1051375-16-6 | (3S,7R)-N-[(2,4-difluorophenyl)methyl]-11-hydroxy-7-methyl-9,12-dioxo-4-oxa-1,8-diazatricyclo[8.4.0.0^{3,8}]tetradeca-10,13-diene-13-carboxamide

1335210-35-9   

dolutegravir 

[1]Patent:WO2019/159199,2019,A1.Locationinpatent:Page/Pagecolumn34;35;36;38;39

[2]AngewandteChemie-InternationalEdition,2018,vol.57,p.7181-7185    Angew.Chem.,2018,vol.130,p.7299-7303,5

[3]Patent:CN109293675,2019,A.Locationinpatent:Paragraph0004;0037-0038

[4]Patent:WO2014/128545,2014,A2.Locationinpatent:Page/Pagecolumn22-23

[5]Patent:WO2016/125192,2016,A2.Locationinpatent:Page/Pagecolumn30;34

[6]Patent:CN106565747,2017,A.Locationinpatent:Paragraph0035-0037;0044-0045

1802141-49-6    1051375-16-6 

[1]CurrentPatentAssignee:KINGLAWRENCE;CIPLALTD-WO2015/177537,2015,A1Locationinpatent:Page/Pagecolumn44

[2]CurrentPatentAssignee:QILUPHARMACEUTICALGROUPCOLTD-CN114835730,2022,ALocationinpatent:Paragraph0143-0152

[3]CurrentPatentAssignee:LAURUSLABSLIMITED-WO2015/110897,2015,A3Locationinpatent:Paragraph00276-00278

1051375-16-6    112-64-1    2248029-86-7 

[1]Sillman,Brady;Bade,AdityaN.;Dash,PrasantaK.;Bhargavan,Biju;Kocher,Ted;Mathews,Saumi;Su,Hang;Kanmogne,GeorgetteD.;Poluektova,LarisaY.;Gorantla,Santhi;McMillan,Joellyn;Gautam,Nagsen;Alnouti,Yazen;Edagwa,Benson;Gendelman,HowardE.[NatureCommunications,2018,vol.9,#1]

[2]CurrentPatentAssignee:GLAXOSMITHKLINEPLC-WO2017/223280,2017,A2Locationinpatent:Page/Pagecolumn10;32

[3]Khuroo,Tahir;Mohamed,EmanM.;Dharani,Sathish;Immadi,Sujana;Nutan,MohammadT.H.;Lu,Dai;Ali,HamedI.;Khan,MansoorA.;Rahman,Ziyaur[JournalofPharmaceuticalSciences,2022,vol.111,#8,p.2312-2321]

[4]Deodhar,Suyash;Sillman,Brady;Bade,AdityaN.;Avedissian,SeanN.;Podany,AnthonyT.;McMillan,JoEllynM.;Gautam,Nagsen;Hanson,Brandon;DyavarShetty,BhagyaL.;Szlachetka,Adam;Johnston,Morgan;Thurman,Michellie;Munt,DanielJ.;Dash,AlekhaK.;Markovic,Milica;Dahan,Arik;Alnouti,Yazen;Yazdi,Alborz;Kevadiya,BhaveshD.;Byrareddy,SiddappaN.;Cohen,SamuelM.;Edagwa,Benson;Gendelman,HowardE.[NatureCommunications,2022,vol.13,#1]

Title: Antiviral Activity of Bictegravir and Cabotegravir against Integrase Inhibitor-Resistant SIVmac239 and HIV-1.

Journal: Antimicrobial agents and chemotherapy 20171201

Title: Impact of HIV-1 Integrase L74F and V75I Mutations in a Clinical Isolate on Resistance to Second-Generation Integrase Strand Transfer Inhibitors.

Journal: Antimicrobial agents and chemotherapy 20170801

Title: Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection.

Journal: Antimicrobial agents and chemotherapy 20150101

Title: Clinical pharmacokinetic, pharmacodynamic and drug-interaction profile of the integrase inhibitor dolutegravir.

Journal: Clinical pharmacokinetics 20131101

Title: Dolutegravir (Tivicay) for HIV.

Journal: The Medical letter on drugs and therapeutics 20130930

Title: Dolutegravir: first global approval.

