Modern Drug Synthesis
Eds.: Li, Jie J.; Johnson, Douglas S.
Modern Drug Synthesis
Eds.: Li, Jie J.; Johnson, Douglas S.
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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.
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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.
Produktdetails
- Produktdetails
- Wiley Series on Drug Synthesis
- Verlag: Wiley & Sons
- Artikelnr. des Verlages: 14552583000
- 1. Auflage
- Seitenzahl: 376
- Erscheinungstermin: 9. August 2010
- Englisch
- Abmessung: 260mm x 183mm x 24mm
- Gewicht: 790g
- ISBN-13: 9780470525838
- ISBN-10: 0470525835
- Artikelnr.: 30589358
- Wiley Series on Drug Synthesis
- Verlag: Wiley & Sons
- Artikelnr. des Verlages: 14552583000
- 1. Auflage
- Seitenzahl: 376
- Erscheinungstermin: 9. August 2010
- Englisch
- Abmessung: 260mm x 183mm x 24mm
- Gewicht: 790g
- ISBN-13: 9780470525838
- ISBN-10: 0470525835
- Artikelnr.: 30589358
JIE JACK LI is a chemist at Bristol-Myers Squibb Company in Wallingford, Connecticut. He is the coauthor of various books, including Palladium in Heterocyclic Chemistry, Name Reactions: A Collection of Detailed Reaction Mechanisms and Synthetic Applications, Name Reactions in Heterocyclic Chemistry, Contemporary Drug Synthesis, The Art of Drug Synthesis, Name Reactions for Functional Group Transformations, Name Reactions for Homologations, Parts 1 and 2, and Name Reactions for Carbocyclic Ring Formations. DOUGLAS JOHNSON is a medicinal chemist and project leader at Pfizer in Groton, Connecticut. He is a coauthor on more than forty publications and patents, including the books The Art of Drug Synthesis and Contemporary Drug Synthesis.
Preface. Contributors. I. Infectious Diseases. Chapter 1. Raltegravir
(Isentress), The First-in-class HIV-1 Integrase Inhibitor (Julianne A.
Hunt). 1.1 Background. 1.2 Pharmacology. 1.3 Structure-Activity
Relationship (SAR). 1.4 Pharmacokinetics and Drug Metabolism. 1.5 Efficacy
and Safety. 1.6 Syntheses. 1.7 References. Chapter 2. Maraviroc
(Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV
(David Price). 2.1 Background. 2.2 Structure-Activity Relationship (SAR).
2.3 Pharmacokinetics and Safety. 2.4 Syntheses. 2.5 References. Chapter 3.
Darunavir (Prezista), A HIV-1 Protease Inhibitor for Treatment of Multidrug
Resistant HIV (Arun K. Ghosh and Cuthbert D. Martyr). 3.1 Background. 3.2
Pharmacology. 3.3 Structure-Activity Relationship (SAR). 3.4
Pharmacokinetics and Drug Metabolism. 3.5 Efficacy and Safety. 3.6
Syntheses. 3.7 References. II. Cancer. Chapter 4. Decitabine (Dacogen), A
DNA Methyltransferase Inhibitor for Cancer (Jennifer A. Van Camp). 4.1
Background. 4.2 Pharmacology. 4.3 Structure-Activity Relationship (SAR).
4.4 Pharmacokinetics and Drug Metabolism. 4.5 Efficacy and Safety. 4.6
Syntheses. 4.7 References. Chapter 5. Capecitabine (Xeloda), An Oral
Chemotherapy Agent (R. Jason Herr). 5.1 Background. 5.2 Pharmacology. 5.3
Structure-Activity Relationship (SAR). 5.4 Pharmacokinetics and Efficacy.
5.5 Syntheses. 5.6 References. Chapter 6. Sorafenib (Nexavar), A
Multi-kinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable
Hepatocellular Carcinoma (Shuanghua Hu). 6.1 Background. 6.2 Pharmacology.
