IP Library Granted Patent US 7,452,884
Granted Patent B2
US 7,452,884 · App. 11/522,238 · Granted Nov 18, 2008

Methods for inhibiting angiogenesis

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Quick Facts
Patent No.
US 7,452,884
App. No.
11/522,238
Granted
Nov 18, 2008
Kind
B2
Abstract

Novel methods for inhibiting angiogenesis and treating diseases associated with angiogenesis are described. The methods may comprise administering to a patient an effective amount of a 1,2-dithiol-3-thione derivative or metabolite thereof. Preferred compounds for use in the methods include 5-(2-pyrazinyl)-4methyl-1,2-dithiol-3-thione (Oltipraz) and its metabolites.

Claims (13)

1. A method for inhibiting angiogenesis in a patient comprising administering to said patient an anti-angiogenically effective amount of a 1,2-dithiol-3-thione derivative selected from the group consisting of 5-(2-pyrazinyl)-1,2-diothiol-3-thione (ADT), and 5-(2-pyrazinyl)-4-methyl-1,2-diothiol-3-thione or a metabolite thereof.

2. A method for inhibiting the growth or metastasis of an angiogenesis-dependent tumor in a patient comprising administering to said patient an effective amount of an anti-angiogenic agent, wherein said anti-angiogenic agent comprises a compound of the following formula (I):

wherein:

Ar is a monocyclic or bicyclic aryl group or a monocylic or bicyclic heteroaryl group containing 1 to 3 —O—, —S— or —N(R 2 ) m heteroatoms wherein m is 0 or 1; and

R1 and R2 are independently hydrogen or an alkyl group;

or a steroisomer, prodrug, metabolite, or pharmaceutically acceptable salt, hydrate or N-oxide thereof.

3. A method for inhibiting the growth or metastasis of an angiogenesis dependent tumor in a patient comprising administering to said patient an effective amount of an anti-angiogenic agent, wherein said anti-angiogenic agent comprises a 1,2-dithiol-3-thione derivative selected from the group consisting of 5-(2-pyrazinyl)-1,2-diothiol-3-thione (ADT), and 5-(2-pyrazinyl)-4-methyl-1,2-diothiol-3-thione or a metabolite thereof.

4. A method for treating a disease or disorder associated with angiogenesis in a patient, said disease or disorder being selected from the group consisting of neoplastic diseases, restenosis, rheumatoid arthritis, Crohn's disease, diabetic retinopathy, psoriasis, endometriosis, macular degeneration, neovascular glaucoma, and adiposity, comprising administering to said patient an effective amount of an anti-angiogenic agent, wherein said anti-angiogenic agent comprises a compound of the following formula (I):

wherein:

Ar is a monocyclic or bicyclic aryl group or a monocyclic or bicyclic heteroaryl group containing 1 to 3 —O—, —S— or —N(R 2 ) m heteroatoms wherein m is 0 or 1; and

R1 and R2 are independently hydrogen or an alkyl group;

or a stereoisomer, prodrug, metabolite, or pharmaceutically acceptable salt, hydrate or N-oxide thereof.

5. A method for treating a disease or disorder associated with angiogenesis in a patient, said disease or disorder being selected from the group consisting of neoplastic diseases, restenosis, rheumatoid arthritis, Crohn's disease, diabetic retinopathy, psoriasis, endometriosis, macular degeneration, neovascular glaucoma, and adiposity, comprising administering to said patient an effective amount of an anti-angiogenic agent, wherein said anti-angiogenic agent comprises a 1,2-dithiol-3-thione derivative selected from the group consisting of 5-(2-pyrazinyl)-1,2-diothiol-3-thione (ADT), and 5-(2-pyrazinyl)-4-methyl-1,2-diothiol-3-thione, or a metabolite thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 8, 2020
From: THE FOX CHASE CANCER CENTER FOUNDATION
To: THE INSTITUTE FOR CANCER RESEARCH
Reel/Frame 053562/0938 →