Nine new fluorine-containing drugs have been approved by the US Food and Drug Administration(FDA)in 2021,which are presented in this review article.These small molecular drugs feature aromatic fluorine,trifluoromethyl...Nine new fluorine-containing drugs have been approved by the US Food and Drug Administration(FDA)in 2021,which are presented in this review article.These small molecular drugs feature aromatic fluorine,trifluoromethyl and chlorodifluoro groups.The therapeutic areas of these fluorine-containing drugs include multiple myeloma,lymphoma,HIV,chronic heart failure,chronic myeloid leukemia,(ANCA)-associated vasculitis,migraines,von Hippel-Lindau disease,and non-small cell lung cancer.The brief biological activities and the synthetic methods have been discussed in this review for each of these nine drugs.展开更多
Thirteen new fluorine-containing drugs,which have been granted approval by the US Food and Drug Administration(FDA)in 2020,are profiled in this review.Therapeutic areas of these new fluorinated pharmaceuticals include...Thirteen new fluorine-containing drugs,which have been granted approval by the US Food and Drug Administration(FDA)in 2020,are profiled in this review.Therapeutic areas of these new fluorinated pharmaceuticals include medicines and diagnostic agents for Cushing's disease,neurofibromatosis,migraine,Alzheimer's disease,myelodysplastic syndromes,hereditary angioedema attacks,and various cancers.Molecules of these approved drugs feature aromatic fluorine(Ar-F)(11 compounds),aromatic Ar-CF_(3)(1),aliphatic CHF(1)and CF_(2)(1)groups.For each compound,we provide a spectrum of biological activity,medicinal chemistry discovery,and synthetic approaches.展开更多
基金the financial support from the National Natural Science Foundation of China(No.21761132021)the Qing-Lan Project of Jiangsu Province(for Han)IKERBASQUE,Basque Foundation for Science(for Soloshonok)。
文摘Nine new fluorine-containing drugs have been approved by the US Food and Drug Administration(FDA)in 2021,which are presented in this review article.These small molecular drugs feature aromatic fluorine,trifluoromethyl and chlorodifluoro groups.The therapeutic areas of these fluorine-containing drugs include multiple myeloma,lymphoma,HIV,chronic heart failure,chronic myeloid leukemia,(ANCA)-associated vasculitis,migraines,von Hippel-Lindau disease,and non-small cell lung cancer.The brief biological activities and the synthetic methods have been discussed in this review for each of these nine drugs.
基金the financial support from the National Natural Science Foundation of China(No.21761132021)IKERBASQUE,Basque Foundation for Science.
文摘Thirteen new fluorine-containing drugs,which have been granted approval by the US Food and Drug Administration(FDA)in 2020,are profiled in this review.Therapeutic areas of these new fluorinated pharmaceuticals include medicines and diagnostic agents for Cushing's disease,neurofibromatosis,migraine,Alzheimer's disease,myelodysplastic syndromes,hereditary angioedema attacks,and various cancers.Molecules of these approved drugs feature aromatic fluorine(Ar-F)(11 compounds),aromatic Ar-CF_(3)(1),aliphatic CHF(1)and CF_(2)(1)groups.For each compound,we provide a spectrum of biological activity,medicinal chemistry discovery,and synthetic approaches.