6.3 Structure-Activity Relationship (SAR). 6.4 Pharmacokinetics and Drug
Metabolism. 6.5 Efficacy and Safety. 6.6 Syntheses. 6.7 References. Chapter
7. Sunitinib (Sutent), An Angiogenesis Inhibitor (Martin Pettersson). 7.1
Background. 7.2 Discovery and Development. 7.3 Syntheses. 7.3.1 Discovery
Route. 7.3.2 Process Route. 7.4 References. Chapter 8. Bortezomib
(Velcade), A First-in-class Proteasome Inhibitor (Benjamin S. Greener and
David S. Millan). 8.1 Background. 8.2 Pharmacology. 8.3 Structure-Activity
Relationship (SAR). 8.4 Pharmacokinetics and Drug Metabolism. 8.5 Efficacy
and Safety. 8.6 Syntheses. 8.7 References. Chapter 9. Pazopanib (Votrient),
A VEGFR Tyrosine Kinase Inhibitor for Cancer (Ji Zhang and Jie Jack Li).
9.1 Background. 9.2 Pharmacology. 9.3 Structure-Activity Relationship
(SAR). 9.4 Pharmacokinetics and Drug Metabolism. 9.5 Efficacy and Safety.
9.6 Syntheses. 9.7 Other VEGFR Inhibitors in Development: Vandetanib and
Cediranib. 9.8 References. III. Cardiovascular and Metabolic Diseases.
Chapter 10. Sitagliptin (Januvia), A Treatment for Type 2 Diabetes (Scott
D. Edmondson, Feng Xu, and Joseph D. Armstrong III). 10.1 Background. 10.2
Pharmacology. 10.3 Structure-Activity Relationship (SAR). 10.4
Pharmacokinetics and Drug Metabolism. 10.5 Efficacy and Safety. 10.6
Syntheses. 10.7 References. Chapter 11. Aliskiren (Tekturna), The
First-in-class Renin Inhibitor for Hypertension (Victor J. Cee). 11.1
Background. 11.2 Pharmacology. 11.3 Structure-Activity Relationship (SAR).
11.4 Pharmacokinetics and Drug Metabolism. 11.5 Efficacy and Safety. 11.6
Syntheses. 11.7 References. Chapter 12. Vernakalant (Kynapid), An
Investigational Drug for the Treatment of Atrial Fibrillation (David L.
Gray). 12.1 Background. 12.2 Pharmacology. 12.3 Structure-Activity
Relationship (SAR). 12.4 Pharmacokinetics and Drug Metabolism. 12.5
Efficacy and Safety. 12.6 Syntheses. 12.7 References. Chapter 13.
Conivaptan (Vaprisol), Vasopressin V1a and V2 Antagonist for Hyponatremia
(Brian A. Lanman). 13.1 Background. 13.2 Pharmacology. 13.3
Structure-Activity Relationship (SAR). 13.4 Pharmacokinetics and Drug
Metabolism. 13.5 Efficacy and Safety. 13.6 Syntheses. 13.7 References.
Chapter 14. Rivaroxaban (Xarelto), A Factor Xa Inhibitor for the Treatment
of Thrombotic Events (Ji Zhang and Jason Crawford). 14.1 Background. 14.2
Pharmacology. 14.3 Structure-Activity Relationship (SAR). 14.4
Pharmacokinetics and Drug Metabolism. 14.5 Efficacy and Safety. 14.6
Syntheses. 14.7 Compounds in Development: Apixaban and Otamixaban. 14.8
References. Chapter 15. Endothelin Antagonists for the Treatment of
Pulmonary Arterial Hypertension (David Edmonds). 15.1 Background. 15.2
Treatment of PAH. 15.3 Endothelin Antagonists. 15.4 Synthesis of Bosentan.
15.5 Synthesis of Sitaxsentan. 15.6 Synthesis of Ambrisentan. 15.7
Conclusion. 15.8 References. IV. Central Nervous System Diseases. Chapter
16. Varenicline (Chantix), An alpha4ß2 Nicotinic Receptor Partial Agonist
for Smoking Cessation (Jotham W. Coe, Frank R. Busch and Robert A. Singer).
16.1 Background. 16.2 Discovery Chemistry Program. 16.3 Pharmacology. 16.4
Pharmacokinetics and Drug Metabolism. 16.5 Efficacy and Safety. 16.6
Syntheses. 16.7 References. Chapter 17. Donepezil, Rivastigmine,
Galantamine: Cholinesterase Inhibitors for Alzheimer's Disease (Subas Sakya
and Kapil Karki). 17.1 Background. 17.2 Pharmacology. 17.3
Structure-Activity Relationship (SAR). 17.4 Pharmacokinetics and Drug
Metabolism. 17.5 Efficacy and Safety. 17.6 Synthesis of Donepezil. 17.7
Synthesis of Rivastigmine. 17.8 Synthesis of Galantamine. 17.9 References.
