Methods for inhibiting angiogenesis
AssigneeAntigen Biologicals Corporation
InventorsHamdi K. Hamdi, Jeffrey H. Tavis, Raquel Castellon
Life of this patent
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Abstract
Methods for inhibiting angiogenisis are disclosed the comprise administering oleouropein and/or the products of its hydrolysis in therapeutically effective amounts. The methods and compositions of the present invention are particularly effective in inhibiting the vascularization of endothelial cells, and may be utilized to treat a wide variety of cancers, ocular diseases, and inflammatory conditions.
Claims30
A method for treating a medical condition which involves angiogenesis in a subject, the method comprising administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical composition having anti-angiogenic activity which contains as an active ingredient a therapeutically effective quantity of a compound of the formula:
- wherein R1 and R2 are hydroxyl functional groups:
- R3 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3 and COOCH3;
- X1-X3 are functional groups selected from the group consisting of oxygen, sulfur, —CH2—, or carboxy;
- R4 is a functional group selected from the group consisting of hydrogen, C1-C6-alkoxy, glucose, B-D-glucopyranose, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, halogen NO2, NH3, carbohydrate, amino acid, nucleotide and lipid;
- and
- R5 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3, and CH3.
A method of inhibiting the vascularization of endothelial cells comprising contacting said cells with a pharmaceutical composition in an amount sufficient to inhibit the vascularization thereof which contains an effective amount of a compound of the formula:
- wherein R1 and R2 are hydroxyl functional groups:
- R3 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3 and COOCH3,
- X1-X3 are functional groups selected from the group consisting of oxygen, sulfur, —CH2—, or carboxy;
- R4 is a functional group selected from the group consisting of hydrogen, C1-C6-alkoxy, glucose, B-D-glucopyranose, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, halogen NO2, NH3, carbohydrate, amino acid, nucleotide, and lipid;
- and
- R5 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3 and CH3.
A method for treating a medical condition in which involves angiogensis in a subject, which comprises administering to a subject in need of such treatment a therapeutic or effective amount of a pharmaceutical composition having anti-angiogenic activity which contains as an active ingredient at least one composition produced by the hydrolysis of a compound of the formula:
- wherein R1 and R2 are hydroxyl functional groups:
- R3 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3 and COOCH3;
- X1-X3 are functional groups selected from the group consisting of oxygen, sulfur, —CH2—, or carboxy;
- R4 is a functional group selected from the group consisting of hydrogen, C1-C6-alkoxy, glucose, B-D-glucopyranose, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, halogen NO2, NH3, carbohydrate, amino acid, nucleotide and lipid;
- and
- R5 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3, and CH3.
A method of enhibiting the vascularization of endothelial cells comprising contacting said cells with a pharmaceutical composition in an amount sufficient to inhibit the vascularization thereof which contains as an effective amount a compound selected from the group consisting of at one composition produced by the hydrolysis of a compound of the formula:
- wherein R1 and R2 are hydroxyl functional groups:
- R3 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3 and COOCH3;
- X1-X3 are functional groups selected from the group consisting of oxygen, sulfur, —CH2—, or carboxy;
- R4 is a functional group selected from the group consisting of hydrogen, C1-C6-alkoxy, glucose, B-D-glucopyranose, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, halogen NO2, NH3, carbohydrate, amino acid, nucleotide and lipid;
- and
- R5 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3, and CH3.
A method of treating cancer in a mammal in need of such treatment which is comprised of administering to said patient a therapeutically effective amount of a compound having the structure:
- wherein R1 and R2 are hydroxyl functional groups:
- R3 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3 and COOCH3,
- X1-X3 are functional groupsmne selected from the group consisting of oxygen, sulfur, —CH2—, or carboxy;
- R4 is a functional group selected from the group consisting of hydrogen, C1-C6-alkoxy, glucose, B-D-glucopyranose, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, halogen NO2, NH3, carbohydrate, amino acid, nucleotide, and lipid;
- and
- R5 is a functional group selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2, NH3, and CH3;
- or a pharmaceutically acceptable salt, prodrug or hydrate thereof.
Dependencies are inferred from the claim text.