1.医薬品開発forWeb.ppt
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2 1 4/15 4/22 CC/TBDD(CADD) 5/ / /15
3 BO:
4 BO: Drug Discovery based on Genome (Information) Combinatorial Chemistry Random screening Lead Optimization target validation
5 Target Validation target : validation: validation
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15 AD.50 AD
16 19 ( O O O O
17 O C 3 O O O O O O O C 3 C 3 COO O O R O O 2
18 20 QOL O C 2 O O O O O C 2 O O COO O O COO
19 2 ( 2 ( Me Me ( but Me Me C ( )
20 (BDD) CC T O O O O O O O O C 2 O C 2 O O COO O 2 Me Me C
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22 ( ( )
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26 CF3 Me Itazigrel Timegadine (seed: (Lead: ) 2 Lead optimization
27 A. Tanaka et al., J. Med. Chem., 37, (1994) itazigrel CF 3 2 R 1 R 2 R 3 timegadine Me R 1 R 2 R 3 IC50, µm IC50, µm Me Me Me Et ipr Me c-hex Me -Me-piperadine morpholine imidazoline aspirin itazigrel timegadine >0.1 > > >1.0 <1.0 > not tested > not tested >600 >
28 ( R 1 R 2 R 3 R 1 =Me R 2 =Me R 3 = ( O O O Cl 2 4,4'-Dimethoxybenzoin (Aldrich, 4,200/25g) Me Me Me Me Me
29 A. Tanaka et al., J. Med. Chem., 37, (1994) itazigrel CF 3 2 R 1 R 2 R 3 timegadine Me R 1 R 2 R 3 IC50, µm IC50, µm Me Me Me Et ipr Me c-hex Me -Me-piperadine morpholine imidazoline aspirin itazigrel timegadine >0.1 > > >1.0 <1.0 > not tested > not tested >600 >
30 2 R 1 R 2 R 1 R 2 IC50, µm IC50, µm Me COMe CO- 3 -py COC 2 -Ph COC 2 Me Me > <0.1 < O C o CO-morpholine COMe CO-iPr A. Tanaka et al., J. Med. Chem., 37, (1994)
31 O R 1 R 2 R R 4-Me-piperadine (FR122047) 2 Me 2 Et 2 C() 2 morpholine piperadine 4-ethanolpiperadine 4-Me-homopiperadine 4-(2-hydroxyethyl)piperadine 2 C 2 -morpholine C 2 C 2-3-Py -piperadino-co-ipr IC50, µm IC50, µm >1 <0.1 <0.01 >0.1 <0.01 > >0.1 >1 >1 <0.1 >1 6.2 not tested >100 > A. Tanaka et al., J. Med. Chem., 37, (1994)
32 CF3 Me Itazigrel Timegadine (seed: O Me (Lead: ) 2
33 ( ( )
34 ( ( ) eed Lead
35 1) / T 2) BDD (tructure based Drug Design) 3) (
36 / T combinatorial= A1 A2 A3 B4 B5 B6 C14 C15 C16 C24 C25 C26 C34 C35 C36 A1 B4 C14 + A B 1 1
37 / T T (igh Throughput creening) throughput= T(igh Throughput creening)
38 BDD (tructure-based Drug Design) (1 2 O O O COO COO FK633(
39 BDD (tructure-based Drug Design) AuroraA:
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