Chapter 18. Aprepitant (Emend), A NK1 Receptor Antagonist for the Treatment
of Post-chemotherapy Emesis (John A. Lowe, III). 18.1 Background. 18.2 In
Vitro Pharmacology and Structure-Activity Relationships. 18.3 In Vivo
Pharmacology. 18.4 Pharmacokinetics and Drug Metabolism. 18.5 Efficacy and
Safety. 18.6 Syntheses. 18.7 References. Chapter 19. Armodafinil (Nuvigil),
A Psychostimulant for the Treatment of Narcolepsy (Ji Zhang and Jason
Crawford). 19.1 Background. 19.2 Pharmacology. 19.3 Pharmacokinetics and
Drug Metabolism. 19.4 Efficacy and Safety. 19.5 Synthesis. 19.6 References.
V. Miscellaneous. Chapter 20. Raloxifene (Evista), A Selective Estrogen
Receptor Modulator (SERM) (Marta Piñeiro-Núñez). 20.1 Background. 20.2
Mechanism of Action. 20.3 Pharmacokinetics and Drug Metabolism. 20.4
Efficacy and Safety. 20.5 Syntheses. 20.6 References. Chapter 21.
Latanoprost (Xalatan), A Prostanoid FP Agonist for Glaucoma (Sajiv K. Nair
and Kevin E. Henegar). 21.1 Background. 21.2 Syntheses. 21.3 References.
Index.
(Isentress), The First-in-class HIV-1 Integrase Inhibitor (Julianne A.
Hunt). 1.1 Background. 1.2 Pharmacology. 1.3 Structure-Activity
Relationship (SAR). 1.4 Pharmacokinetics and Drug Metabolism. 1.5 Efficacy
and Safety. 1.6 Syntheses. 1.7 References. Chapter 2. Maraviroc
(Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV
(David Price). 2.1 Background. 2.2 Structure-Activity Relationship (SAR).
2.3 Pharmacokinetics and Safety. 2.4 Syntheses. 2.5 References. Chapter 3.
Darunavir (Prezista), A HIV-1 Protease Inhibitor for Treatment of Multidrug
Resistant HIV (Arun K. Ghosh and Cuthbert D. Martyr). 3.1 Background. 3.2
Pharmacology. 3.3 Structure-Activity Relationship (SAR). 3.4
Pharmacokinetics and Drug Metabolism. 3.5 Efficacy and Safety. 3.6
Syntheses. 3.7 References. II. Cancer. Chapter 4. Decitabine (Dacogen), A
DNA Methyltransferase Inhibitor for Cancer (Jennifer A. Van Camp). 4.1
Background. 4.2 Pharmacology. 4.3 Structure-Activity Relationship (SAR).
4.4 Pharmacokinetics and Drug Metabolism. 4.5 Efficacy and Safety. 4.6
Syntheses. 4.7 References. Chapter 5. Capecitabine (Xeloda), An Oral
Chemotherapy Agent (R. Jason Herr). 5.1 Background. 5.2 Pharmacology. 5.3
Structure-Activity Relationship (SAR). 5.4 Pharmacokinetics and Efficacy.
5.5 Syntheses. 5.6 References. Chapter 6. Sorafenib (Nexavar), A
Multi-kinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable
Hepatocellular Carcinoma (Shuanghua Hu). 6.1 Background. 6.2 Pharmacology.
6.3 Structure-Activity Relationship (SAR). 6.4 Pharmacokinetics and Drug
Metabolism. 6.5 Efficacy and Safety. 6.6 Syntheses. 6.7 References. Chapter
7. Sunitinib (Sutent), An Angiogenesis Inhibitor (Martin Pettersson). 7.1
Background. 7.2 Discovery and Development. 7.3 Syntheses. 7.3.1 Discovery
Route. 7.3.2 Process Route. 7.4 References. Chapter 8. Bortezomib
(Velcade), A First-in-class Proteasome Inhibitor (Benjamin S. Greener and
David S. Millan). 8.1 Background. 8.2 Pharmacology. 8.3 Structure-Activity
Relationship (SAR). 8.4 Pharmacokinetics and Drug Metabolism. 8.5 Efficacy
and Safety. 8.6 Syntheses. 8.7 References. Chapter 9. Pazopanib (Votrient),
A VEGFR Tyrosine Kinase Inhibitor for Cancer (Ji Zhang and Jie Jack Li).
