US5002956A
Expired / Lapsed
US
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Use of heterocyclic compounds for iontophoretic treatment
Assignee: Individual
•
Filing: 1989-03-22
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Granted: 1991-03-26
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Expires: 2009-03-22
Abstract
Abstract What is disclosed is the use of dissociable heterocycle compounds from the group including aminoacridine, aminocholine and aminopyridine as well as their derivatives substituted on the basic structure, which are present in tautomeric diimine form, for the selective iontophoretic treatment or for production of a pharmaceutical for iontophoretic treatment and relapse prophylaxis of bladder cancer as well as for iontophoretic treatment of malignant skin and mucus membrane tumors. It is further disclosed and proven that the antineoplastic effect observed with use of the above compositions in animal experiments and in clinical treatment is selective and healthy tissue is not damaged. The common denominator for the characteristic and proven antineoplastic selective effect of the three classes of materials is the tautomeric diimine form. As a pre- and/or post-treatment medium with the treatment of bladder cancer, preferably a lubricant, anesthetic and prophylactic medium is used, which includes (a) a nonionic, water miscible lubricant with an electric conductivity lower than 2 mS/cm and a viscosity (at 25° C.) in the range of 50 to 2000 mPa.s, and (b) a local, nonionic mucus membrane anesthetic which does not penetrate into the bloodstream, in which the mixture of (a) and (b) has a pH level between approximately 5 and 7.5, preferably between 6.5 and 6.8.
Inventors
- 👤 Karl H. Thiel
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 20:51
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/47
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
44 words
In the treatment of solid tumors, the improvement comprising applying to the tumor in an iontophoretic process a dissociable heterocyclic compound selected from the group consisting of aminoacridine, aminoquinoline and aminopyridine compounds in tautomeric diimine form in which the active ingredient is a cation.
Claim 2
Dependent Claim
44 words
In the treatment of solid tumors, the improvement comprising applying to the tumor in an iontophoretic process a dissociable heterocyclic compound selected from the group consisting of aminoacridine, aminoquinoline and aminopyridine compounds in tautomeric diimine form in which the active ingredient is a cation.
Claim 3
Dependent Claim
15 words
The treatment of claim 1 in which the heterocyclic compound is present in salt form.
Claim 4
Dependent Claim
17 words
The treatment of claim 2 in which the heterocyclic compound is present as a physiologically compatible salt.
Claim 5
Dependent Claim
22 words
The treatment of claim 3 in which said physiologically compatible salt is selected from mono- or di-chloride, sulfate, lactate or acetate salts.
Claim 6
Dependent Claim
12 words
The treatment of claim 1 in which the heterocyclic compound is proflavine-monohydrochloride.
Claim 7
Dependent Claim
21 words
The treatment of claim 1 in which the heterocyclic compound is present in a mixture with dimethyl sulfoxide in aqueous solution.
Claim 8
Dependent Claim
26 words
The treatment of claim 1 in which the heterocyclic compound is in aqueous solution in a concentration of 0.05 g/l up to the limit of solubility.
Claim 9
Dependent Claim
19 words
The treatment of claim 6 in which said heterocyclic compound is present in a concentration up to 5 g/l.
Claim 10
Dependent Claim
23 words
The treatment of claim 7 in which said dimethyl sulfoxide is employed in aqueous solution in a concentration of 20 to 300 g/l.
Claim 11
Dependent Claim
31 words
The treatment of claim 7 in which the iontophoretic treatment is applied by means of a direct current, and the current density applied is not higher than 0.5 mA/cm 2 .
Claim 12
Dependent Claim
26 words
The treatment of claim 1 in which the malignant tissue is a bladder, and the composition is introduced into the bladder through a positive tubular electrode.
Claim 13
Independent Claim
29 words
A method of treating solid tumors comprising applying to the tumor in an iontophoretic process, a therapeutically effective amount of an aminoacridine salt in its cationic tautomeric diimine form.
Claim 14
Independent Claim
29 words
A method of treating solid tumors comprising applying to the tumor in an iontophoretic process, a therapeutically effective amount of an aminoacridine salt in its cationic tautomeric diimine form.
Claim 15
Dependent Claim
11 words
The method of claim 12 in which the aminoacridine is proflavine-monohydrochloride.
Claim 16
Dependent Claim
52 words
A pharmaceutical composition for the treatment of solid tumors in an iontophoretic process, said composition comprising an aqueous solution of a dissociable heterocyclic compound selected from the group consisting of aminoacridine, aminoquinoline and aminopyridine compounds in their tautomeric diimine form, in which the active ingredient is a cation, in admixture with dimethylsulfoxide.
Claim 17
Dependent Claim
52 words
A pharmaceutical composition for the treatment of solid tumors in an iontophoretic process, said composition comprising an aqueous solution of a dissociable heterocyclic compound selected from the group consisting of aminoacridine, aminoquinoline and aminopyridine compounds in their tautomeric diimine form, in which the active ingredient is a cation, in admixture with dimethylsulfoxide.
Claim 18
Dependent Claim
12 words
The composition of claim 14 in which the compound is an aminoacridine.
Claim 19
Dependent Claim
11 words
The composition of claim 15 in which the aminoacridine is proflavine-monohydrochloride.
Claim 20
Independent Claim
55 words
A method of using a dissociable heterocyclic compound selected from the group consisting of aminoacridine, aminoquinoline and aminopyridine compounds, which are present in their tautomeric diimine form, in which the active ingredient is a cation, comprising adding said compound to an aqueous solution for the iontophoretic treatment and relapse or recidivism prophylaxis of solid tumors.
Claim 21
Independent Claim
55 words
A method of using a dissociable heterocyclic compound selected from the group consisting of aminoacridine, aminoquinoline and aminopyridine compounds, which are present in their tautomeric diimine form, in which the active ingredient is a cation, comprising adding said compound to an aqueous solution for the iontophoretic treatment and relapse or recidivism prophylaxis of solid tumors.
References Cited (Backward Citations)
US4314061A
Cited
US4824676A
Cited
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