| Abbenante et al, "Regioselective Structural and Functional Minicry of Peptides. Design of Hydrolytically-Stable Cyclic Peptidomimetic Inhibitors of HIV-1 Protease," J Am Chem Soc 117(41):10220-10226 (Oct. 18, 1995). |
| Ghosh et al., "Cyclic Sulfone-3-Carboxamides as Novel P2-Ligands for RO 31-8959 Based HIV-1 Protease Inhibitors," Bioorg Med Chem Lett 5(1):83-88 (1994). |
| "HIV Protease Substrate 1 (H-2930): For Fluorimetric Measurement of HIV Protease Activity," Molecular Probes, Inc. (Brochure Advertisement) (Jan. 30, 1992). |
| "Product: recHIV-PR (Recombinant HIV Protease)," Bachem Bioscience Inc. (Analytical Data Sheet) (May 28, 1991). |
| Altenbach, Hans-Josef, "Flexible, Stereocontrolled Routes to Sugar Mimics via Convenient Intermediates," Antibiotics and Antiviral Compounds pp. 359-372 (1993). |
| Anderson et al., "The Discovery of BILA 2011 BS, a Potent Inhibitor of HIV-1 and HIV-2 Protease," AIDS Gordon Conference (4 pages) (Feb. 1995). |
| Billich et al., "Review: Antiviral Assays, Number 1--Assay systems for HIV-1 proteinase and their use for evaluation of inhibitors," Antiviral Chem & Chemo 2(2):65-73 (1991). |
| Block, Eric, "Reactions of Organosulfur Compounds," Organic Chemistry 37:pp. 145-153, 174-175 (1978). |
| Buckheit, Robert W., "Facsimile Letter to Dr. Larry McGee," Frederick Research Center, Southern Research Institute (May 23, 1994). |
| Cere et al., "Synthesis of (E,E)-Thiacyclodeca-4,7-diene and of its 3-Methyl Derivative from D-Mannitol. Stereochemical and Conformational Behavior," J Org Chem 47:3540-3544 (1982). |
| Cere et al., "Transannular Addition of alph-Thia Carbanions to Unactivated Double Bonds. 5. Synthesis of (9R, 10S)-trans-1-Thiadecalin," J Org Chem 53:5689-5694 (1988). |
| Chenera et al., "Nonpeptide HIV Protease Inhibitors Designed to Replace a Bound Water," Bioorg Med Chem Lett 3(12):2717-2722 (1993). |
| Feeder et al., "Sterochemistry of Reduction of a Heterocyclic alpha-Hydroxy-Ketone: The Structure, Conformation and Prparation of the syn and anti-3,3,6,6-Tetramethylthiepan-4,5-diols," Tet Lett 35(8):9095-9098 (1994). |
| Fuzier et al., "Thiosugars From D-Mannitol," Tet Lett 36(36):6443-6446 (1995). |
| Jadhav et al., "Synthesis of 7-Membered Cyclic Oxamides: Novel HIV-1 Protease Inhibitors," Tet Lett 37(8):115-31156 (1996). |
| Jadhav et al., "Synthesis of 8-Membered Cyclic Sulfamides: Novel HIV-1 Protease Inhibitors," Tet Lett 36(36):6383-6386 (1995). |
| Johnson and Berman, "The Photochemical Reactions of 1-Thiacycloheptan-4-one Derivatives. An Approach to Pantothiolactone," J Org Chem 40(21):3046-3051 (1975). |
| Kuszmann et al., "1,6-Anhydro-1(6)-Thio-L-Iditol And -D-Mannitol, And Some Derivatives Thereof," Carb Res 56:105-115 (1977). |
| Kuszmann et al., "Acetalation of 1,6-Anhydro-1(6)-Thio-D-Glucitol," Carb Res 50:45-52 (1976). |
| Kuszmann et al., "Synthesis of 1,6-Thioanhydro-D-Glucitol," Carb Res 48:23-32 (1976). |
| Lam et al., "Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors," Science 263:380-384 (Jan. 21, 1994). |
| Lunney et al., "A Novel Nonpeptide HIV-1 Protease Inhibitor: Elucidation of the Binding Mode and Its Application in the Design of Related Analogs," J Med Chem 37:2664-2677 (1994). |
| Matayoshi et al., "Novel Fluorogenic Substrates for Assaying Retroviral Proteases by Resonance Energy Transfer," Science 247:954-958 (Feb. 23, 1990). |
| Mittendorf et al., "Novel Non-Peptidic HIV-1 Protease Inhibitors by Computer Assisted Molecular Design, Part 1: Synthesis and Biological Activity of a Polyfunctional Piperidine," IXth Int Conf on AIDS, Berlin (Jun. 7-11, 1993). |
| Newlander et al., "A Novel Constrained Reduced-Amide Inhibitor of HIV-1 Protease Derived from the Sequential Incorporation of Gamma-Turn Mimetics into a Model Substrate," J Med Chem 36:2321-2331 (1993). |
| Peyman et al., "Non-Peptide-Based Inhibitors of Human Immunodeficiency Virus-1 Protease," Bioorg Med Chem Lett 4(21):2601-2604 (1994). |
| Prasad et al., "Novel Series of Achiral, Low Molecular Weight, and Potent HIV-1 Protease Inhibitors," J Am Chem Soc 116:6989-6990 (1994). |
| Randad et al., "De Novo Design Of Nonpeptidic HIV-1 Protease Inhibitors: Incorpration Of Structural Water," Bioorg Med Chem Lett 4(1):1247-1252 (1994). |
| Romines et al., "4-Hydroxypyrones and Related Templates as Nonpeptidic HIV Protease Inhibitors," Current Medicinal Chemistry 2:825-838 (1995). |
| Sham et al, "A Novel, Picomolar Inhibitor of Human Immunodeficiency Virus Type 1 Protease," J Med Chem 39:392-397 (1996). |
| Simpkins, Nigel S., "Sulphones in Organic Synthesis," Tetrahedron Organic Chemistry Series 10:308, 309, 326, 327 (1993). |
| Spaltenstein et al., "Synthesis of C2-Symmetric HIV-Protease Inhibitors With Sulfur-Containing Central Units," Tet Lett 34(9):1457-1460 (1993). |
| Thaisrivongs et al., "Structure-Based Design of HIV Protease Inhibitors: 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Non-peptidic Inhibitors," J Med Chem 37:3200-3204 (1994). |
| Wang et al., "Design and Synthesis of New Fluorogenic HIV Protease Substrates Based on Resonance Energy Transfer," Tet Lett 31(45):6493-6496 (1990). |
| Weissberger, Arnold and Taylor, Edward C., "Seven-Membered Rings Containing Sulfur," The Chemistry of Heterocyclic Compounds Chapter 10, pp. 580-667 (1972). |
| Wong et al., "A Pharmacokinetic Evaluation of HIV Protease Inhibitors, Cyclic Ureas, in Rats and Dogs," Biochem Pharm 15:535-544 (1994). |
| Desper et al, "Novel five-coordinate polythioethers--an alternative to macrocyclic chelate formers", CA 120:270030, Source: Angew. Chem. 106(3), 335-8, 1994. |
Patent Grant
5705524