9.1 Background. 9.2 Pharmacology. 9.3 Structure-Activity Relationship
(SAR). 9.4 Pharmacokinetics and Drug Metabolism. 9.5 Efficacy and Safety.
9.6 Syntheses. 9.7 Other VEGFR Inhibitors in Development: Vandetanib and
Cediranib. 9.8 References. III. Cardiovascular and Metabolic Diseases.
Chapter 10. Sitagliptin (Januvia), A Treatment for Type 2 Diabetes (Scott
D. Edmondson, Feng Xu, and Joseph D. Armstrong III). 10.1 Background. 10.2
Pharmacology. 10.3 Structure-Activity Relationship (SAR). 10.4
Pharmacokinetics and Drug Metabolism. 10.5 Efficacy and Safety. 10.6
Syntheses. 10.7 References. Chapter 11. Aliskiren (Tekturna), The
First-in-class Renin Inhibitor for Hypertension (Victor J. Cee). 11.1
Background. 11.2 Pharmacology. 11.3 Structure-Activity Relationship (SAR).
11.4 Pharmacokinetics and Drug Metabolism. 11.5 Efficacy and Safety. 11.6
Syntheses. 11.7 References. Chapter 12. Vernakalant (Kynapid), An
Investigational Drug for the Treatment of Atrial Fibrillation (David L.
Gray). 12.1 Background. 12.2 Pharmacology. 12.3 Structure-Activity
Relationship (SAR). 12.4 Pharmacokinetics and Drug Metabolism. 12.5
Efficacy and Safety. 12.6 Syntheses. 12.7 References. Chapter 13.
Conivaptan (Vaprisol), Vasopressin V1a and V2 Antagonist for Hyponatremia
(Brian A. Lanman). 13.1 Background. 13.2 Pharmacology. 13.3
Structure-Activity Relationship (SAR). 13.4 Pharmacokinetics and Drug
Metabolism. 13.5 Efficacy and Safety. 13.6 Syntheses. 13.7 References.
Chapter 14. Rivaroxaban (Xarelto), A Factor Xa Inhibitor for the Treatment
of Thrombotic Events (Ji Zhang and Jason Crawford). 14.1 Background. 14.2
Pharmacology. 14.3 Structure-Activity Relationship (SAR). 14.4
Pharmacokinetics and Drug Metabolism. 14.5 Efficacy and Safety. 14.6
Syntheses. 14.7 Compounds in Development: Apixaban and Otamixaban. 14.8
References. Chapter 15. Endothelin Antagonists for the Treatment of
Pulmonary Arterial Hypertension (David Edmonds). 15.1 Background. 15.2
Treatment of PAH. 15.3 Endothelin Antagonists. 15.4 Synthesis of Bosentan.
15.5 Synthesis of Sitaxsentan. 15.6 Synthesis of Ambrisentan. 15.7
Conclusion. 15.8 References. IV. Central Nervous System Diseases. Chapter
16. Varenicline (Chantix), An alpha4ß2 Nicotinic Receptor Partial Agonist
for Smoking Cessation (Jotham W. Coe, Frank R. Busch and Robert A. Singer).
16.1 Background. 16.2 Discovery Chemistry Program. 16.3 Pharmacology. 16.4
Pharmacokinetics and Drug Metabolism. 16.5 Efficacy and Safety. 16.6
Syntheses. 16.7 References. Chapter 17. Donepezil, Rivastigmine,
Galantamine: Cholinesterase Inhibitors for Alzheimer's Disease (Subas Sakya
and Kapil Karki). 17.1 Background. 17.2 Pharmacology. 17.3
Structure-Activity Relationship (SAR). 17.4 Pharmacokinetics and Drug
Metabolism. 17.5 Efficacy and Safety. 17.6 Synthesis of Donepezil. 17.7
Synthesis of Rivastigmine. 17.8 Synthesis of Galantamine. 17.9 References.
Chapter 18. Aprepitant (Emend), A NK1 Receptor Antagonist for the Treatment
of Post-chemotherapy Emesis (John A. Lowe, III). 18.1 Background. 18.2 In
Vitro Pharmacology and Structure-Activity Relationships. 18.3 In Vivo
Pharmacology. 18.4 Pharmacokinetics and Drug Metabolism. 18.5 Efficacy and
Safety. 18.6 Syntheses. 18.7 References. Chapter 19. Armodafinil (Nuvigil),
A Psychostimulant for the Treatment of Narcolepsy (Ji Zhang and Jason
Crawford). 19.1 Background. 19.2 Pharmacology. 19.3 Pharmacokinetics and
Drug Metabolism. 19.4 Efficacy and Safety. 19.5 Synthesis. 19.6 References.
