New York University

Yeda Research and Develpment & Co. Ltd

Other

New York Blood Center, Inc.

Gad Lavie

Daniel Meruelo

Yehuda Mazur

David Lavie

Michel Revel

Alfred M Prince

Dalia Rotman

Vincent Vande Velde

A method is provided for preventing or reducing the adverse effects of photodynamic therapy such as collateral damage by regulating the localized phototoxicity of an effector photosensitizer molecule. During photodynamic therapy, the activity of the effector photosensitizer molecule in neighboring tissues of the tissue targeted for destruction is quenched by a quenching photosensitizer molecule.

Method for preventing or reducing collateral phototoxic damage to neighboring tissues during photodynamic therapy of a target tissue

Hypericin, helianthrone and derivatives thereof of general formula (I)wherein the dotted line between positions 11 and 12 represent an optional C11-C12 bond; R is independently selected from the group consisting of hydroxy, C-Calkoxy, NH&#x2014;C-Calkyl, and NH-hydroxy(C-C)alkyl; R' is independently selected from the group consisting of hydroxy and C-Calkoxy; R&#x2033; is independently selected from the group consisting of hydrogen, hydroxy, C-Calkoxy, NH&#x2014;C-Calkyl, and NH-hydroxy(C-C)alkyl; and R, R, R, R, Rand Rare independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C-Calkyl, C-Calkoxy, and C-Calkoxycarbonyl, provided that R&#x2033; is not hydrogen when there is a C11-C12 bond, are useful as inhibitors of angiogenesis and can be used to prevent formation of metastases and restenosis and for the treatment of angiogenesis-associated ophthalmologic disorders. In addition, the helianthrones of formula (I) can be used for the treatment of tumors in the absence of light irradiation. New compounds include those of formula I which are other than hypericin and known hypericin derivatives and there is either a C11-C12 bond or at least one R&#x2033; is other than hydrogen.

Helianthrone derivatives as anti-cancer agents

Novel antiviral (including antiretroviral) compounds are mono- or dicarboxylic acid esters of hypericin in which one or both of the methyl groups of hypericin are substituted by carboxylic acid ester groups of the formula COOR in which R is alkyl, the chain of which is optionally interrupted by one or more oxygen or sulphur atoms. R is preferably methyl, ethyl, propyl, butyl, 2-methoxyethyl or 2-(2-methoxyethoxy)ethyl. The compounds may be formulated into pharmaceutical compositions and may be used in any manner which has previously been known for hypericin.

Antiviral agents

A method for treating cancer comprising administering a 1,3,4,6-tetrahydroxy-helianthrone derivative. The compounds can be used in the absence of light irradiation or for photodynamic therapy of solid tumors wherein the tumor site is subjected to light irradiation after administration of the active ingredient. A preferred compound is 10,13-dimethyl-1,3,4,6-tetrahydroxy-helianthrone.

Disclosed herein are antiviral agents, pharmaceutical formulations comprising effective amounts of these agents and methods for treating mammals suffering from infections caused by viruses. The agents are analogs, isomers, homologs, derivatives and salts of aromatic polycyclic diones.

Compositions and methods for treating viral infections

The invention provides improved methods for delivery of nucleic acids to cells, which comprise forming ternary complexes between a hydrophobic, membrane-binding anion such as hypericin; a polycation such as polylysine; and a nucleic acid such as DNA; and contacting cells with the tenary complexes. Also provided are pharmaceutical formulations comprising these ternary complexes and a pharmaceutically acceptable carrier or diluent. The methods and compositions find use in mediating DNA uptake into cells, including gene therapy applications.

Method for delivery of nucleic acids to cells using hypericin polyamine

T cell-mediated diseases in mammals are treated using compositions comprising a polycyclic aromatic compound, preferably hypericin or pseudohypericin, and related compounds, including isomers, analogs, derivatives, salts, or ion pairs of hypericin or pseudohypericin. The above composition may be administered in combination with an immunosuppressive agent. Pharmaceutical compositions useful for treating a T cell-mediated disease comprise the above polycyclic aromatic compound, alone or in combination with an immunosuppressive agent. The compositions and methods are useful in treating diseases which include multiple sclerosis, myasthenia gravis, scleroderma, polymyositis, graft-versus-host disease, graft rejection, Graves disease, Addison's disease, autoimmune uveoretinitis, autoimmune thyroiditis, pemphigus vulgaris and rheumatoid arthritis. Psoriasis and systemic lups erythematosus. Also provided are methods for diminishing the expression of CD4 Molecules on the surface of a T lymphocyte, and for inducing multidrug resistance in a cell, comprising incubating the cell with an effective concentration of a polycyclic aromatic compound.

Methods and polycyclic aromatic compound containing compositions for

A method for treating a papilloma virus infection comprising topically administering hypericin which is effective to inhibit the replication, growth and/or the infectivity of the virus. The papilloma viruses include those capable of causing benign warts or a malignancy such as human papilloma virus-1 (HPV-1), HPV-2, HPV-6, HPV-11, HPV-16 and HPV-18.

Method of treating papilloma virus infection using hypericin

The present invention provides compositions, articles and methods for inactivating viruses present in whole blood and other body fluids. The method comprises contacting the body fluids with an effective amount of an antiviral compound. Blood bags, vacuum blood tubes, condoms, spermicidal jellies and vaginal lubricants containing effective amounts of the antiviral compounds are also provided.

Biological fluid purification system

Pharmaceutical formulations comprising aromatic polycyclic dione compounds useful for treating mammals suffering from diseases caused by retroviruses are disclosed herein. A method for treating mammals suffering from retrovirus infections is also disclosed.

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New York, NY, United States of America

Gad Lavie