Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – In an organic compound
Reexamination Certificate
1999-05-04
2002-05-28
Russel, Jeffrey E. (Department: 1653)
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
In an organic compound
C424S009340, C424S009400, C424S009600, C514S002600, C530S345000, C530S410000
Reexamination Certificate
active
06395254
ABSTRACT:
This is a national phase filing of the Application No. PCT/DE96/02487, which was filed with the Patent Corporation Treaty on Dec. 20, 1996, and is entitled to priority of the German Patent Application 195 48 114.3, filed Dec. 21, 1995.
1. FIELD OF THE INVENTION
The present invention relates to conjugates, comprising an active substance, a polypeptide and a polyether, a process for the preparation of such conjugates as well as their use.
2. BACKGROUND OF THE INVENTION
There is a great demand of concentrating active substances at their site of action. This applies particularly to active substances for treating tumors and inflamed tissues, respectively. It is very often tried to obtain the active substance concentration by administration of high amounts of active substance. However, this leads to considerable side-effect in patients, particularly in their livers and kidneys.
Therefore, it is the object of the present invention to provide a possibility of concentrating active substances at their site of action.
3. SUMMARY OF THE INVENTION
The present invention relates to conjugates, comprising an active substance, a polypeptide and a polyether, a process for the preparation of such conjugates as well as their use.
4. BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1
shows a conjugate according to the invention, comprising polylysine (PL), 4 polyethylene glycols (PEG), 8 aminofluoresceins (AF1) and 2 diethylenetriaminepentaacetates (DTPA) labeled with
111
In, AF1 being linked via cyanuric chloride to free amino groups of PL, and DTPA being linked to PL via an acid amide bridge (SEQ ID NO:1).
FIG. 2
shows the distribution of the conjugate of
FIG. 1
according to the invention, measured by means of scintiscanning, in tumor tissue.
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Yokoyama et al., 1992, “Preparation of micelle-forming polymer-drug conjugates,”Bioconjugate Chemistry3(4):295-301.
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Fiebig Heinz H.
Maier-Borst Wolfgang
Schrenk Hans-Hermann
Sinn Hannsjörg
Stehle Gerd
Deutsches Krebsforschungszentrum Stiftung des Offentlichen Recht
Russel Jeffrey E.
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