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优秀学术报告示例[AriKoskinen]
Chemistry in Biomedicine; Ari Koskinen
Laboratory of Organic Chemistry;Numberapprovedby;New Drug Development;RD By Geographic Area; 2001;a;Market Exclusivity Times Decrease;Development pipeline;Top 10 Therapies;Top 10 Products;Mergers;Off Patent;Patents expiring;Promising New Drugs;Diversity of Drug Structures;B;H;High Throughput Screening;Drug Development Paradigms
Traditional Approach
Clinical/preclinical
Observations;Drug Development Paradigms
TARGET IDENTIFICATION
General;Chemical Diversity;?;1987;Solid Phase Organic Synthesis
Ph;Combinatorial Library: Split Synthesis Method;a;Spatially Addressable Parallel Synthesis;Spatially Addressable Chemical Libraries;Hydroxylamine Resin
O
HO N;Succinyl Amide Library
O
O;Peptidic and Peptidomimetic Libraries;Crude NMR
80;Analysis;IR on Bead;IR on Bead
FT-IR can monitor progress of reactions:;13C:;Mass spectrometry; Is it feasible to make all possible interesting
molecules combinatorially?
?Only C,H,N,O
?Avg mol wt of permeable drug
molecule ca 500; max 750
?Avogadro’s number 6.1023
?Only one molecule each 10200
molecules
?total mass: 10173 tonnes
?weight of Earth: 6.1021 tonnes!;?; Ari Koskinen
Laboratory of Organic Chemistry; Ari Koskinen
Laboratory of Organic Chemistry;More Sources;Target Oriented, Medicinal Combinatorial
and Diversity Oriented Synthesis;Generating Skeletal Diversity;Small Molecule Discovery; Ari Koskinen
Laboratory of Organic Chemistry;Complexity of Synthetic Targets;O;Trends in Synthetic Methodology;Ari Koskinen;Overlay of model X-ray;Calyculin analysis;Spiroketal Model Studies;Spiroketal Model Studies;Me3Al, THF/CH2Cl;C9-C19 Fragment;C9-C19 Fragment;Boron aldol TS’s;C9-C19 Fragment
C41
O31
C4;C9-C19 Fragment;Conclusions on I.A.I.;R.L.Strausberg and S.L.Schreiber Science, 2003, 300, 294.;β-Turns;β-Turn mimics;N;β-Turn mimics
O
N;Prolines in Turns;Synthesis of Tetrapeptides;-;γ;1;Vectorial Recognition and Cleavage of Proteins; Ari Koskinen
Laboratory of Organic Chemistry;Conc
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