Fluorine-containing pharmaceuticals approved by the FDA in 2020: Synthesis and biological activity
出版年份 2021 全文链接
标题
Fluorine-containing pharmaceuticals approved by the FDA in 2020: Synthesis and biological activity
作者
关键词
Fluorine and compounds, Blockbuster drugs, Modern pharmaceuticals, Synthesis, Drug design and development, Asymmetric synthesis
出版物
CHINESE CHEMICAL LETTERS
Volume 32, Issue 11, Pages 3342-3354
出版商
Elsevier BV
发表日期
2021-05-28
DOI
10.1016/j.cclet.2021.05.042
参考文献
相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。- Chemical Aspects of Human and Environmental Overload with Fluorine
- (2021) Jianlin Han et al. CHEMICAL REVIEWS
- Avapritinib: First Approval
- (2020) Sohita Dhillon DRUGS
- Osilodrostat: First Approval
- (2020) Sean Duggan DRUGS
- Discovery and development of plasma kallikrein inhibitors for multiple diseases
- (2020) Zhouling Xie et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- State-of-the-Art Strategies for Targeting RET-Dependent Cancers
- (2020) Vivek Subbiah et al. JOURNAL OF CLINICAL ONCOLOGY
- Oral cedazuridine/decitabine: a phase 2, pharmacokinetic/pharmacodynamic, randomized, crossover study in MDS and CMML
- (2020) Guillermo Garcia-Manero et al. BLOOD
- Tailor‐Made Amino Acids and Fluorinated Motifs as Prominent Traits in the Modern Pharmaceuticals
- (2020) Haibo Mei et al. CHEMISTRY-A EUROPEAN JOURNAL
- Fluorine-containing drugs approved by the FDA in 2019
- (2020) Haibo Mei et al. CHINESE CHEMICAL LETTERS
- Rimegepant: First Approval
- (2020) Lesley J. Scott DRUGS
- Pemigatinib: First Approval
- (2020) Sheridan M. Hoy DRUGS
- Kitamura Electrophilic Fluorination Using HF as a Source of Fluorine
- (2020) Jianlin Han et al. MOLECULES
- New Targets in Lung Cancer (Excluding EGFR, ALK, ROS1)
- (2020) Alessandro Russo et al. Current Oncology Reports
- Contribution of Organofluorine Compounds to Pharmaceuticals
- (2020) Munenori Inoue et al. ACS Omega
- Perfluorocarbons in Chemical Biology
- (2020) Margeaux A. Miller et al. CHEMBIOCHEM
- Recent Developments in the Asymmetric Detrifluoroacetylative Reactions of in situ Generated Mono-Fluorinated Enolates.
- (2020) Li Wang et al. CURRENT ORGANIC CHEMISTRY
- Absorption, Distribution, Metabolism, and Excretion (ADME) of Capmatinib (INC280) in Healthy Male Volunteers and In Vitro Aldehyde Oxidase Phenotyping of the Major Metabolite
- (2020) Ulrike Glaenzel et al. DRUG METABOLISM AND DISPOSITION
- Selumetinib: First Approval
- (2020) Anthony Markham et al. DRUGS
- Capmatinib: First Approval
- (2020) Sohita Dhillon DRUGS
- Ripretinib: First Approval
- (2020) Sohita Dhillon DRUGS
- Tailor-made amino acid-derived pharmaceuticals approved by the FDA in 2019
- (2020) Zizhen Yin et al. AMINO ACIDS
- The role of fluorine in glycomimetic drug design
- (2020) Rachel Hevey CHEMISTRY-A EUROPEAN JOURNAL
- Decitabine/Cedazuridine: First Approval
- (2020) Sohita Dhillon DRUGS
- Recent advances in fluorine-doped/fluorinated carbon-based materials for supercapacitors
- (2020) Teng Wang et al. Energy Storage Materials
- Current Contributions of Organofluorine Compounds to the Agrochemical Industry
- (2020) Yuta Ogawa et al. iScience
- On thermal decomposition kinetics of poly(ethylene-alt- tetrafluoroethylene) using an autocatalytic model
- (2020) Chun Wang et al. JOURNAL OF FLUORINE CHEMISTRY
- Tau PET imaging in neurodegenerative tauopathies—still a challenge
- (2019) Antoine Leuzy et al. MOLECULAR PSYCHIATRY
- Diagnostic accuracy and safety of 16α-[18F]fluoro-17β-oestradiol PET-CT for the assessment of oestrogen receptor status in recurrent or metastatic lesions in patients with breast cancer: a prospective cohort study
- (2019) Sun Young Chae et al. LANCET ONCOLOGY
- Fluorine‐Containing Drugs Approved by the FDA in 2018
- (2019) Haibo Mei et al. CHEMISTRY-A EUROPEAN JOURNAL
- Relugolix: First Global Approval
- (2019) Anthony Markham DRUGS
- Clinical update on hypomethylating agents
