Abstract: This invention relates to a class of heterocycles and their metal complexes, and is particularly concerned with the use of these compounds in the preparation of prodrugs or as prodrugs that may be activated under hypoxic conditions by enzymes or by therapeutic ionising radiation, in the treatment of cancer. The invention also relates to the use of these heterocycles and the corresponding metal complexes in the preparation of medicaments and to compositions including the heterocycles or their metal complexes and to methods for preparing these compounds.
Type:
Application
Filed:
January 29, 2004
Publication date:
July 15, 2004
Inventors:
William Alexander Denny, William Robert Wilson, David Charles Ware, Graham John Atwell, Jared Bruce Milbank, Ralph James Stevenson
Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form-amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
Type:
Application
Filed:
December 19, 2003
Publication date:
July 8, 2004
Applicant:
Trustees of the University of Pennsylvania
Inventors:
Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang
Abstract: The present invention covers radiosensitizers containing as an active ingredient halogenated derivatives of boronated porphyrins containing multiple carborane cages having the structure
which selectively accumulate in neoplastic tissue within the irradiation volume and thus can be used in cancer therapies including, but not limited to, boron neutron—capture therapy and photodynamic therapy. The present invention also covers methods for using these radiosensitizers in tumor imaging and cancer treatment.
Abstract: The invention relates to the use of paramagnetic 3-, 8-substituted porphyrin derivatives with various substituents in 13- and 17-positions of the porphyrin skeleton as peroxynitrite rearrangement catalysts.
Type:
Application
Filed:
August 27, 2003
Publication date:
July 1, 2004
Applicant:
Merck Patent GmbH
Inventors:
Gisbert Depke, Margrit Hillmann, Guenter Michl, Johannes Platzek, Detlev Suelzle, Roland Neuhaus
Abstract: A method of treating a subject infected with a virus or a method of preventing viral infection of a subject comprising administering to the subject an effective amount of a compound having the structure:
wherein L=L′=2-methylimidazole.
Type:
Grant
Filed:
July 6, 2000
Date of Patent:
June 29, 2004
Assignee:
The Trustees of Columbia University in the City of New
York
Inventors:
Saul J. Silverstein, Erik K. Lium, Jennifer A. Schwartz
Abstract: A method for the protection of wood and other wood materials without affecting dimensional stability or surface integrity of the treated material is described. The method involves treating wood material with an iron salt and selected oxidants where the iron salt is preferably complexed with organic chelating ligands. Preferably, a microbicidal agent is also incorporated into the method to provide treated wood products that demonstrate excellent surface integrity, dimensional stability and retention of the infused microbicidal agents for extended periods of time without incurring the detrimental environmental effects of conventional chromium or copper-based inorganic salt preservation methods.
Abstract: The invention provides pharmaceutical compositions comprising a protoporphyrin precursor photochemotherapeutic agent together with vascular stroma-localizing photosensitizers, optionally together with at least one surface penetration assisting agent and optionally with one or more chelating agents, and use of the same in treating disorders or abnormalities which are responsive to PDT, preferably exhibiting synergistically enhanced therapy, kits comprising same and methods of therapy and diagnosis.
Type:
Grant
Filed:
July 9, 1999
Date of Patent:
June 15, 2004
Assignee:
PhotoCure AS
Inventors:
Qian Peng, Jahn M. Nesland, Karl E. Giercksky, Johan Moan, Trond Warloe
Abstract: Methods of detecting and treating rapidly growing exogenous cells, such as Protista, or parasites, that preferentially accumulate a photoactivatable porphyrin in which 5-aminolevulinic acid or precursor thereof is administered to the patient, or contacted to the exogenous cells, in an amount sufficient to induce synthesis fluorescence and/or photosensitizing concentrations of a protoporphyrin IX in the exogenous cells, followed by exposure of the exogenous cells to light of photoactivating wavelengths.