V. Miscellaneous. Chapter 20. Raloxifene (Evista), A Selective Estrogen
Receptor Modulator (SERM) (Marta Piñeiro-Núñez). 20.1 Background. 20.2
Mechanism of Action. 20.3 Pharmacokinetics and Drug Metabolism. 20.4
Efficacy and Safety. 20.5 Syntheses. 20.6 References. Chapter 21.
Latanoprost (Xalatan), A Prostanoid FP Agonist for Glaucoma (Sajiv K. Nair
and Kevin E. Henegar). 21.1 Background. 21.2 Syntheses. 21.3 References.
Index.
Preface. Contributors. I. Infectious Diseases. Chapter 1. Raltegravir
(Isentress), The First-in-class HIV-1 Integrase Inhibitor (Julianne A.
Hunt). 1.1 Background. 1.2 Pharmacology. 1.3 Structure-Activity
Relationship (SAR). 1.4 Pharmacokinetics and Drug Metabolism. 1.5 Efficacy
and Safety. 1.6 Syntheses. 1.7 References. Chapter 2. Maraviroc
(Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV
(David Price). 2.1 Background. 2.2 Structure-Activity Relationship (SAR).
2.3 Pharmacokinetics and Safety. 2.4 Syntheses. 2.5 References. Chapter 3.
Darunavir (Prezista), A HIV-1 Protease Inhibitor for Treatment of Multidrug
Resistant HIV (Arun K. Ghosh and Cuthbert D. Martyr). 3.1 Background. 3.2
Pharmacology. 3.3 Structure-Activity Relationship (SAR). 3.4
Pharmacokinetics and Drug Metabolism. 3.5 Efficacy and Safety. 3.6
Syntheses. 3.7 References. II. Cancer. Chapter 4. Decitabine (Dacogen), A
DNA Methyltransferase Inhibitor for Cancer (Jennifer A. Van Camp). 4.1
Background. 4.2 Pharmacology. 4.3 Structure-Activity Relationship (SAR).
4.4 Pharmacokinetics and Drug Metabolism. 4.5 Efficacy and Safety. 4.6
Syntheses. 4.7 References. Chapter 5. Capecitabine (Xeloda), An Oral
Chemotherapy Agent (R. Jason Herr). 5.1 Background. 5.2 Pharmacology. 5.3
Structure-Activity Relationship (SAR). 5.4 Pharmacokinetics and Efficacy.
5.5 Syntheses. 5.6 References. Chapter 6. Sorafenib (Nexavar), A
Multi-kinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable
Hepatocellular Carcinoma (Shuanghua Hu). 6.1 Background. 6.2 Pharmacology.
6.3 Structure-Activity Relationship (SAR). 6.4 Pharmacokinetics and Drug
Metabolism. 6.5 Efficacy and Safety. 6.6 Syntheses. 6.7 References. Chapter
7. Sunitinib (Sutent), An Angiogenesis Inhibitor (Martin Pettersson). 7.1
Background. 7.2 Discovery and Development. 7.3 Syntheses. 7.3.1 Discovery
Route. 7.3.2 Process Route. 7.4 References. Chapter 8. Bortezomib
(Velcade), A First-in-class Proteasome Inhibitor (Benjamin S. Greener and
David S. Millan). 8.1 Background. 8.2 Pharmacology. 8.3 Structure-Activity
Relationship (SAR). 8.4 Pharmacokinetics and Drug Metabolism. 8.5 Efficacy
and Safety. 8.6 Syntheses. 8.7 References. Chapter 9. Pazopanib (Votrient),
A VEGFR Tyrosine Kinase Inhibitor for Cancer (Ji Zhang and Jie Jack Li).
9.1 Background. 9.2 Pharmacology. 9.3 Structure-Activity Relationship
(SAR). 9.4 Pharmacokinetics and Drug Metabolism. 9.5 Efficacy and Safety.
9.6 Syntheses. 9.7 Other VEGFR Inhibitors in Development: Vandetanib and
Cediranib. 9.8 References. III. Cardiovascular and Metabolic Diseases.