- (2019) Matthieu Duchmann et al. INTERNATIONAL JOURNAL OF HEMATOLOGY
- An oral fixed-dose combination of decitabine and cedazuridine in myelodysplastic syndromes: a multicentre, open-label, dose-escalation, phase 1 study
- (2019) Michael R Savona et al. Lancet Haematology
- Fluorine and Lithium: Ideal Partners for High-Performance Rechargeable Battery Electrolytes
- (2019) N. von Aspern et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Tau Imaging in Neurodegenerative Diseases Using Positron Emission Tomography
- (2019) Yi Ting Wang et al. Current Neurology and Neuroscience Reports
- Mediator and Additive Free Trifluoromethyl-Fluorination of Terminal Alkenes by Persistent Perfluoroalkyl Radical
- (2019) Azusa Sato et al. EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
- Applications of fluorine-containing amino acids for drug design
- (2019) Haibo Mei et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Perfluoro-3-ethyl-2,4-dimethyl-3-pentyl persistent radical: A new reagent for direct, metal-free radical trifluoromethylation and polymer initiation
- (2019) Haibo Mei et al. JOURNAL OF FLUORINE CHEMISTRY
- A role for fluorine in flavours, fragrances and pheromones?
- (2019) Phillip T. Lowe et al. JOURNAL OF FLUORINE CHEMISTRY
- Detrifluoroacetylative in Situ Generated Cyclic Fluorinated Enolates for the Preparation of Compounds Featuring a C–F Stereogenic Center
- (2019) Jiang Liu et al. ACS Omega
- Oral plasma kallikrein inhibitor BCX7353 for treatment of hereditary angioedema
- (2019) Jacqueline R Hwang et al. Immunotherapy
- The Role of Molecular Testing in the Differential Diagnosis of Salivary Gland Carcinomas
- (2018) Alena Skálová et al. AMERICAN JOURNAL OF SURGICAL PATHOLOGY
- Modern Approaches for Asymmetric Construction of Carbon–Fluorine Quaternary Stereogenic Centers: Synthetic Challenges and Pharmaceutical Needs
- (2018) Yi Zhu et al. CHEMICAL REVIEWS
- Molecular regulation of follicle-stimulating hormone synthesis, secretion and action
- (2018) Nandana Das et al. JOURNAL OF MOLECULAR ENDOCRINOLOGY
- Osimertinib in Untreated EGFR-Mutated Advanced Non–Small-Cell Lung Cancer
- (2018) Jean-Charles Soria et al. NEW ENGLAND JOURNAL OF MEDICINE
- The self-disproportionation of enantiomers (SDE): a menace or an opportunity?
- (2018) Jianlin Han et al. Chemical Science
- Precision Targeted Therapy with BLU-667 for RET -Driven Cancers
- (2018) Vivek Subbiah et al. Cancer Discovery
- Elagolix: First Global Approval
- (2018) Yvette N. Lamb DRUGS
- Oral Plasma Kallikrein Inhibitor for Prophylaxis in Hereditary Angioedema
- (2018) Emel Aygören-Pürsün et al. NEW ENGLAND JOURNAL OF MEDICINE
- Recent progress in the application of fluorinated chiral sulfinimine reagents
- (2018) Haibo Mei et al. JOURNAL OF FLUORINE CHEMISTRY
- Biomarkers for tau pathology
- (2018) Michael Schöll et al. MOLECULAR AND CELLULAR NEUROSCIENCE
- Phosphorus additives for improving high voltage stability and safety of lithium ion batteries
- (2017) Natascha von Aspern et al. JOURNAL OF FLUORINE CHEMISTRY
- Detrifluoroacetylative generation and chemistry of fluorine containing tertiary enolates
- (2017) Lijun Zhang et al. JOURNAL OF FLUORINE CHEMISTRY
- Improved Estrogen Receptor Assessment by PET Using the Novel Radiotracer18F-4FMFES in Estrogen Receptor–Positive Breast Cancer Patients: An Ongoing Phase II Clinical Trial
- (2017) Michel Paquette et al. JOURNAL OF NUCLEAR MEDICINE
- Alectinib versus Crizotinib in Untreated ALK-Positive Non–Small-Cell Lung Cancer
- (2017) Solange Peters et al. NEW ENGLAND JOURNAL OF MEDICINE
- Biological evaluation of both enantiomers of fluoro-thalidomide using human myeloma cell line H929 and others
- (2017) Etsuko Tokunaga et al. PLoS One
- A precision therapy against cancers driven by KIT/PDGFRA mutations
- (2017) Erica K. Evans et al. Science Translational Medicine
- A question of policy: should tests for the self-disproportionation of enantiomers (SDE) be mandatory for reports involving scalemates?
