| 词条 | Lemborexant |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = (1R,2S)-2-[(2,4-Dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide | image = Lemborexant.svg | width = 250px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Experimental drug | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 1369764-02-2 | CAS_supplemental = | ATC_prefix = None | ATC_suffix = | PubChem = 56944144 | DrugBank_Ref = | DrugBank = | KEGG = D11022 | ChemSpiderID_Ref = | ChemSpiderID = 34500836 | synonyms = E-2006 | C=22 | H=20 | F=2 | N=4 | O=2 | molecular_weight = 410.417 g/mol | SMILES = CC1=NC(=NC=C1OCC2(CC2C(=O)NC3=NC=C(C=C3)F)C4=CC(=CC=C4)F)C | StdInChI = 1S/C22H20F2N4O2/c1-13-19(11-25-14(2)27-13)30-12-22(15-4-3-5-16(23)8-15)9-18(22)21(29)28-20-7-6-17(24)10-26-20/h3-8,10-11,18H,9,12H2,1-2H3,(H,26,28,29)/t18-,22+/m0/s1 | StdInChIKey = MUGXRYIUWFITCP-PGRDOPGGSA-N }}Lemborexant ({{abbrlink|INN|International Nonproprietary Name}}) (code name E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development by Eisai for the treatment of insomnia.[1][2][3] In June 2016, Eisai initiated phase 3 clinical trials which are currently underway in the US, France, Germany, Italy, Japan, Poland, Spain and the UK, and are expected to extend to Canada. [4] See also
References1. ^{{cite journal|last1=Christopher|first1=John A|title=Small-molecule antagonists of the orexin receptors|journal=Pharmaceutical Patent Analyst|volume=3|issue=6|year=2014|pages=625–638|issn=2046-8954|doi=10.4155/ppa.14.46|pmid=25489915}} 2. ^{{cite journal|title=Recent Trends in Orexin Research – 2010 to 2015|journal=Bioorganic & Medicinal Chemistry Letters|volume=25|issue=15|pages=2875–2887|author=Cristoph Boss, Catherine Ross|year=2015|doi=10.1016/j.bmcl.2015.05.012|pmid=26045032|url=http://www.sciencedirect.com/science/article/pii/S0960894X1500462X}} 3. ^{{cite journal|last1=Boss|first1=Christoph|title=Orexin receptor antagonists – a patent review (2010 to August 2014)|journal=Expert Opinion on Therapeutic Patents|volume=24|issue=12|year=2014|pages=1367–1381|issn=1354-3776|doi=10.1517/13543776.2014.978859|pmid=25407283}} 4. ^{{Cite web|url=https://www.sps.nhs.uk/medicines/lemborexant/|title=Lemborexant – SPS - Specialist Pharmacy Service – The first stop for professional medicines advice|website=www.sps.nhs.uk|language=en-GB|access-date=2017-11-05}} External links
8 : Carboxamides|Cyclopropanes|Fluoroarenes|Hypnotics|Orexin antagonists|Organofluorides|Pyrimidines|Pyridines |
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