Abstract: Methods of synthesizing a phosphate ester of combretastatin A-4 and trans-isomers thereof in which combretastatin A-4 is reacted with dibenzylphosphite in the presence of carbon tetrabromide, or with 2,2,2-trichloroethyl phosphorodichloridate, to form a phosphate ester of combretastatin A-4 with protecting groups thereon.
Type:
Grant
Filed:
July 17, 2001
Date of Patent:
June 1, 2004
Assignee:
OxiGene, Inc.
Inventors:
Faye Seyedi, Jonathan Gale, Reem Haider, John Hoare, Amy Baldwin
Abstract: Methods of killing tumor or cancer cells in human patients using an aryl N-substituted carboxamide having one or more aryl halo or one or more aromatic nitrogens, and/or acid addition salts thereof. The carboxamide may be an N-substituted nicotinamide or an N-substituted benzamide having such features, and may be used directly as a chemotherapeutic agent, or as a sensitizer for radiation or other chemotherapeutic agents. New compositions for such use include N-(2-diethylamino-ethyl)-4-amino-3-chlorobenzamide, N-(2-diethylamino-ethyl) nicotinamide, and their acid addition salts, e.g. hydrochlorides.
Type:
Grant
Filed:
February 27, 1997
Date of Patent:
March 30, 2004
Assignee:
OXiGENE, Inc.
Inventors:
Ronald W. Pero, Anders Olsson, Tomas Ekberg, Alan Schwartz, David Chaplin
Abstract: Treatment of warm-blooded animals having a tumor or non-malignant hypervascularation, by administering a sufficient amount of a cytotoxic agent formulated into a phosphate prodrug form having substrate specificity for microvessel phosphatases, so that microvessels are destroyed preferentially over other normal tissues, because the less cytotoxic prodrug form is converted to the highly cytotoxic dephosphorylated form.
Abstract: This invention provides a method of killing tumor cells or microorganisms which comprises contacting the tumor cells or the microorganisms with an amount of nicotinamide adenine dinucleotide (NAD) or its analogs effective to increase clonogenic toxicity of cells. This invention also provides a method of killing tumor cells or microoganisms in a subject which comprises administering an amount of nicotinamide adenine dinucleotide or its analogs effective to increase clonogenic toxicity of cells to the subject.
Abstract: N-acetyl-3-chloroprocainamide, its acid addition salts, mixtures thereof, formulations containing the same for therapeutic administration to a human or other animal, and uses thereof in methods of inhibiting or killing tumor or cancer cells and in methods of treating inflammatory disorders.
Abstract: The use of benzamide and nicotinamide analogs, in particular N-substituted benzamides and nicotinamides, other than benzamides with N-pyridinyl substitutions, as anti-inflammatory agents.
Abstract: Selectively administering to humans, as a daily dosage, a combination of carotenoids, nicotinamide (or niacin or a precursor thereof) and a source of zinc, in excess of normal dietary levels, for improving resistance to DNA damage, enhancing DNA repair capacity, and stimulating immune function.
Abstract: A method of administering phenothiazines and their acid addition salts. The phenothiazine or acid addition salt is injected intramuscularly in a formulation with a pH of about 5.5 to about 7.0 and at a concentration of at least about 50 mg/ml, to deliver a dose of one to 5 mg/kg. The drug is administered either in a formulation containing Na.sup.+ ions and at a pH adjusted to reduce extrapyramidal side effects or in a formulation essentially free of Na.sup.+ ions.
Abstract: A method of administering N-substituted benzamides, and their acid addition salts, in particular metoclopramide and its acid addition salts, is disclosed wherein the metoclopramide or acid addition salt is injected intramuscularly in a formulation with a pH of about 5.5 to about 7.0 and at a concentration of at least about 50 mg/ml, to deliver a dose of one to 5 mg/kg.