{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,10]],"date-time":"2026-09-10T20:02:50Z","timestamp":1789070570125,"version":"build-2803163510"},"reference-count":238,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2020,11,1]],"date-time":"2020-11-01T00:00:00Z","timestamp":1604188800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2020,11,1]],"date-time":"2020-11-01T00:00:00Z","timestamp":1604188800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"}],"funder":[{"DOI":"10.13039\/501100002858","name":"China Postdoctoral Science Foundation","doi-asserted-by":"publisher","award":["2018M630840"],"award-info":[{"award-number":["2018M630840"]}],"id":[{"id":"10.13039\/501100002858","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100002858","name":"China Postdoctoral Science Foundation","doi-asserted-by":"publisher","award":["2019T120641"],"award-info":[{"award-number":["2019T120641"]}],"id":[{"id":"10.13039\/501100002858","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000038","name":"U.S. Food and Drug Administration","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100000038","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81973177"],"award-info":[{"award-number":["81973177"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81703326"],"award-info":[{"award-number":["81703326"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2020,11]]},"DOI":"10.1016\/j.ejmech.2020.112667","type":"journal-article","created":{"date-parts":[[2020,7,28]],"date-time":"2020-07-28T21:09:35Z","timestamp":1595970575000},"page":"112667","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":62,"special_numbering":"C","title":["New drug approvals for 2019: Synthesis and clinical applications"],"prefix":"10.1016","volume":"205","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-4273-5625","authenticated-orcid":false,"given":"Shuo","family":"Yuan","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7207-643X","authenticated-orcid":false,"given":"Bin","family":"Yu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hong-Min","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.ejmech.2020.112667_bib1","doi-asserted-by":"crossref","first-page":"79","DOI":"10.1038\/d41573-020-00001-7","article-title":"FDA drug approvals","volume":"19","author":"Mullard","year":"2020","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib2","doi-asserted-by":"crossref","first-page":"85","DOI":"10.1038\/d41573-019-00014-x","article-title":"FDA drug approvals","volume":"18","author":"Mullard","year":"2019","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib3","doi-asserted-by":"crossref","first-page":"85","DOI":"10.1038\/d41573-020-00002-6","article-title":"Value of 2019 FDA approvals: back to the recent average","volume":"19","author":"Baedeker","year":"2020","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib4","doi-asserted-by":"crossref","first-page":"329","DOI":"10.1038\/d41573-019-00070-3","article-title":"FDA new drug approvals in Q1 2019","volume":"18","author":"Urquhart","year":"2019","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib5","doi-asserted-by":"crossref","first-page":"575","DOI":"10.1038\/d41573-019-00121-9","article-title":"FDA new drug approvals in Q2 2019","volume":"18","author":"Urquhart","year":"2019","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib6","doi-asserted-by":"crossref","first-page":"816","DOI":"10.1038\/d41573-019-00177-7","article-title":"FDA new drug approvals in Q3 2019","volume":"18","author":"Urquhart","year":"2019","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib7","doi-asserted-by":"crossref","first-page":"745","DOI":"10.3390\/molecules25030745","article-title":"The pharmaceutical industry in 2019. An analysis of FDA drug approvals from the perspective of molecules","volume":"25","author":"Torre","year":"2020","journal-title":"Molecules"},{"key":"10.1016\/j.ejmech.2020.112667_bib8","doi-asserted-by":"crossref","first-page":"130","DOI":"10.1038\/s41571-020-0336-8","article-title":"Approvals in 2019: international review and a new agnostic molecular entity","volume":"17","author":"Singh","year":"2020","journal-title":"Nat. Rev. Clin. Oncol."},{"key":"10.1016\/j.ejmech.2020.112667_bib9","doi-asserted-by":"crossref","first-page":"3463","DOI":"10.1021\/jm040031v","article-title":"Fragment-based drug discovery","volume":"47","author":"Erlanson","year":"2004","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib10","doi-asserted-by":"crossref","first-page":"1415","DOI":"10.1021\/acs.jmedchem.7b00404","article-title":"Fragment-based drug discovery of phosphodiesterase inhibitors","volume":"61","author":"Svensson","year":"2018","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib11","doi-asserted-by":"crossref","first-page":"6276","DOI":"10.1021\/acs.jmedchem.9b00917","article-title":"Designing around structural alerts in drug discovery","volume":"63","author":"Kalgutkar","year":"2020","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib12","doi-asserted-by":"crossref","first-page":"187","DOI":"10.1038\/nchem.217","article-title":"The rise of fragment-based drug discovery","volume":"1","author":"Murray","year":"2009","journal-title":"Nat. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib13","doi-asserted-by":"crossref","first-page":"660","DOI":"10.1038\/nrd1467","article-title":"Fragment-based lead discovery","volume":"3","author":"Rees","year":"2004","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib14","doi-asserted-by":"crossref","first-page":"538","DOI":"10.1093\/cid\/ciz826","article-title":"Cefiderocol: discovery, chemistry, and in\u00a0vivo profiles of a novel siderophore cephalosporin","volume":"69","author":"Sato","year":"2019","journal-title":"Clin. Infect. Dis."},{"key":"10.1016\/j.ejmech.2020.112667_bib15","doi-asserted-by":"crossref","first-page":"552","DOI":"10.1093\/cid\/ciz828","article-title":"Pharmacokinetic and pharmacodynamic profiles of cefiderocol, a novel siderophore cephalosporin","volume":"69","author":"Katsube","year":"2019","journal-title":"Clin. Infect. Dis."},{"key":"10.1016\/j.ejmech.2020.112667_bib16","doi-asserted-by":"crossref","first-page":"519","DOI":"10.1093\/cid\/ciz823","article-title":"Cefiderocol: a novel siderophore cephalosporin defeating carbapenem-resistant pathogens","volume":"69","author":"Bonomo","year":"2019","journal-title":"Clin. Infect. Dis."},{"key":"10.1016\/j.ejmech.2020.112667_bib17","series-title":"Cephalosporin Having Catechol Group","author":"Yasuhiro","year":"2009"},{"key":"10.1016\/j.ejmech.2020.112667_bib18","first-page":"1246","article-title":"New antibiotic for community-acquired pneumonia","volume":"322","author":"Voelker","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib19","doi-asserted-by":"crossref","first-page":"1661","DOI":"10.1001\/jama.2019.15468","article-title":"Oral lefamulin vs moxifloxacin for early clinical response among adults with community-acquired bacterial pneumonia: the LEAP 2 randomized clinical trial","volume":"322","author":"Alexander","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib20","doi-asserted-by":"crossref","first-page":"1856","DOI":"10.1093\/cid\/ciz090","article-title":"Efficacy and safety of intravenous-to-oral lefamulin, a pleuromutilin antibiotic, for the treatment of community-acquired bacterial pneumonia: the phase III lefamulin evaluation against pneumonia (LEAP 1) trial","volume":"69","author":"File","year":"2019","journal-title":"Clin. Infect. Dis."},{"key":"10.1016\/j.ejmech.2020.112667_bib21","series-title":"Process for the Preparation of Pleuromutilins in Crystalline Form","author":"Riedl","year":"2011"},{"key":"10.1016\/j.ejmech.2020.112667_bib22","doi-asserted-by":"crossref","first-page":"126969","DOI":"10.1016\/j.bmcl.2020.126969","article-title":"Design, synthesis, and biological activity evaluation of a series of pleuromutilin derivatives with novel C14 side chains","volume":"30","author":"Li","year":"2020","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2020.112667_bib23","doi-asserted-by":"crossref","first-page":"1011","DOI":"10.1016\/S2213-2600(19)30376-5","article-title":"Breakthrough in the treatment of drug-resistant tuberculosis","volume":"7","author":"Mushtaq","year":"2019","journal-title":"Lancet Respir. Med."