Integrase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S222800, C514S250000, C544S346000, C544S361000

Reexamination Certificate

active

08008287

ABSTRACT:
Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.

REFERENCES:
patent: 4816570 (1989-03-01), Farquhar
patent: 4968788 (1990-11-01), Farquhar
patent: 5663159 (1997-09-01), Starrett, Jr. et al.
patent: 5683999 (1997-11-01), Jadhav et al.
patent: 5792756 (1998-08-01), Starrett, Jr. et al.
patent: 6245806 (2001-06-01), Dombrowski et al.
patent: 6271402 (2001-08-01), Singh et al.
patent: 6312662 (2001-11-01), Erion et al.
patent: 6395743 (2002-05-01), Heimbuch et al.
patent: 2003/0055071 (2003-03-01), Anthony et al.
patent: WO-91/19721 (1991-12-01), None
patent: WO-96/15111 (1996-05-01), None
patent: WO-99/62513 (1999-12-01), None
patent: WO-99/62520 (1999-12-01), None
patent: WO-00/39086 (2000-07-01), None
patent: WO-00/75122 (2000-12-01), None
patent: WO-01/00578 (2001-01-01), None
patent: WO-02/30426 (2002-04-01), None
patent: WO-02/30930 (2002-04-01), None
patent: WO-02/30931 (2002-04-01), None
patent: WO-02/36734 (2002-05-01), None
patent: WO-02/055079 (2002-07-01), None
patent: WO-2004/035576 (2004-04-01), None
patent: WO 2004/035577 (2004-04-01), None
patent: WO-2004/035577 (2004-04-01), None
patent: WO-2004/096807 (2004-11-01), None
patent: WO-2005/016927 (2005-02-01), None
patent: WO-2005/075475 (2005-08-01), None
patent: WO-2005/117904 (2005-12-01), None
patent: WO-2006/125048 (2006-11-01), None
patent: WO-2007/076005 (2007-07-01), None
Verschueren, W. et al. (2005) “Design and Optimization of Tricyclic Phtalimide Analogues as Novel Inhibitors of HIV-1 Integrase” J. Med. Chem 48:1930-1940.
Daelemans, D. et al. (2007) “Characterization of a Replication-Competent, Integrase-Defective Human Immunodeficiency Virus (HIV)/Simian Virus 40 Chimera as a Powerful Tool for the Discovery and Validation of HIV Integrase Inhibitors” J. of Vir. 81 (8): 4381-4385.
Anan'eva et al. (1983) “(2-lodoethyl) Phosphonic Derivatives,”Zhurnal Obshchei Khimii53(3):554-559.
Artico et al. (1998) “Geometrically and Conformationally Restrained Cinnamoyl Compounds as Inhibitors of HIV-1 Integrase: Synthesis, Biological Evaluation, and Molecular Modeling,”J. Med. Chem. 41:3948-3960.
Asante-Appiah et al. (1999) “HIV-1 Integrase: Structural Organization, Conformational Changes, and Catalysis,”Advances in Virus Research52:351-363.
Benzaria et al. (1996) “Synthesis, in Vitro Antiviral Evaluation, and Stability Studies of Bis(S-acyl-2-thioethyl) Ester Derivatives of 9-2-(Phosphonomethoxy)ethyl)adenine (PMEA) as Potential PMEA Prodrugs with Improved Oral Bioavailability,”J. Med. Chem. 39:4958-4965.
Bhuta et al. (1980) “Analogues of Chloramphenicol: Circular Dichroism Spectra, Inhibition of Ribosomal Peptidyltransferase, and Possible Mechanism of Action,”J. Med. Chem. 23:1299-1305.
Buolamwini et al. (2002) “CoMFA and CoMSIA 3D QSAR and Docking Studies on Conformationally-Restrained Cinnamoyl HIV-1 Integrase Inhibitors: Exploration of a Binding Mode at the Active Site,”J. Med. Chem. 45:841-852.
Campagne et al. (1995) “1H-Benzotriazol-1-yloxy)tris(dimethylamino)phorphonium Hexafluorophosphate- and (1H-Benzotriazol-1-yloxy)tripyrroludinophosphonium Hexafluorophosphate-Mediated Activation of Monophosphonate Esters: Synthesis of Mixed Phosphonate Diesters, the Reactivity of the Benzotriazolyl Phosphonic Esters vs the Reactivity of the Benzotriazolyl Carboxylic Esters,”J. Org. Chem. 60:5214-5223.
Chen et al. (1997) “Design, Synthesis, and Biochemical Evaluation of Phosphonate and Phosphonamidate Analogs of Glutathionylspermidine as Inhibitors of Glutathionylspermidine Synthetase/Amidase fromEscherichia coli,”J. Med. Chem. 40:3842-3850.
Darby, G. (1995) “In Search of the Perfect Antiviral,”Antiviral Chemistry&Chemotherapy6(Suppl. 1):54-63.
