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Darunavir: a review of its use in the management of HIV infection in adults. Drugs. 2009;69(4):477-503.
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Hollow-fiber unit evaluation of a new human immunodeficiency virus type 1 protease inhibitor, BMS-232632, for determination of the linked pharmacod... J Infect Dis. 2001 Apr 1;183(7):1126-9.
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2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
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Fosamprenavir/ritonavir in advanced HIV disease (TRIAD): a randomized study of high-dose, dual-boosted or standard dose fosamprenavir/ritonavir in ... J Antimicrob Chemother. 2009 Aug;64(2):398-410.
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Quantification of HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors in peripheral blood mononuclear cell lysate using liq... J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Feb 15;877(5-6):575-80.
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Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV. Int J Antimicrob Agents. 2009 Apr;33(4):307-20.
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PL-100, a novel HIV-1 protease inhibitor displaying a high genetic barrier to resistance: an in vitro selection study. J Med Virol. 2008 Dec;80(12):2053-63.
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Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
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2011 Pipeline of Boehringer Ingelheim Pharma.
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Clinical pipeline report, company report or official report of Abbott Laboratories (2011)
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Clinical pipeline report, company report or official report of Achillion (2011).
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2011 Pipeline of Bristol-Myers Squibb.
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2011 Pipeline of InterMune.
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Highly drug-resistant HIV-1 clinical isolates are cross-resistant to many antiretroviral compounds in current clinical development. AIDS. 1999 April 16; 13(6): 661-667.
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Clinical pipeline report, company report or official report of Gilead (2011).
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Oxidative modifications of kynostatin-272, a potent human immunodeficiency virus type 1 protease inhibitor: potential mechanism for altered activit... Antimicrob Agents Chemother. 2002 Feb;46(2):402-8.
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Clinical pipeline report, company report or official report of Merck (2011).
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Oral Druggable Space beyond the Rule of 5: Insights from Drugs and Clinical Candidates. Chemistry & Biology Volume 21, Issue 9, 18 September 2014, Pages 1115-1142.
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19 |
2011 Pipeline of Biotron.
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Avanir Licenses Concert's Deuterium-Modified Dextromethorphan Products in Potential US$200 M Deal. Vol 2012 Issue 3 Page(38).
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21 |
ClinicalTrials.gov (NCT01045317) A Study To Investigate The Clearance Of PF-04776548 From The Body Following A Very Low (Micro) Dose Of The Compound Using A Low Level Of Radiotracer To Help Quantify Expected Low Concentrations Of PF-04776548 In The Body. U.S. National Institutes of Health.
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Antiviral activity and cross-resistance profile of P-1946, a novel human immunodeficiency virus type 1 protease inhibitor. Antiviral Res. 2006 Jun;70(2):17-20.
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2011 Pipeline of Vertex.
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Solvation studies of DMP323 and A76928 bound to HIV protease: analysis of water sites using grand canonical Monte Carlo simulations. Protein Sci. 1998 Mar;7(3):573-9.
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Safety and pharmacokinetics of brecanavir, a novel human immunodeficiency virus type 1 protease inhibitor, following repeat administration with and without ritonavir in healthy adult subjects.Antimicrob Agents Chemother.2007 Apr;51(4):1202-8.
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26 |
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors. J Med Chem. 2000 Sep 7;43(18):3386-99.
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27 |
Improved cyclic urea inhibitors of the HIV-1 protease: synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450. Chem Biol. 1996 Apr;3(4):301-14.
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28 |
In vitro and ex vivo anti-human immunodeficiency virus (HIV) activities of a new water-soluble HIV protease inhibitor, R-87366, containing (2S,3S)-3-amino-2-hydroxy-4-phenylbutanoic acid. Biol Pharm Bull. 1997 Feb;20(2):175-80.
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29 |
Improvement of bioavailability of the HIV protease inhibitor SC-52151 in the beagle dog by coadministration of the CYP3A4 inhibitor, ketoconazole. Xenobiotica. 1997 May;27(5):489-97.
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30 |
WO patent application no. 2003,0906,90, Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such.
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31 |
Human serum alpha 1 acid glycoprotein reduces uptake, intracellular concentration, and antiviral activity of A-80987, an inhibitor of the human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother. 1996 Jun;40(6):1491-7.