},{"key":"10.1016\/j.ejmech.2020.112667_bib24","doi-asserted-by":"crossref","first-page":"263","DOI":"10.1002\/med.21602","article-title":"An overview of new antitubercular drugs, drug candidates, and their targets","volume":"40","author":"Bahuguna","year":"2020","journal-title":"Med. Res. Rev."},{"key":"10.1016\/j.ejmech.2020.112667_bib25","doi-asserted-by":"crossref","first-page":"172","DOI":"10.1016\/j.chembiol.2019.10.010","article-title":"Antitubercular triazines: optimization and intrabacterial metabolism","volume":"27","author":"Wang","year":"2020","journal-title":"Cell Chem. Biol."},{"key":"10.1016\/j.ejmech.2020.112667_bib26","doi-asserted-by":"crossref","first-page":"2329","DOI":"10.1021\/acs.jmedchem.7b01581","article-title":"Development of (6R)-2-nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (DNDI-8219): a new lead for visceral leishmaniasis","volume":"61","author":"Thompson","year":"2018","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib27","doi-asserted-by":"crossref","first-page":"637","DOI":"10.1021\/jm801087e","article-title":"Synthesis, reduction potentials, and antitubercular activity of ring A\/B analogues of the bioreductive drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)","volume":"52","author":"Thompson","year":"2009","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib28","doi-asserted-by":"crossref","first-page":"6563","DOI":"10.1021\/jm200377r","article-title":"Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1, 3]oxazine (PA-824)","volume":"54","author":"Thompson","year":"2011","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib29","doi-asserted-by":"crossref","first-page":"5639","DOI":"10.1021\/jm1010644","article-title":"Structure-activity relationships of antitubercular nitroimidazoles. 3. Exploration of the linker and lipophilic tail of ((s)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybe nzyl)amine (6-amino PA-824)","volume":"54","author":"Cherian","year":"2011","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib30","doi-asserted-by":"crossref","first-page":"2256","DOI":"10.1016\/j.bmcl.2008.03.011","article-title":"Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo [2,1-b][1,3]oxazines, analogues of PA-824","volume":"18","author":"Li","year":"2008","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2020.112667_bib31","doi-asserted-by":"crossref","first-page":"1275","DOI":"10.1021\/acsmedchemlett.7b00356","article-title":"Antitubercular nitroimidazoles revisited: synthesis and activity of the authentic 3-nitro isomer of pretomanid","volume":"8","author":"Thompson","year":"2017","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2020.112667_bib32","series-title":"Synthesis Method of PA-824 (Pretomanid) for Treating Tuberculosis","author":"Miao","year":"2018"},{"key":"10.1016\/j.ejmech.2020.112667_bib33","doi-asserted-by":"crossref","first-page":"565","DOI":"10.1093\/cid\/ciz830","article-title":"Treatment options for carbapenem-resistant gram-negative bacterial infections","volume":"69","author":"Doi","year":"2019","journal-title":"Clin. Infect. Dis."},{"key":"10.1016\/j.ejmech.2020.112667_bib34","first-page":"807","article-title":"New antibacterial should be used with caution","volume":"322","author":"Voelker","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib35","doi-asserted-by":"crossref","first-page":"1154","DOI":"10.1016\/j.cmi.2019.01.003","article-title":"A\u00a0novel framework to compare the effectiveness of beta-lactamase inhibitors against extended-spectrum beta-lactamase-producing enterobacteriaceae","volume":"25","author":"Abodakpi","year":"2019","journal-title":"Clin. Microbiol. Infect."},{"key":"10.1016\/j.ejmech.2020.112667_bib36","doi-asserted-by":"crossref","first-page":"928","DOI":"10.1038\/s41598-020-57844-8","article-title":"Effect of amoxicillin in combination with imipenem-relebactam against mycobacterium abscessus","volume":"10","author":"Lopeman","year":"2020","journal-title":"Sci. Rep."},{"key":"10.1016\/j.ejmech.2020.112667_bib37","doi-asserted-by":"crossref","first-page":"994","DOI":"10.1021\/acs.joc.9b02948","article-title":"Diastereoselective FeCl3.6H2O\/NaBH4 reduction of oxime ether for the synthesis of beta-lactamase inhibitor relebactam","volume":"85","author":"Chung","year":"2020","journal-title":"J.\u00a0Org. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib38","doi-asserted-by":"crossref","first-page":"5480","DOI":"10.1021\/ol202195n","article-title":"A\u00a0concise synthesis of a \u03b2-lactamase inhibitor","volume":"13","author":"Mangion","year":"2011","journal-title":"Org. Lett."},{"key":"10.1016\/j.ejmech.2020.112667_bib39","doi-asserted-by":"crossref","first-page":"11792","DOI":"10.1021\/jo502319z","article-title":"N-Boc deprotection and isolation method for water-soluble zwitterionic compounds","volume":"79","author":"Liu","year":"2014","journal-title":"J.\u00a0Org. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib40","series-title":"Preparation of Tert-Butyl 4-((1R,2S,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-Carboxamido Piperidine-1-Carboxylate","author":"Miller","year":"2014"},{"key":"10.1016\/j.ejmech.2020.112667_bib41","doi-asserted-by":"crossref","first-page":"4223","DOI":"10.1021\/jm100226t","article-title":"Structure-activity relationship of an ozonide carboxylic acid (OZ78) against fasciola hepatica","volume":"53","author":"Zhao","year":"2010","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib42","doi-asserted-by":"crossref","first-page":"2587","DOI":"10.1038\/s41598-020-59460-y","article-title":"Novel and selective inactivators of triosephosphate isomerase with anti-trematode activity","volume":"10","author":"Ferraro","year":"2020","journal-title":"Sci. Rep."},{"key":"10.1016\/j.ejmech.2020.112667_bib43","doi-asserted-by":"crossref","first-page":"7779","DOI":"10.1371\/journal.pntd.0007779","article-title":"Evaluation of nitazoxanide treatment following triclabendazole failure in an outbreak of human fascioliasis in Upper Egypt","volume":"13","author":"Ramadan","year":"2019","journal-title":"PLoS Neglected Trop. Dis."},{"key":"10.1016\/j.ejmech.2020.112667_bib44","doi-asserted-by":"crossref","first-page":"458","DOI":"10.1016\/j.pt.2016.03.002","article-title":"Current threat of triclabendazole resistance in fasciola hepatica","volume":"32","author":"Kelley","year":"2016","journal-title":"Trends Parasitol."},{"key":"10.1016\/j.ejmech.2020.112667_bib45","series-title":"A\u00a0Method for Preparing Trichlorobendazole","author":"Li","year":"2009"},{"key":"10.1016\/j.ejmech.2020.112667_bib46","doi-asserted-by":"crossref","first-page":"670","DOI":"10.5897\/AJPP2016.4557","article-title":"Synthesis of 2-(benzylthio)benzimidazole, 2-[(benzimidazol-2-yl)methylthio]benzimidazole and structural analogues against haemoncus contortus","volume":"10","author":"Akpa","year":"2016","journal-title":"Afr. J. Pharm. Pharmacol."},{"key":"10.1016\/j.ejmech.2020.112667_bib47","doi-asserted-by":"crossref","first-page":"97","DOI":"10.1016\/j.jpba.2004.09.049","article-title":"Separation and characterization of synthetic impurities of triclabendazole by reversed-phase high-performance liquid chromatography\/electrospray ionization mass spectrometry","volume":"37","author":"Zhou","year":"2005","journal-title":"J.\u00a0Pharm. Biomed. Anal."},{"key":"10.1016\/j.ejmech.2020.112667_bib48","series-title":"A\u00a0Novel Method for the Preparation of Trichlorobendazole","author":"Shu","year":"2017"},{"key":"10.1016\/j.ejmech.2020.112667_bib49","first-page":"2274","article-title":"Drugs for heart disease with rare cause","volume":"321","author":"Sancar","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib50","doi-asserted-by":"crossref","first-page":"39","DOI":"10.1002\/ejhf.1695","article-title":"Emerging therapies in transthyretin amyloidosis - a new wave of hope after years of stagnancy?","volume":"22","author":"Muller","year":"2020","journal-title":"Eur. J. Heart Fail."},{"key":"10.1016\/j.ejmech.2020.112667_bib51","doi-asserted-by":"crossref","first-page":"185","DOI":"10.1038\/nrd3675","article-title":"Tafamidis","volume":"11","author":"Said","year":"2012","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib52","doi-asserted-by":"crossref","first-page":"1009","DOI":"10.1093\/eurheartj\/ehy697","article-title":"Tafamidis for transthyretin amyloid cardiomyopathy: the solution or just the beginning of the end?","volume":"40","author":"Falk","year":"2019","journal-title":"Eur. Heart J."