Abstract: The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity carborane-containing 5, 10, 15, 20-tetraphenylporphyrin compounds and methods for their use particularly in boron neutron capture therapy (BNCT) and photodynamic therapy (PDT) for the treatment of tumors of the brain, head and neck, and surrounding tissue. The invention is also directed to using these carborane-containing tetraphenyl porphyrin compounds to methods of tumor imaging and/or diagnosis such as MRI, SPECT, or PET.

Abstract: A novel class of tetracyclic compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.

Abstract: The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity carborane-containing 5, 10, 15, 20-tetraphenylporphyrin compounds and methods for their use particularly in boron neutron capture therapy (BNCT) and photodynamic therapy (PDT) for the treatment of tumors of the brain, head, neck, and surrounding tissue. The invention is also directed to using these carborane-containing tetraphenyl porphyrin compounds to methods of tumor imaging and/or diagnosis such as MRI, SPECT, or PET.

Abstract: A method is provided for selectively occluding neovascular vessels formed in the ocular fundus of an eye, which includes intravenously administering a mono-L-aspartyl chlorin compound to a patient; subsequently estimating an appropriate time point when the mono-L-aspartyl chlorin compound has decreased in its concentration or has been eliminated from the retinal normal vascular vessels of the patient but is still remaining at an appropriate concentration in the vascular walls of the neovascular vessels of the ocular fundus; irradiating a laser light at a 664 nm-wavelength which is initiated at the appropriate time; and using the irradiation of the laser light to target lesions comprising the neovascular vessels, at a controlled power.

Abstract: The present invention is directed to novel photosensitive compounds that can be replicated with great certainty and provide applications for photodynamic therapy.

Abstract: Compositions comprising microaggregates containing hydrophobic drugs, as well as methods for their production, are described. Such microaggregates may include micelle structures or combinations thereof with liposomes, and constitute an effective delivery vehicle for a hydrophobic agent. Methods for microaggregate production include the use of preferred lipid compounds and processing conditions favoring the production of small aggregates for improved filter sterilization.

Abstract: The invention relates to medicine and concerns a photosensitizer for detecting and curing tumors. The inventive photosensitizer is embodied in the form of a composition containing chlorin in the form of salt and alkali metals. The chlorin is composed of 80-90% of chlorin e6, 5-20 of purpurin 5 and the rest being purpurin 18 -chlorin p6. Said photosensitizer is produced by extracting Spirulina biomass with the aid of acetone. Afterwards said biomass is exposed to acid treatment, neutralization, hydrolysis, extraction of pheophorbide a, dissolution in acetone, addition of a strong base, neutralization and reprecipitation of chlorin e6.

Abstract: Tetrahydrocarbazoles of formula where Q is —SO2—; —O—; or —(CO)—; X is —(CH)—; or —N—; m is from 1 to 3; t is 0 or 1 and the remaining substituents are as defined herein, are useful as antimicrobial active ingredients.

Abstract: Water-soluble mono-PEGylated tetrapyrrole derivatives are disclosed, having a formula given by formula 1, 2, or 3 in the specification. A method to produce the above water-soluble mono-PEGylated compounds is also disclosed, comprising an interaction of a tetrapyrrole with an aminopolyethylene glycol containing a functionalized terminal fragment, as well as their use as photosensitizers in photodynamic therapy.

Abstract: Compounds represented by the general formula (I): which two DNA strands can be interstrand-crossliked: A-L-B-X-B-L-A??(I) wherein B represents a chemical structure capable of recognizing the nucleotide sequence of DNA; A represents a chemical structure capable of binding to one of the bases of DNA; L represents a linker by which the chemical structures of A and B can be linked to each other; X represents a spacer by which the A-L-B components can be linked to each other. A method of interstrand-crosslinking DNA by using these compounds; and medicinal compositions containing interstarand-crosslinking agents of DNA.

Abstract: Biologically active xanthone derivatives, as well as compositions prepared from such derivatives, possessing anti-cancer activity, anti-inflammatory activity, anti-obesity activity, and/or hair growth promotion activity, and a method for producing such derivatives and compositions. The derivatives are obtained by utilizing a heating, extracting and condensing system that efficiently recovers the derivatives from a raw material.

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.

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.

Abstract: Cobalt-porphyrin (Co-P) complexes for use as anti-obesity agents, and compositions and methods related thereto. The Co-P complexes exhibit reduced redox activity compared to cobalt mesoporphyrin (Co-MP) and cobalt protoporphyrin (Co-PP), which alleviates the deleterious effects associated with administration of Co-P associated with oxidative stress, particularly in the context of injection site toxicity.

Abstract: The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Abstract: The present invention discloses novel photoactive compounds that may be crosslinked to target substrates. Methods for the preparation and use of the compounds, as well as compositions comprising them, are also disclosed.

Abstract: Liposomal pharmaceutical formulations incorporating porphyrin photosensitizers useful for photodynamic therapy or diagnosis of malignant cells. The liposomal formulations comprise a porphyrin photosensitizer, particularly the hydro-mono benzoporphyrine (BPD) having light absorption maxima in the range of 670-780 nanometers, a disaccharide or polysaccharide and one or more phospholipids.

