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Title:  Conjugate for treating inflammatory infectious and/or skin diseases

United States Patent:  6,706,713

Issued:  March 16, 2004

Inventors:  Sinn; Hansjorg (Wiesloch, DE); Schrenk; Hans-Hermann (Zeiskamm, DE); Maier-Borst; Wolfgang (Dossenheim, DE); Stehle; Gerd (Jahnstrasse 1, D-89584 Ehingen, DE)

Assignee:  Deutsches Krebsforschungszentrum Stiftung des Offentlichen Rechts (Heidelberg, DE); Stehle; Gerd (Ehingen, DE)

Appl. No.:  949592

Filed:  October 14, 1997

PCT Filed:  April 12, 1996

PCT NO:  PCT/DE96/00644

PCT PUB.NO.:  WO96/32133

PCT PUB. Date:  October 17, 1996

Abstract

This invention relates to the use of a conjugate comprising an active substance and a native protein which is not recognized as foreign protein for the production of a pharmaceutical preparation for treating and/or diagnosing inflammatory, infectious and/or skin diseases.

SUMMARY OF THE INVENTION

This invention relates to the use of a conjugate comprising an active substance and a native protein which is not recognized as foreign protein for the production of a pharmaceutical preparation for treating and/or diagnosing inflammatory, infectious and/or skin diseases.

DETAILED DESCRIPTION OF THE INVENTION

According to the present invention a conjugate consisting of a tumor-active compound and a native protein which is not recognized as a foreign protein (see, DE-A-41 22 210) is used for the production of a pharmaceutical preparation for treating and/or diagnosing inflammatory, infectious and/or skin diseases such as psoriasis.

The expression "active substance" comprises compounds of any kind, which can be used for treating and/or diagnosing inflammatory, infectious and/or skin diseases. Examples of such compounds are photoactive compounds and chemotherapeutic agents. Examples of photoactive compounds are porphins such as o-, n-, and/or p-tetracarboxyphenyl porphines chlorins, bacteriochlorins, phthalocyanines and derivatives thereof. The photoactive compounds may optionally include a metal and/or a metal ion. Examples of chemotherapeutic agents are cytostatic agents and antibiotics. Representatives thereof are, e.g., doxorubicin, daunorubicin, tetracyclines, antraquinone-2-carboxylic acid, carminic acid, platinum complexes and methotrexate (MTX).

The above compounds may be labeled detectably. This may be effected, e.g., by means of a radioactive substance such as iodine. It is also favorable for the above compounds to have an acid function, e.g., a carboxyl group. This facilitates their bonding to the "protein".

One or more of the above compounds may be present in a conjugate used according to the invention. If several compounds are present, they may be the same or differ from one another.

The expression "protein" comprises proteins of any kind, which are suitable to enrich above compounds linked therewith in cells or tissues which are affected with the above diseases. Examples of such proteins are those proteins that have a molecular weight up to 90,000 dalton such as albumin, especially human serum albumin (HSA), and transferrin.

Conjugates used according to the invention may be produced according to conventional methods. For example, the production may be carried out according to the process described in DE-A-41 22 210.

Conjugates used according to the invention distinguish themselves by accumulating in cells and tissues which are affected with inflammatory processes. Therefore, minor doses of these conjugates suffice to treat such processes, which minimizes the load for the body. Hence the conjugates used according to the invention are suited in the best possible way to treat and/or diagnose inflammatory, infectious and/or skin diseases.

The below example explains the invention in more detail. The following preparations and example are given to enable those skilled in the art to more clearly understand and to practice the present invention. The present invention, however, is not limited in scope by the exemplified embodiments, which are intended as illustrations of single aspects of the invention only, and methods which are functionally equivalent are within the scope of the invention. Indeed, various modifications of the invention in addition to those described herein will become apparent to those skilled in the art from the foregoing description and accompanying drawings. Such modifications are intended to fall within the scope of the appended claims.

Claim 1 of 14 Claims

What is claimed is:

1. A method of diagnosing an inflammatory disease comprising administering a pharmaceutical composition comprising a conjugate and a pharmaceutically acceptable carrier, said conjugate comprising:

(a) an active substance selected from the group consisting of porphines, chlorins, bacteriochlorins, phthalocyanines, doxorubicin, daunorubicin, tetracyclines, anthraquinone-2-carboxylic acid, carminic acid and methotrexate; and

(b) albumin,

wherein the active substance is covalently bound to the albumin, and the albumin is in its native form.





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