},{"key":"10.1016\/j.ejmech.2020.112667_bib53","doi-asserted-by":"crossref","first-page":"8274","DOI":"10.1021\/acs.jmedchem.9b01037","article-title":"Binding of monovalent and bivalent ligands by transthyretin causes different short- and long-distance conformational changes","volume":"62","author":"Corazza","year":"2019","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib54","series-title":"Compositions and Methods for Stabilizing Transthyretin and Inhibiting Transthyretin Misfolding","author":"Kelly","year":"2004"},{"key":"10.1016\/j.ejmech.2020.112667_bib55","doi-asserted-by":"crossref","first-page":"7506","DOI":"10.1002\/ejoc.201901468","article-title":"Iodine promoted one-pot synthesis of 2-aryl benzoxazoles from amidoximes via oxidative cyclization and ring contraction","volume":"45","author":"Zhang","year":"2019","journal-title":"Eur. J. Org Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib56","series-title":"Preparation of Benzoxazolecarboxylate Compounds for the Treatment of Familial Amyloid Polyneuropathy","author":"Kandula","year":"2013"},{"key":"10.1016\/j.ejmech.2020.112667_bib57","series-title":"Compositions and Methods for the Treatment of Familial Amyloid Polyneuropathy","author":"Kandula","year":"2015"},{"key":"10.1016\/j.ejmech.2020.112667_bib58","doi-asserted-by":"crossref","first-page":"604","DOI":"10.1001\/jama.2019.11515","article-title":"Another option for hypoactive sexual desire","volume":"322","author":"Sancar","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib59","doi-asserted-by":"crossref","first-page":"1599","DOI":"10.1007\/s40265-019-01187-w","article-title":"Bremelanotide: first approval","volume":"79","author":"Dhillon","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib60","doi-asserted-by":"crossref","first-page":"1137","DOI":"10.2174\/156802607780906681","article-title":"Melanocortins in the treatment of male and female sexual dysfunction","volume":"7","author":"Shadiack","year":"2007","journal-title":"Curr. Top. Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib61","doi-asserted-by":"crossref","first-page":"899","DOI":"10.1097\/AOG.0000000000003500","article-title":"Bremelanotide for the treatment of hypoactive sexual desire disorder: two randomized phase 3 trials","volume":"134","author":"Kingsberg","year":"2019","journal-title":"Obstet. Gynecol."},{"key":"10.1016\/j.ejmech.2020.112667_bib62","doi-asserted-by":"crossref","first-page":"1065","DOI":"10.1016\/j.bmcl.2004.12.025","article-title":"Detection and control of aspartimide formation in the synthesis of cyclic peptides","volume":"15","author":"Flora","year":"2005","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2020.112667_bib63","series-title":"Solid Phase Synthesis of Bremelanotide","author":"Yang","year":"2010"},{"key":"10.1016\/j.ejmech.2020.112667_bib64","series-title":"A\u00a0Synthetic Method for Bremelanotide","author":"Yan","year":"2017"},{"key":"10.1016\/j.ejmech.2020.112667_bib65","series-title":"Compositions and Methods for Treatment of Sexual Dysfunction","author":"Blood","year":"2004"},{"key":"10.1016\/j.ejmech.2020.112667_bib66","doi-asserted-by":"crossref","first-page":"779","DOI":"10.1007\/s40265-019-01121-0","article-title":"Brexanolone: first global approval","volume":"79","author":"Scott","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib67","doi-asserted-by":"crossref","first-page":"975","DOI":"10.1016\/S2215-0366(19)30292-5","article-title":"US food and drug administration approval of esketamine and brexanolone","volume":"6","author":"Cristea","year":"2019","journal-title":"Lancet Psychiat."},{"key":"10.1016\/j.ejmech.2020.112667_bib68","doi-asserted-by":"crossref","first-page":"7810","DOI":"10.1021\/acs.jmedchem.7b00846","article-title":"Neuroactive Steroids. 2. 3\u03b1-hydroxy-3\u03b2-methyl-21-(4-cyano-1H-pyrazol-1\u2019-yl)-19-nor-5\u03b2-pregnan-20-one (SAGE-217): a clinical next generation neuroactive steroid positive allosteric modulator of the (\u03b3-aminobutyric acid)A Receptor","volume":"60","author":"Martinez Botella","year":"2017","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib69","doi-asserted-by":"crossref","first-page":"5979","DOI":"10.1021\/acs.jmedchem.8b01651","article-title":"Allosteric modalities for membrane-bound receptors: insights from drug hunting for brain diseases","volume":"62","author":"Coughlin","year":"2019","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib70","doi-asserted-by":"crossref","first-page":"107494","DOI":"10.1016\/j.pharmthera.2020.107494","article-title":"A\u00a0hypothesis of monoamine (5-HT) - glutamate\/GABA long neural circuit: aiming for fast-onset antidepressant discovery","volume":"208","author":"Li","year":"2020","journal-title":"Pharmacol. Ther."},{"key":"10.1016\/j.ejmech.2020.112667_bib71","doi-asserted-by":"crossref","first-page":"1058","DOI":"10.1016\/S0140-6736(18)31551-4","article-title":"Brexanolone injection in post-partum depression: two multicentre, double-blind, randomised, placebo-controlled, phase 3 trials","volume":"392","author":"Meltzer-Brody","year":"2018","journal-title":"Lancet"},{"key":"10.1016\/j.ejmech.2020.112667_bib72","doi-asserted-by":"crossref","first-page":"643","DOI":"10.1135\/cccc2008187","article-title":"Preparation of steroid sulfamates and their interaction with GABAA receptor","volume":"74","author":"Kapras","year":"2009","journal-title":"Collect. Czech Chem. Commun."},{"key":"10.1016\/j.ejmech.2020.112667_bib73","doi-asserted-by":"crossref","first-page":"5203","DOI":"10.1021\/jm050271q","article-title":"Novel 17\u00e2-substituted conformationally constrained neurosteroids that modulate GABAA receptors","volume":"48","author":"Souli","year":"2005","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib74","series-title":"Preparation of Steroid Analogues for Neuroprotection","author":"MacNevin","year":"2009"},{"key":"10.1016\/j.ejmech.2020.112667_bib75","doi-asserted-by":"crossref","first-page":"6012","DOI":"10.1021\/jm900712n","article-title":"Development and screening of water-soluble analogues of progesterone and allopregnanolone in models of brain injury","volume":"52","author":"MacNevin","year":"2009","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib76","doi-asserted-by":"crossref","first-page":"559","DOI":"10.1212\/WNL.0000000000007894","article-title":"Suppression of the photoparoxysmal response in photosensitive epilepsy with cenobamate (YKP3089)","volume":"93","author":"Kasteleijn-Nolst Trenite","year":"2019","journal-title":"Neurology"},{"key":"10.1016\/j.ejmech.2020.112667_bib77","doi-asserted-by":"crossref","first-page":"133","DOI":"10.1038\/s41582-019-0309-7","article-title":"Cenobamate for focal seizures - a game changer?","volume":"16","author":"French","year":"2020","journal-title":"Nat. Rev. Neurol."},{"key":"10.1016\/j.ejmech.2020.112667_bib78","first-page":"18","article-title":"Novel alternative for partial-onset seizures","volume":"323","author":"Voelker","year":"2020","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib79","series-title":"Preparation of Triazoles and Tetrazoles Containing Carbamoyl Group as Anticonvulsants","author":"Choi","year":"2005"},{"key":"10.1016\/j.ejmech.2020.112667_bib80","series-title":"Preparation of Carbamic Acid (R)-1-aryl-2-tetrazolyl-ethyl Esters","author":"Lim","year":"2010"},{"key":"10.1016\/j.ejmech.2020.112667_bib81","first-page":"1246","article-title":"Add-on drug approved for \u201coff\u201d episodes of Parkinson disease","volume":"322","author":"Voelker","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib82","doi-asserted-by":"crossref","first-page":"18018","DOI":"10.1038\/s41598-017-18339-1","article-title":"The effect of istradefylline for Parkinson\u2019s disease: a meta-analysis","volume":"7","author":"Sako","year":"2017","journal-title":"Sci. Rep."},{"key":"10.1016\/j.ejmech.2020.112667_bib83","doi-asserted-by":"crossref","first-page":"593","DOI":"10.1007\/s40265-019-01098-w","article-title":"Contemporary options for the management of motor complications in Parkinson\u2019s disease: updated clinical review","volume":"79","author":"Cabreira","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib84","doi-asserted-by":"crossref","first-page":"3427","DOI":"10.1016\/j.bmcl.2013.03.070","article-title":"Novel adenosine A2A receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A2A receptor antagonists for extending into extracellular space","volume":"23","author":"Jorg","year":"2013","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2020.112667_bib85","doi-asserted-by":"crossref","first-page":"4155","DOI":"10.1039\/c003382k","article-title":"An efficient route to xanthine based A2A adenosine receptor antagonists and functional derivatives","volume":"8","author":"Labeaume","year":"2010","journal-title":"Org. Biomol. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib86","first-page":"241","article-title":"Synthesis of antiparkinsonian agent istradefylline","volume":"41","author":"Li","year":"2010","journal-title":"Chin. J. Pharm."},{"key":"10.1016\/j.ejmech.2020.112667_bib87","doi-asserted-by":"crossref","first-page":"113644","DOI":"10.1016\/j.bcp.2019.113644","article-title":"The 5-hydroxytryptamine receptor 1F stimulates mitochondrial biogenesis and angiogenesis in endothelial cells","volume":"169","author":"Dupre","year":"2019","journal-title":"Biochem. Pharmacol."},{"key":"10.1016\/j.ejmech.2020.112667_bib88","doi-asserted-by":"crossref","first-page":"1989","DOI":"10.1007\/s40265-019-01225-7","article-title":"Lasmiditan: first approval","volume":"79","author":"Lamb","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib89","doi-asserted-by":"crossref","first-page":"4681","DOI":"10.1111\/bph.14832","article-title":"Characterization of binding, functional activity, and contractile responses of the selective 5-HT1F receptor agonist lasmiditan","volume":"176","author":"Rubio-Beltran","year":"2019","journal-title":"Br. J. Pharmacol."},{"key":"10.1016\/j.ejmech.2020.112667_bib90","doi-asserted-by":"crossref","first-page":"6600","DOI":"10.1021\/acs.jmedchem.9b01810","article-title":"Blocking the CGRP pathway for acute and preventive treatment of migraine: the evolution of success","volume":"63","author":"Dubowchik","year":"2020","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib91","doi-asserted-by":"crossref","first-page":"2222","DOI":"10.1212\/WNL.0000000000006641","article-title":"Lasmiditan is an effective acute treatment for migraine: a phase 3 randomized study","volume":"91","author":"Kuca","year":"2018","journal-title":"Neurology"},{"key":"10.1016\/j.ejmech.2020.112667_bib92","doi-asserted-by":"crossref","first-page":"1894","DOI":"10.1093\/brain\/awz134","article-title":"Phase 3 randomized, placebo-controlled, double-blind study of lasmiditan for acute treatment of migraine","volume":"142","author":"Goadsby","year":"2019","journal-title":"Brain"},{"key":"10.1016\/j.ejmech.2020.112667_bib93","series-title":"Preparation of Pyridinoylpiperidines as 5-HT1F Agonists","author":"Cohen","year":"2003"},{"key":"10.1016\/j.ejmech.2020.112667_bib94","doi-asserted-by":"crossref","first-page":"287","DOI":"10.1124\/jpet.117.241422","article-title":"In\u00a0vitro and in silico characterization of lemborexant (E2006), a novel dual orexin receptor antagonist","volume":"362","author":"Beuckmann","year":"2017","journal-title":"J.\u00a0Pharmacol. Exp. Ther."},{"key":"10.1016\/j.ejmech.2020.112667_bib95","doi-asserted-by":"crossref","first-page":"76","DOI":"10.1093\/sleep\/zsz076","article-title":"Preclinical in\u00a0vivo characterization of lemborexant (E2006), a novel dual orexin receptor antagonist for sleep\/wake regulation","volume":"42","author":"Beuckmann","year":"2019","journal-title":"Sleep"},{"key":"10.1016\/j.ejmech.2020.112667_bib96","doi-asserted-by":"crossref","first-page":"6371","DOI":"10.1021\/jm400772t","article-title":"Synthesis and evaluation of novel radioligands for positron emission tomography imaging of the orexin-2 receptor","volume":"56","author":"Oi","year":"2013","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib97","doi-asserted-by":"crossref","first-page":"260","DOI":"10.1093\/sleep\/zsy260","article-title":"On-the-road driving performance the morning after bedtime administration of lemborexant in healthy adult and elderly volunteers","volume":"42","author":"Vermeeren","year":"2019","journal-title":"Sleep"},{"key":"10.1016\/j.ejmech.2020.112667_bib98","doi-asserted-by":"crossref","first-page":"4648","DOI":"10.1021\/acs.jmedchem.5b00217","article-title":"Discovery of (1R,2S)-2-{[(2,4-dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): a potent and efficacious oral orexin receptor antagonist","volume":"58","author":"Yoshida","year":"2015","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib99","doi-asserted-by":"crossref","first-page":"598","DOI":"10.1038\/s41386-018-0251-1","article-title":"Dopamine D2 receptor occupancy of lumateperone (ITI-007): a positron emission tomography study in patients with schizophrenia","volume":"44","author":"Vanover","year":"2019","journal-title":"Neuropsychopharmacology"},{"key":"10.1016\/j.ejmech.2020.112667_bib100","doi-asserted-by":"crossref","first-page":"343","DOI":"10.1001\/jamapsychiatry.2019.4265","article-title":"The potential role of lumateperone-something borrowed? Something new?","volume":"77","author":"Kantrowitz","year":"2020","journal-title":"JAMA Psychiatr."},{"key":"10.1016\/j.ejmech.2020.112667_bib101","doi-asserted-by":"crossref","first-page":"349","DOI":"10.1001\/jamapsychiatry.2019.4379","article-title":"Efficacy and safety of lumateperone for treatment of schizophrenia: a randomized clinical trial","volume":"77","author":"Correll","year":"2020","journal-title":"JAMA Psychiatr."},{"key":"10.1016\/j.ejmech.2020.112667_bib102","series-title":"Process for Preparation of Heterocycle Fused \u03b3-carbolines","author":"Tomesch","year":"2008"},{"key":"10.1016\/j.ejmech.2020.112667_bib103","doi-asserted-by":"crossref","first-page":"2670","DOI":"10.1021\/jm401958n","article-title":"Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders","volume":"57","author":"Li","year":"2014","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib104","series-title":"Method for the Manufacture of Lumateperone and its Salts","author":"Berecz","year":"2019"},{"key":"10.1016\/j.ejmech.2020.112667_bib105","series-title":"Substituted Heterocycle Fused \u03b3-carbolines Solid","author":"Tomesch","year":"2011"},{"key":"10.1016\/j.ejmech.2020.112667_bib106","doi-asserted-by":"crossref","first-page":"10375","DOI":"10.1021\/acs.jmedchem.8b00407","article-title":"Lead-like drugs: a perspective","volume":"61","author":"Raymer","year":"2018","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib107","doi-asserted-by":"crossref","first-page":"252","DOI":"10.1093\/sleep\/zsz252","article-title":"Evaluation of the abuse potential of pitolisant, a selective H3-receptor antagonist\/inverse agonist, for the treatment of adult patients with narcolepsy with or without cataplexy","volume":"43","author":"Setnik","year":"2019","journal-title":"Sleep"},{"key":"10.1016\/j.ejmech.2020.112667_bib108","doi-asserted-by":"crossref","first-page":"23","DOI":"10.1016\/j.smrv.2018.09.006","article-title":"Neurobiological and immunogenetic aspects of narcolepsy: implications for pharmacotherapy","volume":"43","author":"Szabo","year":"2019","journal-title":"Sleep Med. Rev."},{"key":"10.1016\/j.ejmech.2020.112667_bib109","doi-asserted-by":"crossref","first-page":"174","DOI":"10.1093\/sleep\/zsz174","article-title":"Long-term use of pitolisant to treat patients with narcolepsy: Harmony III Study","volume":"42","author":"Dauvilliers","year":"2019","journal-title":"Sleep"},{"key":"10.1016\/j.ejmech.2020.112667_bib110","series-title":"Preparation Method of 1-(3-(3-(4-chlorphenyl) Propoxy) Propyl) Piperidine Hydrochloride","author":"Li","year":"2013"},{"key":"10.1016\/j.ejmech.2020.112667_bib111","series-title":"Preparation Method of 1-(3-(3-(4-chlorphenyl) Propoxy) Propyl) Piperidine Hydrochloride","author":"Hu","year":"2014"},{"key":"10.1016\/j.ejmech.2020.112667_bib112","first-page":"111","article-title":"Synthesis of pitolisant as a histamine H3 receptor antagonist\/invers","volume":"23","author":"Qu","year":"2013","journal-title":"Chin. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib113","doi-asserted-by":"crossref","first-page":"1009","DOI":"10.1007\/s40265-019-01140-x","article-title":"Siponimod: first global approval","volume":"79","author":"Al-Salama","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib114","doi-asserted-by":"crossref","first-page":"196","DOI":"10.1016\/S1474-4422(19)30487-9","article-title":"Feast or famine in multiple sclerosis therapeutics","volume":"19","author":"Fox","year":"2020","journal-title":"Lancet Neurol."