Chapter 10. Sitagliptin (Januvia), A Treatment for Type 2 Diabetes (Scott
D. Edmondson, Feng Xu, and Joseph D. Armstrong III). 10.1 Background. 10.2
Pharmacology. 10.3 Structure-Activity Relationship (SAR). 10.4
Pharmacokinetics and Drug Metabolism. 10.5 Efficacy and Safety. 10.6
Syntheses. 10.7 References. Chapter 11. Aliskiren (Tekturna), The
First-in-class Renin Inhibitor for Hypertension (Victor J. Cee). 11.1
Background. 11.2 Pharmacology. 11.3 Structure-Activity Relationship (SAR).
11.4 Pharmacokinetics and Drug Metabolism. 11.5 Efficacy and Safety. 11.6
Syntheses. 11.7 References. Chapter 12. Vernakalant (Kynapid), An
Investigational Drug for the Treatment of Atrial Fibrillation (David L.
Gray). 12.1 Background. 12.2 Pharmacology. 12.3 Structure-Activity
Relationship (SAR). 12.4 Pharmacokinetics and Drug Metabolism. 12.5
Efficacy and Safety. 12.6 Syntheses. 12.7 References. Chapter 13.
Conivaptan (Vaprisol), Vasopressin V1a and V2 Antagonist for Hyponatremia
(Brian A. Lanman). 13.1 Background. 13.2 Pharmacology. 13.3
Structure-Activity Relationship (SAR). 13.4 Pharmacokinetics and Drug
Metabolism. 13.5 Efficacy and Safety. 13.6 Syntheses. 13.7 References.
Chapter 14. Rivaroxaban (Xarelto), A Factor Xa Inhibitor for the Treatment
of Thrombotic Events (Ji Zhang and Jason Crawford). 14.1 Background. 14.2
Pharmacology. 14.3 Structure-Activity Relationship (SAR). 14.4
Pharmacokinetics and Drug Metabolism. 14.5 Efficacy and Safety. 14.6
Syntheses. 14.7 Compounds in Development: Apixaban and Otamixaban. 14.8
References. Chapter 15. Endothelin Antagonists for the Treatment of
Pulmonary Arterial Hypertension (David Edmonds). 15.1 Background. 15.2
Treatment of PAH. 15.3 Endothelin Antagonists. 15.4 Synthesis of Bosentan.
15.5 Synthesis of Sitaxsentan. 15.6 Synthesis of Ambrisentan. 15.7
Conclusion. 15.8 References. IV. Central Nervous System Diseases. Chapter
16. Varenicline (Chantix), An alpha4ß2 Nicotinic Receptor Partial Agonist
for Smoking Cessation (Jotham W. Coe, Frank R. Busch and Robert A. Singer).
16.1 Background. 16.2 Discovery Chemistry Program. 16.3 Pharmacology. 16.4
Pharmacokinetics and Drug Metabolism. 16.5 Efficacy and Safety. 16.6
Syntheses. 16.7 References. Chapter 17. Donepezil, Rivastigmine,
Galantamine: Cholinesterase Inhibitors for Alzheimer's Disease (Subas Sakya
and Kapil Karki). 17.1 Background. 17.2 Pharmacology. 17.3
Structure-Activity Relationship (SAR). 17.4 Pharmacokinetics and Drug
Metabolism. 17.5 Efficacy and Safety. 17.6 Synthesis of Donepezil. 17.7
Synthesis of Rivastigmine. 17.8 Synthesis of Galantamine. 17.9 References.
Chapter 18. Aprepitant (Emend), A NK1 Receptor Antagonist for the Treatment
of Post-chemotherapy Emesis (John A. Lowe, III). 18.1 Background. 18.2 In
Vitro Pharmacology and Structure-Activity Relationships. 18.3 In Vivo
Pharmacology. 18.4 Pharmacokinetics and Drug Metabolism. 18.5 Efficacy and
Safety. 18.6 Syntheses. 18.7 References. Chapter 19. Armodafinil (Nuvigil),
A Psychostimulant for the Treatment of Narcolepsy (Ji Zhang and Jason
Crawford). 19.1 Background. 19.2 Pharmacology. 19.3 Pharmacokinetics and
Drug Metabolism. 19.4 Efficacy and Safety. 19.5 Synthesis. 19.6 References.
V. Miscellaneous. Chapter 20. Raloxifene (Evista), A Selective Estrogen
Receptor Modulator (SERM) (Marta Piñeiro-Núñez). 20.1 Background. 20.2
Mechanism of Action. 20.3 Pharmacokinetics and Drug Metabolism. 20.4
Efficacy and Safety. 20.5 Syntheses. 20.6 References. Chapter 21.