Davies et al. (1988) “Dinucleotide Analogues as Inhibitors of Thymidine Kinase, Thymidylate Kinase, and Ribonucleotide Reductase,”J. Med. Chem. 31:1305-1308.
De Lombaert et aI. (1994) “N-Phosphonomethyl Dipeptides and Their Phosphonate Prodrugs, a New Generation of Neutral Endopeptidase (NEP, EC 3.4.24.11) Inhibitors,”J. Med. Chem. 37:498-511.
Espeseth et al. (2000) “HIV-1 Integrase Inhibitors that Compete with the Target DNA Substrate Define a Unique Strand Transfer Conformation for Integrase,”PNAS97(21):11244-11249.
Farnet et al. (1996) “Differential Inhibtion of HIV-1 Preintegration Complexes and Purified Integrase Protein by Small Molecules,”Proc. Natl. Acad. Sci. USA93:9742-9747.
Farquhar et al. (1983) “Biologically Reversible Phosphate-Protective Groups,”Journal of Pharmaceutical Sciences72(3):324-325.
Galeotti et al. (1996) “A Straightforward Synthesis of α-Amino Phosphonate Monoesters Using BroP or TPyCIU,”Tetrahedron Letters37(23):3997-3998.
Goldgur et al. (1999) “Structure of the HIV-1 Integrase Catalytic Domain Complexed with an Inhibitor: A Platform for Antiviral Drug Design,”PNAS96(23):13040-13043.
Hazuda et al. (1994) “A Novel Assay for the DNA Strand-Transfer Reaction of HIV-1 Integrase,”Nucleic Acids Research22(6):1121-1122.
Hazuda et al. (1997) “Differential Divalent Cation Requirements Uncouple the Assembly and Catalytic Reactions of Human Immunodeficiency Virus Type I Intergrase,”Journal of Virology71(9):7005-7011.
Hazuda et al. (1997) “Discovery and Analysis of Inhibitors of the Human Immunodeficiency Integrase,”Drug Design and Discovery15:17-24.
Hazuda et al. (2000) “Inhibitors of Strand Transfer that Prevent Integration and Inhibit HIV-1 Replication in Cells,”Science287:646-650.
Jacob, P. III (1982) “Resolution of -5-Bromonornicotine. Synthesis of (R)- and (S)- Nornicotine of High Enantiomeric Purity,”J. Org. Chem. 47:4165-4167.
Jing et al. (2002) “Potassium-Dependent Folding: A Key to Intracellular Delivery of G-Quartet Oligonucleotides as HIV Inhibitors,”Biochemistry41:5397-5403.
Katzman et al. (1999) “Substrate Recognition by Retroviral Integrases,”Advances in Virus Research52:371-395.
Khamnei et al. (1996) “Neighboring Group Catalysis in the Design of Nucleotide Prodrugs,”J. Med. Chem. 39:4109-4115.
Lafemina et al. (1992) “Requirement of Active Human Immunodeficiency Virus-Type 1 Integrase Enzyme for Productive Infection of Human T-Lymphoid Cells,”Journal of Virology66(12):7414-7419.
Le Bas et al. (2001) “Oxidation of 2-and 3-Halogenated Quinolines: An Easy Access to 5- and 6-Halogenopyridine-2,3-dicarboxylic Acids,”Synthesis16:2495-2499.
Lochmuller, C. (1975) “Chromatographic Resolution of Enantiomers Selective Review,”Journal of Chromatography113:283-302.
Mikhailopulo et al. (2000) “Pyrophosphoryl, Derivatives of 1-(2-Deoxy-3-O Phosphonomethyl -β-and -α-D-erythro-Pentofuranosyl)Thymine: Synthesis and Substrate Properties Towards Some DNA Polymerases,”Nucleosides, Nucleotides & Nucleic Acids19(10-12):1885-1909.
Mitchell et al. (1992) “Bioreversible Protection for the Phospho Group: Bioactivation of the Di-(4-acyloxybenzyl) and Mono(4-acyloxybenzyl) Phosphoesters of Methylphosphonate and Phosphonoacetate,”J. Chem. Soc. Perkin Trans. I2345-2353.
Morgan et al. (1994) “Structure-Based Design of an Inhibitor of the Zinc Peptidase Thermolysin,”J. Am. Chem. Soc. 116:3251-3260.
Musiol et al. (1994) “On the Synthesis of Phosphonamidate Peptides,”J. Org. Chem. 59:6144-6146.
Nair, V. (2002) “HIV Integrase as a Target for Antiviral Chemotherapy,”Rev. Med. Virol. 12:179-193.
Okamoto et al. (1990) “Optical Resolution of Dihydropyridine Enantiomers by High-Perfomance Liquid Chromatography Using Phenylcarbamates of Polysaccharides as a Chiral Stationary Phase,”Journal of Chromatography513:375-378.
Pais et al. (2002) “Structure Activity of 3-Aryl-1-1,3-diketo-Containing Compounds as HIV-1 Integra

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