},{"key":"10.1016\/j.ejmech.2020.112667_bib115","doi-asserted-by":"crossref","first-page":"336","DOI":"10.1016\/S1474-4422(19)30391-6","article-title":"Advances in oral immunomodulating therapies in relapsing multiple sclerosis","volume":"19","author":"Derfuss","year":"2020","journal-title":"Lancet Neurol."},{"key":"10.1016\/j.ejmech.2020.112667_bib116","doi-asserted-by":"crossref","first-page":"1440","DOI":"10.1016\/j.cell.2019.11.034","article-title":"Siponimod chips away at progressive MS","volume":"179","author":"Longbrake","year":"2019","journal-title":"Cell"},{"key":"10.1016\/j.ejmech.2020.112667_bib117","doi-asserted-by":"crossref","first-page":"24","DOI":"10.3390\/cells8010024","article-title":"Mechanism of siponimod: anti-inflammatory and neuroprotective mode of action","volume":"8","author":"Behrangi","year":"2019","journal-title":"Cells"},{"key":"10.1016\/j.ejmech.2020.112667_bib118","doi-asserted-by":"crossref","first-page":"1263","DOI":"10.1016\/S0140-6736(18)30475-6","article-title":"Siponimod versus placebo insecondary progressive multiple sclerosis (EXPAND): a double-blind, randomised, phase 3 study","volume":"391","author":"Kappos","year":"2018","journal-title":"Lancet"},{"key":"10.1016\/j.ejmech.2020.112667_bib119","doi-asserted-by":"crossref","first-page":"2069","DOI":"10.1001\/jama.2018.6256","article-title":"Drug slows disability progression in multiple sclerosis","volume":"319","author":"Slomsk","year":"2018","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib120","doi-asserted-by":"crossref","first-page":"333","DOI":"10.1021\/ml300396r","article-title":"Discovery of BAF312 (siponimod), a potent and selective S1P receptor modulator","volume":"4","author":"Pan","year":"2013","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2020.112667_bib121","series-title":"Compounds for the Treatment of Peripheral Neuropathies","author":"Leppert","year":"2010"},{"key":"10.1016\/j.ejmech.2020.112667_bib122","series-title":"New polymorphic form of 1- (4-{l-[(e)-4-cyclohexyl-3-trifluoromethyl benzyloxyimino]-ethyl)-2-ethyl-benzyl)-azetidine-3-carboxylic","author":"Liu","year":"2010"},{"key":"10.1016\/j.ejmech.2020.112667_bib123","series-title":"Process for Preparing N-(4-Cyclohexyl-3-Trifluoromethyl-Benzyloxy)-Acetimidic Acid Ethyl Ester","author":"Gallou","year":"2013"},{"key":"10.1016\/j.ejmech.2020.112667_bib124","doi-asserted-by":"crossref","first-page":"364","DOI":"10.1016\/j.chest.2018.11.005","article-title":"Solriamfetol for the treatment of excessive sleepiness in OSA: a placebo-controlled randomized withdrawal study","volume":"155","author":"Strollo","year":"2019","journal-title":"Chest"},{"key":"10.1016\/j.ejmech.2020.112667_bib125","doi-asserted-by":"crossref","first-page":"785","DOI":"10.1007\/s40265-019-01123-y","article-title":"Solriamfetol: first global approval","volume":"79","author":"Markham","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib126","doi-asserted-by":"crossref","first-page":"220","DOI":"10.1093\/sleep\/zsz220","article-title":"Long-term study of the safety and maintenance of efficacy of solriamfetol (JZP-110) in the treatment of excessive sleepiness in participants with narcolepsy or obstructive sleep apnea","volume":"43","author":"Malhotra","year":"2020","journal-title":"Sleep"},{"key":"10.1016\/j.ejmech.2020.112667_bib127","doi-asserted-by":"crossref","first-page":"359","DOI":"10.1002\/ana.25423","article-title":"A\u00a0randomized study of solriamfetol for excessive sleepiness in narcolepsy","volume":"85","author":"Thorpy","year":"2019","journal-title":"Ann. Neurol."},{"key":"10.1016\/j.ejmech.2020.112667_bib128","doi-asserted-by":"crossref","first-page":"1421","DOI":"10.1164\/rccm.201806-1100OC","article-title":"Solriamfetol for excessive sleepiness in obstructive sleep apnea (TONES 3). A randomized controlled trial","volume":"199","author":"Schweitzer","year":"2019","journal-title":"Am. J. Respir. Crit. Care Med."},{"key":"10.1016\/j.ejmech.2020.112667_bib129","series-title":"Process of Preparing O-Carbamoyl Compounds in the Presence of Active Amine Group","author":"Choi","year":"2005"},{"key":"10.1016\/j.ejmech.2020.112667_bib130","doi-asserted-by":"crossref","first-page":"2230","DOI":"10.1056\/NEJMoa1813049","article-title":"Ubrogepant for the treatment of migraine","volume":"381","author":"Dodick","year":"2019","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2020.112667_bib131","doi-asserted-by":"crossref","first-page":"338","DOI":"10.1038\/s41582-018-0003-1","article-title":"CGRP as the target of new migraine therapies - successful translation from bench to clinic","volume":"14","author":"Edvinsson","year":"2018","journal-title":"Nat. Rev. Neurol."},{"key":"10.1016\/j.ejmech.2020.112667_bib132","first-page":"408","article-title":"New migraine drug gains approval","volume":"323","author":"Voelker","year":"2020","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib133","series-title":"Piperidinone Carboxamide Azaindane CGRP Receptor Antagonists","author":"Bell","year":"2012"},{"key":"10.1016\/j.ejmech.2020.112667_bib134","series-title":"Process for Making CGRP Receptor Antagonists","author":"Belyk","year":"2013"},{"key":"10.1016\/j.ejmech.2020.112667_bib135","doi-asserted-by":"crossref","first-page":"48","DOI":"10.1056\/NEJMoa1411481","article-title":"Afamelanotide for erythropoietic protoporphyria","volume":"373","author":"Langendonk","year":"2015","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2020.112667_bib136","doi-asserted-by":"crossref","first-page":"68","DOI":"10.1001\/2013.jamadermatol.386","article-title":"The efficacy of afamelanotide and narrowband UV-B phototherapy for repigmentation of vitiligo","volume":"149","author":"Grimes","year":"2013","journal-title":"JAMA Dermatol."},{"key":"10.1016\/j.ejmech.2020.112667_bib137","doi-asserted-by":"crossref","first-page":"9320","DOI":"10.1021\/acs.jmedchem.7b01295","article-title":"Design of MC1R selective \u03b3-MSH analogues with canonical amino acids leads to potency and pigmentation","volume":"60","author":"Zhou","year":"2017","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib138","doi-asserted-by":"crossref","first-page":"42","DOI":"10.1001\/jamadermatol.2014.1875","article-title":"Afamelanotide and narrowband UV-B phototherapy for the treatment of vitiligo: a randomized multicenter trial","volume":"151","author":"Lim","year":"2015","journal-title":"JAMA Dermatol."},{"key":"10.1016\/j.ejmech.2020.112667_bib139","first-page":"1854","article-title":"First treatment for rare photosensitivity","volume":"322","author":"Sancar","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib140","series-title":"Aromatic Amides Absorbing the u.V","author":"Robert","year":"1987"},{"key":"10.1016\/j.ejmech.2020.112667_bib141","doi-asserted-by":"crossref","first-page":"144","DOI":"10.1021\/acs.jmedchem.8b00238","article-title":"Developing a biased unmatched bivalent ligand (BUmBL) design strategy to target the GPCR homodimer allosteric signaling (cAMP over \u03b2-arrestin 2 recruitment) within the melanocortin receptors","volume":"62","author":"Lensing","year":"2019","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib142","doi-asserted-by":"crossref","first-page":"1905","DOI":"10.1007\/s40265-019-01218-6","article-title":"Trifarotene: first approval","volume":"79","author":"Scott","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib143","doi-asserted-by":"crossref","first-page":"1736","DOI":"10.1016\/j.bmcl.2018.04.036","article-title":"Structure-based design of trifarotene (CD5789), a potent and selective RAR\u03b3 agonist for the treatment of acne","volume":"28","author":"Thoreau","year":"2018","journal-title":"Bioorg. Med. Chem. Lett"},{"key":"10.1016\/j.ejmech.2020.112667_bib144","doi-asserted-by":"crossref","first-page":"1691","DOI":"10.1016\/j.jaad.2019.02.044","article-title":"Randomized phase 3 evaluation of trifarotene 50 \u03bcg\/g cream treatment of moderate facial and truncal acne","volume":"80","author":"Tan","year":"2019","journal-title":"J.\u00a0Am. Acad. Dermatol."