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US 9,133,136 B2Granted
Dual small molecule inhibitors of cancer and angiogenesis
AssigneeUniversity of Virginia Patent Foundation
InventorMilton L. Brown
Life of this patent
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Abstract
The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.
Claims10
A method to treat retinal or choroidal neovascularization or a disease associated therewith in a subject in need thereof comprising administering to said subject an effective amount of at least one compound having the general structure of formula I:
- wherein R1, R3, and R4 are independently selected from the group consisting of NO2, H, halo, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C1-C4 alkoxy, C5-C7 aryl, mono-, di- or tri-chloro, and mono-, di- or tri-methyl, R2 is H or R3 and R2 taken together with the atoms to which they are attached form an optionally substituted heterocyclic fused ring, or R3 and R4 taken together with the atoms to which they are attached form an optionally substituted cycloalkyl fused ring;
- X is selected from the group consisting of NR5, —(NH(CH2)n)—, CH2, CHR5 and CO;
- wherein n is 1 or 2;
- Z is selected from the group consisting of a bond, O, NH, S, CO, COO, CH2O, CH2NH, CONH, C1-C4 alkyl, C1-C4 alkenyl, and C1-C4 alkynyl;
- and
- R2 and R5 are independently selected from the group consisting of H, halo, C5-C6 aryl, C1-C4 alkyl, C1-C4 alkenyl, and C1-C4 alkynyl, or R3 and R5 taken together with the atoms to which they are attached form an optionally substituted heterocyclic fused ring,
- thereby treating retinal or choroidal neovascularization or a disease associated therewith in said subject, wherein the disease associated with retinal or choroidal neovascularization is diabetic retinopathy, retinopathy of prematurity, macular degeneration, or chronic retinal detachment.
4 more elements
Dependencies are inferred from the claim text.