Abstract: Porphyrins containing one or more neutral or negatively-charged, closo- or nido-carborane substituents are useful as chelators. The carbon-carbon bonds linking the boron-containing groups to the porphyrin ring make the compounds highly resistant to hydrolysis. These compounds have potential for use in selective binding to specific ligands. These compounds are highly stable, soluble in water and organic solvents, and have low toxicity.
Abstract: The invention provides methods for treating cancer and compounds that are useful for the treatment of tumors, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates useful for preparing the compounds.
Type:
Grant
Filed:
May 8, 2002
Date of Patent:
June 1, 2004
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Yanhong Dong, Phalguni Gosh
Abstract: The invention is generally related to the field of photodynamic therapy by use of photosensitizers and stabilized formulations of the photosensitizers. These formulations may be used to deliver a photosensitizer as a pharmaceutical, agricultural, or industrial agent. The photosensitizer containing formulations and compositions of the invention comprise one or more block copolymers. Furthermore, the invention relates to processes for the production of, and application of, said formulations and compositions as photosensitizer drug delivery systems.
Abstract: Conjugates of chlorophyll (Chl) and bacteriochlorophyll (Bchl) derivatives with amino acids, peptides and proteins are provided by the invention. The amino acid, peptide or protein residue is linked to the 17-propionic acid group of a Chl or Bchl residue directly or through a chain. The conjugates are for use as photosensitizers in photodynamic therapy and in diagnostics of tumors. Conjugation with cell-specific ligands, such as hormones, growth factors or tumor-specific antibodies, will target the Chl or Bchl moiety to the tumor site. Thus, conjugates with melanocyte stimulating hormones are suitable for photodynamic therapy of melanoma tumors.
Abstract: The present invention includes novel N-heterocyclic carbene substituted porphyrins and porphyrinoids. The invention also includes complexes of metals and N-heterocyclic carbene substituted porphyrins and porphyrinoids. The invention further includes N-heterocyclic carbene substituted porphyrins and porphyrinoids. and metal complexes of N-heterocyclic carbene substituted porphyrins and porphyrinoids that also includes a targeting moiety or group. The compositions of the present invention are useful in the fields of diagnosis and treatment of many medical ailments.
Type:
Application
Filed:
November 28, 2003
Publication date:
May 20, 2004
Inventors:
Wiley J. Youngs, Claire A. Tessier, William G. Kofron, Richard S. Simons, Jered C. Garrison
Abstract: Water soluble tin mesoporphyrin compounds are described. Methods of preparation of water soluble metal mesoporphyrin compounds and pharmaceutical preparations are also described.
Abstract: This invention provides a cochleate and nano-cochleate systems wherein the agents bridging lipid bilayer are organic multi-valent cations. This invention also provides a method for preparing the cochleate system comprising direct cochleation and hydrogel-isolated procedure. The preparation method comprises using the charge ration between the bridging agents and lipids to control the particle sizes. This cochleate or nano-cochleate system may be used for microencapsulation and delivery of therapeutics wherein the therapeutic agents are loaded in the cochleate structure as the bridging agents between lipid bilayers. Finally, this invention provides other uses of these new cochleate and nano-cochleate systems.
Abstract: A selective chemotherapy method includes the step of contacting tumor cells with a mineral ascorbate/vitamin C metabolite composition. A chemotherapeutic composition comprises the mineral ascorbate/vitamin C metabolite composition in a pharmacologically acceptable intravenous carrier.
Abstract: A treatment method more effective in treating tumors such as cancer by administering activated lymphocytes in combination with a photodynamic therapy procedure within a specific period of time preceding or following the procedure is provided. By treating the patient with the combination of PDT procedure and the activated lymphocyte administration, a remarkable effect is achieved in reducing and suppressing various types of tumors, including stomach cancer in particular, and also desirable results are achieved even when tumors not responsive to PDT procedure alone are treated in this manner, due to the synergy of the PDT procedure and the activated lymphocyte administration. Provided that the activated lymphocytes are used in combination with a PDT procedure, even activated lymphocytes not necessarily achieving cancer specificity can be expected to improve the treatment effect in destroying or suppressing the growth of tumors such as cancers.
