Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

Abstract: The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels and thus improve the effectiveness of treatment regimens involving these drugs. Further agents such as methotrexate and AZT can also be used in cancer and HIV-positive patients employing camptothecin drugs.

Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: Compounds of the formula (I) wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing them and their use in medicine are disclosed.

Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.

Abstract: Synthesis of novel substituted indeno[1,2-b]indole derivatives of the type of 5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-diones and 5H-indeno[1,2-b]indole-6,9,10-triones, which show pronounced inhibition of the human protein kinase CK2, and the use thereof as active ingredients in medicaments and/or drug products in particular for the treatment of neoplastic diseases.

Abstract: Liposomal gel hydrophobic phthalocyanine (FCH) preparation for photodynamic therapy of tumors and other diseases is composed of lecithin liposomes or liposomes on the basis of other lipids, with incorporated curing drug, which can be chosen either from a group including hydrophobic hydroxyaluminum phthalocyanine, hydrophobic aluminum phthalocyanine, hydrophobic zinc phthalocyanine, hydrophobic silicone phthalocyanine, or organic silicone phthalocyanine, or hydrophobic phthalocyanine without the core metal; while resulting liposomes are mixed in ratios of 10:1 to 1:10 with a translucent gel, advantageously on the basis of carboxymethylcellulose. The added curing drug can be coated by glucose or other saccharides, by polyethylenglycol or other usable polymers, as lecithin or other lipids, or by sodium chloride or other salts usable in pharmacology.

Abstract: This inventive subject matter relates to novel metal complex protein kinases inhibitors, methods for making such compounds, and methods for using such compounds for treating diseases and disorders mediated by kinase activity.

Abstract: The present invention relates to compounds which are perylenequinone derivatives, their stereoisomers and atropisomers. These compounds can be particularly useful as photosensitizers or sononsensitizers in photodynamic or sonodynamic therapy. The invention also relates to various methods for using these compounds in photodynamic and/or sonodynamic therapy. The compounds also are useful as therapeutic agents for treating various hyperproliferative disorders.

Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.

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: The present invention relates to the constitutive activity of the Hedgehog pathway in non-small cell lung carcinoma (NSCLC). A method for diagnosing NSCLC by detecting the level of a component of the Hedgehog pathway is provided, as is a method for identifying subjects that will respond positively to treatment with a Hedgehog pathway antagonist. Methods for treating subjects with cancer or cancers resistant to Hedgehog pathway antagonists are also provided.

Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Abstract: A formulation or preparation for treating and preventing arterial and venous thrombi is provided. This preparation includes a non-metal containing photodynamic dye and a fat soluble vitamin. A method of administration for treatment and prophylaxis of arterial and venous thrombi is also provided. This method includes steps of: combining a non-metal containing photodynamic dye and a fat soluble vitamin; combining the non-metal containing photodynamic dye and fat soluble vitamin with a sodium solution; and administering the combination of non-metal containing photodynamic dye, fat soluble vitamin, and sodium solution as an intravenous drip.

Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.

Abstract: The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly frailty, osteoporosis, osteopenia, and male and female sexual dysfunction comprising administering to a patient in need thereof an effective amount of a compound of formula (I).

Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

Abstract: A method for treatment of depression and depressive mood disorders. The patient is administered an amount of a compound that increases the catalytic activity of MAO-A, so as to increase synaptic metabolism of serotonin to 5-HIAL. The effective compound is preferably reserpine, administered in a dosage of less than about 0.03 mg per day. The reserpine may be administered transdermally at a dosage in the range from about 0.002 mg per day to about 0.02 mg per day. A caffeine compound may be administered simultaneously so as to compensate for an antihypertensive effect of the reserpine. The caffeine compound may be combined with the reserpine in a transdermal cream.

Abstract: Use of the tetramerous derivative of indole-3-carbinol having formula I for preparing a medicinal having anti-carcinogenic activity, and method of synthesis of the tetramerous derivative having formula I, in which indole-3-carbinol is reacted with an oxidizing agent so as to cause a polymeric oxidation of indole-3-carbinol.

Abstract: An electrical stimulation method for the treatment of peripheral neuropathy is disclosed. In a preferred embodiment, the method utilizes an electrical stimulation device that includes a plurality of channels of electrodes each of which includes a first and second electrode positioned in electrical contact with tissue of a target region suffering from peripheral neuropathy. Agonist/antagonist muscles involved in abduction/adduction, flexion/extension, supination/pronation, protraction/retraction, and/or eversion/inversion in the peripheral body regions are stimulated with a patterned series of electrical pulses through channels of electrodes in accordance with a procedure for treating peripheral neuropathy.