- (2017) Vadim A. Soloshonok et al. TETRAHEDRON-ASYMMETRY
- Fluorinated Compounds in U.S. Fast Food Packaging
- (2017) Laurel A. Schaider et al. Environmental Science & Technology Letters
- Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas
- (2016) Yu Zhou et al. CHEMICAL REVIEWS
- Prophylaxis of hereditary angioedema attacks: A randomized trial of oral plasma kallikrein inhibition with avoralstat
- (2016) Emel Aygören-Pürsün et al. JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY
- Fluoride ion batteries: Theoretical performance, safety, toxicity, and a combinatorial screening of new electrodes
- (2016) F. Gschwind et al. JOURNAL OF FLUORINE CHEMISTRY
- Synthesis and quality control of [18F]T807 for tau PET imaging
- (2016) Daniel P. Holt et al. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
- 18F-Fluoroestradiol PET: Current Status and Potential Future Clinical Applications
- (2016) G. J. Liao et al. JOURNAL OF NUCLEAR MEDICINE
- Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors
- (2016) Zhe Li et al. ACS Medicinal Chemistry Letters
- Polyfluorinated Ethanes as Versatile Fluorinated C2-Building Blocks for Organic Synthesis
- (2015) Valentine G. Nenajdenko et al. CHEMICAL REVIEWS
- Use of Second- and Third-Generation Tyrosine Kinase Inhibitors in the Treatment of Chronic Myeloid Leukemia: An Evolving Treatment Paradigm
- (2015) Elias Jabbour et al. Clinical Lymphoma Myeloma & Leukemia
- Applications of Fluorine in Medicinal Chemistry
- (2015) Eric P. Gillis et al. JOURNAL OF MEDICINAL CHEMISTRY
- Tau imaging: early progress and future directions
- (2015) Victor L Villemagne et al. LANCET NEUROLOGY
- Identification and characterization of RET fusions in advanced colorectal cancer
- (2015) Anne-France Le Rolle et al. Oncotarget
- A comprehensive examination of the self-disproportionation of enantiomers (SDE) of chiral amides via achiral, laboratory-routine, gravity-driven column chromatography
- (2015) Yuya Suzuki et al. RSC Advances
- Modern Carbon–Fluorine Bond Forming Reactions for Aryl Fluoride Synthesis
- (2014) Michael G. Campbell et al. CHEMICAL REVIEWS
- Enzymatic Fluorination and Biotechnological Developments of the Fluorinase
- (2014) David O’Hagan et al. CHEMICAL REVIEWS
- Beyond the Balz–Schiemann Reaction: The Utility of Tetrafluoroborates and Boron Trifluoride as Nucleophilic Fluoride Sources
- (2014) Alexander J. Cresswell et al. CHEMICAL REVIEWS
- Synthetic Methods for Compounds Having CF3–S Units on Carbon by Trifluoromethylation, Trifluoromethylthiolation, Triflylation, and Related Reactions
- (2014) Xiu-Hua Xu et al. CHEMICAL REVIEWS
- Trifluoromethyltrimethylsilane: Nucleophilic Trifluoromethylation and Beyond
- (2014) Xiao Liu et al. CHEMICAL REVIEWS
- Electrophilic Trifluoromethylation by Use of Hypervalent Iodine Reagents
- (2014) Julie Charpentier et al. CHEMICAL REVIEWS
- 19F Magnetic Resonance Imaging (MRI): From Design of Materials to Clinical Applications
- (2014) Ilaria Tirotta et al. CHEMICAL REVIEWS
- Successful fluorine-containing herbicide agrochemicals
- (2014) Tomoya Fujiwara et al. JOURNAL OF FLUORINE CHEMISTRY
- Recent advances in the trifluoromethylation methodology and new CF3-containing drugs
- (2014) Wei Zhu et al. JOURNAL OF FLUORINE CHEMISTRY
- Design, Synthesis, and Pharmacological Evaluation of Fluorinated Tetrahydrouridine Derivatives as Inhibitors of Cytidine Deaminase