Abstract: Tertrapyrrolic macrocycles selected from 5,10,15,20-tetraaryl-porphyrins and 5,10,15-triaryl-corrloes, wherein said aryl radical is a carboaryl, a heteroaryl or a mixed carboaryl-heteroaryl radical and at least two of said aryl radicals are positively charged, inhibit growth factor (e.g. bFGF, VEGF) receptor tyrosine kinase activity, and are useful for inhibition of cell proliferation mediated by growth factor receptor tyrosine kinase activity for example for inhibition of angiogenesis, or vascular smooth muscle cell proliferation in disorders including atherosclerosis, hyperthrophic heart failure and postsurfical restenosis, and of cell proliferation and migration in the treatment of primary tumors and metastasis. Some of the 5,10,15,20-tetraaryl-prophyrins are novel compounds.
Type:
Grant
Filed:
July 18, 2001
Date of Patent:
May 4, 2004
Assignees:
Yeda Research and Development Co. Ltd., Technion Research and Development Foundation Ltd.
Abstract: A method of preventing HIV-1 or HIV-2 infection by administering to a human a pharmaceutically effective anti-HIV-1 or anti-HIV-2 amount of a tin or silicon protoporphyrin IX or tin or silicon mesoporphyrin IX, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 21, 1994
Date of Patent:
April 27, 2004
Assignee:
New York Blood Center, Inc.
Inventors:
Alexander R. Neurath, Shibo Jiang, Asim Kumar Debnath
Abstract: The present invention relates to a method using nanoparticles of cyclic tetrapyrrolic compounds as gene and drug delivery agents. Pharmaceutical agents can be packed or condensed inside nanoparticles of cyclic tetrapyrrolic compounds and delivered to cells. In vitro experiments showed nanoparticles of cyclic tetrapyrrolic compounds can be effectively delivered into cells.
Abstract: Method for treating dermal pre-melanoma conditions which include administering an effective amount of a photosensitive agent to a dermal pre-melanoma cell and activating the photosensitive agent, thereby treating a dermal pre-melanoma condition.
Abstract: Disclosed are pharmaceutical compositions comprising gold(III) complexes of porphyrins, Schiff-bases, bis(pyridyl)carboxamides and bis(pyridyl)sulfonamides. Also disclosed are methods for using the pharmaceutical compositions as anti-tumor and anti-HIV agents.
Abstract: Recreational or process water can be treated by uniformly dissolving in the water a singlet oxygen-generating photosensitizer selected from the group consisting of condensed aromatic compounds, acridine dyes, coumarin dyes, crystal violet, fluorene derivatives, porphyrin derivatives, chlorins, thiazine dyes, thioketones, xanthene dyes, or by uniformly dissolving in the water a singlet oxygen-generating photosensitizer having an absorption maximum less than 659 nm and sufficiently strong coloration so that the presence of the photosensitizer can be visually detected in the water. Exposure of the photosensitizer and ambient or added oxygen to sufficient light or other activating energy causes the generation of singlet oxygen and the destruction or control of microorganisms.
Type:
Application
Filed:
March 12, 2003
Publication date:
March 25, 2004
Inventors:
Stephan M. Hubig, Matthew J. Finley, Robert D.P. Hei
Abstract: High affinity nanoparticles are provided, as well as methods for their synthesis and use. The nanoparticles of the invention comprise high affinity molecules incorporated in a polymeric nanoparticle. The high affinity nanoparticles range in size from about 1 to about 1000 nm. The high affinity molecules of the nanoparticle have moieties that have high affinity for target molecules, resulting in the ability of the high affinity nanoparticle to selectively non-covalently bind to molecular targets. The molecular recognition capability of these particles enables their use in research, diagnostic, therapeutic, and separation applications. The nanoparticles of the invention may be formed by contacting target template molecules with a set of building blocks (which includes the high affinity molecule as one subset of the building block set), which are then polymerized into a network.