},{"key":"10.1016\/j.ejmech.2020.112667_bib145","series-title":"Novel Ligands that Modulate Rar Receptors, and Use Thereof in Human Medicine and in Cosmetics","author":"Biadatti","year":"2006"},{"key":"10.1016\/j.ejmech.2020.112667_bib146","doi-asserted-by":"crossref","first-page":"1753","DOI":"10.1053\/j.gastro.2018.08.021","article-title":"Efficacy of secretagogues in patients with irritable bowel syndrome with constipation: systematic review and network meta-analysis","volume":"155","author":"Black","year":"2018","journal-title":"Gastroenterology"},{"key":"10.1016\/j.ejmech.2020.112667_bib147","doi-asserted-by":"crossref","first-page":"1897","DOI":"10.1007\/s40265-019-01215-9","article-title":"Tenapanor: first approval","volume":"79","author":"Markham","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib148","doi-asserted-by":"crossref","first-page":"281","DOI":"10.14309\/ajg.0000000000000516","article-title":"Efficacy of tenapanor in treating patients with irritable bowel syndrome with constipation: a 12-week, placebo-controlled phase 3 trial (T3MPO-1)","volume":"115","author":"Chey","year":"2020","journal-title":"Am. J. Gastroenterol."},{"key":"10.1016\/j.ejmech.2020.112667_bib149","doi-asserted-by":"crossref","first-page":"1171","DOI":"10.1007\/s40265-018-0950-2","article-title":"Targeting gastrointestinal transport proteins to control hyperphosphatemia in chronic kidney disease","volume":"78","author":"Fouque","year":"2018","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib150","doi-asserted-by":"crossref","first-page":"1933","DOI":"10.1681\/ASN.2016080855","article-title":"Effect of tenapanor on serum phosphate in patients receiving hemodialysis","volume":"28","author":"Block","year":"2017","journal-title":"J.\u00a0Am. Soc. Nephrol."},{"key":"10.1016\/j.ejmech.2020.112667_bib151","series-title":"Solid Forms of Tenapanor and Method of Preparation of Tenapanor","author":"Richter","year":"2019"},{"key":"10.1016\/j.ejmech.2020.112667_bib152","doi-asserted-by":"crossref","first-page":"579","DOI":"10.1097\/MIB.0000000000000314","article-title":"Ferric maltol is effective in correcting iron deficiency anemia in patients with inflammatory bowel disease: results from a phase-3 clinical trial program","volume":"21","author":"Gasche","year":"2015","journal-title":"Inflamm. Bowel Dis."},{"key":"10.1016\/j.ejmech.2020.112667_bib153","doi-asserted-by":"crossref","first-page":"558","DOI":"10.1093\/ecco-jcc\/jjz203.813","article-title":"P685 healthcare resource use associated with ferric maltol and IV iron treatment for iron deficiency anaemia in patients with inflammatory bowel disease","volume":"14","author":"Howaldt","year":"2020","journal-title":"J.\u00a0Crohn\u2019s. Colitis."},{"key":"10.1016\/j.ejmech.2020.112667_bib154","doi-asserted-by":"crossref","first-page":"259","DOI":"10.1111\/apt.13665","article-title":"Ferric maltol therapy for iron deficiency anaemia in patients with inflammatory bowel disease: long-term extension data from a phase 3 study","volume":"44","author":"Schmidt","year":"2016","journal-title":"Aliment. Pharmacol. Ther."},{"key":"10.1016\/j.ejmech.2020.112667_bib155","first-page":"448","article-title":"Synthesis and properties of metal chelates from natural \u03b3-pyrone maltol","volume":"15","author":"Mukha","year":"2007","journal-title":"Chem. Sustain. Dev."},{"key":"10.1016\/j.ejmech.2020.112667_bib156","series-title":"Methods for Producing Ferric Maltol Compositions from Ferrous Hydroxides","author":"Powell","year":"2017"},{"key":"10.1016\/j.ejmech.2020.112667_bib157","series-title":"Crystalline Forms of Ferric Maltol","author":"Childs","year":"2016"},{"key":"10.1016\/j.ejmech.2020.112667_bib158","doi-asserted-by":"crossref","first-page":"1865","DOI":"10.1182\/blood-2018-08-868893","article-title":"A\u00a0phase 1\/2 ascending dose study and open-label extension study of voxelotor in patients with sickle cell disease","volume":"133","author":"Howard","year":"2019","journal-title":"Blood"},{"key":"10.1016\/j.ejmech.2020.112667_bib159","doi-asserted-by":"crossref","first-page":"1235","DOI":"10.1126\/science.365.6459.1235","article-title":"Sickle cell drug raises hopes and doubts","volume":"365","author":"Wadman","year":"2019","journal-title":"Science"},{"key":"10.1016\/j.ejmech.2020.112667_bib160","doi-asserted-by":"crossref","first-page":"1795","DOI":"10.1182\/blood-2019-03-900936","article-title":"Priority lane to cDC1 open for IRF8+ progenitors","volume":"133","author":"Guilliams","year":"2019","journal-title":"Blood"},{"key":"10.1016\/j.ejmech.2020.112667_bib161","doi-asserted-by":"crossref","first-page":"509","DOI":"10.1056\/NEJMoa1903212","article-title":"A\u00a0phase 3 randomized trial of voxelotor in sickle cell disease","volume":"381","author":"Vichinsky","year":"2019","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2020.112667_bib162","doi-asserted-by":"crossref","first-page":"321","DOI":"10.1021\/acsmedchemlett.6b00491","article-title":"Discovery of GBT440, an orally bioavailable R-state stabilizer of sickle cell hemoglobin","volume":"8","author":"Metcalf","year":"2017","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2020.112667_bib163","series-title":"Substituted Benzaldehyde Compounds and Methods for Their Use in Increasing Tissue Oxygenation","author":"Metcalf","year":"2013"},{"key":"10.1016\/j.ejmech.2020.112667_bib164","series-title":"Compounds and Uses Thereof for the Modulation of Hemoglobin","author":"Metcalf","year":"2014"},{"key":"10.1016\/j.ejmech.2020.112667_bib165","doi-asserted-by":"crossref","first-page":"2001","DOI":"10.1007\/s40265-019-01233-7","article-title":"Elexacaftor\/ivacaftor\/tezacaftor: first approval","volume":"79","author":"Hoy","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib166","doi-asserted-by":"crossref","first-page":"1809","DOI":"10.1056\/NEJMoa1908639","article-title":"Elexacaftor-tezacaftor-ivacaftor for cystic fibrosis with a single Phe508del allele","volume":"381","author":"Middleton","year":"2019","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2020.112667_bib167","doi-asserted-by":"crossref","first-page":"l6347","DOI":"10.1136\/bmj.l6347","article-title":"Cystic fibrosis: triple therapy shows promising results","volume":"367","author":"Mahase","year":"2019","journal-title":"Br. Med. J."},{"key":"10.1016\/j.ejmech.2020.112667_bib168","first-page":"2068","article-title":"Patients with cystic fibrosis have new triple-drug combination","volume":"322","author":"Voelker","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib169","series-title":"Methods of Treatment for Cyctic Fibrosis","author":"Haseltine","year":"2019"},{"key":"10.1016\/j.ejmech.2020.112667_bib170","series-title":"Modulator of Cystic Fibrosis Transmembrane Conductance Regulator, Pharmaceutical Compositions, Methods of Treatment, and Process for Making the Modulator","author":"Abela","year":"2018"},{"key":"10.1016\/j.ejmech.2020.112667_bib171","doi-asserted-by":"crossref","first-page":"1819","DOI":"10.1007\/s40265-019-01211-z","article-title":"Upadacitinib: first approval","volume":"79","author":"Duggan","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib172","doi-asserted-by":"crossref","first-page":"1788","DOI":"10.1002\/art.41032","article-title":"Upadacitinib versus placebo or adalimumab in patients with rheumatoid arthritis and an inadequate response to methotrexate: results of a phase III, double-blind, randomized controlled trial","volume":"71","author":"Fleischmann","year":"2019","journal-title":"Arthritis Rheum."},{"key":"10.1016\/j.ejmech.2020.112667_bib173","doi-asserted-by":"crossref","first-page":"2123","DOI":"10.1053\/j.gastro.2020.01.047","article-title":"Efficacy and safety of upadacitinib in a randomized trial of patients with crohn\u2019s disease","volume":"158","author":"Sandborn","year":"2020","journal-title":"Gastroenterology"},{"key":"10.1016\/j.ejmech.2020.112667_bib174","doi-asserted-by":"crossref","first-page":"1454","DOI":"10.1136\/annrheumdis-2019-215764","article-title":"Safety and effectiveness of upadacitinib or adalimumab plus methotrexate in patients with rheumatoid arthritis over 48 weeks with switch to alternate therapy in patients with insufficient response","volume":"78","author":"Fleischmann","year":"2019","journal-title":"Ann. Rheum. Dis."},{"key":"10.1016\/j.ejmech.2020.112667_bib175","series-title":"Novel Tricyclic Compounds","author":"Wishart","year":"2011"},{"key":"10.1016\/j.ejmech.2020.112667_bib176","series-title":"Processes for the Preparation of (3S,4R)-3-Ethyl-4-(3h-Imidazo[1,2-A]pyrrolo[2,3-E]-Pyrazin-8-Yl)-N-(2,2,2-Trifluoroethyl)pyrrolidine-1-Carboxamide and Solid State Forms Thereof for Disease Treatment","author":"Pangan","year":"2018"},{"key":"10.1016\/j.ejmech.2020.112667_bib177","doi-asserted-by":"crossref","first-page":"347","DOI":"10.1016\/S1470-2045(19)30372-9","article-title":"Alpelisib plus fulvestrant for PIK3CA-mutated breast cancer","volume":"20","author":"Stirrups","year":"2019","journal-title":"Lancet Oncol."