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1. WO2007025763 - HIGHLY CROSS-LINKED REAGENTS FOR MODIFYING BIOPHARMACEUTICALS, PRODUCTION AND USE THEREOF

Publication Number WO/2007/025763
Publication Date 08.03.2007
International Application No. PCT/EP2006/008538
International Filing Date 31.08.2006
Chapter 2 Demand Filed 02.07.2007
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
C07C 323/52 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
323Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
50containing thio groups and carboxyl groups bound to the same carbon skeleton
51having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
52the carbon skeleton being acyclic and saturated
C07C 323/60 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
323Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
50containing thio groups and carboxyl groups bound to the same carbon skeleton
51having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
60with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
C07D 207/46 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
46with hetero atoms directly attached to the ring nitrogen atom
C07B 61/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
61Other general methods
A61K 31/40 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
CPC
A61K 31/40
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
Applicants
  • CELARES GMBH [DE]/[DE] (AllExceptUS)
  • KRÄHMER, Ralf [DE]/[DE] (UsOnly)
  • LEENDERS, Frank [DE]/[DE] (UsOnly)
Inventors
  • KRÄHMER, Ralf
  • LEENDERS, Frank
Agents
  • WEICKMANN & WEICKMANN
Priority Data
10 2005 041 570.901.09.2005DE
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) HOCH VERZWEIGTE REAGENZIEN ZUR MODIFIKATION VON BIOPHARMAZEUTIKA, DEREN HERSTELLUNG UND ANWENDUNG
(EN) HIGHLY CROSS-LINKED REAGENTS FOR MODIFYING BIOPHARMACEUTICALS, PRODUCTION AND USE THEREOF
(FR) REACTIFS HAUTEMENT RAMIFIES DESTINES A LA MODIFICATION DE PRODUITS BIOPHARMACEUTIQUES, LEUR PRODUCTION ET LEUR UTILISATION
Abstract
(DE)
Die vorliegende Erfindung betrifft Verbindungen, welche zur Kopplung an Pharmazeutika, insbesondere Biopharmazeutika geeignet sind, sowie Konjugate aus den Verbindungen mit Biomolekülen oder pharmazeutischen Wirkstoffen. Die erfindungsgemässen Verbindungen sind hoch verzweigt und können auf einfache Weise durch Verwendung eines zentralen Verzweigungsbausteins gebildet werden. Ein weiterer Gegenstand der Erfindung ist die Verwendung der Konjugate als verbesserte Formulierung von Pharmazeutika sowie deren Herstellung.
(EN)
The invention relates to compounds, which are suitable for coupling to pharmaceuticals, in particular biopharmaceuticals, in addition to conjugates from the compounds comprising biomolecules or pharmaceutically active substances. The inventive compounds are highly cross-linked and can be formed in a simple manner by using a central cross-linking module. The invention also relates to the use of conjugates as an improved formulation of pharmaceuticals and to the production thereof.
(FR)
La présente invention concerne des composés convenant au couplage à des produits pharmaceutiques, notamment à des produits biopharmaceutiques, ainsi que des conjugués de ces composés avec des biomolécules ou des principes actifs pharmaceutiques. Les composés selon l'invention sont hautement ramifiés et peuvent être formés de manière simple par l'utilisation d'un bloc de ramification central. En outre, l'invention concerne l'utilisation des conjugués en tant que formulation améliorée de produits pharmaceutiques et leur production.
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