Abstract: Compounds of formula useful for treating tumors, particularly mammary carcinoma and colon carcinoma.

Abstract: A method in which photodynamic therapy is employed to inhibit, stabilize or reduce occlusions within the cardiovascular system by utilizing light within the spectral region of approximately 390 to approximately 610 nm.

Abstract: The present invention describes the use of fumitremorgin A, B and C and a series of diketopiperazines of Formula (I) to resensitize multidrug resistant (MDR) cancer cells to the cytotoxic effects of chemotherapeutic drugs.

Abstract: A novel class of tetracyclic compounds represented by the formula I wherein R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, and n are as defined is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.

Abstract: The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: The present invention relates to the use of an EP4 receptor ligand in the manufacture of a medicament for use in the treatment of neuropathic pain, colon cancer, migraine, and for increasing the latency of HIV infection.

Abstract: The present invention relates to fluoro sugar and other sugar derivatives of indolopyrrolocarbazoles, their salts and hydrates, which exhibit selective topoisomerase I (topo I) activity, are useful in inhibiting the proliferation of tumor cells and exhibit an antitumor effect, as well as processes for their preparation.

Abstract: Development of colorectal neoplasia in a patient subject or predisposed to colorectal neoplasia is reduced by the steps of (a) determining a patient is subject or predisposed to colorectal neoplasia; and (b) enterically delivering into the gut of the person an effective amount of an aminoglycoside antibiotic having poor gut absorption, whereby the development of the colorectal neoplasia is reduced as compared with otherwise similar non-treated patients.

Abstract: Compound of formula (I): wherein: R represents hydrogen or a group selected from alkenyl and optionally substituted alkyl, each of R1 to R8, which may be identical or different, represents hydrogen or a group selected from alkyl, alkenyl, hydroxy, alkoxy, alkenyloxy, arylalkyl, arylalkoxy, carboxy, acyloxy and arylcarbonyloxy, or one of R1 to R8 forms with an adjacent one R1 to R8 an alkylenedioxy group, its optical isomers when they exist, and addition salts thereof with a pharmaceutically acceptable acid or base, with the proviso that: when R does not represent hydrogen, then at least one of R1 to R8 represents hydroxy or acyloxy, and the compounds of formula (I) are other than indeno[1,2-b]indol-10(5H)-one and medicinal products containing the same which are useful for treatment of disorders of the melatoninergic system.

Abstract: The present invention is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones.

Abstract: The present invention relates to a novel FKA-25 substance, which inhibits formation of the foam macrophage originated from mouse, having inhibitory action against formation of the foam macrophage and a process for production thereof. The process includes culturing Pseudobotrytis sp. FKA-25 belonging to genus Pseudobotrytis sp. and having ability to produce FKA-25 substance in a medium, accumulating FKA-25 substance in the cultured medium, and collecting FKA-25 substance from the cultured mass. The obtained FKA-25 substance specifically inhibits the formation of the foam macrophage originated from mouse and is expected to be useful for prevention and treatment of arteriosclerosis and causative diseases therefrom.

Abstract: Carbamate compounds an compositions useful in photodynamic therapy for treating opthalmic, cardiovascular, and skin diseases.

Abstract: Methods for preventing damage to the epidermis during PDT induced using a pre-photosensitizing agent are provided. The methods of the present invention utilize spatial confinement to control formation of a photoactive species from a topically-applied pre-photosensitizing agent. In one embodiment, thermal inhibition is used to prevent the metabolism of a pre-photosensitizing agent in epithelial tissue surrounding a treatment site. In another embodiment, a chemical inhibitor can be applied to the epithelial tissue to inhibit the conversion of a pre-photosensitizing agent into a phototoxic species.

Abstract: Methods for preventing damage to epithelial tissue during PDT induced using a photosensitizing agent or pre-photosensitizing agent are provided. The methods of the present invention utilize spatial confinement to control photoactivation of the photoactive species to protect the epithelial tissue. In one embodiment, epithelial tissue surrounding a targeted treatment site can be protecting by decreasing the oxygen-content in the tissue, thereby preventing the conversion of the photosensitizer into the phototoxic species in the epithelial tissue.

Abstract: Novel group B streptogramin-like compounds of general formula (I), and a method for preparing streptogramines by mutasynthesis using a mutated micro-organism to influence the biosynthesis of at least one of the precursors of group B streptogramins are disclosed. Novel nucleotide sequences involved in the biosynthesis of said precursors, and their uses, are also disclosed.

Abstract: The present invention provides a class of porphyrins and metal chelated porphyrins for use as inhibitors of heme iron uptake. The porphyrin/metal chelated porphyrin molecules of the invention are tetra-positively charged porphyrins based on meso-tetra(4-pyridyl)porphines. Several such agents are shown herein to cause inhibition of iron uptake in vivo and in vitro. The invention further provides therapeutic compositions including the porphyrins and/or metalloporphyrins of the invention. In addition, methods of inhibition of heme iron uptake in vivo are taught, as well as methods of treatment of diseases characterized by iron-overload. These methods include the administration of a porphyrin or metalloporphyrin in a therapeutic composition of the invention to prevent uptake of heme iron, thus preventing replenishment of a patient's iron stores.