Abstract: The present invention relates to a compound having benzopyran core, a preparation method of the derivatives by liquid phase synthesis and solid phase synthesis through diversity-oriented synthesis, and an anticancer agent comprising the compound that exhibit excellent cytotoxicity against cancer cells.

Abstract: The present invention relates to indolone derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.

Abstract: The present invention provides Caspofungin and salts thereof substantially free of Caspofungin C0 and salts thereof. The present invention also provides processes for the preparation of said Caspofungin and salts thereof and processes for the determination of the amount of Caspofungin C0 and salts thereof present in Caspofungin and salts thereof. The present invention further provides pharmaceutical compositions comprising said Caspofungin and salts thereof.

Abstract: A method of performing transurethral surgery on the human or animal body. A tissue is cut using a first active cutting electrode and a second neutral electrode, both electrodes being immersed in an electrically conductive aqueous fluid and connected to a power source for applying a voltage and a current between the electrodes. According to the invention, the electrical conductivity of the fluid is at least 25 mS/cm at room temperature. With the invention, complications of surgery can be significantly reduced.

Abstract: The present invention relates to a pharmaceutical composition for photodynamic treatment of a fungal skin disorder, said pharmaceutical composition comprising a photosensitizer and an enhancer, wherein the photosensitizer is a cationic photosensitizer and the enhancer is chosen from the group of i) an acid, and ii) a metal chelating agent. Such a composition is capable of eliminating both conidiae and hy-phae. The invention also relates to a method for the preparation of the pharmaceutical composition.

Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Abstract: A method of making a bacteriochlorin is carried out by condensing a pair of compounds of Formula II to produce the bacteriochlorin, wherein R is an acetal or aldehyde group. The condensing may be carried out in an organic solvent, preferably in the presence of an acid. The bacteriochlorins are useful for a variety of purposes such as active agents in photodynamic therapy, luminescent compounds in flow cytometry, solar cells, light harvesting arrays, and molecular memory devices.

Abstract: The present invention provides compounds of the general Formula DI: along with methods of making such compounds, formulations containing the same, and methods of using the same (e.g., in photodynamic therapy, for the production of solar cells, etc.

Abstract: Novel crystalline forms of lestaurtinib are described, including six co-crystal forms, nineteen solvate forms, three anhydrate forms and one hemihydrate form. Methods of their preparation and use are also described.

Abstract: The present invention provides novel tetracyclic indole compounds of Formula (I) either as in vivo imaging agents or as therapeutic agents. A method for the preparation of the in vivo imaging agent compound is also provided by the invention, as well as a precursor for use in said method. Pharmaceutical compositions comprising the compounds of the invention are additionally provided. Where the pharmaceutical composition comprises a compound suitable for in vivo imaging, a kit is provided for the preparation of the pharmaceutical composition. In a further aspect, use of the compound for in vivo imaging or treatment of conditions associated with PBR is provided.

Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.

Abstract: The present invention relates to a method of preparing a porphyrin derivative from a meso-acrylonitrile-substituted porphyrin compound. According to the invention a Vilsmeier reagent carrying an aromatic ring is used, wherein said Vilsmeier reagent is a soft electrophile. The use of this Vilsmeier reagent results in a porphyrin derivative having the ring system of the Vilsmeier reagent condensed to its porphyrin macrocycle via two new 6 membered rings. Thus a new class of porphyrin derivatives is provided, wherein said derivatives are photodynamically more active than the starting compound. The invention also relates to a porphyrin derivative, use of said porphyrin derivative and a pharmaceutical composition containing said porphyrin derivative.

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: The present application describes deuterium-enriched asenapine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Enzyme-activatable photosensitizing polymer conjugates are disclosed for photochemotherapeutic treatment of human diseases and disorders, bacteriologic or virologic indications, cosmetic applications and other pathologic situations. These polymer conjugates may comprise a polymer carrier, a photosensitizer, a quencher, a targeting molecule and/or a biocompatibilizing unit. These macromolecular conjugates may be designed to guide to the target tissue a photosensitizing agent in an inactive, non-phototoxic form. However, upon entering the target environment, in which certain enzymes are presently active, the conjugate may release its photosensitizers in its fully active form, resulting in a highly localized activation of the photoactive agent. Also described here are methods, compositions and kits for the preparation and testing of such photochemotherapcutic conjugates.

