Abstract: The present invention provides certain non-symmetric tripyrranes; that is, tripyrranes that do not contain a mirror plane of symmetry perpendicular to the plane containing the tripyrrane. Further, the invention includes texaphyrin compounds and sapphyrin compounds, as well as other polypyrrolic macrocycles, prepared using tripyrranes of Formula I as a precursor. These macrocycles are characterized by a tripyrrolic portion of the macrocyclic ring having substituents that cause the heterocycle to lack a plane of symmetry perpendicular to the plane of the macrocycle.

Abstract: Methods for identifying compound useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. In one embodiment, the method comprises contacting a microbial cell comprising: 1) a selectable marker under the control of a transcription factor responsive element and 2) a transcription factor, with a compound under conditions which allow interaction of the compound with the microbial cell; and measuring the ability of the compound to affect the growth or survival of the microbial cell as an indication of whether the test compound modulates the activity of a transcription factor.

Abstract: The invention provides antioxidant salen-metal complexes, compositions of such antioxidant salen-metal complexes having superoxide activity, catalase activity, and/or peroxidase activity, compositions of salen-metal complexes in a form suitable for pharmaceutical administration to treat or prevent a disease associated with cell or tissue damage produced by free radicals such as superoxide, and cosmetic and free radical quenching formulations of salen metal compounds.

Abstract: A method of potentiating the phototoxicity of photodynamic therapy by co-administering a photosensitizing agent with a photodynamic potentiator from the group consisting of uridioxicolic acid analogs and conjugates thereof having the photo-toxicity potentiating effect and allowing for retention of the co-administered agent and acid in the target tissue. The target tissue is then irradiated. A tool for potentiating apoptosis consists of a photosensitizing agent and a non-toxic photodynamic potentiator. Further, a method of potentiating drug induced apoptosis is provided by administering a photosensitizing agent and then decreasing the threshold of responsiveness of a target tissue to a photokilling effect of the photosensitizing agent.

Abstract: Vanadium compounds as anti-proliferative agents. These compounds act to disrupt mitotic and meiotic spindle formation and thus are useful to prevent cell mitosis (proliferation) and meiosis.

Abstract: Dialysis solutions comprising aqueous solutions including physiologically acceptable salts and a polyglycol osmotic agent are disclosed. The subject solutions provide an improved osmotic gradient resulting in reduced dialysis times and/or reduced volumes of required dialysis solution. Moreover, the subject osmotic agents do not significantly migrate into the patient's blood over the time period of dialysis nor are the subject osmotic agents as susceptible to forming detrimental degradation products during gamma sterilization. The use of free radical scavengers is also described along with the use of a filter to reduce the introduction of bacteria into the peritoneal cavity.

Abstract: The present invention relates to novel porphyrin and porphyrin-based chromophores and sets of porphyrin and porphyrin-based chromophores, which may be particularly useful in a range of photodynamic applications, including photochemotherapy and fluorescence analysis and imaging. In particular, the present invention provides new and useful porphyrin, chlorin and bacteriochlorin chromophores; methods for the production of such chromophores; and methods for the use of such chromophores in analysis and in medicine.

Abstract: Novel derivatives of metallotexaphyrins are prepared by modifying the apical ligands associated with the central metal component of a metallotexaphyrin.

Abstract: Antimicrobial compositions containing a singlet oxygen-generating agent and a lubricant exhibit very effective antimicrobial activity against a variety of organisms, including Gram-positive bacteria, Gram-negative bacteria, fungi and yeast. The compositions have particular utility as beverage container lubricants. The passage of a container along a conveyor is antimicrobially lubricated by applying a lubricant to at least a portion of the container-contacting surface of the conveyor or to at least a portion of the conveyor-contacting surface of the container and generating singlet oxygen in situ. This method provides effective control of microbes on a beverage conveyor line, at rates comparable to purely chemical biocidal systems.

