPR119 for the treatment of Type II Diabetes
Jamie Scott
PDF iconPDF (1718k)  

New approaches to traditional anti-mitotic chemotherapy: structure based drug design of the Eg5 inhibitor NVP-BQS481, from computer to clinic
Paul Barsanti
PDF iconPDF (1245k)  

Medicinal chemistry experts in pharma are helping us to generate freely available probes for target discovery
Chas Bountra
PDF iconPDF (1422k)  

Molecule properties and compound developability – what’s new?
Tim Ritchie
PDF iconPDF (401k)  

176 compound fragment screen to preclinical candidates novel allosteric protease-helicase inhibitors for HCV
David Norton
PDF iconPDF (185k)  

Free ligand conformational populations in solution – a powerful drug discovery tool
Thorsten Nowak
PDF iconPDF (166k)  

Structure based drug design utilising stabilised receptors (StaRs): Identification of a selective muscarinic M1 pre-clinical candidate
Mark Pickworth
PDF iconPDF (40k)  

Advances on the discovery of potential antimalarial therapies derived from phenotypic screening
Margarita Puente
PDF iconPDF (175k)  

Design and synthesis of N-myristoyltranferase inhibitors: a promising treatment for malaria
Mark Rackham
PDF iconPDF (142k)  

The discovery and optimisation of the first reported small-molecule inhibitors of human 5’- tyrosyl DNA phosphodiesterase (Tdp2)
Kate Smith
PDF iconPDF (55k)  

A potent, stable cathepsin C inhibitor with a step change in properties achieved through lead hopping
Anna-Karin Tiden
PDF iconPDF (39k)  

Identification of the first small molecule inhibitors of the VPS10P family sorting receptor Sortilin
Steve Watson
PDF iconPDF (79k)  

Inhibitors of plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1), a novel target for the potential treatment of malaria
Timothy Chapman
PDF iconPDF (1078k)  

Discovery of novel imidazolines and imidazoles as selective TAAR1 partial agonists for the treatment of psychiatric disorders
Giuseppe Cecere
PDF iconPDF (321k)  

CRTh2: Can Residence Time help?
Rick Roberts
PDF iconPDF (761k)  

Improving success in the development of novel PET ligands for CNS indications
Elizabeth Beck
PDF iconPDF (816k)  


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