The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
May. 08, 2007

Filed:

May. 02, 2001
Applicants:

Lutz F. Tietze, Göttingen, Tammannstr. 2 37077 Göttingen, DE;

Tobias Herzig, 33739 Bielefeld, DE;

Anja Fecher, 79576 Weil am Rhein, DE;

Inventors:

Lutz F. Tietze, Göttingen, Tammannstr. 2 37077 Göttingen, DE;

Tobias Herzig, 33739 Bielefeld, DE;

Anja Fecher, 79576 Weil am Rhein, DE;

Assignee:

Other;

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/403 (2006.01); A61K 31/437 (2006.01); C07D 209/82 (2006.01); C07D 209/94 (2006.01); C07D 221/12 (2006.01);
U.S. Cl.
CPC ...
Abstract

The chemotherapy of malignant tumours is greatly restricted by the generally slight differentiation of the available cytostatic agents between normal and malignant tissue. In order to achieve an improvement of the selectivity in cancer therapy, novel prodrugs have been developed from 6-hydroxy-2,3-dihydro-1H-indolene, 5-hydroxy-1,2-dihydro-3H-pyrrolo[3,2-e]indolene and 5-hydroxy-1,2-dihydro-3H-benzo[e]indolene as well as from 6-hydroxy-1,2,3,4-tetrahydro-benzo[f]-quinolines, that may be used within the framework of the ADEP therapy (antibody directed enzyme prodrug therapy). The new prodrugs are characterised by a high difference in toxicity between the prodrug and underlying drug and by a very high efficacy of the drug. After splitting off of the glycosidic and/or acetal group on the phenolic hydroxy groups of the prodrugs, a spirocyclopropacyclohexadiene is formed which, being a highly toxic group, effects an alkylation of the DNA or RNA.


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