Abstract: The present invention relates to medicine and veterinary, namely, to immunology, and to methods aimed at correcting the immune system of a living organism. The essence of the invention is in the immunocorrection of the organism using pharmacologically appropriate amino derivatives of 2,3-dihydrophthalazine-1,4˜dione in their effective doses ranging from 0.2 &mgr;g to 1,000 mg.

Abstract: Methods, compounds and compositions are disclosed for treating amyloidogenic diseases, like Alzheimer's disease and type 2 diabetes, and particularly prion diseases associated with conversion of protease sensitive PrP (PrP-sen) to protease resistant PrP (PrP-res), by administering therapeutically effective amounts of a tetrapyrrole. Particular disclosed tetrapyrroles having this activity include phthalocyanines, deuteroporphyrins, and meso-substituted porphines. Complexes of certain of the pyrroles with metals or metal ions produce compounds that are particularly effective in converting the conversion of PrP-sen to PrP-sen. The treatment of the present invention is particularly suited for preventing or inhibiting the progression of prion related diseases, such as transmissible spongiform encephalopathies.

Abstract: The present invention includes a precursor compound pertaining to a 1,2,4-Triazolo[4,3-a][1,3,5]Triazine compound, particularly a 1,2,4-Triazolo[4,3-a][1,3,5]Triazine-3,5,7-Triamine, and novel fused ring structures such as triazolyl-tetrazinyl-aminotriazine compounds, and complexes and salts thereof, and other such chemical structures.

Abstract: There is provided a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, Y1, Y2, Y3, Z, M, A-B and C-D have meanings given in the description, which are useful in the treatment of medical conditions for which a photodynamic compound is indicated. Compositions, apparatus and methods of treatment of a medical condition for which a photodynamic compound is indicated are also disclosed.

Abstract: Provided are methods and compositions for the photodynamic therapy (PDT) of ocular conditions characterized by the presence of unwanted choroidal neovasculature, for example, neovascular age-related macular degeneration. The selectivity and sensitivity of the PDT method can be enhanced by combining the PDT with an anti-angiogenesis factor, for example, angiostatin or endostatin, or with an apoptosis-modulating factor. Furthermore, the selectivity and sensitivity of the PDT may be further enhanced by coupling a targeting moiety to the photosensitizer so as to target the photosensitizer to choroidal neovasculature.

Abstract: According to the present invention there is provided a compound for use as a photosensitiser in PDT, in photochemical internalisation in the production of a cancer vaccine or in the diagnosis or detection of medical conditions, the compound having a photosensitising chromophoric system, a sulphonamido functionality and a carboxy functionality.

Abstract: Novel compounds that either preferentially absorb into hyperproliferative tissue and absorb light efficiently at a wavelength of between about 700 and about 850 nm or act as intermediates for such absorbing compounds.

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: Provided are methods and compositions for the photodynamic therapy (PDT) of ocular conditions characterized by the presence of unwanted choroidal neovasculature, for example, neovascular age-related macular degeneration. The selectivity and sensitivity of the PDT method can be enhanced by combining the PDT with an anti-angiogenesis factor, for example, angiostatin or endostatin, or with an apoptosis-modulating factor. Furthermore, the selectivity and sensitivity of the PDT may be further enhanced by coupling a targeting moiety to the photosensitizer so as to target the photosensitizer to choroidal neovasculature.

Abstract: Efficient methods and compositions are provided for the targeted delivery of effective concentrations of compounds, including nucleic acid molecules and oligonucleotides such as EGSs, ribozymes and antisense, proteins, peptides, carbohydrate, and synthetic organic and inorganic molecules, or combinations thereof, to cells, especially hepatocytes. In the preferred embodiment, the compound is an negatively charged oligonucleotide which binds in a stoichiometric ratio to a water soluble, positively charged macrocycle such as a porphyrin, which targets and protects the oligonucleotide. The porphyrin protects the compound to be delivered and delivers the compound preferentially to certain cells and tissue types. In another embodiment, the porphyrin has anti-human hepatitis virus activity, when administered alone, which is significantly enhanced when in combination with an antiviral compound, especially an oligonucleotide.

