- HIV PROTEASE INHIBITORS
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Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which
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Page/Page column 43
(2013/05/21)
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- SULFONAMIDES AS HIV PROTEASE INHIBITORS
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Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HW protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines
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Page/Page column 47
(2012/05/19)
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- Epsilon substituted lysinol derivatives as HIV-1 protease inhibitors
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A series of HIV-1 protease inhibitors containing an epsilon substituted lysinol backbone was synthesized. Two novel synthetic routes using N-boc-l-glutamic acid alpha-benzyl ester and 2,6-diaminopimelic acid were developed. Incorporation of this epsilon s
- Jones, Kristen L.G.,Holloway, M. Katharine,Su, Hua-Poo,Carroll, Steven S.,Burlein, Christine,Touch, Sinoeun,DiStefano, Daniel J.,Sanchez, Rosa I.,Williams, Theresa M.,Vacca, Joseph P.,Coburn, Craig A.
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body text
p. 4065 - 4068
(2010/09/04)
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- LYSINE-BASED PRODRUGS OF ASPARTYL PROTEASE INHIBITORS AND PROCESSES FOR THEIR PREPARATION
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The present invention provides processes for synthesizing lysine based compounds of the Formula (I); wherein R1 may be, for example, (HO)2P(O)-, (NaO)2P(O)-, wherein X may be, for example, NH2, Y may be H, F, Cl, or Br, and wherein n, X', Y', R2, R3, R4, R5 and R6 are as defined herein.
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Page/Page column 60
(2008/06/13)
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- Lysine sulfonamides as novel HIV-protease inhibitors: Nε-Acyl aromatic α-amino acids
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A series of lysine sulfonamide analogues bearing Nε-acyl aromatic amino acids were synthesized using an efficient synthetic route. Evaluation of these novel protease inhibitors revealed compounds with high potency against wild-type and multiple-protease inhibitor-resistant HIV viruses.
- Stranix, Brent R.,Lavallee, Jean-Francois,Sevigny, Guy,Yelle, Jocelyn,Perron, Valerie,LeBerre, Nicholas,Herbart, Dominik,Wu, Jinzi J.
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p. 3459 - 3462
(2007/10/03)
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- Lysine based compounds
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The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.
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Page/Page column 20
(2010/02/15)
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- LYSINE BASED COMPOUNDS
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The present invention provides lysine based compounds of the formula (I); and when the compound of formula (I) comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein Rl may be, for example, (HO)2P(O)-, (NaO)2P(O)-, alkyl-CO- or cycloalkyl-CO-, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein. These lysine based compounds have a physiologically cleavable unit, namely R1 , whereby upon cleavage of the unit, an HIV aspartyl protease inhibitor is released,
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Page/Page column 44
(2008/06/13)
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- METHOD FOR IMPROVING PHARMACOKINETICS OF PROTEASE INHIBITORS AND PROTEASE INHIBITOR PRECURSORS
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The present invention provides methods for improving the pharmacokinetics of protease inhibitors and protease inhibitor precursors and pharmaceutical composition comprising protease inhibitors or protease inhibitor precursors of formula I and a cytochrome P450 monooxigenase inhibitor; Formula (I) when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)-, (NaO)2P(O)-, alkyl- CO- or cycloalkyl-CO-, wherein X may be, for example, F, CI, and Br, and wherein R2 and R3 are as defined herein.
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Page/Page column 74
(2010/11/24)
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- Aromatic derivatives as HIV aspartyl protease inhibitors
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The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1may be, for example,
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- Pictet-Spengler cyclization of 3,3-diphenylalanine (DIP) (III), synthesis of optically pure 1,2,3,4-tetrahydro-4-phenyl-3-isoquinolinecarboxylic acids, novel α-amino acids for peptides of biological interest
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All four isomers of 1,2,3,4-tetrahydro-4-phenyl-3-isoquinolinecarboxylic acid have been synthesized in high optical purity for the synthesis of peptides of biological interest.
- Chen,Goel
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