Abstract: A series of ortho isomers of meso tetrakis N-alkylpyridylporphyrins (alkyl being methyl, ethyl, n-propyl, n-butyl, n-hexyl, and n-octyl) and their Mn(III) complexes were synthesized and characterized by elemental analysis, uv/vis spectroscopy, electrospray ionization mass spectrometry and electrochemistry. An increase in the number of carbon atoms in the alkyl chains from 1 to 8 is accompanied by an increase in: (a) lipophilicity measured by the chromatographic retention factor, Rf; (b) metal-entered redox potential, E1/2 from +220 to +367 mV vs NHE, and (c) proton dissociation constant, pKa2 from 10.9 to 13.2. A linear correlation was found between E1/2 and Rf of the Mn(III) porphyrins and between the pKa2 and Rf of the metal-free compounds. As the porphyrins become increasingly more lipophilic, the decrease in hydration disfavors the separation of charges, while enhancing the electron-withdrawing effect of the positively charged pyridyl nitrogen atoms.
Type:
Application
Filed:
June 9, 2003
Publication date:
March 25, 2004
Applicant:
DUKE UNIVERSITY
Inventors:
Ines Batinic-Haberle, Ivan Spasojevic, Irwin Fridovich
Abstract: Metal-complexable substituted bis-indole derivatives comprising the structure shown in formula (I) hereunder: enantiomers and pharmaceutically acceptable salts thereof and metal complexes thereof, wherein L, R1, R2, R3, C1, C2, m, n, p, q and r are as defined in claim 1 for use as constrats agents.
Type:
Application
Filed:
October 23, 2003
Publication date:
March 18, 2004
Inventors:
Erwin Cresens, Yicheng Ni, Paul Adriaens, Alfons Verbruggen, Guy Marchal
Abstract: The invention provides a method of treating certain skin disorders, including, for example, psoriasis. Pulsed or scanned coherent or incoherent radiation, when applied to a target region, both activates a photosensitizer disposed within the region and induces selective photothermolysis of blood vessels disposed within region. The combination of photodynamic therapy and selective photothermal damage in the target region provides an effective and long lasting treatment of the skin disorder.
Abstract: The invention provides nanoparticles containing photosensitizers and their use in the field of photodynamic therapy (PDT). The invention also provides methods for the preparation of such nanoparticles as well as for their sterilization.
Type:
Application
Filed:
May 15, 2003
Publication date:
March 11, 2004
Inventors:
Eric Allemann, Yvette Konan, Robert Gurny, Ronald E. Boch
Abstract: The invention relates to the site specific delivery of drugs in an organism. The described methods facilitate the delivery of a therapeutic or diagnostic drug by increasing vascular permeability in a site specific manner. Vascular permeability is enhanced in the disclosed methods by using a combination of a photosensitizer and radiation applied to a site of interest.
Abstract: Photodynamic therapy of conditions of the eye characterized by unwanted neovasculature, such as age-related macular degeneration, is effective using green porphyrins as photoactive agents, preferably as liposomal compositions.
Abstract: A method is provided for inactivating viral and/or bacterial contamination in blood cellular matter, such as erythrocytes and platelets, or protein fractions. The cells or protein fractions are mixed with chemical sensitizers and irradiated with, for example, UV, visible, gamma or X-ray radiation.
Type:
Application
Filed:
August 5, 2003
Publication date:
February 19, 2004
Inventors:
Thomas Marinus Albert Remko Dubbelman, Johannes Wilhelmus Maris Lagerberg
Abstract: Novel coordination polymers, their pharmaceutical formulations, useful for treating atheroma, tumors and other neoplastic tissue, as well as other conditions that are responsive to the induction of targeted oxidative stress, are disclosed.
