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El. knyga: Drug Discovery with Privileged Building Blocks: Tactics in Medicinal Chemistry

(Revolution Medicines, California, USA),
  • Formatas: 320 pages
  • Išleidimo metai: 21-Oct-2021
  • Leidėjas: CRC Press
  • Kalba: eng
  • ISBN-13: 9781000416015
Kitos knygos pagal šią temą:
Drug Discovery with Privileged Building Blocks: Tactics in Medicinal ChemistryDidesnis paveikslėlis
  • Formatas: 320 pages
  • Išleidimo metai: 21-Oct-2021
  • Leidėjas: CRC Press
  • Kalba: eng
  • ISBN-13: 9781000416015
Kitos knygos pagal šią temą:

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"Drug Discovery with Privileged Building Blocks traces back PharmaBlock§s founding philosophy of designing privileged building blocks. High-quality building blocks are crucial not only to molecules' biological activities but also to ADMET properties, which eventually will impact the success rate of drug discovery projects. A thorough study of how building blocks perform in drug molecules and regular analysis of new building block structures in the latest researches has proven to be a fruitful strategy togenerate novel building blocks. Using this strategy, PharmaBlock has supplied the drug industry with a great number of building blocks, which are increasingly being adopted by drug hunters, and these are identified in this book. Each chapter may be read and studied without learning the previous chapters. This book will be a good starting point for novice medicinal chemists and veteran medicinal chemists find it useful as well"--

Drug Discovery with Privileged Building Blocks traces back PharmaBlock's founding philosophy of designing privileged building blocks. High-quality building blocks are crucial not only to molecules’ biological activities but also to ADMET properties, which eventually will impact the success rate of drug discovery projects. A thorough study of how building blocks perform in drug molecules and regular analysis of new building block structures in the latest researches has proven to be a fruitful strategy to generate novel building blocks. Using this strategy, PharmaBlock has supplied the drug industry with a great number of building blocks, which are increasingly being adopted by drug hunters, and these are identified in this book.

Each chapter may be read and studied without learning the previous chapters. This book will be a good starting point for novice medicinal chemists and veteran medicinal chemists find it useful as well.



Drug Discovery with Privileged Building Blocks traces back PharmaBlock's founding philosophy of designing privileged building blocks. Each chapter may be read and studied without learning the previous chapters. This book will be a good starting point for novice medicinal chemists and veteran medicinal chemists find it useful as well.