Abstract: The present invention is directed tometal-phthalocyanines of general formula (I) to the corresponding conjugates, the processes for their preparation and use in the photodynamic therapy of microbial infections (viral, bacterial and mycotic), tumor, pre-cancerous and proliferative pathologies and/or in the diagnosis, as well as for blood and blood derivatives sterilization.

Abstract: Disclosed herein are methods for treating ocular neovascular disease using anti-VEGF therapy in combination with a second therapy that inhibits the development of ocular neovascularization or destroys abnormal blood vessels in the eye, such as photodynamic therapy.

Abstract: The present invention covers halogenated derivatives of boronated phorphyrins containing multiple carborane cages having the formula 1

Abstract: The present invention relates to a pharmaceutically acceptable dosage form of water insoluble porphyrins, particularly metal containing porphyrins such as tin porphyrin, which can be complexed with a lipid, reconstituted from a lyophilizate and administrated to a patient in the treatment of cancer and other diseases.

Abstract: The present invention is directed to compositions and methods for affecting metallocorrinoid uptake. The compositions and methods of the present invention are particularly useful in enhancing the uptake or availability of biologically active metallocorrinoids (e.g. cobalamin and its analogs). The present invention is particularly useful in the treatment or prevention of conditions that result from low expression or activity of proteins involved in the processing of metallocorrinoids, as well as in conditions which would benefit from enhanced uptake or availability of cobalamin or its biologically active analogs of cobalamin (e.g. cobalamnin drug conjugates).

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: The present invention is an antimicrobially-treated material which has a coloring preventing function and is in contact with water or moisture or contains water, comprising (A) a silver-based antimicrobial agent which dissociates silver ions in the water system and (B) a silver ion trapping agent for trapping silver ions comprising one or more kinds of compounds selected from the group consisting of purine bases, pyrimidine bases, thiabendazole, and potassium iodide, wherein a ratio of(A)/(B) is 1/1 to 100/1 by weight.

Abstract: The invention relates to a polymeric micellar structure comprising an ionic porphyrin dendrimer represented by general formula [1]

Abstract: The invention relates to compounds of the formula: 1 (I) 1 R1 = R2 = R3 = R4 = —CH3 T4MPyP —CH3 —CH2(CH2)4CH3 mono-C6 —CH2(CH2)8CH3 mono-C10 —CH2(CH2)12CH3 mono-C14 —CH2(CH2)16CH3 mono-C18 —CH2(CH2)20CH3 mono-C22 2 mono-benzyl R1 = R2 = R3 = R4 = tetra-CS —CH2(CH2)4CH3

Abstract: The present invention relates to novel compositions comprising, (i) at least one of Taxol, Taxotere, bleomycin, carmustine, carboplatin, and doxorubicin; and (ii) MGd, a compound of Formula I. The present invention also relates to and methods of using said compositions to treat Cancer.

Abstract: Solid forms of tin ethyl etiopurpurin (SnET2), including crystalline form I, crystalline Form II, disordered Form II, and an amorphous form are disclosed. Also disclosed are the 1,2-dichloroethane solvate of SnET2 and the N,N-dimethylformamide solvate of SnET2. These solid forms of SnET2 are useful as pharmaceuticals that exhibit pharmacological activity when irradiated with light and thus are useful in photodynamic therapy. Also disclosed are methods for making these solid forms of SnET2 and pharmaceuticals including these solid forms of SnET2.

Abstract: Photodynamic therapy of conditions of the eye, especially those conditions characterized by unwanted neovasculature, such as age-related macular degeneration, results in enhanced visual acuity for treated subjects.

Abstract: Novel C-132-COXR1, C-172-COXR2 and C-132-COXR1, C-172-COXR1 derivatives of chlorophyll and bacteriochlorophyll compounds are provided wherein X is O, S or N and R1 and R2, the same or different, may be an optionally substituted hydrocarbyl, amino acid, peptide, protein or saccharide radical. The compounds are for use in photodynamic therapy (PDT), for diagnosis of tumors, and for killing cells and infectious agents such as bacteria and virus, both in biological products and in living tissues.