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CGP 53437, an orally bioavailable inhibitor of human immunodeficiency virus type 1 protease with potent antiviral activity. Antimicrob Agents Chemother. 1993 Oct;37(10):2087-92.
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33 |
Design and selection of DMP 850 and DMP 851: the next generation of cyclic urea HIV protease inhibitors. Chem Biol. 1998 Oct;5(10):597-608.
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DPC 681 and DPC 684: potent, selective inhibitors of human immunodeficiency virus protease active against clinically relevant mutant variants. Antimicrob Agents Chemother. 2001 Nov;45(11):3021-8.
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JE-2147: a dipeptide protease inhibitor (PI) that potently inhibits multi-PI-resistant HIV-1. Proc Natl Acad Sci U S A. 1999 Jul 20;96(15):8675-80.
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36 |
Quantitative determination of CGP 61755, a protease inhibitor, in plasma and urine by high-performance liquid chromatography and fluorescence detection. J Chromatogr B Biomed Sci Appl. 1997 Aug 15;696(1):123-30.
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37 |
CN patent application no. 101115713, Hiv protease inhibitors.
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Current and Novel Inhibitors of HIV Protease. Viruses. 2009 December; 1(3): 1209-1239.
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Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors. J Med Chem. 1995 Dec 22;38(26):4968-71.
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Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors. J Med Chem. 1994 Sep 30;37(20):3200-4.
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In vitro anti-human immunodeficiency virus (HIV) activity of XM323, a novel HIV protease inhibitor. Antimicrob Agents Chemother. 1993 Dec;37(12):2606-11.
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42 |
Exploring the energy landscapes of molecular recognition by a genetic algorithm: analysis of the requirements for robust docking of HIV-1 protease and FKBP-12 complexes. Proteins. 1996 Jul;25(3):342-53.
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Ly316340: A potent HIV-1 protease inhibitor containing a high affinity octahydrothienopyridine hydroxyethylamine isostere. Bioorganic & Medicinal Chemistry Letters Volume 5, Issue 23, 7 December 1995, Pages 2885-2890.
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HIV protease inhibitor HOE/BAY 793, structure-activity relationships in a series of C2-symmetric diols. Bioorg Med Chem. 1995 May;3(5):559-71.
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Antiviral properties of aminodiol inhibitors against human immunodeficiency virus and protease. Antimicrob Agents Chemother. 1995 Feb;39(2):374-9.
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Determination of BMS-186318 in dog, rat and monkey plasma by liquid chromatography-ionspray mass spectrometry. J Pharm Biomed Anal. 1995 Dec;14(1-2):43-8.
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Oral bioavailability of a poorly water soluble HIV-1 protease inhibitor incorporated into pH-sensitive particles: effect of the particle size and nutritional state. J Control Release. 2000 Aug 10;68(2):291-8.
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A mutation in human immunodeficiency virus type 1 protease at position 88, located outside the active site, confers resistance to the hydroxyethylurea inhibitor SC-55389A. Antimicrob Agents Chemother. 1997 Mar;41(3):515-22.
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49 |
US patent application no. 2008,0161,324, Compositions and methods for treatment of viral diseases.
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KNI-102, a novel tripeptide HIV protease inhibitor containing allophenylnorstatine as a transition-state mimic. Chem Pharm Bull (Tokyo). 1991 Nov;39(11):3088-90.
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Antiviral properties of palinavir, a potent inhibitor of the human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother. 1997 May;41(5):965-71.
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52 |
Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere. J Med Chem. 1994 Sep 16;37(19):3100-7.
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53 |
Effects of U-75875, a peptidomimetic inhibitor of retroviral proteases, on simian immunodeficiency virus infection in rhesus monkeys. Antimicrob Agents Chemother. 1994 Jun;38(6):1277-83.
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[Mechanism of action of aspartic proteases. III. Conformational characteristics of HIV-1 protease inhibitor JG-365]. Bioorg Khim. 1999 Jun;25(6):418-22.
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Impeded progression of Friend disease in mice by an inhibitor of retroviral proteases. J Acquir Immune Defic Syndr. 1993 Jan;6(1):24-31.
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