Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
  • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
  • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
  • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

• aryloxy means aryl -O- and "aryloyl” means aryl -CO.
• Aryl substituent groups or aryl-containing substituent groups may comprise one or more further substituents.
• J is an alkylene or arylene group and X is the residue of a functional group capable of reacting with a hydroxy group.
• the coupling reagents (III) and (IV) may be prepared by procedures such as those described in Reaction Schemes 2 and 3. It will be appreciated that coupling reagents of general formulae (III) and (IV) may be prepared by modification of the procedures shown in Reaction Schemes 1 and 2 in accordance with conventional synthetic organic chemistry.
• the compound of formula (IV) may be used to produce a compound of formula (II) by reaction with a second molecule M 2 -OH.
• the compound of formula (II) is then coupled with a compound of formula (I).
• the thiol group of the compound of formula (VI) is particularly suited to further derivatisation or functionalisation and can, for example, provide a site for attachment of a labelling, reporter or effector group. Accordingly, the invention further provides a chemical compound of the formula (VII)
• Reaction mixture was then evaporated to dryness, redissolved in ethylacetate and washed successively with ice-cold 5% wt. citric acid, water, sodium bicarbonate and brine, dried over sodium sulfate, and evaporated to a light brown foam.
• the residue was chromatographed on silica gel column eluted by 15-5% hexane in ethylacetate - 0.5% triethylamine, appropriate fractions were pooled and evaporated to give 1.3045 g (95%) of the title product as a white foam.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Chemical & Material Sciences (AREA)
• Veterinary Medicine (AREA)
• Engineering & Computer Science (AREA)
• Medicinal Chemistry (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• General Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Proteomics, Peptides & Aminoacids (AREA)
• Epidemiology (AREA)
• Peptides Or Proteins (AREA)
• Medicinal Preparation (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Applications Claiming Priority (5)

Publications (1)

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• 2000
  • 2000-08-25 CA CA002382499A patent/CA2382499A1/en not_active Abandoned
  • 2000-08-25 JP JP2001520148A patent/JP2003508450A/ja active Pending
  • 2000-08-25 WO PCT/GB2000/003306 patent/WO2001015737A2/en not_active Application Discontinuation
  • 2000-08-25 AU AU68539/00A patent/AU6853900A/en not_active Abandoned
  • 2000-08-25 EP EP00956666A patent/EP1207909A2/de not_active Withdrawn

Non-Patent Citations (1)

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