EP1207909A2 - Procede de couplage de molecules - Google Patents

Procede de couplage de molecules

Info

Publication number
EP1207909A2
EP1207909A2 EP00956666A EP00956666A EP1207909A2 EP 1207909 A2 EP1207909 A2 EP 1207909A2 EP 00956666 A EP00956666 A EP 00956666A EP 00956666 A EP00956666 A EP 00956666A EP 1207909 A2 EP1207909 A2 EP 1207909A2
Authority
EP
European Patent Office
Prior art keywords
group
chemical compound
compound according
formula
residue
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP00956666A
Other languages
German (de)
English (en)
Inventor
Michael John Gait
Dmitry Stetsenko
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Medical Research Council
Original Assignee
Medical Research Council
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
Priority claimed from GBGB9920397.8A external-priority patent/GB9920397D0/en
Priority claimed from GB0012083A external-priority patent/GB0012083D0/en
Application filed by Medical Research Council filed Critical Medical Research Council
Publication of EP1207909A2 publication Critical patent/EP1207909A2/fr
Withdrawn legal-status Critical Current

Links

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.

Landscapes

  • 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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne un procédé de liaison d'une première molécule M1-NH2 avec une seconde molécule M2-OH, consistant à faire réagir un composé représenté par la formule (I) M1-NH-CO-A-CO-SR1 avec un composé représenté par la formule (II). Dans la formule (I), M1 est le résidu d'une molécule portant un groupe amino, A représente un groupe alkylène ou arylène, et R1 représente alkyle ou aryle. Dans la formule (II), M2 est le résidu d'une molécule portant un groupe hydroxy, B est un liant, D représente un groupe alkylène C¿1-4? ou un groupe arylène C3-12, et R?2¿ représente hydrogène ou un groupe de protection de thiol. L'invention concerne également des produits de conjugaison de la réaction de couplage, des réactifs destinés à modifier M1-NH2 et M2-OH, et des kits comprenant ces réactifs.
EP00956666A 1999-08-27 2000-08-25 Procede de couplage de molecules Withdrawn EP1207909A2 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB9920397.8A GB9920397D0 (en) 1999-08-27 1999-08-27 Method for coupling molecules
GB9920397 1999-08-27
GB0012083 2000-05-18
GB0012083A GB0012083D0 (en) 2000-05-18 2000-05-18 Method for coupling molecules
PCT/GB2000/003306 WO2001015737A2 (fr) 1999-08-27 2000-08-25 Procede de couplage de molecules

Publications (1)

Publication Number Publication Date
EP1207909A2 true EP1207909A2 (fr) 2002-05-29

Family

ID=26244310

Family Applications (1)

Application Number Title Priority Date Filing Date
EP00956666A Withdrawn EP1207909A2 (fr) 1999-08-27 2000-08-25 Procede de couplage de molecules

Country Status (5)

Country Link
EP (1) EP1207909A2 (fr)
JP (1) JP2003508450A (fr)
AU (1) AU6853900A (fr)
CA (1) CA2382499A1 (fr)
WO (1) WO2001015737A2 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7569392B2 (en) 2004-01-08 2009-08-04 Vanderbilt University Multiplex spatial profiling of gene expression
AU2010306940A1 (en) 2009-10-12 2012-06-07 Smith, Larry Methods and compositions for modulating gene expression using oligonucleotide based drugs administered in vivo or in vitro
RU2708237C2 (ru) 2014-08-22 2019-12-05 Общество с ограниченной ответственностью "НооГен" Модифицированные олигонуклеотиды и способ их получения
JP7194635B2 (ja) * 2019-04-25 2022-12-22 あおみ建設株式会社 隙間の充填工法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0115737A2 *

Also Published As

Publication number Publication date
AU6853900A (en) 2001-03-26
CA2382499A1 (fr) 2001-03-08
JP2003508450A (ja) 2003-03-04
WO2001015737A3 (fr) 2001-11-15
WO2001015737A2 (fr) 2001-03-08

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