},{"key":"10.1016\/j.ejmech.2020.112667_bib178","doi-asserted-by":"crossref","first-page":"1929","DOI":"10.1056\/NEJMoa1813904","article-title":"Alpelisib for PIK3CA-mutated, hormone receptor-positive advanced breast cancer","volume":"380","author":"Andre","year":"2019","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2020.112667_bib179","doi-asserted-by":"crossref","first-page":"1249","DOI":"10.1007\/s40265-019-01161-6","article-title":"Alpelisib: first global approval","volume":"79","author":"Markham","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib180","doi-asserted-by":"crossref","first-page":"1558","DOI":"10.1200\/JCO.19.00201","article-title":"Local consolidative therapy vs. maintenance therapy or observation for patients with oligometastatic non-small-cell lung cancer: long-term results of a multi-institutional, phase II, randomized study","volume":"37","author":"Gomez","year":"2019","journal-title":"J.\u00a0Clin. Oncol."},{"key":"10.1016\/j.ejmech.2020.112667_bib181","doi-asserted-by":"crossref","first-page":"4475","DOI":"10.1001\/jamaoncol.2018.4475","article-title":"Alpelisib plus fulvestrant in PIK3CA-altered and PIK3CA-wild-type estrogen receptor-positive advanced breast cancer: a phase 1b clinical trial","volume":"5","author":"Juric","year":"2019","journal-title":"JAMA Oncol."},{"key":"10.1016\/j.ejmech.2020.112667_bib182","doi-asserted-by":"crossref","first-page":"570","DOI":"10.1016\/S1470-2045(18)30905-7","article-title":"Olaparib and \u03b1-specific PI3K inhibitor alpelisib for patients with epithelial ovarian cancer: a dose-escalation and dose-expansion phase 1b trial","volume":"20","author":"Konstantinopoulos","year":"2019","journal-title":"Lancet Oncol."},{"key":"10.1016\/j.ejmech.2020.112667_bib183","doi-asserted-by":"crossref","first-page":"610","DOI":"10.1158\/2159-8290.CD-16-0795","article-title":"A\u00a0phase Ib dose-escalation study of encorafenib and cetuximab with or without alpelisib in metastatic BRAF-mutant colorectal cancer","volume":"7","author":"Geel","year":"2017","journal-title":"Cancer Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib184","series-title":"Thiazole Derivatives Used as PI3 Kinase Inhibitors","author":"Caravatti","year":"2009"},{"key":"10.1016\/j.ejmech.2020.112667_bib185","series-title":"Organic Compounds","author":"Caravatti","year":"2010"},{"key":"10.1016\/j.ejmech.2020.112667_bib186","doi-asserted-by":"crossref","first-page":"3741","DOI":"10.1016\/j.bmcl.2013.05.007","article-title":"Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase \u03b1 inhibitor selected for clinical evaluation","volume":"23","author":"Furet","year":"2013","journal-title":"Bioorg. Med. Chem. Lett"},{"key":"10.1016\/j.ejmech.2020.112667_bib187","doi-asserted-by":"crossref","first-page":"1813","DOI":"10.1007\/s40265-019-01212-y","article-title":"Darolutamide: first approval","volume":"79","author":"Markham","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib188","doi-asserted-by":"crossref","first-page":"1235","DOI":"10.1056\/NEJMoa1815671","article-title":"Darolutamide in nonmetastatic, castration-resistant prostate cancer","volume":"380","author":"Fizazi","year":"2019","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2020.112667_bib189","doi-asserted-by":"crossref","first-page":"111608","DOI":"10.1016\/j.ejmech.2019.111608","article-title":"Discovery and biological evaluation of darolutamide derivatives as inhibitors and down-regulators of wild-type AR and the mutants","volume":"182","author":"Yu","year":"2019","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib190","doi-asserted-by":"crossref","first-page":"335","DOI":"10.1038\/s41585-019-0186-2","article-title":"Enzalutamide, apalutamide, or darolutamide: are apples or bananas best for patients?","volume":"16","author":"Higano","year":"2019","journal-title":"Nat. Rev. Urol."},{"key":"10.1016\/j.ejmech.2020.112667_bib191","series-title":"Process for the Preparation of Androgen Receptor Antagonists and Intermediates Thereof","author":"Laitinen","year":"2016"},{"key":"10.1016\/j.ejmech.2020.112667_bib192","series-title":"Process and Intermediates for Preparation of Androgen Receptor Antagonist","author":"Pan","year":"2018"},{"key":"10.1016\/j.ejmech.2020.112667_bib193","series-title":"Androgen Receptor Modulating Carboxamides","author":"T\u00f6rm\u00e4kangas","year":"2012"},{"key":"10.1016\/j.ejmech.2020.112667_bib194","doi-asserted-by":"crossref","first-page":"1477","DOI":"10.1007\/s40265-019-01177-y","article-title":"Entrectinib: first global approval","volume":"79","author":"Al-Salama","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib195","doi-asserted-by":"crossref","first-page":"3604","DOI":"10.1038\/s41467-019-11496-z","article-title":"The new-generation selective ROS1\/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models","volume":"10","author":"Katayama","year":"2019","journal-title":"Nat. Commun."},{"key":"10.1016\/j.ejmech.2020.112667_bib196","doi-asserted-by":"crossref","first-page":"3392","DOI":"10.1021\/acs.jmedchem.6b00064","article-title":"Discovery of entrectinib: a new 3-aminoindazole as a potent anaplastic lymphoma kinase (ALK), c-ros oncogene 1 kinase (ROS1), and pan-tropomyosin receptor kinases (Pan-TRKs) inhibitor","volume":"59","author":"Menichincheri","year":"2016","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib197","doi-asserted-by":"crossref","first-page":"2563","DOI":"10.1038\/s41375-019-0576-8","article-title":"Revisiting NTRKs as an emerging oncogene in hematological malignancies","volume":"33","author":"Joshi","year":"2019","journal-title":"Leukemia"},{"key":"10.1016\/j.ejmech.2020.112667_bib198","series-title":"Indazole Compounds for Inhibiting Kinase Activity, Their Composition and Application in Field of Medical Technology","author":"Wang","year":"2018"},{"key":"10.1016\/j.ejmech.2020.112667_bib199","series-title":"Substituted Indazole Derivatives Active as Kinase Inhibitors","author":"Borgia","year":"2009"},{"key":"10.1016\/j.ejmech.2020.112667_bib200","doi-asserted-by":"crossref","first-page":"2905","DOI":"10.1021\/acs.jmedchem.8b01531","article-title":"Fibroblast growth factor receptor 4 (FGFR4) selective inhibitors as hepatocellular carcinoma therapy: advances and prospects","volume":"62","author":"Lu","year":"2019","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib201","doi-asserted-by":"crossref","first-page":"614","DOI":"10.3390\/cells8060614","article-title":"Fibroblast growth factor Receptors (FGFRs): structures and small molecule inhibitors","volume":"8","author":"Dai","year":"2019","journal-title":"Cells"},{"key":"10.1016\/j.ejmech.2020.112667_bib202","doi-asserted-by":"crossref","first-page":"1017","DOI":"10.1007\/s40265-019-01142-9","article-title":"Erdafitinib: first global approval","volume":"79","author":"Markham","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib203","doi-asserted-by":"crossref","first-page":"1373","DOI":"10.1038\/s41467-019-09068-2","article-title":"Aberrant FGFR signaling mediates resistance to CDK4\/6 inhibitors in ER+ breast cancer","volume":"10","author":"Formisano","year":"2019","journal-title":"Nat. Commun."