Chirality in Drug Compounds


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Chirality in Drug Compounts conference taking place May 18-19, 2009 in Philadelphia, PA

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Chirality in Drug Compounds

  1. 1. Register by 3/13/2009 for the All-Access Pass and Save $898 (See page 5 for details.) Chirality in May 18-19, 2009 • Philadelphia, PA Drug Compounds TM Techniques to obtain the molecule with the right pharmalogical profile Benefits of Attending: • Achieve efficacy of pharmaceutical compounds • Increase percentage yield • Discover new chiral structures to expand research options • Minimize research costs • Reduce time to market • Drive efficiency and cut waste Presenting Companies Include: Bristol-Myers Squibb Cornerstone Pharmaceuticals Johnson & Johnson Lundbeck Research USA Pfizer Pharmacopeia Rigel Pharmaceuticals Sapphire Therapeutics, Inc. University of the Sciences in Philadelphia Sponsors: Media Partners:
  2. 2. Chirality in May 18-19, 2009 • Philadelphia, PA Drug Compounds TM Who Should Attend Dear Colleague, This conference is designed scientists from both pharmaceuticals and academia with a focus in: In the current cost-conscious health care environment, the pharmaceu Discovery industry must take full advantage tical • of available resources to provide • Green Chemistry desperately needed new product opportunities. Scientists operating Research & Development this environment must increase thei within • r awareness and utilization of an arra Chemical Engineering new technologies in cooperative part y of • nerships to compete successfully in • Biotransformation today’s market. These technologies not only accelerate time to the des Organic Chemistry ired • decision point, but also offer long -term opportunities for superior effic • Biochemistry during commercial route developmen iency t and manufacturing. • Analytic Chemistry The necessity to analyze and purify chiral compounds has increased. Sponsorship and As demanded by the FDA, chiral pha rmaceuticals should be developed Exhibition Opportunities reach the market as single enantio and Sponsorships and Exhibits are excellent mer products. This fact makes robu chiral separation methods essentia st opportunities for your company to showcase l for product quality control analysis its products and services to high-level, targeted because the unwanted enantiomer , decision makers attending the conference. is often the most critical product impurity. Pharma IQ and Chirality in Drug Compounds will help companies like yours achieve sales, marketing and branding Here’s a rundown at what you’ll exp objectives by setting aside a limited number of erience at Chirality in Drug Compou event sponsorships and exhibit spaces – all of • Discover new research - the opportunities to enc nds: which are custom-tailored to help your ounter cutting-edge science are endless company create a platform to maximize its • Advanc exposure at the event. e your career while enhancing you r skills • Make Connection For more information on Sponsoring and s - network through unparalleled • Learn how you opportunities Exhibiting at Chirality in Drug Compounds, r peers are successfully utilizing tech please contact Thomas Boccard at 1-866-232- nology 8660 or I look forward to greeting you in Phil adelphia! Conferences and Webinars available: Visit us at and see what other Sincerely, exciting and information-packed conferences and webinars being offered by the International Quality & Productivity Center. About the Organizer: Pharma IQ, the pharmaceutical division Michelle Cardinal of IQPC, provides a forum to address the Sr. Conference Director critical issues facing the pharmaceutical IQPC-NY industry today. Pharma IQ utilizes workshop, conference and training course formats to facilitate a learning environment for pharmaceutical professional working in all areas of drug development from Discovery to Post-Marketing. 2 1-800-882- 8684 •
  3. 3. Pre-Conference Workshops Monday, May 18, 2009 8:00 Workshop Registration 11:00 Workshop Registration Workshop A 8:30 – 11:00 Workshop B 11:30 – 2:00 (Lunch will be served) Approaches to Diastereomeric Crystallization to Separate Enzymatic Biotransformation: Practical Tools for Enantiomers from Racemic Mixtures Drug Synthesis Optical resolution through diastereomeric crystallization chemically separates Enzymatic synthesis has left the realm of whole-cell fermentation enantiomers from racemic mixture by producing a salt. Because of the experimental and voluminous processing to enter an era of isolated consistency and easy adoption to manufacturing scale, it provides the most rapid and commercial biocatalysts performing as reagents, thereby cost-effective access to high-purity chiral drug intermediates and robust large-scale becoming more accessible and usable by today’s laboratory industrial processes. This workshop will include discussions on: scientists. The first step in enabling their use is a general • Rapid process optimization using high-throughput screening understanding of the available catalysts, their ease of use, and • Resolution of neutral racemates their relative likelihood of success. The second step is the • Resolution of molecules with multiple chiral centers incorporation of this new understanding in route design and • Going from bench-top to scale-up development for application toward API synthesis. It will also focus on the “Green Chemistry” aspects like: • Achieve high success rates with enzymes as reagents in • Minimizing the amount