Abstract: New compounds useful in photodynamic therapy are of the formula and their 1,4-diene isomers and the metallated and/or labeled and/or conjugated forms thereof wherein each R1 is independently alkyl (1-6C); each n is independently an integer of 0-6; and R2 is vinyl or a derivative form thereof.

Abstract: Provided are compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds and compositions are useful for treating viral infections caused by the Flaviviridae family of viruses.

Abstract: The present disclosure involves the use of metal-containing texaphyrins and zinc (II) reagents for the treatment of tumors, atheromas and other neoplastic tissue. The present application demonstrates increased oxidative stress, alterations in zinc homeostasis, cell cycle arrest, and apoptosis of cancer cells in the presence of texaphyrins and/or zinc. One aspect is to monitor oxidative stress and/or alterations in zinc homeostasis in target cells prior to and/or after treatment with metal-containing texaphyrins and/or zinc (II) reagents as a predictor for treatment efficacy. The present disclosure provides molecular basis for the cell cycle arrest and apoptosis on cancer cells in the presence of texaphyrins and zinc. Another aspect is to monitor different genes involved in response to treatment with texaphyrins and zinc prior to and/or after treatment as predictors for treatment efficacy.

Abstract: A method of making a bacteriochlorin is carried out by condensing a pair of compounds of Formula II to produce the bacteriochlorin, wherein R is an acetal or aldehyde group. The condensing may be carried out in an organic solvent, preferably in the presence of an acid. The bacteriochlorins are useful for a variety of purposes such as active agents in photodynamic therapy, luminescent compounds in flow cytometry, solar cells, light harvesting arrays, and molecular memory devices.

Abstract: Methods of treating diseases of a subject through selective occlusion of blood vessels. The methods include identifying and/or mapping the blood vessels supplying nutrients to the diseased or unwanted tissue, delivering an appropriate dose of an occlusion-forming photosensitizer to the subject, and exciting the photosensitizer with sufficient light irradiation in the vicinity of the blood vessels to cause vessel occlusion. The vessel occlusion cuts off nutrient supply to the diseased or unwanted tissue resulting in cell death of that tissue and any other tissue served by the occluded vessels.

Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.

Abstract: The present invention relates to insecticidal compositions comprising compounds having an inhibitory activity versus acyl CoA: cholesterol acyltransferase (ACAT) or salts thereof as effective ingredients. The compounds having inhibitory activity versus ACAT have an excellent insecticidal effect by inhibiting sterol metabolism in noxious insects. Therefore, the compounds of the present invention can be used as safe and effective insecticides.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention relates to a method and kits for treating bipolar disorder in a mammal, including a human, the treatments including treatment of bipolar disorder including rapid-cycling, treatment of symptoms of bipolar disorder including acute mania or hypomania and depression, and episodes or occurrences including both acute mania or hypomania and depression; treatment for effecting mood stabilization; treatment for preventing relapse into bipolar episodes, and for the treatment of suicidal thoughts and tendencies associated with bipolar disorder, comprising administering to said mammal an effective amount of a compound of Formula or a pharmaceutically acceptable salt, solvate, hydrate or optical isomer thereof.

Abstract: A tetrapyrollic photosensitizer compound having at least one pendant —CH2CH2CON(CH2CON(CH2COOH)2)2 or —N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has the formula: or a pharmaceutically acceptable derivative thereof, wherein R1-R8 and R10 are various substituents and R9 is substituted or unsubstituted —CH2CH2CON(CH2CON(CH2COOH)2)2; or —N(CH2COOH)2. The invention also includes a method of treatment by photodynamic therapy by treatment with light after injecting the compound and a method of imaging by fluorescence after injection of the compound.

Abstract: Compositions comprising motexafin gadolinium, as well as methods for using these compositions in the treatment of brain metastases, are described herein.

Abstract: The present invention relates to tetracyclic indole derivatives of formula (I): wherein Ar, A, R1, R2, L, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.

Abstract: The invention relates to derivatives of porphyrin, particularly chlorins and/or bacteriochlorins, which can be used in photodynamic therapy. According to the formulas of the invention, X1, X2, X3, X4, X5, X6, X7, X8, which maybe identical or different, each represent halogen atoms or hydrogen atoms. R1, R2, R3, R4, which may be identical or different, are each selected from the following groups: —OH, amino acids, —OR and —NHR and/or a chlorine atom, wherein R is an alkyl group having between 1 and 12 carbon atoms. The invention also relates to an anticancer and/or antiviral and/or antimicrobial medicament for human or animal use, which contains one or more compounds as the main active ingredient.