Journal: Drugs 20130901

Title: Dolutegravir versus raltegravir in antiretroviral-experienced, integrase-inhibitor-naive adults with HIV: week 48 results from the randomised, double-blind, non-inferiority SAILING study.

Journal: Lancet (London, England) 20130824

Title: Antiretroviral therapy: dolutegravir sets SAIL(ING).

Journal: Lancet (London, England) 20130824

Title: Impact of primary elvitegravir resistance-associated mutations in HIV-1 integrase on drug susceptibility and viral replication fitness.

Journal: Antimicrobial agents and chemotherapy 20130601

Title: In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20130201

Title: The activity of the integrase inhibitor dolutegravir against HIV-1 variants isolated from raltegravir-treated adults.

Journal: Journal of acquired immune deficiency syndromes (1999) 20121101

Title: Prevalence of HIV-1 integrase mutations related to resistance to dolutegravir in raltegravir naïve and pretreated patients.

Journal: Clinical microbiology and infection : the official publication of the European Society of Clinical Microbiology and Infectious Diseases 20121001

Title: The use of HIV-1 integrase inhibitors in antiretroviral naive patients.

Journal: Current opinion in HIV and AIDS 20120901

Title: Pharmacology of HIV integrase inhibitors.

Journal: Current opinion in HIV and AIDS 20120901

Title: HIV integrase inhibitors in ART-experienced patients.

Journal: Current opinion in HIV and AIDS 20120901

Title: Tolerability of HIV integrase inhibitors.

Journal: Current opinion in HIV and AIDS 20120901

Title: From in vitro EC₅₀ to in vivo dose-response for antiretrovirals using an HIV disease model. Part I: a framework.

Journal: Journal of pharmacokinetics and pharmacodynamics 20120801

Title: Update on raltegravir and the development of new integrase strand transfer inhibitors.

Journal: Southern medical journal 20120701

Title: Dolutegravir for the treatment of HIV.

Journal: Expert opinion on investigational drugs 20120401

Title: Effect of a single supratherapeutic dose of dolutegravir on cardiac repolarization.

Journal: Pharmacotherapy 20120401

Title: Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviral-naive adults with HIV: planned interim 48 week results from SPRING-1, a dose-ranging, randomised, phase 2b trial.

Journal: The Lancet. Infectious diseases 20120201

Title: Genetic barrier to the development of resistance to integrase inhibitors in HIV-1 subtypes CRF01_AE and B.

Journal: Intervirology 20120101

Title: Cross-resistance profile of the novel integrase inhibitor Dolutegravir (S/GSK1349572) using clonal viral variants selected in patients failing raltegravir.

Journal: The Journal of infectious diseases 20111201

Title: Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572).

Journal: Molecular pharmacology 20111001

Title: Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults.

Journal: AIDS (London, England) 20110910

Title: Effect of atazanavir and atazanavir/ritonavir on the pharmacokinetics of the next-generation HIV integrase inhibitor, S/GSK1349572.

Journal: British journal of clinical pharmacology 20110701

Title: Prevalence of resistance mutations related to integrase inhibitor S/GSK1349572 in HIV-1 subtype B raltegravir-naive and -treated patients.

Journal: The Journal of antimicrobial chemotherapy 20110701

Title: Pharmacokinetics of the HIV integrase inhibitor S/GSK1349572 co-administered with acid-reducing agents and multivitamins in healthy volunteers.

Journal: The Journal of antimicrobial chemotherapy 20110701

Title: S/GSK1349572, a new integrase inhibitor for the treatment of HIV: promises and challenges.

Journal: Expert opinion on investigational drugs 20110401

Title: Implications of integrase inhibitors for HIV-infected transplantation recipients: raltegravir and dolutegravir (S/GSK 1349572).

Journal: Bioscience trends 20110101

Title: Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers.

Journal: Antimicrobial agents and chemotherapy 20100101

Title: Kobayashi M, et al. In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21.

Title: Hare S, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72.

Title: Moss L, et al. The comparative disposition and metabolism of dolutegravir, a potent HIV-1 integrase inhibitor, in mice, rats, and monkeys. Xenobiotica. 2015 Jan;45(1):60-70.