of chemicals retrosynthesis • Avoiding the use of toxic chemicals • Create user-friendly biotransformation in the laboratory setting • Solvent-less reactions • Optimize enzyme reactions • Reuse of chemicals • Design strategies for basic enzyme engineering Heightened proficiency with modern techniques and added familiarity with pertinent • Navigate regulatory implications of biotransformation examples of industrial application will convey greater expertise to practitioners of chiral drug synthesis. Workshop leader is to be announced. Please check the website at for updates and Niteen A. Vaidya, PhD announcements. CTO ChiroSolve Inc. Main Conference Day One Monday, May 18, 2009 2:00 Registration for Main Conference application of these technologies are depended on selectivity, sample solubility, sample size, and system availability. Examples, pros and 2:30 Chairperson’s Opening Remarks cons of these technologies are discussed Tony Yan 2:40 Opening Keynote: Importance of Chirality in Drugs Principal Scientist The importance of chirality in drugs and other pharmaceutical Pfizer Global R&D products cannot be understated. Modern synthetic methods now allow the use of asymmetric reactions with chiral catalysts or reagents Bob Depianta to obtain desired isomers. Powerful separations techniques have also Scientist been developed to achieve the same goal. These create new Pfizer Global R&D opportunities in drug discovery and development. This opening Jim Bradow keynote will cover: Scientist • Importance of chirality Pfizer Global R&D • Enantiomeric consideration and the revolutionary changes to drug development Laurence Philippe • Effects of chirality on intellectual property Associate Research Fellow Pfizer Global R&D Adeboye Adejare, PhD Professor & Chair, Department of Pharmaceutical Sciences, 4:30 Asymmetric Hydrogenation for Early Stage Drug Philadelphia College of Pharmacy Development University of the Sciences in Philadelphia New techniques for phase-transfer hydrogenation as well as inexpensive parallel pressure reactors have revolutionized reaction 3:40 Panel: Preparative Chromatography for Chiral screening to deliver maximum speed and efficiency. New Resolutions of Pharmaceutical Intermediates in hydrogenation technologies and approaches that provide the Drug Discovery and Development Stages potential for accelerated discovery of chiral route opportunities using Chromatographic technology has been widely used for the hydrogenation will be a focal point. enantiomer resolution in early stages of drug discovery and development. Supercritical fluid chromatography (SFC) is used Christopher A. Teleha predominately in drug discovery stage due to its rapid sample turn Research Fellow around and less organic solvent usage. Other technologies such as Johnson & Johnson simulated moving bed (SMB), steady state recycling (SSR), and batch HPLC are also used in the drug development stage. The selection and 5:15 Close of Day One 3 1-800-882- 8684 •
  4. 4. Main Conference Day Two Tuesday, May 19, 2009 8:00 Registration & Coffee 1:45 Practical Approaches to Chiral Chromatography by Supercritical Fluid 8:30 Chairperson’s Recap of Day One Chromatographic (SFC) Techniques Enantiopure drug compounds are essential for toxicity and 8:45 Marfey’s Reagent: Past, Present, & Future efficacy studies since chirality can influence or exhibit Uses for the Pre-column Derivatizing Reagent substantially different chemical and toxicological effects. Chiral for the Separation of Enantiomeric Isomers of chromatography is broadly used as a rapid tool to separate and Amino Acids & Amine Compounds isolate these pure enantiomers and SFC has emerged as the The present abstract describes characteristics and application preferred technique to support the various stages of drug of Marfey’s reagent (MR) including general synthesis of the development. The scope of this presentation highlights some reagent and diastereomers along with advantages, real-world uses of SFC for analysis and purification of chirally disadvantages and the required precautions. Applications, and active pharmaceutical compounds. comparison with other derivatizing agents, for the resolution Christine Aurigemma of complex mixtures of DL-amino acids, amines and non- Principal Scientist proteinogenic amino acids, peptides/amino acids. Pfizer Global R&D Deepak Gupta, PhD Senior Scientist 2:45 A Parallel Normal Phase Gradient Screen Cornerstone Pharmaceuticals Approach to Rapid Chiral Method Development 9:45 Building a Highly Automated 5 Pump (3 • The Normal Phase Parallel Gradient Screen Approach allows Gradient, 2 Isocratic), 4 Detector (2 UV, ELSD the user to simultaneously screen multiple chiral stationary & MS) Super-Critical Fluid Chromatography phases and solvent combinations in a shorter time (SFC) System For Chiral Purification In Drug • The parallel approach increases the speed of method Discovery development by at least a factor of five When building our gradient SFC/MS based chiral purification • The gradient approach further extends the success of the platform for drug discovery, Lundbeck Research designed method for a wide range of molecules to achieve a directly specifications based solely on the existing practices of the scaleable, rapid isocratic chiral separation method medicinal chemists and business need. Specifically, they Douglas Moore concluded that we must routinely inject ≥100 mg and yield 10 g Associate Research Scientist II per day of high purity (95-99% ee) for any number of compounds Bristol-Myers Squibb (1-100). These