},{"key":"10.1016\/j.ejmech.2020.112667_bib204","series-title":"Pyrazolyl Quinazoline Kinase Inhibitors","author":"Saxty","year":"2011"},{"key":"10.1016\/j.ejmech.2020.112667_bib205","series-title":"Quinoxaline Derivatives Useful as FGFR Kinase Modulators","author":"Vermeulen","year":"2015"},{"key":"10.1016\/j.ejmech.2020.112667_bib206","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pone.0222280","article-title":"[Fam-] trastuzumab deruxtecan (DS-8201a)-induced antitumor immunity is facilitated by the anti-CTLA-4 antibody in a mouse model","volume":"14","author":"Iwata","year":"2019","journal-title":"PLoS One"},{"key":"10.1016\/j.ejmech.2020.112667_bib207","first-page":"408","article-title":"Another targeted therapy for ERBB2-positive breast cancer","volume":"323","author":"Voelker","year":"2020","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib208","doi-asserted-by":"crossref","first-page":"610","DOI":"10.1056\/NEJMoa1914510","article-title":"Trastuzumab deruxtecan in previously treated HER2-positive breast cancer","volume":"382","author":"Modi","year":"2020","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2020.112667_bib209","series-title":"Treatment of Immunological Disorders Using Anti-CD30 Antibodies","author":"Law","year":"2003"},{"key":"10.1016\/j.ejmech.2020.112667_bib210","series-title":"Pentapeptide Compounds and Uses Related Thereto","author":"Doronina","year":"2002"},{"key":"10.1016\/j.ejmech.2020.112667_bib211","series-title":"Hexa-cyclic Compound","author":"Terasawa","year":"1998"},{"key":"10.1016\/j.ejmech.2020.112667_bib212","doi-asserted-by":"crossref","first-page":"855","DOI":"10.1021\/bc025536j","article-title":"Cathepsin B-labile dipeptide linkers for lysosomal release of doxorubicin from internalizing immunoconjugates: model studies of enzymatic drug release and antigen-specific in\u00a0vitro anticancer activity","volume":"13","author":"Dubowchik","year":"2002","journal-title":"Bioconjugate Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib213","doi-asserted-by":"crossref","first-page":"2426","DOI":"10.1182\/blood-2018-01-791491","article-title":"The role of JAK2 inhibitors in MPNs 7 years after approval","volume":"131","author":"Passamonti","year":"2018","journal-title":"Blood"},{"key":"10.1016\/j.ejmech.2020.112667_bib214","doi-asserted-by":"crossref","first-page":"1719","DOI":"10.1007\/s40265-019-01205-x","article-title":"Fedratinib: first approval","volume":"79","author":"Blair","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib215","series-title":"Compositions and Methods for Treating Myelofibrosis","author":"Tefferi","year":"2012"},{"key":"10.1016\/j.ejmech.2020.112667_bib216","doi-asserted-by":"crossref","first-page":"266","DOI":"10.1093\/brain\/awz363","article-title":"Microglial depletion prevents extracellular matrix changes and striatal volume reduction in a model of Huntington\u2019s disease","volume":"143","author":"Crapser","year":"2020","journal-title":"Brain"},{"key":"10.1016\/j.ejmech.2020.112667_bib217","doi-asserted-by":"crossref","first-page":"1805","DOI":"10.1007\/s40265-019-01210-0","article-title":"Pexidartinib: first approval","volume":"79","author":"Lamb","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib218","doi-asserted-by":"crossref","first-page":"690","DOI":"10.1158\/1078-0432.CCR-19-1486","article-title":"Colony-stimulating factor 1 receptor (CSF1R) activates AKT\/mTOR signaling and promotes T-cell lymphoma viability","volume":"26","author":"Murga-Zamalloa","year":"2020","journal-title":"Clin. Cancer Res."},{"key":"10.1016\/j.ejmech.2020.112667_bib219","first-page":"807","article-title":"First therapy for rare joint tumor is approved","volume":"322","author":"Voelker","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib220","doi-asserted-by":"crossref","first-page":"2564","DOI":"10.1055\/s-0037-1612421","article-title":"Exploratory process development of pexidartinib through the tandem tsuji-trost reaction and heck coupling","volume":"51","author":"Chen","year":"2019","journal-title":"Synthesis"},{"key":"10.1016\/j.ejmech.2020.112667_bib221","series-title":"Synthesis of 1H-Pyrrolo[2,3-B]pyridin Derivatives that Modulate Kinases","author":"Ibrahim","year":"2017"},{"key":"10.1016\/j.ejmech.2020.112667_bib222","doi-asserted-by":"crossref","first-page":"1485","DOI":"10.1007\/s40265-019-01188-9","article-title":"Selinexor: first global approval","volume":"79","author":"Syed","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2020.112667_bib223","doi-asserted-by":"crossref","first-page":"2546","DOI":"10.1182\/blood-2018-06-858852","article-title":"Selinexor plus low-dose bortezomib and dexamethasone for patients with relapsed or refractory multiple myeloma","volume":"132","author":"Bahlis","year":"2018","journal-title":"Blood"},{"key":"10.1016\/j.ejmech.2020.112667_bib224","first-page":"393","article-title":"Combination approved for advanced multiple myeloma","volume":"322","author":"Voelker","year":"2019","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2020.112667_bib225","series-title":"Hydrazide Containing Nuclear Transport Modulators and Uses Thereof","author":"Sandanayaka","year":"2013"},{"key":"10.1016\/j.ejmech.2020.112667_bib226","series-title":"Novel Crystalline Forms of Selinexor and Process for Their Preparation","author":"Muthusamy","year":"2018"},{"key":"10.1016\/j.ejmech.2020.112667_bib227","doi-asserted-by":"crossref","first-page":"851","DOI":"10.1182\/blood.2019001160","article-title":"Phase 1 study of the selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL","volume":"134","author":"Tam","year":"2019","journal-title":"Blood"},{"key":"10.1016\/j.ejmech.2020.112667_bib228","doi-asserted-by":"crossref","first-page":"2555","DOI":"10.1038\/s41375-019-0592-8","article-title":"What is new in the treatment of waldenstrom macroglobulinemia?","volume":"33","author":"Castillo","year":"2019","journal-title":"Leukemia"},{"key":"10.1016\/j.ejmech.2020.112667_bib229","doi-asserted-by":"crossref","first-page":"7923","DOI":"10.1021\/acs.jmedchem.9b00687","article-title":"Discovery of zanubrutinib (BGB-3111), a novel, potent, and selective covalent inhibitor of bruton\u2019s tyrosine kinase","volume":"62","author":"Guo","year":"2019","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib230","series-title":"Fused Heterocyclic Compounds as Protein Kinase Inhibitors","author":"Guo","year":"2014"},{"key":"10.1016\/j.ejmech.2020.112667_bib231","doi-asserted-by":"crossref","first-page":"1191","DOI":"10.1007\/s11427-018-9342-2","article-title":"Artificial intelligence in drug design","volume":"61","author":"Zhong","year":"2018","journal-title":"Sci. China Life Sci."},{"key":"10.1016\/j.ejmech.2020.112667_bib232","doi-asserted-by":"crossref","first-page":"915","DOI":"10.1080\/17460441.2019.1626821","article-title":"Contemporary medicinal-chemistry strategies for discovery of blood coagulation factor Xa inhibitors","volume":"14","author":"Hao","year":"2019","journal-title":"Expet Opin. Drug Discov."},{"key":"10.1016\/j.ejmech.2020.112667_bib233","doi-asserted-by":"crossref","first-page":"9375","DOI":"10.1021\/acs.jmedchem.9b00359","article-title":"Overview of recent strategic advances in medicinal chemistry","volume":"62","author":"Wu","year":"2019","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib234","doi-asserted-by":"crossref","first-page":"375","DOI":"10.4155\/fmc-2018-0397","article-title":"Discovery of novel anti-influenza agents via contemporary medicinal chemistry strategies (2014-2018 update)","volume":"11","author":"Jia","year":"2019","journal-title":"Future Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib235","doi-asserted-by":"crossref","first-page":"112374","DOI":"10.1016\/j.ejmech.2020.112374","article-title":"Medicinal chemistry insights into novel CDC25 inhibitors","volume":"201","author":"Tao","year":"2020","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2020.112667_bib236","article-title":"Natural products as LSD1 inhibitors for cancer therapy","author":"Fang","year":"2020","journal-title":"Acta Pharm. Sin. B"},{"key":"10.1016\/j.ejmech.2020.112667_bib237","first-page":"481","article-title":"Identification of anti-cancer compounds from natural products","volume":"18","author":"Lu","year":"2020","journal-title":"Chin. J. Nat. Med."},{"issue":"7","key":"10.1016\/j.ejmech.2020.112667_bib238","doi-asserted-by":"crossref","first-page":"1695","DOI":"10.1016\/j.cclet.2020.03.028","article-title":"New techniques and strategies in drug discovery","volume":"31","author":"Du","year":"2020","journal-title":"Chin. Chem. Lett."}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523420306395?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523420306395?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,5,13]],"date-time":"2026-05-13T12:52:08Z","timestamp":1778676728000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0223523420306395"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2020,11]]},"references-count":238,"alternative-id":["S0223523420306395"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2020.112667","relation":{},"ISSN":["0223-5234"],"issn-type":[{"value":"0223-5234","type":"print"}],"subject":[],"published":{"date-parts":[[2020,11]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"New drug approvals for 2019: Synthesis and clinical applications","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2020.112667","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2020 Elsevier Masson SAS. All rights reserved.","name":"copyright","label":"Copyright"}],"article-number":"112667"}}