New Halogen-Containing Drugs Approved by FDA in 2021: An Overview on Their Syntheses and Pharmaceutical Use

被引:107
作者
Tiz, Davide Benedetto [1 ]
Bagnoli, Luana [1 ]
Rosati, Ornelio [1 ]
Marini, Francesca [1 ]
Sancineto, Luca [1 ]
Santi, Claudio [1 ]
机构
[1] Univ Perugia, Dept Pharmaceut Sci, Grp Catalysis Synth & Organ Green Chem, Via Liceo 1, I-06100 Perugia, Italy
关键词
fluorine; chlorine; halogens; FDA; drugs; INHIBITOR; DISCOVERY; FLUORINE; POTENT; EFFICIENT;
D O I
10.3390/molecules27051643
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
This review describes the recent Food and Drug Administration (FDA)-approved drugs (in the year 2021) containing at least one halogen atom (covalently bound). The structures proposed throughout this work are grouped according to their therapeutical use. Their synthesis is presented as well. The number of halogenated molecules that are reaching the market is regularly preserved, and 14 of the 50 molecules approved by the FDA in the last year contain halogens. This underlines the emergent role of halogens and, in particular, of fluorine and chlorine in the preparation of drugs for the treatment of several diseases such as viral infections, several types of cancer, cardiovascular disease, multiple sclerosis, migraine and inflammatory diseases such as vasculitis.
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页数:23
相关论文
共 78 条
[1]  
Abele S., 2008, New Process for the Preparation of 2-Imino-Thiazolidin-4-One Derivatives, Patent No. [WO-2008062376-A3, 2008062376]
[2]   Tackling Antibiotic Resistance with Compounds of Natural Origin: A Comprehensive Review [J].
Alvarez-Martinez, Francisco Javier ;
Barrajon-Catalan, Enrique ;
Micol, Vicente .
BIOMEDICINES, 2020, 8 (10) :1-30
[3]  
[Anonymous], 2013, Retina
[4]  
[Anonymous], FOTIVDA
[5]   Synthesis and evaluation of technetium-99m-and rhenium-labeled inhibitors of the prostate-specific membrane antigen (PSMA) [J].
Banerjee, Sangeeta R. ;
Foss, Catherine A. ;
Castanares, Mark ;
Mease, Ronnie C. ;
Byun, Youngjoo ;
Fox, James J. ;
Hilton, John ;
Lupold, Shawn E. ;
Kozikowski, Alan P. ;
Pomper, Martin G. .
JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (15) :4504-4517
[6]  
Bell I.M., 2012, Piperidinone Carboxamide Azaindane Cgrp Receptor Antagonists, Patent No. [2012064910 A1, 2012064910, WO2012064910A1]
[7]   Use of fluorinated functionality in enzyme inhibitor development: Mechanistic and analytical advantages [J].
Berkowitz, David B. ;
Karukurichi, Kannan R. ;
de la Salud-Bea, Roberto ;
Nelson, David L. ;
McCune, Christopher D. .
JOURNAL OF FLUORINE CHEMISTRY, 2008, 129 (09) :731-742
[8]   2-Imino-thiazolidin-4-one Derivatives as Potent, Orally Active S1P1 Receptor Agonists [J].
Bolli, Martin H. ;
Abele, Stefan ;
Binkert, Christoph ;
Bravo, Roberto ;
Buchmann, Stephan ;
Bur, Daniel ;
Gatfield, John ;
Hess, Patrick ;
Kohl, Christopher ;
Mangold, Celine ;
Mathys, Boris ;
Menyhart, Katalin ;
Mueller, Claus ;
Nayler, Oliver ;
Scherz, Michael ;
Schmidt, Gunther ;
Sippel, Virginie ;
Steiner, Beat ;
Strasser, Daniel ;
Treiber, Alexander ;
Weller, Thomas .
JOURNAL OF MEDICINAL CHEMISTRY, 2010, 53 (10) :4198-4211
[9]  
Bombardieri M, 2020, CLIN EXP RHEUMATOL, V38, pS3
[10]   Manufacturing Process Development for Belzutifan, Part 2: A Continuous Flow Visible-Light-Induced Benzylic Bromination [J].
Bottecchia, Cecilia ;
Levesque, Francois ;
McMullen, Jonathan P. ;
Ji, Yining ;
Reibarkh, Mikhail ;
Peng, Feng ;
Tan, Lushi ;
Spencer, Glenn ;
Nappi, Jarod ;
Lehnherr, Dan ;
Narsimhan, Karthik ;
Wismer, Michael K. ;
Chen, Like ;
Lin, Yipeng ;
Dalby, Stephen M. .
ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2022, 26 (03) :516-524