Table of Contents
Section Summary
1 Executive Summary
2 Introduction
- Lead Optimization as an Integral Part of Drug Discovery
3 Background and Strategy
- What is an "Optimized Lead Molecule?"
- Why Preclinical Candidates are Discontinued: Starting Points for Lead Optimization
- Economy: The Impact of Compound Attrition at Various Stages
- Tuning Lead Discovery towards Later Lead Optimization
- Outsourcing Medicinal Chemistry: Lead Optimization By Third Parties
4 The Technology of Lead Optimization - In Vitro and In Silico
- Technology of Lead Optimization - A Paradigm Change
- The Parallel Synthesis Approach
- Measuring, Modifying and Predicting Physico-Chemical Properties
- Molecular Modeling and Docking: Modifying a Pharmacophore In Silico
- Experimental Determination of Interaction Mode and QSARs in Solution
- Predictive ADMET: The Greatest Challenge
- Pharma Informatics: Bringing It All Together
5 Patenting and Regulatory Affairs: More Than Just Paperwork
- Lead Optimization and Intellectual Property
- Regulatory Issues In Lead Optimization
6 Case Studies In Lead Optimization
- Anti-Tumor and Neuroprotective Kinase Inhibitors Derived From K-252
- Second-Generation Galantamine Congeners
- HIV Protease Inhibitors
- The Bisphosphonates - A Story of Evolution in Osteoporosis Drugs
7 Profiles of Selected Companies In The Lead Optimization Business
8 Summary and Outlook
9 Companies Mentioned In This Report |
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