specifications tend to require gradient operation and significantly exceed those of the off the shelf instrumentation Michael Hicks, PhD more commonly used in this setting, particularly with regard to Senior Investigator I mass per injection for many compounds. Hear how they set out Bristol-Myers Squibb to find better ways to use the available instruments and ultimately meet their business need. 3:45 Networking Break Mark Hayward, PhD 4:15 Super-Critical Fluid Chromatography (SFC) Associate Director, Analytical Chemistry Department, Discovery with Tandem Mass Spectrometry (MS/MS) to Automation Department Evaluate the Disposition of Individual Stereo- Lundbeck Research Isomers of Drugs Frequently, candidate compounds in drug discovery and 10:45 Networking Break development programs are chiral. Separations for measurement of these compounds are typically done with 11:30 Chiral Supercritical Fluid Chromatography in normal phase LC (NP-LC) or supercritical fluid chromatography Drug Discovery: from Analytical to (SFC). Mass spectrometry (MS) can dramatically enhance Multigram-Scale sensitivity and specificity of detection which can be of high • Higher throughput with higher flow rate and shorter cycle value for samples coming from in vitro and in vivo studies. time However, only SFC (not NP-LC) can be easily interfaced with a • Less solvent consumption/disposal cost MS. Hear how Lundbeck Research • Less packaging time after preparative separations • Coupled analytical-scale SFC with both single-quadrupole • Solubility issues minimized (SFC/MS) and triple-quadrupole (SFC/MS/MS) mass • Higher efficiency than HPLC, ideal for challenging separations spectrometers while comparing the benefits of each Dauh-Rurng Wu • Used this combination to take advantage of the low viscosity Principal Scientist in SFC for fast chiral separations simultaneously with the Bristol-Myers Squibb high sensitivity and specificity of MS (or MS/MS) Mark Hayward, PhD 12:30 Networking Lunch Associate Director, Analytical Chemistry Department, Discovery Automation Department Lundbeck Research 5:15 Close of Conference 4 1-800-882- 8684 •
  5. 5. 5 EASY WAYS TO REGISTER: Chirality in 1 Web: 2 Call: 1-800-882-8684 or 1-646-378-6026 3 Email: Drug Compounds TM 4 Fax: 1-646-378-6025 5 Mail: IQPC 535 5th Avenue, 8th Floor, New York, NY 10017 REGISTRATION CARD About Our Sponsors Avantium Technologies’ core competency resides in solid state pharmaceutical chemistry and crystal engineering for small YES! Please register me for molecules. We provide fast-paced, high-throughput crystallization services to the pharmaceutical industry. We support your chemical and pharmaceutical development efforts from pre-clinical stages to Chirality in Drug Compounds NDA and help accelerate the APIs time-to-market. Key service elements: • Identification, characterization, selection of and recommendations for optimal ❑ Conference Only ❑ Conference + 2 Workshops polymorphs, salts and co-crystals + scale-ups • Amorphous API stabilization via solid dispersions ❑ Conference + 1 Workshop ❑ Workshop Only • Comprehensive form space identification: define & safeguard IP rights for Phase II and molecules • Comprehensive solubility screening programs Name ________________________________________________________ • Crystallization process development optimization, enantiomer separation via chiral resolution. Website: Job Title ______________________________________________________ Organization __________________________________________________ Approving Manager ____________________________________________ Pricing Address ______________________________________________________ QUALIFIED Register by Register by Standard END-USERS: March 13, 2009 April 24, 2009 Price City __________________________________________________________ Conference Only (save $400) (save $200) $999 $1,199 $1,399 State ________________________________________________________ All-Access Pass: (save $898) (save $698) (save $498) Main Conference $1,599 $1,799 $1,999 Zip __________________________________________________________ + 2 Workshops Workshop only $549 each $549 each $549 each Phone ________________________________________________________ OTHERS Register by Register by Standard Fax __________________________________________________________ March 13, 2009 April 24, 2009 Price Conference Only (save $600) (save $400) E-mail ________________________________________________________ $1,399 $1,599 $1,999 All-Access Pass: (save $1,098) (save $898) (save $498) ❑ Please keep me informed via email about this and other related events. 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For IQPC’s Cancellation, Postponement and Substitution Policy, please visit The Content Package allows you to not only listen to but also view the presentations from our events. Following the conference you will Venue: receive a CD-Rom that contains the conference presentations and audio Venue and accommodations are to be announced. Please check the web site at for updates and announcements. files that you can follow for your own personal training or for the Special Dietary Needs: If you have a dietary restriction, please contact Customer Service at 1- training of your team. 800-882-8684 to discuss your specific needs. ©2009 IQPC. All Rights Reserved. The format, design, content and arrangement of this For more information, visit or brochure constitute a trademark of IQPC. Unauthorized reproduction will be actionable call 1-800-882-8684. under the Lanham Act and common law principles. 5 1-800-882- 8684 •