Progress in Medicinal Chemistry, Volume 57, provides a review of eclectic developments in medicinal chemistry, with this volume including chapters on the CaSR field, CFTR modulators in cystic fibrosis, macrocycles, VMAT2 inhibitors, and Big Data in Drug Discovery.
- Provides extended, timely reviews of topics in medicinal chemistry
- Contains targets and technologies relevant to the discovery of tomorrows drugs
- Presents analyses of successful drug discovery programs
Contributors |
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vii | |
Preface |
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1 Discovery and Development of Calcimimetic and Calcilytic Compounds |
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1 | (86) |
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2 | (1) |
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2 The Extracellular Calcium Receptor |
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3 | (6) |
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3 Screening for Calcimimetics and Calcilytics |
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9 | (2) |
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11 | (32) |
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43 | (23) |
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6 Molecular Mechanism of Action ol Calcimimetics and Calcilytics |
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66 | (7) |
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73 | (14) |
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74 | (13) |
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2 VMAT2 Inhibitors and the Path to Ingrezza (Valbenazine) |
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87 | (26) |
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87 | (2) |
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89 | (3) |
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3 Tetrabenazine and Metabolites |
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92 | (1) |
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4 TBZ Metabolite Pharmacologic Characterization |
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93 | (2) |
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5 Prodrugs of R,R,R-DHTBZ |
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95 | (9) |
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104 | (9) |
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108 | (5) |
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3 Current Trends in Macrocyclic Drug Discovery and beyond-Ro5 |
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113 | (122) |
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114 | (2) |
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2 Synthetic Approaches Towards Macrocycles |
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116 | (34) |
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3 Physicochemical Properties and Rational Design of Macrocycles |
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150 | (34) |
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4 Scale-Up Considerations for Macrocycles |
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184 | (9) |
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5 Novel !ethnologies Towards Macrocyclic Libraries |
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193 | (7) |
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6 Patent Overview (2015S to Aug. 2017) |
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200 | (8) |
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208 | (27) |
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210 | (1) |
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210 | (25) |
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4 Recent Progress in the Discovery and Development of Small-Molecule Modulators of CFTR |
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235 | (42) |
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236 | (1) |
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2 CFTR Mutations Implicated in CF |
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237 | (1) |
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3 Molecular Structure of CFTR |
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238 | (1) |
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239 | (3) |
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5 Discovery of Potentiators |
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242 | (12) |
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6 Discovery of CFTR Correctors/Amplifiers |
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254 | (13) |
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7 Therapeutic Potential of CFTR Modulators |
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267 | (2) |
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8 Summary and future Perspectives |
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269 | (8) |
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270 | (1) |
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270 | (7) |
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5 Big Data in Drug Discovery |
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277 | (67) |
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278 | (1) |
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279 | (10) |
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289 | (1) |
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289 | (11) |
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300 | (28) |
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328 | (1) |
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7 Big Data in Clinical Trials and Health Care |
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329 | (14) |
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343 | (1) |
References |
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Dr David Witty has more than 20 years experience in the pharmaceutical industry as a medicinal chemist and project leader working principally in areas of anti-infectives, metabolic diseases, cognition and pain, delivering clinical candidates for several conditions. He led IT Strategy within the Neurology division of GSK, developing and deploying the first Electronic Notebooks for drug discovery to sites in the UK and Singapore. He has contributed more than 90 scientific papers, reviews, patents and books on medicinal and synthetic chemistry.In 2010 David and several colleagues successfully raised $35M in venture funding to found Convergence Pharmaceuticals, a specialist ion channel company focused on the development of novel treatments for pain, based in Cambridge UK. David presently leads their discovery programme and manages scientific operations within the business.David is chairman of the Fine Chemicals Group of the Society of Chemical Industry, with responsibility for the delivery of conferences, seminars and training courses for chemists throughout the UK and Europe, and advising parliamentary bodies on matters of relevance to the UK chemical industry.Since 2008 David has been a STEM ambassador for SETPOINT, introducing school students at both primary and secondary level to the excitement and possibilities of pursuing scientific careers, through workshops, lectures and competitions. Professor Brian Cox is at University of Sussex, Brighton, UK