Medicinal Chemistry Reviews

Volume 52, Chapter 1

Discovery of TAK-063, a PDE10A Inhibitor with Balanced Activation of Direct and Indirect Pathways

1.          Introduction                                                                                                               3

2.         Strategy for Drug Screening                                                                                     5

3.         Hit Identification and Strategy for Chemistry                                                        6

4.         Candidate Identification                                                                                          7

5.         Characterization of Compounds 6e and 7b                                                           15

            5.1        PDE10A Selectivity and PK Profile of 6e and 7b                                        15

            5.2       In Vivo Pharmacological Profile of 6e and 7b                                            15

            5.3       Safety Profile of 7b                                                                                       18

6.         Conclusions                                                                                                               19

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