The Institute for Scientific Exchange, Inc. Presents:

ISE Training Courses in Drug Development:

October 11-12, 2004

Boston, MA, USA

Symposium Venue:  Sheraton Commander Hotel Cambridge

 Travel information at bottom of page or click REGISTER NOW

 

 

Monday, October 11, 2004

 

Physical and Chemical Compound Properties in Drug Discovery 

 

Course Director:  Dr. Christopher A. Lipinski, Adjunct Senior Research Fellow, Pfizer Global R&D, Groton New London Labs

 

Christopher A. Lipinski, Ph.D.
Adjunct Senior Research Fellow
Pfizer Global R&D, Groton New London Labs (retired)
MS8200-36
Eastern Point Road
Groton, CT 06340
860 715-4656
lipinskica@groton.pfizer.com
American Chemical Society 2004 Medicinal Chemistry Award winner

http://myprofile.cos.com/lipinskica

 

Course Description:  A comprehensive one day course on the physical and chemical properties required for an orally active drug including an in depth discussion of the appropriate use of a variety of  filters (e.g. the rule of five) as well as the chemistry structural features likely to be found in a successful drug.  The course is designed for the discovery stage competent synthetic chemist who is a novice practitioner in medicinal chemistry and also as a refresher course for veterans of the field.  The lecture will end with an open discussion on the latest findings.  Students are encouraged to bring “real life” problems for discussion.

 

Length of Lecture:  1 day

 

Course syllabus:

 

8:00 AM – 9:00 AM – Registration

 

9:00 AM – 10:30 AM - Definition of chemistry physical and chemical compound properties.  Current status of compound properties; comparison to drugs:  Cost, time, and challenges.

 

10:30 AM – 10:45 AM – BREAK

 

10:45 AM – 11:00 AM – Quality chemical structures in drug discovery.

 

11:00 AM – 12:15 PM – Medicinal chemistry and the chemistry structure

·          Structural features to avoid

·          Solving problems using bioisosteres

·          Structural features to include

·          Privileged structures, molecular anchors, masterkeys

 

12:15 PM – 1:45 PM - LUNCH

 

1:45 PM – 2:30 PM - Solubility

·          Importance of aqueous and DMSO solubility

·          Computational and experimental approaches to solubility

·          Compound handling, storage and when to change the chemistry isolation procedure

 

2:30 PM – 3:15 PM – Permeability

·          GI and blood brain permeability - how it depends on the chemical structure

·          Computational and experimental approaches to permeability

·          How chemistry can improve permeability

 

3:15 PM – 3:30 PM – BREAK

 

3:30 PM – 4:15 PM – Chemistry structure and the discovery process

·          Chemistry and HTS screening errors

·          Lead-like versus drug-like

·          Hit to lead and lead optimization chemistry

 

4:15 PM – 5:00 PM – Summary of lecture and open discussion

 

END OF LECTURE

 

Tuesday, October 12, 2004

 

Course Director:  Dr. Albert P. Li, Founding Chairman, President  & CEO; Advanced Pharmaceutical Sciences, Inc. (Baltimore, MD)

 

Albert P. Li, Ph.D., MBA
Founding Chairman, President & CEO
Advanced Pharmaceutical Sciences, Inc.
PMB #146
6400 Baltimore National Pike
Baltimore, MD 21228
410-869-9037
lialbert@apsciences.com

www.apsciences.com

Biography

 

Course Description:  A comprehensive one and one-half day course on the theory and practice of in vitro evaluation of drug properties including absorption, metabolism, drug-drug interactions, and toxicity.  The course is designed for novice practitioners who intend to apply in vitro ADMET assays in drug development and also as a refresher course for veterans of the field.  The lecture will end with an open discussion on the latest findings.  Students are encouraged to bring “real life” problems for discussion.

 

Length of Lecture:  1 day

 

Course syllabus:

 

8:00 AM – 9:00 AM – Registration

 

9:00 AM – 10:30 AM - Definition of ADMET.  Current status of drug development:  Cost, time, and challenges.

 

10:30 AM – 10:45 AM – BREAK

 

10:45 AM – 11:00 AM - Role of in vitro ADMET systems in drug development.

 

11:00 AM – 12:15 PM - Evaluation of drug absorption

·          Mechanisms of drug absorption

·          Cell-based systems for drug absorption

·          Artificial membrane systems

 

12:15 PM – 1:45 PM - LUNCH

 

1:45 PM – 2:30 PM - Drug metabolism

·          Drug metabolizing enzymes

·          Metabolic stability evaluation

·          Metabolite identification

·          Species comparison

 

2:30 PM – 3:15 PM – Drug-drug interactions

·          Examples of drug-drug interactions

·          Enzyme inhibition

·          Enzyme induction

·          Transporter-based drug interactions

 

3:15 PM – 3:30 PM – BREAK

 

3:30 PM – 4:15 PM - Toxicity screening

·          Examples of toxic drugs and toxic mechanisms

·          Screening for acute drug toxicity including general cytotoxicity, hepatotoxicity, neurotoxicity, and cardiotoxicity

·          Genotoxicity evaluation

·          Toxicogenomics

 

 

4:15 PM – 5:00 PM – Summary of lecture and open discussion

 

 

END OF CONFERENCE

About the Institute for Scientific Exchange

 

The mission of The Institute for Scientific Exchange, Inc. is to advance science via communication – (i. e. symposia, training courses, publications).  The events held by the Institute are highly selective, timely, and of the highest professional caliber.  One major goal of the Institute, as exemplified by this symposium, is to foster communication among industrial, regulatory, and academic practitioners. Please visit our web site at www.isciencex.com.

 

Travel Information Boston:

Built in 1927, the Sheraton Commander Hotel, Harvard Square's premiere hotel, possesses unparalleled style and grace. Situated on historic Cambridge Common, near the site where George Washington took command of the Continental Army, our Mount Vernon inspired entrance stands as a stately reminder and starting point for Cambridge's rich culture and history. Located on the North side of the Charles River, which separates us from Boston, we are surrounded by Harvard University and just minutes from Lesley, Tufts, and MIT, as well as a wealth of shopping and fine dining.

 

Hotel Information

The Sheraton Commander Hotel Cambridge is located at 16 Garden Street, Cambridge, MA, USA.  PLease contact the hotel at 617-547-4800, fax 617-234-1302 or online at www.sheraton.com/commander .

 

Both:      US $1500.00________ (SPECIAL DISCOUNT)

Lipinski  US $950.00________

Li             US $950.00________

 

 

Payment

Payment may be made by check or credit card.  Checks should be made in US $, payable to Institute for Scientific Exchange, Inc.  Mail to: ISE, Inc., 5707 Calverton Street, Suite 2C, Baltimore, MD 21228, USA

 

Cancellation Policy

All cancellations are subjected to a $250.00 cancellation fee. Longer than 30 days, 100% refund (less cancellation fee). Less than 30 days, no refund but registration may be transferred to another person.  All refund requests must be in writing.  All refunds will be issued after the meeting has occurred. No refunds requests will be accepted after January 23, 2004. Please submit cancellation and refund requests including transferring of registration to:

 

Fax:  410-869-9560

E-mail: nola@isciencex.com

Deadline: September 11, 2004

 

Email to nola@isciencex.com or mail/fax completed form with remittance to: ISE, Inc. 5707 Calverton Street, Suite 2C, Baltimore, MD 21228, USA; FAX No:  (410) 869-9560.  Payment may be made by check in US$, payable to Institute for Scientific Exchange, Inc. or by credit card.

 

Payment Method:  ____Check _____Credit Card (American Express, Master Card, VISA)