Modern Drug Synthesis / Edition 1

Modern Drug Synthesis / Edition 1

by Jie Jack Li
     
 

ISBN-10: 0470525835

ISBN-13: 9780470525838

Pub. Date: 08/09/2010

Publisher: Wiley

Following Contemporary Drug Synthesis and The Art of Drug Synthesis (Wiley, 2004 and 2007), two well-received works, is this new book that demystifies the process of modern drug discovery for practitioners and students. An enhanced introduction covers areas such as background, pharmacology, SAR, PK/PD, efficacy, and safety. Focusing on the advantages of process

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Overview

Following Contemporary Drug Synthesis and The Art of Drug Synthesis (Wiley, 2004 and 2007), two well-received works, is this new book that demystifies the process of modern drug discovery for practitioners and students. An enhanced introduction covers areas such as background, pharmacology, SAR, PK/PD, efficacy, and safety. Focusing on the advantages of process synthesis versus the discovery synthetic route, Modern Drug Synthesis features authoritative coverage by distinguished editors and authors (some chapter authors are the actual inventor of the drug) of twenty different drug molecules.

Product Details

ISBN-13:
9780470525838
Publisher:
Wiley
Publication date:
08/09/2010
Series:
Wiley Series on Drug Synthesis Series
Pages:
376
Product dimensions:
7.20(w) x 10.00(h) x 0.90(d)

Related Subjects

Table of Contents

Preface

Contributors

I Infectious Diseases 1

Chapter 1 Raltegravir (Isentress): The First-in-Class HIV-1 Integrase Inhibitor Julianne A. Hunt Hunt, Julianne A. 3

1.1 Background 3

1.2 Pharmacology 5

1.3 Structure-Activity Relationship (SAR) 6

1.4 Pharmacokinetics and Drug Metabolism 8

1.5 Efficacy and Safety 9

1.6 Syntheses 10

1.7 References 13

Chapter 2 Maraviroc (Selzentry): The First-in-Class CCR5 Antagonist for the Treatment of HIV David Price Price, David 17

2.1 Background 17

2.2 Structure-Activity Relationship (SAR) 19

2.3 Pharmacokinetics and Safety 21

2.4 Syntheses 22

2.5 References 27

Chapter 3 Darunavir (Prezista): A HIV-1 Protease Inhibitor for Treatment of Multidrug Resistant HIV Cuthbert D. Martyr Martyr, Cuthbert D. 29

3.1 Background 29

3.2 Pharmacology 32

3.3 Structure-Activity Relationship (SAR) 32

3.4 Pharmacokinetics and Drug Metabolism 33

3.5 Efficacy and Safety 33

3.6 Syntheses 34

3.7 References 42

II Cancer

Chapter 4 Decitabine (Dacogen): A DNA Methyltransferase Inhibitor for Cancer Jennifer A. Van Camp Van Camp, Jennifer A. 47

4.1 Background 47

4.2 Pharmacology 49

4.3 Structure-Activity Relationship (SAR) 49

4.4 Pharmacokinetics and Drug Metabolism 50

4.5 Efficacy and Safety 50

4.6 Syntheses 51

4.7 References 54

Chapter 5 Capecitabine (Xeloda): An Oral Chemotherapy Agent R. Jason Herr Herr, R. Jason 57

5.1 Background 57

5.2 Pharmacology 60

5.3 Structure-Activity Relationship (SAR) 62

5.4 Pharmacokinetics and Efficacy 63

5.5 Syntheses 64

5.6 References 70

Chapter 6 Sorafenib (Nexavar): A Multikinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable Hepatocellular Carcinoma Yazhong Huang Huang, Yazhong 73

6.1 Background 73

6.2 Pharmacology 75

6.3 Structure-Activity Relationship (SAR) 77

6.4 Pharmacokinetics and Drug Metabolism 78

6.5 Efficacy and Safety 78

6.6 Syntheses 79

6.7 References 84

Chapter 7 Sunitinib (Sutent): An Angiogenesis Inhibitor Martin Pettersson Pettersson, Martin 87

7.1 Background 87

7.2 Discovery and Development 89

7.3 Syntheses 91

7.3.1 Discovery Route 91

7.3.2 Process Route 92

7.4 References 97

Chapter 8 Bortezomib (Velcade): A First-in-Class Proteasome Inhibitor David S. Millan Millan, David S. 99

8.1 Background 99

8.2 Pharmacology 101

8.3 Structure-Activity Relationship (SAR) 102

8.4 Pharmacokinetics and Drug Metabolism 104

8.5 Efficacy and Safety 104

8.6 Syntheses 105

8.7 References 109

Chapter 9 Pazopanib (Votrient): A VEGFR Tyrosine Kinase Inhibitor for Cancer Jie Jack Li Jie, Jack Li 111

9.1 Background 111

9.2 Pharmacology 113

9.3 Structure-Activity Relationship (SAR) 114

9.4 Pharmacokinetics and Drug Metabolism 117

9.5 Efficacy and Safety 118

9.6 Syntheses 118

9.7 Other VEGFR Inhibitors in Development: Vandetanib and Cediranib 120

9.8 References 121

III Cardiovascular and Metabolic Diseases 123

Chapter 10 Sitagliptin (Januvia): A Treatment for Type 2 Diabetes Joseph D. Armstrong III Armstrong, Joseph D., III 125