Abstract: The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent protein kinase a neural cell subject to growth repulsion mediated by a neural cell growth repulsion factor. The activator may comprise a direct or an indirect activator of the protein kinase; the repulsion factor typically comprises one or more natural, endogenous proteins mediating localized repulsion or inhibition of neural cell growth; and the target cells are generally vertebrate neurons, typically injured mammalian neurons. The subject compositions include mixtures comprising a neural cell, an activator of a cyclic nucleotide dependent protein kinase and a neural cell growth repulsion factor.

Abstract: The invention provides &bgr;-cyclodextrin dimers and phthalocyanines which can be used in photodynamic therapy of cancer.

Abstract: The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent protein kinase a neural cell subject to growth repulsion mediated by a neural cell growth repulsion factor. The activator may comprise a direct or an indirect activator of the protein kinase; the repulsion factor typically comprises one or more natural, endogenous proteins mediating localized repulsion or inhibition of neural cell growth; and the target cells are generally vertebrate neurons, typically injured mammalian neurons. The subject compositions include mixtures comprising a neural cell, an activator of a cyclic nucleotide dependent protein kinase and a neural cell growth repulsion factor.

Abstract: This invention provides a soluble nano-sized particles formed of a core (water-insoluble lipophilic compound or hydrophilic compound) and an amphiphilic polymer and which demonstrated improved solubility and/or stability. The lipophilic compound within the soluble nano-sized soluble (“solu-nanoparticles”) may consist of pharmaceutical compounds, food additives, cosmetics, agricultural products and veterinary products.

Abstract: The present invention relates to use of a compound of Formula I: 1

Abstract: This invention provides antioxidant cyclic salen-metal compounds, compositions of such antioxidant cyclic salen-metal compounds having superoxide activity, catalase activity and/or peroxidase activity and methods of using such antioxidant cyclic salen-metal compositions to treat or prevent a disease associated with cell or tissue damage produced by free radicals, such as superoxide.

Abstract: The present invention is based on the discovery that cells associated with seizure have selective intake of photoactive compounds. The present invention provides methods of triggering cell death in cells associated with seizure conditions by exposing such cells to photoactive compounds and irradiating the photoactive compounds contained within the cells. The present invention also provides methods of labeling cells associated with seizure conditions by exposing such cells with photoactive compounds. In addition, the present invention provides model systems useful for studying seizure conditions.

Abstract: A method for inactivating ocular viral pathogens and for treating associated lesions on tissue by means of selectively activating a tissue-associated photosensitizing agent with light. The photosensitizing agent, preferably tin ethyl etiopurpurin, is administered to a patient to concentrate within the lesionous target tissue of the eye. The photosensitizer-laden target tissue is irradiated with photoactivating light. In pre-clinical in vitro studies, the photoactivated photosensitizer drug within the lesionous target tissue inactivates both cell free Herpes simplex virus (HSV) and cell-associated HSV and cytomegalovirus (CMV). The use of PDT for treating ocular viral diseases reduces the toxicity to the biological system when compared with prior art therapeutic procedures.

Abstract: Nitrosylation of proteins and amino acid groups enables selective regulation of protein function, and also endows the proteins and amino acids with additional smooth muscle relaxant and platelet inhibitory capabilities. Thus, the invention relates to novel compounds achieved by nitrosylation of protein thiols. Such compounds include: S-nitroso-t-PA, S-nitroso-cathepsin; S-nitroso-lipoprotein; and S-nitroso-immunoglobulin. The invention also relates to therapeutic use of S-nitroso-protein compounds for regulating protein function, cellular metabolism and effecting vasodilation, platelet inhibition, relaxation of non-vascular smooth muscle, and increasing blood oxygen transport by hemoglobin and myoglobin. The compounds are also used to deliver nitric oxide in its most bioactive form in order to achieve the effects described above, or for in vitro nitrosylation of molecules present in the body.