Type:
Application
Filed:
May 1, 2003
Publication date:
February 19, 2004
Inventors:
Darren Magda, Dale Miles, Nikolay Gerasimchuk, Cheryl Lepp
Abstract: The invention is generally related to the field of photodynamic therapy by use of photosensitizers and stabilized formulations of the photosensitizers. These formulations may be used to deliver a photosensitizer as a pharmaceutical, agricultural, or industrial agent. The photosensitizer containing formulations and compositions of the invention comprise one or more block copolymers. Furthermore, the invention relates to processes for the production of, and application of, said formulations and compositions as photosensitizer drug delivery systems.
Type:
Grant
Filed:
May 8, 2001
Date of Patent:
February 17, 2004
Assignee:
The University of British Columbia (UBC)
Abstract: Photodynamic therapy (PDT) is used to stimulate and/or restore hair growth in areas of hair loss. Methods and compositions relating to PDT treatment for alopecia are disclosed. In light of PDT use to remove unwanted hair by inactivating or destroying hair follicles or destroying the tissue feeding the hair follicles, such methods and compositions relate to a surprising and unexpected discovery. PDT permits a means to treat conditions relating to hair loss such as androgenic alopecia, alopecia areata and drug-induced alopecia.
Type:
Application
Filed:
April 23, 2003
Publication date:
February 12, 2004
Inventors:
Guillermo O. Simkin, Anna M. Richter, David W. C. Hunt, John Robert North, Peter Lutwyche, Ronald Erwin Boch, Jean-Marie Houle
Abstract: The present invention relates to a pharmaceutical composition for use as a medicament, preferably for the treatment or diagnosis of disorders or abnormalities of epithelial-lined surfaces, preferably mucosa-lined surfaces, comprising a photochemotherapeutic agent together with a mucoadhesive agent, optionally together with at least one surface penetration assisting agent and optionally with one or more chelating agents, and products and kits for performing the invention.
Type:
Application
Filed:
August 5, 2003
Publication date:
February 12, 2004
Inventors:
Jo Klaveness, Vidar Hansson, Aslak Godal
Abstract: Compounds, pharmaceutical formulations and methods for use in neutron capture therapy are provided, useful for treating diseases characterized by neoplastic tissue and arteriosclerosis.
Type:
Application
Filed:
February 25, 2003
Publication date:
February 5, 2004
Inventors:
Tarak D Mody, Jonathan L Sessler, Stuart W Young
Abstract: The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating cellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.
Type:
Application
Filed:
January 23, 2003
Publication date:
February 5, 2004
Applicants:
NATIONAL JEWISH MEDICAL AND RESEARCH CENTER, AEOLUS PHARMACEUTICALS, INC., DUKE UNIVERSITY
Inventors:
James D. Crapo, Brian J. Day, Michael P. Trova, Polivina Jolicia F. Gauuan, Douglas B. Kitchen, Irwin Fridovich, Ines Batinic-Haberle
Abstract: The invention relates to novel, water-soluble porphyrin platinum compounds of the tetraarylporphyrin platinum derivatives type or of the hematoporphyrin platinum derivatives type with high tumor selectivity and their use for the treatment of benign and malignant tumor diseases. In particular, the compounds are suitable for photodynamic anti-tumor therapy.
Type:
Application
Filed:
January 27, 2003
Publication date:
February 5, 2004
Inventors:
Karl-Christian Bart, Guenther Bernhardt, Henri Brunner, Christian Lottner
Abstract: Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.
Type:
Application
Filed:
July 14, 2003
Publication date:
January 29, 2004
Applicant:
PG-TXL Company, L.P.