Preface xi
Authors xiii
Chapter 1 Alkynes 1(16)
Alkyne-Containing Drugs
1(2)
Alkynes in Drug Discovery
3(8)
Synthesis of Some Alkyne-Containing Drugs
11(3)
References
14(3)
Chapter 2 Azaindoles 17(12)
Azaindole-Containing Drugs
17(2)
Azaindoles in Drug Discovery
19(2)
Synthesis of Some Azaindole-Containing Drugs
21(5)
Bartoli Reaction
21(1)
Batcho-Leimgruber Reaction
22(1)
Radical Aromatization
23(1)
Suzuki Coupling
24(1)
Sonogashira Reaction
25(1)
References
26(3)
Chapter 3 Azetidines 29(4)
Azetidine-Containing Drugs
29(1)
Azetidines in Drug Discovery
29(2)
Synthesis of Some Azetidine-Containing Drugs
31(1)
References
32(1)
Chapter 4 Bicyclic Pyridines Containing Ring-Junction N 33(8)
Bicyclic Pyridine-Containing Drugs
33(1)
Bicyclic Pyridines in Drug Discovery
34(3)
Synthesis of Some Bicyclic Pyridines
37(2)
References
39(2)
Chapter 5 Bicyclo[ 1.1.1]pentyl (BCP) as an spa Carbon-Rich Bioisostere for para-Phenyl and tert-Butyl Groups 41(8)
There is Something about BCP
41(3)
Bicyclo[ 1.1.1]pentanes in Drug Discovery
44(2)
Synthesis of Some Bicyclo[ 1.1.1]pentane-Containing Drugs
46(2)
References
48(1)
Chapter 6 Bicyclo[ 2.2.2]octane (BCO) as a 3D-Rich Bioisostere for the para-Phenyl Group 49(8)
Merits of sp3-Rich Carbon Bioisosteres-Escape from Flatland
49(1)
Bicyclo[ 2.2.2]octanes in Drug Discovery
50(3)
Synthesis of Some Bicyclo[ 2.2.2]octane-Containing Drugs
53(2)
References
55(2)
Chapter 7 Bicyclo[ 3.1.0]hexanes 57(10)
Bicyclo[ 3.1.0]hexane-Containing Drugs
57(2)
Bicyclo[ 3.1.0]hexanes in Drug Discovery
59(4)
Bicyclo[ 3.1.0]hexanes as Bioisosteres of Cyclohexanes
59(2)
Utility of Bicyclo[ 3.1.0]hexanes in Medicinal Chemistry
61(2)
Synthesis of Some Bicyclo[ 3.1.0]hexane-Containing Drugs
63(2)
References
65(2)
Chapter 8 Bridge-Fused Rings as m-Phenyl Bioisosteres 67(8)
3-D-Rich Bioisosteres for the Phenyl Ring in Drug Discovery
68(3)
Synthesis of Some Drugs Containing 3-D-Rich Bioisosteres for the m-Phenyl Ring
71(2)
References
73(2)
Chapter 9 Cubanes, Are We There Yet? 75(10)
Cubane-Containing Drugs
75(1)
Cubanes in Drug Discovery
75(5)
Synthesis of Some Cubane-Containing Building Blocks
80(2)
References
82(3)
Chapter 10 Cyclobutanes 85(8)
Cyclobutane-Containing Drugs
85(1)
Cyclobutanes in Drug Discovery
86(3)
Synthesis of Some Cyclobutane-Containing Drugs
89(1)
References
90(3)
Chapter 11 Cyclohexanes 93(14)
Cyclohexane-Containing Drugs
93(3)
Cyclohexanes in Drug Discovery
96(5)
Synthesis of Some Cyclohexane-Containing Drugs
101(3)
References
104(3)
Chapter 12 Cyclopentanes 107(6)
Cyclopentane-Containing Drugs
107(1)
Cyclopentanes in Drug Discovery
108(2)
Synthesis of Some Cyclopentane-Containing Drugs
110(2)
References
112(1)
Chapter 13 Cyclopropane Derivatives as Metabolically More Robust Bioisosteres for Linear Alkyl Substituents 113(4)
References
116(1)
Chapter 14 Deazapurines 117(4)
References
120(1)
Chapter 15 Furopyridines 121(8)
Furopyridine-Containing Drugs
121(2)
Furopyridines in Drug Discovery
123(3)
Synthesis of Some Furopyridine-Containing Drugs
126(1)
References
127(2)
Chapter 16 Indazoles 129(14)
Indazole-Containing Drugs
129(1)
Indazoles in Drug Discovery
130(7)
Synthesis of Some Indazole-Containing Drugs
137(3)
References
140(3)
Chapter 17 Indoles 143(10)
Indole-Containing Drugs
143(3)
Indoles in Drug Discovery
146(3)
Representative Bioisosteres
146(2)
Possible Liabilities of Drugs Containing 3-Methylindole
148(1)
Synthesis of Some Indole-Containing Drugs
149(2)
References
151(2)
Chapter 18 Oxetanes 153(6)
Oxetane-Containing Drugs
153(1)
Oxetanes in Drug Discovery
153(4)
Synthesis of Some Oxetane-Containing Drugs
157(1)
References
158(1)
Chapter 19 Piperidine, the Enchanted Ring 159(4)
Piperidine-Containing Drugs
159(1)
Piperidine Improves Aqueous Solubility of Drugs
160(1)
Piperidine Addresses Drug-Resistance Issues
161(1)
Synthesis of Some Piperidine-Containing Drugs
161(1)
References
162(1)
Chapter 20 Pyrazines 163(10)
Pyrazine-Containing Drugs
163(2)
Pyrazines in Drug Discovery
165(3)
Synthesis of Some Pyrazine-Containing Drugs
168(3)
References
171(2)
Chapter 21 Pyrazoles 173(14)