10.1 Background 125

10.2 Pharmacology 126

10.3 Structure-Activity Relationship (SAR) 127

10.4 Pharmacokinetics and Drug Metabolism 128

10.5 Efficacy and Safety 129

10.6 Syntheses 130

10.7 References 138

Chapter 11 Aliskiren (Tekturna), The First-in-Class Renin Inhibitor for Hypertension Victor J. Cee Cee, Victor J. 141

11.1 Background 141

11.2 Pharmacology 144

11.3 Structure-Activity Relationship (SAR) 145

11.4 Pharmacokinetics and Drug Metabolism 146

11.5 Efficacy and Safety 147

11.6 Syntheses 148

11.7 References 156

Chapter 12 Vernakalant (Kynapid): An Investigational Drug for the Treatment of Atrial Fibrillation David L. Gray Gray, David L. 159

12.1 Background 159

12.2 Pharmacology 163

12.3 Structure-Activity Relationship (SAR) 163

12.4 Pharmacokinetics and Drug Metabolism 164

12.5 Efficacy and Safety 165

12.6 Syntheses 166

12.7 References 171

Chapter 13 Conivaptan (Vaprisol), Vasopressin Via and V2 Antagonist for Hyponatremia Brian A. Lanman Lanman, Brian A. 175

13.1 Background 175

13.2 Pharmacology 177

13.3 Structure-Activity Relationship (SAR) 179

13.4 Pharmacokinetics and Drug Metabolism 181

13.5 Efficacy and Safety 182

13.6 Syntheses 183

13.7 References 189

Chapter 14 Rivaroxaban (Xarelto): A Factor Xa Inhibitor for the Treatment of Thrombotic Events Jason Crawford Crawford, Jason 191

14.1 Background 191

14.2 Pharmacology 193

14.3 Structure-Activity Relationship (SAR) 194

14.4 Pharmacokinetics and Drug Metabolism 196

14.5 Efficacy and Safety 197

14.6 Syntheses 198

14.7 Compounds in Development: Apixaban and Otamixaban 203

14.8 References 204

Chapter 15 Endothelin Antagonists for the Treatment of Pulmonary Arterial Hypertension David J. Edmonds Edmonds, David J. 207

15.1 Background 208

15.2 Treatment of PAH 209

15.3 Endothelin Antagonists 211

15.4 Synthesis of Bosentan 215

15.5 Synthesis of Sitaxsentan 217

15.6 Synthesis of Ambrisentan 219

15.7 Conclusion 221

15.8 References 221

IV Central Nervous System Diseases 225

Chapter 16 Varenicline (Chantix), An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation Robert A. Singer Singer, Robert A. 227

16.1 Background 227

16.2 Discovery Chemistry Program 229

16.3 Pharmacology 231

16.4 Pharmacokinetics and Drug Metabolism 231

16.5 Efficacy and Safety 232

16.6 Syntheses 232

16.7 References 244

Chapter 17 Donepezil, Rivastigmine, and Galantamine: Cholinesterase Inhibitors for Alzheimer Disease Kapil Karki Karki, Kapil 249

17.1 Background 250

17.2 Pharmacology 251

17.3 Structure-Activity Relationship (SAR) 253

17.4 Pharmacokinetics and Drug Metabolism 256

17.5 Efficacy and Safety 258

17.6 Synthesis of Donepezil 259

17.7 Synthesis of Rivastigmine 262

17.8 Synthesis of Galantamine 265

17.9 References 271

Chapter 18 Aprepitant (Emend): A NKi Receptor Antagonist for the Treatment of Postchemotherapy Emesis John A. Lowe III Lowe, John A., III 275

18.1 Background 275

18.2 In Vitro Pharmacology and Structure-Activity Relationships 279

18.3 In Vivo Pharmacology 281

18.4 Pharmacokinetics and Drug Metabolism 282

18.5 Efficacy and Safety 282

18.6 Syntheses 283

18.7 References 289

Chapter 19 Armodafinil (Nuvigil): A Psychostimulant for the Treatment of Narcolepsy Jason Crawford Crawford, Jason 291

19.1 Background 291

19.2 Pharmacology 293

19.3 Pharmacokinetics and Drug Metabolism 294

19.4 Efficacy and Safety 295

19.5 Synthesis 296

19.6 References 303

V Miscellaneous 307

Chapter 20 Raloxifene (Evista): A Selective Estrogen Receptor Modulator (SERM) Marta Pineiro-Nunez Pineiro-Nunez, Marta 309

20.1 Background 309

20.2 Mechanism of Action 313

20.3 Pharmacokinetics and Drag Metabolism 313

20.4 Efficacy and Safety 314

20.5 Syntheses 315

20.6 References 325

Chapter 21 Latanoprost (Xalatan): A Prostanoid FP Agonist for Glaucoma Kevin E. Henegar Henegar, Kevin E. 329

21.1 Background 329

21.2 Syntheses 331

21.3 References 337

Index 339

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