Inventors:
Chun Li, Sidney Wallace, Dong-Fang Yu, David J. Yang
Abstract: The invention relates to the use of photodynamic therapy (PDT) to treat macular edemas, including DME, CRVO and BRVO. It provides an alternative to photocoagulation and the disadvantages associated therewith.
Type:
Application
Filed:
July 17, 2003
Publication date:
January 29, 2004
Inventors:
Janice North, Peter Hnik, H. Andrew Strong
Abstract: The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating intra- and extracellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.
Type:
Application
Filed:
June 9, 2003
Publication date:
January 29, 2004
Applicants:
DUKE UNIVERSITY, UNIVERSITY OF ALABAMA AT BIRMINGHAM RESEARCH FOUNDATION, AEOLUS PHARMACEUTICALS, INC.
Inventors:
James D. Crapo, Irwin Fridovich, Tim Oury, Brian J. Day, Rodney J. Folz, Bruce A. Freeman, Michael P. Trova, Ines Batinic-Haberle
Abstract: The invention is generally related to the field of drug delivery systems comprising micelles. These systems may be used to deliver a photosensitizer as a pharmaceutical, agricultural, or industrial agent. The photosensitizer-containing formulations and compositions of the invention comprise one or more PEG-containing phospholipids. Furthermore, the invention relates to processes for the production of, and application of, said formulations and compositions as a drug delivery system.
Type:
Application
Filed:
November 1, 2002
Publication date:
January 22, 2004
Inventors:
Theresa Mary Allen, Ronald Erwin, Anthony Seng Kee Boey
Abstract: The invention relates to a method of inactivating micro-organisms present in a liquid containing stem cells, where the method comprises the steps of -combining said liquid with a photosensitiser, and -activating the photosensitiser. In accordance with the present invention, a positively-charged sensitizer is used having a defined structure. Surprisingly, the use of these compounds minimize the damage to the stem cells.
Type:
Application
Filed:
August 5, 2003
Publication date:
January 22, 2004
Inventors:
Thomas Martinus Albert Remko Dubbelman, Johannes Wilhelmus Maria Lagerberg, Laurence Lilianne Annette Trannoy, Agatha Brand
Abstract: The invention describes the synthesis of a panel of novel carbon-carbon linked carboranyl-containng 5,10,15,20-tetraphenylporphyrins bearing 25-44% boron by weight. Preliminary in vitro evaluation of several of these compounds, using both rat and human brain tumor cell lines, shows that these compounds display very low cytotoxicities, are capable of delivering substantial amounts of boron intracellularly, and are retained for long periods of time.
Type:
Application
Filed:
April 2, 2003
Publication date:
January 22, 2004
Inventors:
M. G. H. Vicente, S.J. Shetty, L. Jaquinod, K.M. Smith
Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
Type:
Grant
Filed:
October 16, 2000
Date of Patent:
December 30, 2003
Assignee:
Mallinckrodt, Inc.
Inventors:
Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj
Abstract: Novel methods of synthesizing heteroatom-containing porphyrins and metalloporphyrins are disclosed. Novel heteroatom-containing porphyrin and metalloporphyrin compounds are also disclosed. The new methods advantageously utilize metal-catalyzed cross-coupling and amination reactions to produce porphyrin compounds useful in a variety of practical applications.
Type:
Application
Filed:
March 27, 2003
Publication date:
December 25, 2003
Applicant:
University of Tennessee Research Corporation
Inventors:
X. Peter Zhang, Ying Chen, Guangyao Gao, Andrew J. Colvin
Abstract: Vanadium (IV) complexes containing a substituted or unsubstituted catecholate ligand, and the spermicidal activity of such compounds. Preferred compounds are vanadocene (IV) complexes containing alkyl substituted catecholate ligands.
Type:
Grant
Filed:
July 23, 2002
Date of Patent:
December 23, 2003
Assignee:
Parker Hughes Institute
Inventors:
Phalguni Ghosh, Faith M. Uckun, Osmond D′Cruz