WO2002068586A3 - Inhibiteurs de proteases de vih/vif - Google Patents

Inhibiteurs de proteases de vih/vif Download PDF

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Publication number
WO2002068586A3
WO2002068586A3 PCT/US2002/001695 US0201695W WO02068586A3 WO 2002068586 A3 WO2002068586 A3 WO 2002068586A3 US 0201695 W US0201695 W US 0201695W WO 02068586 A3 WO02068586 A3 WO 02068586A3
Authority
WO
WIPO (PCT)
Prior art keywords
hiv
drug
protease inhibitors
resistant
fiv
Prior art date
Application number
PCT/US2002/001695
Other languages
English (en)
Other versions
WO2002068586A2 (fr
Inventor
Chi-Huey Wong
Original Assignee
Scripps Research Inst
Chi-Huey Wong
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Scripps Research Inst, Chi-Huey Wong filed Critical Scripps Research Inst
Priority to AU2002255485A priority Critical patent/AU2002255485A1/en
Publication of WO2002068586A2 publication Critical patent/WO2002068586A2/fr
Publication of WO2002068586A3 publication Critical patent/WO2002068586A3/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D277/06—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • AIDS & HIV (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Le recours à la modélisation moléculaire et à des analyses structurales radiographiques de protéases de VIH résistant à l'action des médicaments a permis de développer un nouveau type d'inhibiteurs présentant un reste P3 limité. Ces inhibiteurs sont efficaces contre le VIH et ses mutants résistant à l'action des médicaments, ainsi que contre le VIF. La modification d'inhibiteurs de protéases du VIH existants par réduction de la taille du reste P3 présente le même effet. Cette découverte constitue une nouvelle stratégie de développement d'inhibiteurs de protéases du VIH efficaces contre les mutants de type sauvage et résistant à l'action des médicaments et fait apparaître que la protéase du VIF est un modèle utile pour des protéases du VIH résistant à l'action des médicaments, lesquelles sont souvent développées par réduction de la taille de la région de liaison du groupe P3 ou des groupes P3 et P1 combinés.
PCT/US2002/001695 2001-01-19 2002-01-22 Inhibiteurs de proteases de vih/vif WO2002068586A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002255485A AU2002255485A1 (en) 2001-01-19 2002-01-22 Hiv/fiv protease inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26284601P 2001-01-19 2001-01-19
US60/262,846 2001-01-19

Publications (2)

Publication Number Publication Date
WO2002068586A2 WO2002068586A2 (fr) 2002-09-06
WO2002068586A3 true WO2002068586A3 (fr) 2007-11-15

Family

ID=22999309

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/001695 WO2002068586A2 (fr) 2001-01-19 2002-01-22 Inhibiteurs de proteases de vih/vif

Country Status (2)

Country Link
AU (1) AU2002255485A1 (fr)
WO (1) WO2002068586A2 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112014010042B1 (pt) * 2011-10-26 2022-03-03 Allergan, Inc Derivados de amida de aminoácidos n-ureia substituídos como moduladores de receptor tipo receptor de peptídeo formila 1 (fprl-1)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6043357A (en) * 1994-12-02 2000-03-28 The University Of Queensland HIV protease inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6043357A (en) * 1994-12-02 2000-03-28 The University Of Queensland HIV protease inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MAK ET AL.: "Design, synthesis and biological evaluation of HIV-FIV protease inhibitors incorporating a coformationally contrained macrocyte and a small P3' residue", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 11, no. 2, 22 January 2001 (2001-01-22), pages 219 - 222, XP004314852 *

Also Published As

Publication number Publication date
AU2002255485A8 (en) 2008-01-10
AU2002255485A1 (en) 2002-09-12
WO2002068586A2 (fr) 2002-09-06

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