Abstract: The present invention relates to a method for making an indolopyrrolocarbazole compound of the general formula [I], where the method includes the step of reacting a bisindolylmaleimide compound with an oxidizing agent in the presence of an oxygen containing gas at a temperature and for a time sufficient to yield the indolopyrrolocarbazole compound of the general formula [I]. Methods of making rebeccamycin analogs using the indolopyrrolocarbazole compound are also provided.

Abstract: This invention is directed to macroheterocyclic compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.

Abstract: Compound of formula (I): 1

Abstract: The present invention relates to a &bgr;;3 adrenergic receptor agonist of formula I: (1); or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.

Abstract: The radiation sensitization potential of a candidate compound can be screened by determine its ability to generate one or more reactive oxygen species under appropriate conditions. Compounds determined to have radiation sensitization potential are employed in methods for treating atheroma, tumors and other neoplastic tissue as well as other conditions that typically responsive to radiation sensitization.

Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the general formula (I) or a physiologically acceptable salt thereof: 1

Abstract: Spiro compounds of the formula (I), in which at least one of the radicals K1, L, M, N1, R1, R2, R3, R4 is one of the following groups are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.

Abstract: Novel meso-aryl substituted expanded porphyrins comprising of alternate arrangement of more than six of pyrrole units bridged by a methine group whose hydrogen is substituted with Ar-group; and their synthetic method. Ar-group is either a 2,6-substituted phenyl group which can possess a substituent at the other 3, 4, and 5 positions, or 9-anthryl group which can possess a substituent at the other positions of the anthracence, or a cyclohexyl group which can possess a substituent at the other positions of the cyclohexyl group. The substituents at the 2 and 6 positions mentioned above can be selected independently from halogen atom or lower alkyl group of carbon number 1 to 4, substituents at 3-5 positions, 9-anthryl group and cyclohexyl group can be selected independently from the group consisting of substituted or non-substituted alkyl of carbon number 5 or 6, substituted or non-substituted aryl group, besides above mentioned substituents at 2 and 6 positions. Each Ar-group can be different.

Abstract: A method of treating a subject having unwanted cell proliferation which includes: inducing differentiation in a cell; providing said cell with a photosensitizer; and activating said PS, thereby the treating unwanted cell proliferation.

Abstract: The invention provides compositions containing a ligand such as human epidermal growth factor (EGF) or human vascular endothelial growth factor (VEGF), an anti-tumor agent and a human transferrin ligand. The compositions are useful for the delivery of anti-tumor agents to a host having a tumor.

Abstract: The invention provides methods useful for the delivery of anti-tumor agents to a host having a tumor. The methods of the invention involve the administration of compositions containing a ligand such as human epidermal growth factor (EGF) or human vascular endothelial growth factor (VEGF), an anti-tumor agent and a human transferrin ligand to a host having a tumor.

Abstract: A method of treating pain in a subject is disclosed which consists of administering a pharmaceutically effective amount of a porphyrin compound. In particular, the porphyrin is a green porphyrin and the pain is associated with a nerve injury pain or neuralgia.

Abstract: This invention features ring-substituted pyrrolo-&bgr;-carboline derivatives and ring-substitution and structural derivatives of 3-(1H-indol-3-yl)-1H-pyrrole-2,5-dione of formulas I-III, which are useful as neuroprotective and anti-proliferative compounds. Also disclosed are methods for the preparation of these compounds, selected biological profiles and uses of these compounds in the treatment of various neurodegenerative and inflammatory diseases of the human nervous system and in the treatment of various other proliferative disorders characterized by loss of growth or cellular differentiation control including, but not limited to, cancer and inflammation.

Abstract: Use of the tetramerous derivative of indole-3-carbinol having formula I 1

Abstract: Long-term dialysis requires provision of safe and reliable vascular access, often in the form of an arteriovenous (AV) fistula. The primary cause of AV fistula loss or failure is stenosis caused by intimal hyperplasia (IH) in the graft at the venous anastomosis or the distal vein. Disclosed are methods of using photodynamic therapy (PDT) to inhibit IH in blood vessels which may also be used to inhibit IH and SMC growth at the anastomosis of an AV fistula in vivo.

Abstract: The present invention provides a drug delivery system wherein a “parachute” structure is coupled to a therapeutic compound. The “parachute” structure comprises hydrophilic branched molecules with a defined action diameter. The complex (a parachute structure coupled with a therapeutic compound) is either fixed at a cell membrane or delivered to a defined distance from the membrane within the cell. The membrane-anchoring/localizing effect of the parachute is achieved by hydrophilic structures linked with a branching unit of desired therapeutic compounds. Furthermore, the parachute structures can be connected by a spacer (e.g. &bgr;-amino acids, &ggr;-amino butyric acid, or poly-amino acids) instead of directly binding to the therapeutic compound, so that the therapeutic compounds can be localized within the cells at a defined distance from the cell membrane. A spacer containing a breaking point can determine the time span, during which the drug exhibits its therapeutic activity.