Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1997-09-23
1999-05-25
Jarvis, William R. A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514152, 514183, 514249, A61K 3838, A61K 3840, A61K 3165, A61K 3133, A61K 3150
Patent
active
059069775
DESCRIPTION:
BRIEF SUMMARY
I. FIELD OF THE INVENTION
The present invention relates to the use of conjugates comprising an active substance, a linker and a carrier, for treating and/or diagnosing inflammatory diseases.
II. BACKGROUND OF THE INVENTION
For treating inflammatory diseases such as infectious and/or autoimmune and/or skin diseases, pharmaceutical preparations which have to be administered in very high doses have been used so far. This represents a major load for the liver. In addition, these pharmaceutical preparations concentrate in many tissues which represents a further load for the body.
DE-A 39 12 792 and DE-A-40 17 439 disclose conjugates of the above kind which can be used for treating and/or diagnosing tumors.
Surprisingly, it has not been found that these conjugates are also suitable for treating and/or diagnosing inflammatory diseases such as infectious and/or autoimmune and/or skin diseases and/or inflammatory neovascularizations, e.g., in the cornea of the eye, without being accompanied by the drawbacks of the pharmaceutical preparations used for this purpose so far.
Thus, the above conjugates are used according to the invention for the treating and/or diagnosing inflammatory diseases such as infectious and/or autoimmune and/or skin diseases, such as psoriasis, and/or inflammatory neovascularizations, e.g., in the cornea of the eye.
III. SUMMARY OF THE INVENTION
The present invention relates pharmaceutical compositions comprising a conjugate of an active substance, a linker and a carrier for the treatment and/or diagnosis of inflammatory diseases. The present invention further relates to methods using such pharmaceutical compositions for treating and diagnosing of inflammatory diseases including, but not limited to, infectious diseases, autoimmune diseases, skin diseases, and inflammatory neovascularization.
IV. BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 shows the linkage of radioactively labeled tyramine-N-1'-deoxysorbitol (TDS) to albumin via cyanuric chloride,
FIG. 2 shows the linkage of tetracarboxyphenylporphyrin (TCPP) to albumin,
FIG. 3 shows the linkage of tetrahydroxyphenylporphyrin (THOPP) to methoxypolyethylene glycol (MPEG) via cyanuric chloride, and
FIG. 4 shows the concentration of conjugates in inflammatory tissue.
V. DETAILED DESCRIPTION OF THE INVENTION
The expression "active substance" comprises compounds of any kind which can be used for treating and/or diagnosing inflammatory diseases, particularly infectious and/or autoimmune and/or skin diseases and/or inflammatory neovascularizations. Examples of the above compounds are radioactively labeled aromatic compounds, photodynamically active compounds and chemotherapeutic agents. Examples of photodynamically active compounds are porphyrin derivatives such as tetracarboxyphenylporphyrin (TCPP) and tetrahydroxyphenylporphyrin (THOPP), chlorines and bacteriochlorines. Examples of chemotherapeutic agents are cytostatic agents and antibiotics. Representatives thereof are, e.g., doxorubicin, daunorubicin, tetracycline and derivatives thereof as well as antimetabolites such as methotrexate. The above photodynamically active compounds and chemotherapeutic agents may also be labeled, e.g., by means of a radioactive substance such as iodine. In addition, a conjugate used according to the invention may not only contain a single but also several of the compounds.
The expression "linker" comprises compounds of any kind which are suitable for linking two components of the conjugate, particularly protein and active substance. Examples of such linkers are cyanuric chloride and derivatives thereof which are used as educt for forming the conjugate. Furthermore, a linker may already be part of the active substance, so that no further linker has to be incorporated into the conjugate. An example of this is given in FIG. 2.
The expression "carrier" comprises compounds of any kind which are suitable for concentrating the conjugate in a tissue damaged by an above disease. Examples thereof are proteins which are not considered exogenous and polyethylene glyco
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Hamblin et al., "Conjugates Between Proteins and Fluorescent Dyes as Potential Photosensitizers," Photodynamic Therapy and Biomedical Lasers, Proceedings of the International Conference on Photodynamic Therapy and Medical Laser Applications, Milan, Jun. 24-27, 1992, P. Spinelli, M. Dal Fante, R. Marchesini, Istituto Nazionale per lo Studio e la Cura dei Tumori, 20133 Milan, Italy, Excerpta Medica, Amsterdam-London-New York-Tokyo, pp. 169-173.
Maxwell et al., 1988, "Insulin-.sup.125 I-Tyramine, an Improved Residualizing Label for Studies on Sites of Catabolism of Circulating Proteins," Journal of Biological Chemistry 263(28):14122-14127.
Winkelman, James W., 1967, "Metabolic Studies on the Accumulation of Tetraphenylporphinesulfonate in Tumors," Experientia 23(11):949-50.
Heene Dieter Ludwig
Hoff-Biederbeck Dirk
Maier-Borst Wolfgang
Schrenk Hans-Hermann
Sinn Hansjorg
Deutsches Krebsforschungszentrum Stiftung des offentlichen Recht
Jarvis William R. A.
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