Latanoprost (Xalatan), A Prostanoid FP Agonist for Glaucoma (Sajiv K. Nair
and Kevin E. Henegar). 21.1 Background. 21.2 Syntheses. 21.3 References.
Index.
(Isentress), The First-in-class HIV-1 Integrase Inhibitor (Julianne A.
Hunt). 1.1 Background. 1.2 Pharmacology. 1.3 Structure-Activity
Relationship (SAR). 1.4 Pharmacokinetics and Drug Metabolism. 1.5 Efficacy
and Safety. 1.6 Syntheses. 1.7 References. Chapter 2. Maraviroc
(Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV
(David Price). 2.1 Background. 2.2 Structure-Activity Relationship (SAR).
2.3 Pharmacokinetics and Safety. 2.4 Syntheses. 2.5 References. Chapter 3.
Darunavir (Prezista), A HIV-1 Protease Inhibitor for Treatment of Multidrug
Resistant HIV (Arun K. Ghosh and Cuthbert D. Martyr). 3.1 Background. 3.2
Pharmacology. 3.3 Structure-Activity Relationship (SAR). 3.4
Pharmacokinetics and Drug Metabolism. 3.5 Efficacy and Safety. 3.6
Syntheses. 3.7 References. II. Cancer. Chapter 4. Decitabine (Dacogen), A
DNA Methyltransferase Inhibitor for Cancer (Jennifer A. Van Camp). 4.1
Background. 4.2 Pharmacology. 4.3 Structure-Activity Relationship (SAR).
4.4 Pharmacokinetics and Drug Metabolism. 4.5 Efficacy and Safety. 4.6
Syntheses. 4.7 References. Chapter 5. Capecitabine (Xeloda), An Oral
Chemotherapy Agent (R. Jason Herr). 5.1 Background. 5.2 Pharmacology. 5.3
Structure-Activity Relationship (SAR). 5.4 Pharmacokinetics and Efficacy.
5.5 Syntheses. 5.6 References. Chapter 6. Sorafenib (Nexavar), A
Multi-kinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable
Hepatocellular Carcinoma (Shuanghua Hu). 6.1 Background. 6.2 Pharmacology.
6.3 Structure-Activity Relationship (SAR). 6.4 Pharmacokinetics and Drug
Metabolism. 6.5 Efficacy and Safety. 6.6 Syntheses. 6.7 References. Chapter
7. Sunitinib (Sutent), An Angiogenesis Inhibitor (Martin Pettersson). 7.1
Background. 7.2 Discovery and Development. 7.3 Syntheses. 7.3.1 Discovery
Route. 7.3.2 Process Route. 7.4 References. Chapter 8. Bortezomib
(Velcade), A First-in-class Proteasome Inhibitor (Benjamin S. Greener and
David S. Millan). 8.1 Background. 8.2 Pharmacology. 8.3 Structure-Activity
Relationship (SAR). 8.4 Pharmacokinetics and Drug Metabolism. 8.5 Efficacy
and Safety. 8.6 Syntheses. 8.7 References. Chapter 9. Pazopanib (Votrient),
A VEGFR Tyrosine Kinase Inhibitor for Cancer (Ji Zhang and Jie Jack Li).
9.1 Background. 9.2 Pharmacology. 9.3 Structure-Activity Relationship
(SAR). 9.4 Pharmacokinetics and Drug Metabolism. 9.5 Efficacy and Safety.
9.6 Syntheses. 9.7 Other VEGFR Inhibitors in Development: Vandetanib and
Cediranib. 9.8 References. III. Cardiovascular and Metabolic Diseases.
Chapter 10. Sitagliptin (Januvia), A Treatment for Type 2 Diabetes (Scott
D. Edmondson, Feng Xu, and Joseph D. Armstrong III). 10.1 Background. 10.2
Pharmacology. 10.3 Structure-Activity Relationship (SAR). 10.4
Pharmacokinetics and Drug Metabolism. 10.5 Efficacy and Safety. 10.6
Syntheses. 10.7 References. Chapter 11. Aliskiren (Tekturna), The
First-in-class Renin Inhibitor for Hypertension (Victor J. Cee). 11.1
Background. 11.2 Pharmacology. 11.3 Structure-Activity Relationship (SAR).
11.4 Pharmacokinetics and Drug Metabolism. 11.5 Efficacy and Safety. 11.6
Syntheses. 11.7 References. Chapter 12. Vernakalant (Kynapid), An
Investigational Drug for the Treatment of Atrial Fibrillation (David L.
