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SC7: Modern Lead Generation Strategies - Part 2
Tuesday, June 14 | 3:30 – 6:30 pm


Lead Generation is where chemical project assets are first created, and as such it is the area of Medicinal Chemistry that most strongly influences timelines and attrition rates. This discipline has undergone significant paradigm changes within recent years as new hit generation techniques have emerged and novel lead characterization methods have been invented. This two-part short course will give a comprehensive and up-to-date review of the field along with many practical examples and is intended for a broader audience ranging from beginner to advanced level.

Part 2 will center on how to convert these hits to leads and the most recent trends in lead generation.

Podcast Download Podcast with Joerg Holenz


Arrive early to attend Part 1 which introduces lead generation and the different hit generation methods available today.

Chairperson:

Joerg Holenz, Ph.D., Director, Discovery and Preclinical Sciences; Project Leader, Neuroscience iMed, AstraZeneca Neuroscience


Instructors:

Dean Brown, Ph.D., Director, Discovery and Preclinical Sciences, AstraZeneca

John Mathias, Ph.D., Senior Director, Cystic Fibrosis Program Leader, Pfizer, Inc.

Erin F. DiMauro, Ph.D., Principal Scientist, Medicinal Chemistry, Amgen, Inc.

Ivan Cornella-Taracido, Senior Principal Scientist, Discovery Chemistry, Merck

Jeremy Green, Ph.D., Senior Director, Chemistry, Vertex

Detailed Agenda:

Hit to Lead Phase

Dean Brown, Ph.D., Director, Discovery and Preclinical Sciences, AstraZeneca

Lead Quality Metrics

Jeremy Green, Ph.D., Senior Director, Chemistry, Vertex

Lead Characterization Techniques, Affinity Screens, Biacore SPR, NMR, ITC, Protein Melting Temperature Methods, etc.

John Mathias, Ph.D., Senior Director, Cystic Fibrosis Program Leader, Pfizer, Inc.

Amgen Tankyrase Program: A Case Study in Rapid Generation of Quality Leads

Erin F. DiMauro, Ph.D., Principal Scientist, Medicinal Chemistry, Amgen, Inc.

Latest Trends in Lead Generation: Dark Chemical Matter, Programmable Cells, Chemical Biology, etc.

Ivan Cornella-Taracido, Senior Principal Scientist, Discovery Chemistry, Merck

Hit to Lead Exercise:

Joerg Holenz, Ph.D., Director, Discovery and Preclinical Sciences; Project Leader, Neuroscience iMed, AstraZeneca Neuroscience

Participants will receive a sheet with hit structures (along with information on the target) and will have to select hits they would prioritize for hit expansion.

Instructor Bios:


 Joerg_HolenzJoerg Holenz, Ph.D., Director, Discovery and Preclinical Sciences; Project Leader, Neuroscience iMed, AstraZeneca Neuroscience

Joerg is a trained Organic and Medicinal Chemist and acquired his Ph.D. in Germany on the synthesis of alkaloids as antimalarial agents. He started his professional career in 1998 as Process Chemist at Grunenthal Pharmaceuticals in Germany, leading the preclinical activities of the later marketed analgesic Tapentadol. From 2003 to 2006, he headed the Medicinal Chemistry Department of Barcelona-based Laboratorios Esteve. In 2006, Joerg joined AstraZeneca’s CNS/PainResearch Unit in Sodertalje, Sweden, as a Project Leader, and later headed the Lead Generation Section within the Medicinal Chemistry Department. In 2012, Jorg was selected to join the newly formed ‘virtual’ Neuroscience Unit in Boston as Project Director, and in this role is responsible for pioneering a novel concept of driving Research and Development via increased use of academic and industry collaborative networks. In his career, Joerg worked predominantly with peripheral and central targets in the Pain/Neuroscience disease areas, where hedelivered several clinical candidates (e.g. Rosonabant, E-6199, E-52862, or AZD3839). Joerg has edited, authored or contributed to more than 45 publications, 50 patent applications and several books and book chapters.

 Dean_BrownDean Brown, Ph.D., Director, Discovery and Preclinical Sciences, AstraZeneca

Dean G. Brown joined AstraZeneca (then Zeneca) in 1997 at the Wilmington Delaware site. He earned his Ph.D at the University of Minnesota in organic chemistry conducting methodology and natural product total synthesis. During his tenure at AstraZeneca, Dean helped to build many new programs as part of the CNSP Lead Generation group, several resulting in clinical candidates. Dean was also instrumental in the rebuild of the AZ corporate and fragment screening collections from 2004-2010. In 2010, Dean joined AZ Infection, and led a chemistry section with a primary focus of creating new programs for multi-drug resistant infections and respiratory viral infections. He is now Director of Discovery and Preclinical Sciences at AstraZeneca Neurosciences in Cambridge, MA. Dean is listed as an author or co-author on more than 40 publications and patent applications, including several granted patents on clinical candidates.

 John_MathiasJohn Mathias, Ph.D., Senior Director, Cystic Fibrosis Program Leader, Pfizer, Inc.

John Mathias received his PhD with Prof Fraser Stoddart from Sheffield University in 1991 & Post Doctoral training with Prof George Whitesides at Harvard University from 1991-1993. He joined Pfizer in Sandwich in 1993 and has worked as a Medicinal Chemist in the areas of Anti-Virals, Sexual Health, Urology & Allergy & Respiratory leading compounds into the clinic versus an array of different molecular targets including PDE5 inhibitors, Alpha 1 Receptor Antagonists, PDE4 inhibitors & p38 inhibitors. In 2006 he became an Associate Research Fellow working within the Lead Discovery Group in Sandwich with a remit to explore the potential for Slow Offset Kinetics & Biophysical Methods to impact on hit identification. He also led the establishment of Fragment-Based Drug Discovery methods in Sandwich & worked as part of the Inhalation by Design Medicinal Chemistry Initiative. In Feb 2009 he became Global Head of the High Throughput Screening Centre of Emphasis, with responsibility for leading the HTS groups Hit Identification efforts for all of Pfizer’s Research Units. In May 2011 he was appointed Head of Medicinal Chemistry for the Inflammation & Remodelling Group within the BioTherapeutics Chemistry Organisation. Since January 2013 he has been the Research Program Leader for the Pfizer – Cystic Fibrosis Foundation Therapeutics Collaboration.

 Erin_DemauroErin F. DiMauro, Ph.D., Principal Scientist, Medicinal Chemistry, Amgen, Inc.

In 1998, Erin received a B.S. in Chemistry from Wesleyan University, where she conducted research in synthetic organic chemistry with Professors Peter Jacobi and Albert Fry. In 2003, Erin obtained a Ph.D. in organic chemistry from the University of Pennsylvania, where she worked on bifunctional asymmetric catalysis with Professor Marisa Kozlowski. Erin is currently a Principal Scientist and Group Leader in Medicinal Chemistry at Amgen in Cambridge, MA, USA. At Amgen, Erin has contributed to programs in the therapeutic areas of neuroscience, inflammation, and oncology. Her teams have focused on lead generation for a variety of target classes including kinases, GPCRs, proteases, ion channels, PARPs, and transporters.

Ivan Cornella-Taracido, Senior Principal Scientist, Discovery Chemistry, Merck

 

Jeremy Green, Ph.D., Senior Director, Chemistry, Vertex


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SPONSORSHIPS & EXHIBITS

The exhibit hall has sold out the past four years, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2016, contact:

Joseph Vacca, M.S.,
Associate Director, Business Development
781-972-5431
jvacca@healthtech.com