- (2014) Dana Ferraris et al. JOURNAL OF MEDICINAL CHEMISTRY
- The landscape of kinase fusions in cancer
- (2014) Nicolas Stransky et al. Nature Communications
- Development of Electrolytes towards Achieving Safe and High-Performance Energy-Storage Devices: A Review
- (2014) Yu Wang et al. ChemElectroChem
- Gonadotropin-releasing hormone receptors as molecular therapeutic targets in prostate cancer: Current options and emerging strategies
- (2013) Patrizia Limonta et al. CANCER TREATMENT REVIEWS
- Fluorine in Pharmaceutical Industry: Fluorine-Containing Drugs Introduced to the Market in the Last Decade (2001–2011)
- (2013) Jiang Wang et al. CHEMICAL REVIEWS
- Optical Purifications via Self-Disproportionation of Enantiomers by Achiral Chromatography: Case Study of a Series of α-CF3-containing Secondary Alcohols
- (2013) Alexander E. Sorochinsky et al. CHIRALITY
- Emerging Paradigms in the Development of Resistance to Tyrosine Kinase Inhibitors in Lung Cancer
- (2013) Justin F. Gainor et al. JOURNAL OF CLINICAL ONCOLOGY
- Synthesis of fluorine-containing α-amino acids in enantiomerically pure form via homologation of Ni(II) complexes of glycine and alanine Schiff bases
- (2013) José Luis Aceña et al. JOURNAL OF FLUORINE CHEMISTRY
- Synthesis and uses of fluorous and highly fluorinated macrocyclic and spherical molecules
- (2013) Wen-Bin Yi et al. JOURNAL OF FLUORINE CHEMISTRY
- A Phase 2 Study of 16α-[18F]-fluoro-17β-estradiol Positron Emission Tomography (FES-PET) as a Marker of Hormone Sensitivity in Metastatic Breast Cancer (MBC)
- (2013) Lanell M. Peterson et al. MOLECULAR IMAGING AND BIOLOGY
- Crizotinib versus Chemotherapy in Advanced ALK-Positive Lung Cancer
- (2013) Alice T. Shaw et al. NEW ENGLAND JOURNAL OF MEDICINE
- Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors
- (2013) Erik L. Meredith et al. ACS Medicinal Chemistry Letters
- A systematic review on fluoridated food in caries prevention
- (2012) Maria Grazia Cagetti et al. ACTA ODONTOLOGICA SCANDINAVICA
- Unconventional preparation of racemic crystals of isopropyl 3,3,3-trifluoro-2-hydroxypropanoate and their unusual crystallographic structure: the ultimate preference for homochiral intermolecular interactions
- (2012) José Luis Aceña et al. CHEMICAL COMMUNICATIONS
- GnRH Receptors in Cancer: From Cell Biology to Novel Targeted Therapeutic Strategies
- (2012) Patrizia Limonta et al. ENDOCRINE REVIEWS
- Oxime formation for fluorine-18 labeling of peptides and proteins for positron emission tomography (PET) imaging: A review
- (2012) Xiang-Guo Li et al. JOURNAL OF FLUORINE CHEMISTRY
- Discovery of (5S,6S,9R)-5-Amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): An Oral Calcitonin Gene-Related Peptide (CGRP) Antagonist in Clinical Trials for Treating Migraine
- (2012) Guanglin Luo et al. JOURNAL OF MEDICINAL CHEMISTRY
- RET fusion genes are associated with chronic myelomonocytic leukemia and enhance monocytic differentiation
- (2012) P Ballerini et al. LEUKEMIA
- KIF5B-RET fusions in lung adenocarcinoma
- (2012) Takashi Kohno et al. NATURE MEDICINE
- Efficient and Scalable Enantioselective Synthesis of a CGRP Antagonist
- (2012) David K. Leahy et al. ORGANIC LETTERS
- Self-disproportionation of enantiomers of non-racemic chiral amine derivatives through achiral chromatography
- (2012) Tsuyoshi Nakamura et al. TETRAHEDRON
- Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine
- (2012) Guanglin Luo et al. ACS Medicinal Chemistry Letters