Gray). 12.1 Background. 12.2 Pharmacology. 12.3 Structure-Activity
Relationship (SAR). 12.4 Pharmacokinetics and Drug Metabolism. 12.5
Efficacy and Safety. 12.6 Syntheses. 12.7 References. Chapter 13.
Conivaptan (Vaprisol), Vasopressin V1a and V2 Antagonist for Hyponatremia
(Brian A. Lanman). 13.1 Background. 13.2 Pharmacology. 13.3
Structure-Activity Relationship (SAR). 13.4 Pharmacokinetics and Drug
Metabolism. 13.5 Efficacy and Safety. 13.6 Syntheses. 13.7 References.
Chapter 14. Rivaroxaban (Xarelto), A Factor Xa Inhibitor for the Treatment
of Thrombotic Events (Ji Zhang and Jason Crawford). 14.1 Background. 14.2
Pharmacology. 14.3 Structure-Activity Relationship (SAR). 14.4
Pharmacokinetics and Drug Metabolism. 14.5 Efficacy and Safety. 14.6
Syntheses. 14.7 Compounds in Development: Apixaban and Otamixaban. 14.8
References. Chapter 15. Endothelin Antagonists for the Treatment of
Pulmonary Arterial Hypertension (David Edmonds). 15.1 Background. 15.2
Treatment of PAH. 15.3 Endothelin Antagonists. 15.4 Synthesis of Bosentan.
15.5 Synthesis of Sitaxsentan. 15.6 Synthesis of Ambrisentan. 15.7
Conclusion. 15.8 References. IV. Central Nervous System Diseases. Chapter
16. Varenicline (Chantix), An alpha4ß2 Nicotinic Receptor Partial Agonist
for Smoking Cessation (Jotham W. Coe, Frank R. Busch and Robert A. Singer).
16.1 Background. 16.2 Discovery Chemistry Program. 16.3 Pharmacology. 16.4
Pharmacokinetics and Drug Metabolism. 16.5 Efficacy and Safety. 16.6
Syntheses. 16.7 References. Chapter 17. Donepezil, Rivastigmine,
Galantamine: Cholinesterase Inhibitors for Alzheimer's Disease (Subas Sakya
and Kapil Karki). 17.1 Background. 17.2 Pharmacology. 17.3
Structure-Activity Relationship (SAR). 17.4 Pharmacokinetics and Drug
Metabolism. 17.5 Efficacy and Safety. 17.6 Synthesis of Donepezil. 17.7
Synthesis of Rivastigmine. 17.8 Synthesis of Galantamine. 17.9 References.
Chapter 18. Aprepitant (Emend), A NK1 Receptor Antagonist for the Treatment
of Post-chemotherapy Emesis (John A. Lowe, III). 18.1 Background. 18.2 In
Vitro Pharmacology and Structure-Activity Relationships. 18.3 In Vivo
Pharmacology. 18.4 Pharmacokinetics and Drug Metabolism. 18.5 Efficacy and
Safety. 18.6 Syntheses. 18.7 References. Chapter 19. Armodafinil (Nuvigil),
A Psychostimulant for the Treatment of Narcolepsy (Ji Zhang and Jason
Crawford). 19.1 Background. 19.2 Pharmacology. 19.3 Pharmacokinetics and
Drug Metabolism. 19.4 Efficacy and Safety. 19.5 Synthesis. 19.6 References.
V. Miscellaneous. Chapter 20. Raloxifene (Evista), A Selective Estrogen
Receptor Modulator (SERM) (Marta Piñeiro-Núñez). 20.1 Background. 20.2
Mechanism of Action. 20.3 Pharmacokinetics and Drug Metabolism. 20.4
Efficacy and Safety. 20.5 Syntheses. 20.6 References. Chapter 21.
Latanoprost (Xalatan), A Prostanoid FP Agonist for Glaucoma (Sajiv K. Nair
and Kevin E. Henegar). 21.1 Background. 21.2 Syntheses. 21.3 References.
Index.
"All chapters are very well written, and the used schemes and tables are conveniently arranged. The information and explanations given are strengthened by well-chosen examples and so the reader can easily follow the discussion. The comprehensive referenced literature placed at the end of each chapter enables further reading, and a detailed keyword index in combination with a logically structured Table of Content allows fast access to the topic of interest." -- ChemMedChem, 2010