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SC4: Modern Lead Generation Strategies - Part 1
Tuesday, June 14 | 12:00 – 3:00 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 1 will introduce lead generation and the different hit generation methods available today.

Podcast Download Podcast with Joerg Holenz


Stay on to attend Part 2 which focuses on how to convert these hits to leads and the most recent trends in lead generation.

Chairperson:

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


Instructors:

Tim Cernak, Ph.D., Associate Principal Scientist, Discovery Chemistry, Automation & Capabilities Enhancement, Merck Boston

Rajiah Aldrin Denny, Ph.D., Senior Principal Scientist, Cheminformatics and Computational Chemist, Pfizer, Inc.

Ivan V. Efremov, Ph.D., Senior Principal Scientist, Worldwide Medicinal Chemistry, Pfizer, Inc.

Matthew Clark, Ph.D., Senior Vice President, Research, X-Chem


Detailed Agenda:

Introduction: How Lead Generation Paradigms Have Changed in Recent Years to Cope with Increasing Demands of Target Space and Reducing Attrition

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

HTS, Mid-Throughput Screening (MTS), Iterative Screening, Focused Libraries, New Chemical Space

Tim Cernak, Ph.D., Associate Principal Scientist, Discovery Chemistry, Automation & Capabilities Enhancement, Merck Boston

Virtual Screening and Rational Lead Design

Rajiah Aldrin Denny, Ph.D., Senior Principal Scientist, Cheminformatics and Computational Chemist, Pfizer, Inc.

Competitive-Based Lead Generation, SOSA, Fast Follower

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

Fragment-Based Lead Generation

Ivan V. Efremov, Ph.D., Senior Principal Scientist, Worldwide Medicinal Chemistry, Pfizer, Inc.

DNA Encoded Libraries

Matthew Clark, Ph.D., Senior Vice President, Research, X-Chem

Exercise: Developing an Active Generation Plan for Three Projects

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

 

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.

 Tim_CernakTim Cernak, Ph.D., Associate Principal Scientist, Discovery Chemistry, Automation & Capabilities Enhancement, Merck Boston

Dr Tim Cernak received his Ph.D. from McGill University and was a postdoctoral researcher at Columbia University before joining Merck Research Labs, Rahway, in 2009. As part of the Rahway Discovery Chemistry team, Tim pursued novel treatments for diabetes and hypertension. Tim is interested in technology enablement with a focus on applications of catalysis, parallel synthesis, and C-H activation in medicinal chemistry. In 2014, Tim joined Merck Boston where he is an Associate Principal Scientist with the Automation and Capabilities Enhancement group. Tim is a member of the Scientific Advisory Board for the National Science Foundation Center in Selective C-H Functionalization.

Rajah_Aldrin_Denny Rajiah Aldrin Denny, Ph.D., Senior Principal Scientist, Cheminformatics and Computational Chemist, Pfizer, Inc.

Rajiah is a senior principal scientist in World Wide Medicinal Chemistry at Pfizer Global R&D. Prior to that he was an independent consultant and worked at Jus Consulting (later Avila Therapeutics now Celgene). He was a structural biology researcher in the Computational Drug Design Group at Biogen-Idec.

 Ivan_EfremovIvan V. Efremov, Ph.D., Senior Principal Scientist, Worldwide Medicinal Chemistry, Pfizer, Inc.

Ivan Efremov joined Pfizer in 2001 after completing his Ph.D. in the laboratory of Prof. Leo Paquette at the Ohio State University working on total synthesis of neoclerodane diterpenoids. During his career at Pfizer, he made key contributions to delivery of several clinical assets in Neuroscience and Immunology therapeutic areas. He was a key player in implementation of platform technologies such as parallel medicinal chemistry, fragment-based drug design and hit-to-lead workflow. Currently, he is a medicinal chemistry leader of a phenotypic project in the Rare Disease therapeutic area.

 Matthew_ClarkMatthew Clark, Ph.D., Senior Vice President, Research, X-Chem

Matthew A. Clark joined X-Chem Pharmaceuticals in 2010 as VP of Chemistry, and currently serves as SVP for Research. Before coming to X-Chem, Matthew was Director of Chemistry at Praecis Pharmaceuticals, later GlaxoSmithKline, where he led a group responsible for design and synthesis of DNA-encoded chemical libraries. At Praecis, Matthew was involved in the early development and implementation of the DNA-encoded library platform. Matthew received his B.S. in Biochemistry from the University of California, San Diego, and his Ph.D in Chemistry from Cornell University. He conducted post-doctoral studies at the Massachusetts Institute of Technology.


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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