Preface | |
Contributors | |
Infectious Diseases | |
Raltegravir (Isentress), The First-in-class HIV-1 Integrase Inhibitor | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Maraviroc (Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV | |
Background | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Safety | |
Syntheses | |
References | |
Darunavir (Prezista), A HIV-1 Protease Inhibitor for Treatment of Multidrug Resistant HIV | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Cancer | |
Decitabine (Dacogen), A DNA Methyltransferase Inhibitor for Cancer | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Capecitabine (Xeloda), An Oral Chemotherapy Agent | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Efficacy | |
Syntheses | |
References | |
Sorafenib (Nexavar), A Multi-kinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable Hepatocellular Carcinoma | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Sunitinib (Sutent), An Angiogenesis Inhibitor | |
Background | |
Discovery and Development | |
Syntheses | |
Discovery Route | |
Process Route | |
References | |
Bortezomib (Velcade), A First-in-class Proteasome Inhibitor | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Pazopanib (Votrient), A VEGFR Tyrosine Kinase Inhibitor for Cancer | |
Background | |
Pharmacology | |
Structure?Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
Other VEGFR Inhibitors in Development: Vandetanib and Cediranib | |
References | |
Cardiovascular and Metabolic Diseases | |
Sitagliptin (Januvia), A Treatment for Type 2 Diabetes | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Aliskiren (Tekturna), The First-in-class Renin Inhibitor for Hypertension | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Vernakalant (Kynapid), An Investigational Drug for the Treatment of Atrial Fibrillation | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Conivaptan (Vaprisol), Vasopressin V1a and V2 Antagonist for Hyponatremia | |
Background | |
Pharmacology | |
Structure-Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Rivaroxaban (Xarelto), A Factor Xa Inhibitor for the Treatment of Thrombotic Events | |
Background | |
Pharmacology | |
Structure?Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
Compounds in Development: Apixaban and Otamixaban | |
References | |
Endothelin Antagonists for the Treatment of Pulmonary Arterial Hypertension | |
Background | |
Treatment of PAH | |
Endothelin Antagonists | |
Synthesis of Bosentan | |
Synthesis of Sitaxsentan | |
Synthesis of Ambrisentan | |
Conclusion | |
References | |
Central Nervous System Diseases | |
Varenicline (Chantix), An ¿4ß2 Nicotinic Receptor Partial Agonist for Smoking Cessation | |
Background | |
Discovery Chemistry Program | |
Pharmacology | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Donepezil, Rivastigmine, Galantamine: Cholinesterase Inhibitors for Alzheimer's Disease | |
Background | |
Pharmacology | |
Structure?Activity Relationship (SAR) | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Synthesis of Donepezil | |
Synthesis of Rivastigmine | |
Synthesis of Galantamine | |
References | |
Aprepitant (Emend), A NK1 Receptor Antagonist for the Treatment of Post-chemotherapy Emesis | |
Background | |
In Vitro Pharmacology and Structure-Activity Relationships | |
In Vivo Pharmacology | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Armodafinil (Nuvigil), A Psychostimulant for the Treatment of Narcolepsy | |
Background | |
Pharmacology | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Synthesis | |
References | |
Miscellaneous | |
Raloxifene (Evista), A Selective Estrogen Receptor Modulator (SERM) | |
Background | |
Mechanism of Action | |
Pharmacokinetics and Drug Metabolism | |
Efficacy and Safety | |
Syntheses | |
References | |
Latanoprost (Xalatan), A Prostanoid FP Agonist for Glaucoma | |
Background | |
Syntheses | |
References | |
Index | |
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