Pyrazole-Containing Drugs
173(2)
Pyrazoles in Drug Discovery
175(5)
Pyrazole as a Bioisostere of Arenes and Hetarenes
175(3)
Pyrazole as Hydrogen Bond Donor and Acceptor
178(2)
Synthesis of Some Pyrazole-Containing Drugs
180(5)
References
185(2)
Chapter 22 Pyridazines 187(10)
Pyridazine-Containing Drugs
187(2)
Pyridazines in Drug Discovery
189(3)
Boost a Drug's Aqueous Solubility
189(1)
Facilitate Formation of Crystalline, Water-Soluble Solid Salts
190(1)
As a Bioisostere of Hetaryl Rings
191(1)
Synthesis of Some Pyridazine-Containing Drugs
192(3)
References
195(2)
Chapter 23 Pyridines-The Magic of Phenyl-Pyridyl Switch 197(12)
Pyridine-Containing Drugs
197(2)
Pyridines in Drug Discovery
199(3)
Boosting Biochemical Potency
199(1)
Fixing CYP450 Liability
200(1)
Elevating Permeability
200(1)
Addressing Protein Binding Issue
201(1)
Synthesis of Some Pyridine-Containing Drugs
202(5)
Loratadine (Claritin, 1)
202(1)
Nevirapine (Viramune, 2)
203(1)
Omeprazole (Prilosec, 3)
203(1)
Netupitant (4)
204(1)
Abemaciclib (Verzenio, 5)
205(1)
Lorlatinib (Lorbrena, 6)
205(1)
Apalutamide (Erleada, 7)
206(1)
References
207(2)
Chapter 24 Pyrimidines 209(10)
Pyrimidine-Containing Drugs
209(4)
Pyrimidines in Drug Discovery
213(3)
Pyrimidine as a Bioisostere
213(1)
Interactions with Target Proteins
214(2)
Synthesis of Some Pyrimidine-Containing Drugs
216(2)
References
218(1)
Chapter 25 Pyrrolidines 219(14)
Pyrrolidine-Containing Drugs
219(5)
Pyrrolidines in Drug Discovery
224(4)
Synthesis of Some Pyrrolidine-Containing Drugs
228(3)
References
231(2)
Chapter 26 Pyrrolotriazines 233(10)
Pyrrolotriazine-Containing Drugs
233(2)
Pyrrolotriazines in Drug Discovery
235(3)
Synthesis of Some Pyrrolotriazine-Containing Drugs
238(2)
References
240(3)
Chapter 27 Spiroazetidines 243(8)
Spiroazetidines in Drug Discovery
243(5)
Spiroazetidines as Bioisosteres
243(3)
Utility of Spiroazetidines in Medicinal Chemistry
246(2)
Synthesis of Some Spiroazetidines
248(2)
References
250(1)
Chapter 28 Spirocyclic Piperidines 251(8)
Spirocyclic Piperidine-Containing Drugs
251(1)
Spirocyclic Piperidines in Drug Discovery
251(3)
Synthesis of Some Spirocyclic Piperidines
254(2)
References
256(3)
Chapter 29 Spirocyclic Pyrrolidines 259(10)
Spirocyclic Pyrrolidine-Containing Drugs
259(1)
Spirocyclic Pyrrolidines in Drug Discovery
260(3)
Synthesis of Some Spirocyclic Pyrrolidine-Containing Drugs
263(4)
References
267(2)
Chapter 30 Spirooxetanes 269(6)
Spirooxetanes in Drug Discovery
269(3)
Synthesis of Some Spirooxetane-Containing Drugs
272(1)
References
273(2)
Chapter 31 Tetrahydropyrans 275(12)
Tetrahydropyran-Containing Drugs
275(2)
Tetrahydropyrans in Drug Discovery
277(4)
Synthesis of Some Tetrahydropyran-Containing Drugs
281(4)
References
285(2)
Chapter 32 Trifluoromethylpyridines 287(10)
Trifluoromethylpyridine-Containing Drugs
288(1)
Trifluoromethylpyridines in Drug Discovery
289(3)
Synthesis of Some Trifluoromethylpyridine-Containing Drugs
292(3)
References
295(2)
Index 297
Dr. Jie Jack Li is an established chemist with over 20 years of experience in both medicinal chemistry and process chemistry. He is also widely published as an author or co-author of 34 peer-reviewed articles, 12 patents, and 29 books. Prior to joining ChemPartner, Dr. Li worked at Pfizer, BMS, and Revolution Medicines in oncology, antivirals, metabolic disease, CNS, anti-inflammatory, and dermatology, targeting enzymes, receptors, or ion channels. Dr. Li was also a professor at the University of San Francisco for four years, teaching organic and medicinal chemistry. He earned his Ph.D. from Indiana University and was a post-doctoral fellow at MIT.

Dr. Minmin Yang received his PhD in organic synthesis from Auburn University, US in 2001, and did post-doctoral training at the same school from 2002 to 2004. Prior to founding PharmaBlock, he worked with increasing responsibilities from group leader to section head of medicinal chemistry at Roche Palo Alto and Roche China for 4 years. Dr. Yang has authored 80 publications, including 16 international patents.
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