Infectious Diseases -- Entecavir (Baraclude): A Carbocyclic Nucleoside for the Treatment of Chronic Hepatitis B -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Syntheses -- References -- Telaprevir (Incivek) and Boceprevir (Victrelis): NS3/4A Inhibitors for Treatment for Hepatitis C Virus (HCV) -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- PK and Drug Metabolism -- Efficacy and Safety -- Synthesis -- Conclusions -- References -- Daclatasvir (Daklinza): The First-in-Class HCV NS5A Replication Complex Inhibitor -- Background -- Discovery Medicinal Chemistry -- Mode of Action -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Syntheses -- References -- Sofosbuvir (Sovaldi): The First-in-Class HCV NS5B Nucleotide Polymerase Inhibitor -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Syntheses -- Summary -- References -- Bedaquiline (Sirturo): A Diarylquinoline that Blocks Tuberculosis ATP Synthase for the Treatment of Multi-Drug Resistant Tuberculosis -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Syntheses -- References -- Cancer -- Enzalutamide (Xtandi): An Androgen Receptor Antagonist for Late-Stage Prostate Cancer -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Synthesis -- Compounds in Development -- References -- Crizotinib (Xalkori): The First-in-Class ALK/ROS Inhibitor for Non-small Cell Lung Cancer -- Background: Non-small Cell Lung Cancer (NSCLC) Treatment -- Discovery Medicinal Chemistry Effort: SAR and Lead Optimization of Compound 2 as a c-Met Inhibitor -- ALK and ROS in Non-small Cell Lung Cancer (NSCLC) Treatment -- Preclinical Model Tumor Growth Inhibition Efficacy and Pharmacology -- Human Clinical Trials -- Introduction to the Synthesis and Limitations of the Discovery Route to Crizotinib Analogs -- Process Chemistry: Initial Improvements -- Process Chemistry: Enabling Route to Crizotinib -- Development of the Commercial Process -- Commercial Synthesis of Crizotinib -- References -- Ibrutinib (Imbruvica): The First-in-Class Btk Inhibitor for Mantle Cell Lymphoma, Chronic Lymphocytic Leukemia, and Waldenstrom's Macroglobulinemia -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Syntheses -- References -- Palbociclib (Ibrance): The First-in-Class CDK4/6 Inhibitor for Breast Cancer -- Background -- Pharmacology -- Discovery Program -- Preclinical Profile of Palbociclib -- Clinical Profile of Palbociclib -- Early Process Development for Palbociclib -- Commercial Process for Preparation of Palbociclib -- References -- Cardiovascular Diseases -- Ticagrelor (Brilinta) and Dabigatran Etexilate (Pradaxa): P₂Y₁₂ Platelet Inhibitors as Anti-coagulants -- Introduction -- Dabigatran Etexilate -- Ticagrelor -- The Future -- References -- CNS Drugs -- Suvorexant (BELSOMRA): The First-in-Class Orexin Antagonist for Insomnia -- Background -- Pharmacology -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Structure-Activity Relationship (SAR) -- Synthesis -- References -- Lorcaserin (Belviq): Serotonin 2C Receptor Agonist for the Treatment of Obesity -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Synthesis -- References -- Fingolimod (Gilenya): The First Oral Treatment for Multiple Sclerosis -- Background -- Structure-Activity Relationship (SAR) -- Pharmacology -- Human Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Syntheses -- Summary -- References -- Perampanel (Fycompa): AMPA Receptor Antagonist for the Treatment of Seizure -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Syntheses -- References -- Anti-Inflammatory Drugs -- Tofacitinib (Xeljanz): The First-in-Class JAK Inhibitor for the Treatment of Rheumatoid Arthritis -- Background -- Structure-Activity Relationships (SAR) -- Safety, Pharmacology and Pharmacokinetics -- Syntheses -- Development of the Commercial Manufacturing Process -- References -- Miscellaneous Drugs -- Ivacaftor (Kalydeco): A CFTR Potentiator for the Treatment of Cystic Fibrosis -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Syntheses -- References -- Febuxostat (Uloric): A Xanthine Oxidase Inhibitor for the Treatment of Gout -- Background -- Pharmacology -- Structure-Activity Relationship (SAR) -- Pharmacokinetics and Drug Metabolism -- Efficacy and Safety -- Syntheses -- Drug in Development: Lesinurad Sodium -- References