Conjugate of an active agent, a polyether and possibly a native

Details Conjugate of an active agent, a polyether and possibly a native Conjugate of an active agent, a polyether and possibly a native

1997-10-14

2000-11-21

Davenport, Avis M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530324, 530403, 424 854, A61K 3800, A61K 3816, C07K 100, C07K 700

Patent

active

061503274

DESCRIPTION:

BRIEF SUMMARY
This is a national phase filing of the Application No. PCT/DE96/00653, which was filed with the Patent Corporation Treaty on Apr. 12, 1996, and is entitled to priority of the German Patent Application 195 14 087.7, filed Apr. 13, 1995.


I. FIELD OF THE INVENTION

The present invention relates to a conjugate comprising an active substance component, a polyether component and optionally a native protein component which is not regarded as exogenous, a process for the preparation of such a conjugate as well as its use.


II. BACKGROUND OF THE INVENTION

It has long been a demand of concentrating pharmaceutical preparations in well-calculated fashion at the site of action. In particular when tumoral diseases, infectious diseases, skin diseases and/or diseases of the immune system are treated, it is desired to concentrate pharmaceutical preparations in the cells and tissues affected by these diseases. In addition, it is intended to eliminate the pharmaceutical preparations in case they do not reach the site of action. This is to serve for minimizing the strain of the body, caused by the pharmaceutical preparations.
Therefore, it is the object of the present invention to provide a possibility serving for achieving the above.


III. SUMMARY OF THE INVENTION

The present invention relates to a conjugate comprising an active substance component, a polyether component and optionally a native protein component which is not regarded as exogenous, the components being linked via an acid amide and/or acid ester bond.
In addition, this invention relates to a process for the preparation of such a conjugate as well as its use.


IV. BRIEF DESCRIPTION OF THE DRAWINGS

FIGS. 1A and 1B show the preparation of a conjugate according to the invention consisting of TCPP, amino PEG and HSA.
FIG. 2 shows the preparation of a conjugate according to the invention consisting of THPP and 4 PEGs.
FIG. 3 shows the preparation of a conjugate according to the invention consisting of aluminum-phthalocyanintetrasulfonate-aminoPEG.
FIG. 4 shows the scintigraphic detection of the absorption of the HSA-TCPP-aminoPEG conjugate (FIGS. 1A and 1B) by a Walker carcinosarcoma as compared to the cardiac and liver regions.


V. DETAILED DESCRIPTION OF THE INVENTION

It has long been a demand of concentrating pharmaceutical preparations in well-calculated fashion at the site of action. According to the invention this is attained by a conjugate comprising an active substance component, a polyether component and optionally a native protein component not regarded as exogenous, which is characterized in that the components are linked via an acid amide and/or acid ester bond.
The components of the conjugate according to the invention are given as educts below. In the conjugate according to the invention they are present in derivatized form.
The expression "active substance" comprises compounds of any kind which can be used for treating and/or diagnosing diseases such as tumoral diseases, infectious diseases, skin diseases and/or diseases of the immune system, and which are capable of forming acid amide and/or acid ester bonds.
Such compounds may be chemotherapeutic agents, e.g., antibiotics, virostatics, antiprotozoals and cytostatic agents. Examples of antibiotics are sulfonamides, tetracyclines, e.g., 7-chlorotetracycline, fusidic acid, gyrase inhibitors, e.g., quinolones, amphotericin, isoniazid, pyrazine-2-carboxylic acid and pyrazinamide. Examples of virostatics are amantadine and rimantadine. Examples of antiprotozoals are mefloquin and primaquin. Examples of cytostatic agents are anthracyclines, e.g., doxorubicin, topoisomerase inhibitors, mitomyclin A and C, bleomycinic acid, chlorambucil, melphalan and antifolates, e.g., methotrexate.
In addition, such a compound may be a photoactive compound, particularly a photoactive compound which is photoactive in aqueous media. Examples thereof are porphyrins, such as o-, m- and/or p-tetrahydroxyphenylporphin (THPP), o-, m- and/or p-tetracarboxyphenylporphin (TCPP), and o-, m- and/or p-tetrasulfophenylporphin,

REFERENCES:
patent: 4902502 (1990-02-01), Nitecki et al.
patent: 5382657 (1995-01-01), Karasiewicz et al.
Bonina et al., 1995, "In Vitro and In Vivo Evaluation of Polyoxyethylene omethacin Esters as Dermal Prodrugs," Journal of Controlled Release 34(3):223-232.
Miron et al., 1993, "A Simplified Method for the Preparation of Succinimidyl Carbonate Polyethylene Glycol for Coupling to Proteins," Bioconjugate Chemistry 4(6):568-569.

Affiliated with

Also associated with

Rating

Conjugate of an active agent, a polyether and possibly a native does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Conjugate of an active agent, a polyether and possibly a native , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Conjugate of an active agent, a polyether and possibly a native will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1257175