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.

Abstract: Elevated levels of homocysteine have been implicated as an important risk factor for cardiovascular and other diseases. A composition for decreasing levels of plasma homocysteine and a method for administering the composition are provided the composition containing dextromethorphan (DM), folic acid and vitamins B6 and B12. The composition provides a synergistic therapeutic effect so that lower amounts of the above ingredients may be employed to minimize any undesirable side effects caused by the use of high levels of a component such as DM. Preferred compositions for cardiovascular diseases further include lecithin, vitamin E, beta-carotene, procyanidins/flavonoids, trimethylglycine, garlic oil and minerals. Other compositions for treating glaucoma include bilberry, bioflavonoids and beta-carotene and for treating tardive dyskinesia include an antioxidant such as grape seed extract and pine bark extract, lecithin and oligomeric proanthocyanidins.

Abstract: The present invention is drawn to methods and compounds for photodynamic therapy (PDT) of a target tissue or compositions in a mammalian subject, using a light source that preferably transmits light to a treatment site transcutaneously. The method provides for administering to the subject a therapeutically effective amount of a photosensitizing agent. This photosensitizing agent preferentially associates with the target tissue. Light at a wavelength or waveband corresponding to that which is absorbed by the photosensitizing agent is then administered. The light intensity is relatively low, but a high total fluence is employed to ensure the activation of the photosensitizing agent.

Abstract: Pro-drug forms of linear polyamine-bridged platinum compounds and methods for their production and use are provided. The polyamine-bridge portion of the compounds is based on spermine or spermidine, and the central amines of the polyamine-bridge are chemically bonded to labile blocking groups. The presence of the blocking groups serves to minimize the toxicity of the Pt compounds upon administration. Selective removal of the blocking groups and release of the active, unblocked species occurs upon exposure to suitable environmental conditions.

Abstract: A method of increasing the multi-photon absorption cross-section of a porphyrin-based photosensitizer by attaching at least one TPA-chromophore at the meso- or beta-positions of a porphyrin structure of the porphyrin-based photosensitizer, and at least one intersystem crossing enhancing substituent to meso- or beta-positions of a porphyrin structure of the porphyrin-based photosensitizer, to thereby increase multi-photon absorption cross-section of the porphyrin-based photosensitizer to at least about 30 GM units at about its maximum wavelength for two-photon absorption. The TPA-chromophore is selected from a group of &pgr;-conjugated structures. The resulting porphyrin-based photosensitizer absorbs two photons of radiation in the range of about 700 nm to about 1300 nm.

Abstract: Metallotetrapyrrolic compounds having photherapeutic properties useful in photodetection and phototherapy of target issues, particularly porphyrins and azaporphyrins that including gallium in the central pyrrolic core. Also disclosed are methods of using metallotetrapyrrolic compounds for the treatment or detection of cardiovascular disease.

Abstract: The invention provides antioxidant salen-metal complexes, compositions of such antioxidant salen-metal complexes having superoxide activity, catalase activity, and/or peroxidase activity, compositions of salen-metal complexes in a form suitable for pharmaceutical administration to treat or prevent a disease associated with cell or tissue damage produced by free radicals such as superoxide, and cosmetic and free radical quenching formulations of salen metal compounds.

Abstract: A series of novel positively-charged porphyrins is disclosed which exhibit a markedly increased efficiency in photosensitizing both Gram-positive and Gram-negative bacteria to the action of visible light, causing death to such bacteria when present at much lower concentrations and much shorter irradiation times than those porphyrins taught in the prior art. These porphyrins are characterized by the presence of up to four positive charges in the peripheral substituents and at least one hydrophobic tail comprising between 6 and 22 carbons inclusive, originating at one or more of the charged sites.

Abstract: Substituted porphyrin and azaporphyrin deviations with various substitutents in the 12- and 17-positions of the porphyrin skeleton as pharmaceutical agents for use in photodynamic therapy, MRI diagnosis, and radiodiagnostics.