- Delineation of the Molecular Mechanisms of Nucleoside Recognition by Cytidine Deaminase through Virtual Screening
- (2011) Stefano Costanzi et al. ChemMedChem
- Biomimetic Transamination – a Metal-Free Alternative to the Reductive Amination. Application for Generalized Preparation of Fluorine-Containing Amines and Amino Acids
- (2011) Jianlin Han et al. CURRENT ORGANIC SYNTHESIS
- Self-Disproportionation of Enantiomers via Sublimation; New and Truly Green Dimension in Optical Purification
- (2011) Jianlin Han et al. CURRENT ORGANIC SYNTHESIS
- A transforming KIF5B and RET gene fusion in lung adenocarcinoma revealed from whole-genome and transcriptome sequencing
- (2011) Y. S. Ju et al. GENOME RESEARCH
- Discovery of 1-{4-[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor
- (2011) Kazuhiro Miwa et al. JOURNAL OF MEDICINAL CHEMISTRY
- Erlotinib versus chemotherapy as first-line treatment for patients with advanced EGFR mutation-positive non-small-cell lung cancer (OPTIMAL, CTONG-0802): a multicentre, open-label, randomised, phase 3 study
- (2011) Caicun Zhou et al. LANCET ONCOLOGY
- Gefitinib vs. chemotherapy as first-line therapy in advanced non-small cell lung cancer: Meta-analysis of phase III trials
- (2011) Geoffrey Y. Ku et al. LUNG CANCER
- Bradykinin and the Pathogenesis of Hereditary Angioedema
- (2011) Allen P. Kaplan World Allergy Organization Journal
- Hereditary Angioedema
- (2010) Jerrold H. Levy et al. ANESTHESIA AND ANALGESIA
- Fluorine in health care: Organofluorine containing blockbuster drugs
- (2010) David O’Hagan JOURNAL OF FLUORINE CHEMISTRY
- Rhodium-Catalyzed Asymmetric Arylation ofN-Tosyl Ketimines
- (2010) Ryo Shintani et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Rational application of self-disproportionation of enantiomers via sublimation—a novel methodological dimension for enantiomeric purifications
- (2010) Hisanori Ueki et al. TETRAHEDRON-ASYMMETRY
- Self-disproportionation of enantiomers of α-trifluoromethyl lactic acid amides via sublimation
- (2009) Manabu Yasumoto et al. JOURNAL OF FLUORINE CHEMISTRY
- Self-disproportionation of enantiomers of isopropyl 3,3,3-(trifluoro)lactate via sublimation: Sublimation rates vs. enantiomeric composition
- (2009) Manabu Yasumoto et al. JOURNAL OF FLUORINE CHEMISTRY
- Discrimination of enantiomeric excess of optically active trifluorolactate by distillation: Evidence for a multi-center hydrogen bonding network in the liquid state
- (2009) Toshimasa Katagiri et al. JOURNAL OF FLUORINE CHEMISTRY
- Self-disproportionation of enantiomers of 3,3,3-trifluorolactic acid amides via sublimation
- (2009) Manabu Yasumoto et al. JOURNAL OF FLUORINE CHEMISTRY
- Synthesis of Deoxytetrahydrouridine
- (2009) Jolanna Norton et al. JOURNAL OF ORGANIC CHEMISTRY
- Evolution of decitabine development
- (2008) Elias Jabbour et al. CANCER
- The Many Roles for Fluorine in Medicinal Chemistry
- (2008) William K. Hagmann JOURNAL OF MEDICINAL CHEMISTRY
- Quantitative Imaging of Estrogen Receptor Expression in Breast Cancer with PET and 18F-Fluoroestradiol
- (2008) L. M. Peterson et al. JOURNAL OF NUCLEAR MEDICINE
Find Funding. Review Successful Grants.
Explore over 25,000 new funding opportunities and over 6,000,000 successful grants.
ExploreCreate your own webinar
Interested in hosting your own webinar? Check the schedule and propose your idea to the Peeref Content Team.
Create Now