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1. WO2004008101 - THE USE OF ISOCYANATE LINKERS TO MAKE HYDROLYZABLE ACTIVE AGENT BIOPOLYMER CONJUGATES

Publication Number WO/2004/008101
Publication Date 22.01.2004
International Application No. PCT/US2003/021839
International Filing Date 11.07.2003
Chapter 2 Demand Filed 02.02.2004
IPC
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
CPC
A61K 47/60
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • BIOMARIN PHARMACEUTICAL INC. [US]/[US] (AllExceptUS)
  • CHEN, Qingqi [CA]/[CA] (UsOnly)
  • SOWA, Damian [CA]/[CA] (UsOnly)
  • GABATHULER, Reinhard [CA]/[CA] (UsOnly)
Inventors
  • CHEN, Qingqi
  • SOWA, Damian
  • GABATHULER, Reinhard
Agents
  • NABEELA, R., McMillian, Ph., D.
Priority Data
60/395,76212.07.2002US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) THE USE OF ISOCYANATE LINKERS TO MAKE HYDROLYZABLE ACTIVE AGENT BIOPOLYMER CONJUGATES
(FR) UTILISATION D'AGENTS DE LIAISON ISOCYANATE POUR PRODUIRE DES CONJUGUES BIOPOLYMERE-SUBSTANCE ACTIVE HYDROLYSABLES
Abstract
(EN)
The invention provides bioconjugates of the formula: (I) in which A is an active agent comprising an active hydroxy or amino functionality and B is a biopolymer comprising an active hydroxy or amino functionality, and X1 and X2 are independently N or O, and R is substituted alkyl or unsubstituted alkyl or unsubstituted or substituted heteroalkyl from 1 to about 30 atoms in length. The biopolymer may for instance be a transport protein or an antibody directed to a transport protein (e.g., a p97 protein or antibody thereto). The active agent may be a therapeutic agent such as a chemotherapeutic agent or an antineoplastic agent or an enzyme. The bioconjugates find therapeutic usages according to the therapeutic indications of the active agents. Methods of making the bioconjugates and bifunctional isocyanate cross linking reagents of use in making such bioconjugates are provided.
(FR)
La présente invention concerne des bioconjugués de formule (I) dans laquelle: A est une substance active ayant une fonctionnalité hydroxy ou amino active et B est un biopolymère ayant une fonctionnalité hydroxy ou amino active; X1 et X2 sont indépendamment N ou R; et R est alkyle substitué ou non ou hétéroalkyle substitué ou non de longueur de 1 à environ 30 atomes. Le biopolymère peut par exemple être une protéine de transport ou un anticorps dirigé contre une protéine de transport (par ex. une protéine p97 ou un anticorps dirigé contre celle-ci). La substance active peut être un agent thérapeutique tel qu'un agent de chimiothérapie ou un agent antinéoplasique ou une enzyme. Les bioconjugués trouvent des applications thérapeutiques en fonctions des indications thérapeutiques de la substance active. L'invention a également pour objet des procédés pour produire les bioconjugués et des réactifs de réticulation isocyanate bifonctionnels utilisés pour produire lesdits bioconjugués.
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