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EP0737077A1 - Conjugues de medicaments a ciblage hepatocytaire - Google Patents

Conjugues de medicaments a ciblage hepatocytaire

Info

Publication number
EP0737077A1
EP0737077A1 EP95908490A EP95908490A EP0737077A1 EP 0737077 A1 EP0737077 A1 EP 0737077A1 EP 95908490 A EP95908490 A EP 95908490A EP 95908490 A EP95908490 A EP 95908490A EP 0737077 A1 EP0737077 A1 EP 0737077A1
Authority
EP
European Patent Office
Prior art keywords
conjugate
crosslinker
ligand
covalently bonded
carrier molecule
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Withdrawn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
EP95908490A
Other languages
German (de)
English (en)
Inventor
Robert Plourde, Jr.
Ellen Carmichael
George L. Spitalny
Mark A. Findeis
Michael F. Ernst
Brett Robinson
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.)
TargeTech Inc
Original Assignee
TargeTech Inc
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 TargeTech Inc filed Critical TargeTech Inc
Publication of EP0737077A1 publication Critical patent/EP0737077A1/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Withdrawn legal-status Critical Current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
    • 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
    • A61K47/56—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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/61—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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof

Landscapes

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

Abstract

Cette invention concerne des conjugués utilisés pour cibler un agent thérapeutique sur une cellule comprenant des récepteurs d'asialoglycoprotéine. Ces conjugués comprennent un agent thérapeutique et un ligand destiné au récepteur d'asialoglycoprotéine, ledit agent thérapeutique et ledit ligand étant liés par un agent de pontage. L'agent de pontage peut être un agent de réticulation, une molécule porteuse polyfonctionnelle ou un agent de réticulation et une molécule porteuse polyfonctionnelle. Dans une forme de réalisation préférée l'agent thérapeutique est un analogue nucléosidique ou de la colchicine et le ligand est de l'asialoorosomucoïde, de l'arabinogalactane ou un tri-(N-acétyle galactosamine aminohexyle glycoside) amide de tyrosyl(glutamyl)-glutamate. Les agents de réticulation préférés comprennent les dérivés d'aminoacyle, les dérivés de carboxyacyle, le phosphate, les peptides et les agents de réticulation labiles par réduction. Les molécules porteuses polyfonctionnelles comprennent les acides polyamino et les polysaccharides. On peut utiliser les conjugués de cette invention pour cibler un agent thérapeutique sur une cellule, par exemple pour inhiber la réplication d'ADN viral dans un hépatocyte infecté par un virus.
EP95908490A 1994-01-11 1995-01-11 Conjugues de medicaments a ciblage hepatocytaire Withdrawn EP0737077A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18020794A 1994-01-11 1994-01-11
US180207 1994-01-11
PCT/US1995/000448 WO1995018636A2 (fr) 1994-01-11 1995-01-11 Conjugues de medicaments a ciblage hepatocytaire

Publications (1)

Publication Number Publication Date
EP0737077A1 true EP0737077A1 (fr) 1996-10-16

Family

ID=22659615

Family Applications (1)

Application Number Title Priority Date Filing Date
EP95908490A Withdrawn EP0737077A1 (fr) 1994-01-11 1995-01-11 Conjugues de medicaments a ciblage hepatocytaire

Country Status (5)

Country Link
EP (1) EP0737077A1 (fr)
JP (1) JPH09510696A (fr)
AU (1) AU1679195A (fr)
CA (1) CA2180348A1 (fr)
WO (1) WO1995018636A2 (fr)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6296844B1 (en) 1995-09-27 2001-10-02 The General Hospital Corporation Asialocytokines and treatment of liver disease
WO1997021452A2 (fr) * 1995-12-14 1997-06-19 Advanced Magnetics, Inc. Promedicaments macromoleculaires d'analogues de nucleotides
US6919076B1 (en) 1998-01-20 2005-07-19 Pericor Science, Inc. Conjugates of agents and transglutaminase substrate linking molecules
JP5750209B2 (ja) * 2007-03-16 2015-07-15 アプタ バイオサイエンス リミテッド 機能性分子、機能性分子合成用アミダイド、及び標的物質解析方法
JP2013516967A (ja) * 2010-01-14 2013-05-16 グラクソ グループ リミテッド 肝臓標的化ドメイン抗体
JP5849336B2 (ja) * 2010-10-27 2016-01-27 公立大学法人横浜市立大学 アデニル酸シクラーゼの活性調節剤
US12064445B2 (en) 2015-12-03 2024-08-20 Biosight Ltd. Cytarabine conjugates for cancer therapy
US12071450B2 (en) 2015-12-03 2024-08-27 Biosight Ltd. Salts of conjugates for cancer therapy
WO2017093993A1 (fr) * 2015-12-03 2017-06-08 Biosight Ltd. Conjugués de cytarabine pour le traitement du cancer
IL259569B2 (en) 2015-12-03 2024-03-01 Biosight Ltd Salts of cytarabine-amino acids conjugates
CN108610384B (zh) * 2018-05-31 2022-02-22 沈阳药科大学 基于肠道mct1载体蛋白设计的前药及其制备方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0538268A4 (en) * 1990-05-11 1993-05-12 The University Of Connecticut Targeted protection from cytotoxins
US5656609A (en) * 1992-09-24 1997-08-12 University Of Connecticut Method of enhancing and/or prolonging expression of gene introduced into a cell using colchicine

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9518636A2 *

Also Published As

Publication number Publication date
AU1679195A (en) 1995-08-01
WO1995018636A2 (fr) 1995-07-13
WO1995018636A3 (fr) 1995-08-10
CA2180348A1 (fr) 1995-07-13
JPH09510696A (ja) 1997-10-28

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Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

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17P Request for examination filed

Effective date: 19960802

AK Designated contracting states

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18W Application withdrawn

Withdrawal date: 19991102