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Theme: Drug Discovery

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9 matching courses


Chemistry: DD1 The Drug Discovery Process Wed 15 Jan 2020   14:00 [Places]

Drug discovery is a complex multidisciplinary process with chemistry as the core discipline. A small molecule New Chemical Entity (NCE) (80% of drugs marketed) has had its genesis in the mind of a chemist. A successful drug is not only biologically active (the easy bit), but is also therapeutically effective in the clinic – it has the correct pharmacokinetics, lack of toxicity, is stable and can be synthesised in bulk, selective and can be patented. Increasingly, it must act at a genetically defined sub-population of patients. Medicinal chemists therefore work at the centre of a web of disciplines – biology, pharmacology, molecular biology, toxicology, materials science, intellectual property and medicine. This fascinating interplay of disciplines is the intellectual space within which a chemist has to make the key compound that will become an effective medicine. It happens rarely, despite enormous investment in time, money and effort. What factors make a program successful? I would like to briefly outline the process, but importantly to offer some key with examples of success

Chemistry: DD2 The Drug Discovery Process Fri 17 Jan 2020   14:00 [Places]

Drug discovery is a complex multidisciplinary process with chemistry as the core discipline. A small molecule New Chemical Entity (NCE) (80% of drugs marketed) has had its genesis in the mind of a chemist. A successful drug is not only biologically active (the easy bit), but is also therapeutically effective in the clinic – it has the correct pharmacokinetics, lack of toxicity, is stable and can be synthesised in bulk, selective and can be patented. Increasingly, it must act at a genetically defined sub-population of patients. Medicinal chemists therefore work at the centre of a web of disciplines – biology, pharmacology, molecular biology, toxicology, materials science, intellectual property and medicine. This fascinating interplay of disciplines is the intellectual space within which a chemist has to make the key compound that will become an effective medicine. It happens rarely, despite enormous investment in time, money and effort. What factors make a program successful? I would like to briefly outline the process, but importantly to offer some key with examples of success

Chemistry: DD3 Modern Tactics to Optimise Potency Fri 24 Jan 2020   14:00 [Places]

When you have 1000s of possible compounds you could make from any one start point what do you make first? This lecture will cover some general basic principles on designing more potent molecules, as well as some practical tips on how to run an optimization program and how to focus synthetic efforts. Binding modalities (reversible, covalent) will be briefly covered, as well as some newer non-traditional modalities. This lecture will also serve as an introduction to the medicinal chemistry game.

Chemistry: DD5 Medicinal Chemistry Game Workshop Fri 31 Jan 2020   14:00 [Places]

A real drug discovery example will be used. After a brief introduction to the task and the chemical startpoint, we will split into teams and iteratively try to design improved analogues. Molecules will be marked “in real time” during the session to recreate the design-make-test-analysis cycle, then teams can compare their optimized molecules, and we can compare them to what happened in real life.

Chemistry: DD4 Pharmacokinetics Wed 29 Jan 2020   14:00 [Places]

Predicting and controlling how a chemical molecule will be processed by the body is vital to developing a successful drug. This lecture will discuss the path a molecule takes from initial dose through to elimination, describe the ADME (Absorption, Distribution, Metabolism and Excretion) processes that take place and how these are related to compound structure and physicochemical properties. In addition to standard small molecule PK some other new modalities will be also be introduced to illustrate how methods such as PEGylation and lipoparticle encapsulation can be employed to modulate compound pharmacokinetic properties.

Chemistry: DD6 Toxicity and Drug Safety Wed 5 Feb 2020   14:00 [Places]

Drug safety remains the primary cause of compound attrition when developing new medicines and consequently the ability to understand and predict toxicity is regarded as high priority within the pharmaceutical sector. This lecture will describe some common safety liabilities and ongoing work to build a greater understanding of the relationships between chemical structure and toxicity risk that are being harnessed to guide the design of safer compounds

Chemistry: DD7 Kinase Inhibitor Case Studies Fri 7 Feb 2020   14:00 [Places]

Kinase drug discovery remains to be an area of significant and growing interest across academia and in the pharmaceutical industry - there are approximately 30 FDA approved small molecule inhibitors which target kinases, half of which were approved in the last 3 years. This lecture will give an insight into the medicinal chemistry story behind one clinical candidate and 2 marketed drugs. Crystal structures will be used to explain general principles behind designing for kinase inhibition, and some more advanced topics will be covered such as prodrugs, covalent inhibition and consideration of mutation status in drug discovery

Chemistry: DD9 Process Chemistry Fri 14 Feb 2020   13:00 [Places]

Two complementary lecture from industry experts on process chemistry from GSK and Syngenta will share their experiences and challenges gathered over many years of experience.

Chemistry: DD10 Process Chemistry Workshop new Tue 3 Mar 2020   10:00 [Places]

TBC

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