Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo.

Abstract: The invention relates to the use of anti-cancer drug of a natural compound of vegetal origin, known as aloe-emodin (AE). Indeed, said compound has proved to have a specific biological activity of inhibition on the growth of neuroectodermal tumors, without evident toxic effects. The compound, according to the present invention, has also proved to be cell-specific and it does not show any inhibition on the growth of other cell types such as, for instance, fibroblasts. This pharmacological profile, i.e., tumor-targeting and absence of toxicity, makes said compound particularly advantageous in the treatment of neuroectodermal tumors. Pharmaceutical compositions containing said pharmacological agent can therefore be usefully used in the treatment of the foresaid pathologies.

Abstract: The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.

Abstract: This invention provides various biquinone and trimeric quinone derivatives. The invention also provides a method for synthesis of a multi-quinone compound including reacting a hydroxyquinone anion with a first quinone possessing a first directing group at a C-2 of the first quinone and a second directing group at a C-3 of the first quinone and obtaining a biquinone having one of the first and second directing groups at a C-3 of a first quinone monomer and a hydroxyl group at a C-3′ of a second quinone monomer. The biquinone can be further reacted to obtain various biquinone derivatives or with a second hydroxyquinone anion to obtain trimeric quinone derivatives, including trimeric naphthoquinone derivatives. The biquinones and trimeric quinones of this invention demonstrate antiviral activity and can be used to treat viral infections, particularly HIV infections.

Abstract: The invention relates to novel stilbene compounds having the general formula (I): 1

Abstract: This invention relates to the use of a conjugate comprising an active substance and a native protein which is not recognized as foreign protein for the production of a pharmaceutical preparation for treating and/or diagnosing inflammatory, infectious and/or skin diseases.

Abstract: The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds including uses in the treatment of disease states mediated by chemokines. The relevant chemokines may for example be monocyte chemoattractant protein-one (MCP-1) or interleukin-8 (IL-8), and the relevant chemokine receptors may for example be corresponding chemokine receptors (CCR-2, CCR-4, CXCR-1, and CXCR-2). In one aspect, the invention provides for the use of phenanthrene-9,10-dione in the treatment of multiple sclerosis.

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: Pharmaceutical compositions and methods for treating androgen related disorders. The pharmaceutical compositions may include a 5&agr;-reductase inhibitor, such as natural and synthetic flavanoids, catechols, curcumin-related substances, quinones, catechins, particularly epigallocatechin derivatives, fatty acids, and the salts, esters, analogues, pro-drugs, isomers, racemic mixtures, or derivatives of any of the foregoing. The use of testosterone (or DHT) combinations with the aforementioned 5&agr;-reductase inhibitor compounds is also contemplated.

Abstract: Methods and compositions are provided for the treatment of cancer that take advantage of the increased uptake of glucose-anti-neoplastic agent conjugates in cancer cells relative to normal cells.

Abstract: Described herein is an invention that relates to chemiluminescence-directed antiviral activities of natural and synthesized light-sensitive compounds. Methods are described herein for inactivating infectious virus particles outside and inside an organism. These methods incorporate coupling the antiviral activity of various light-sensitive compounds with chemiluminescence directed by native as well as foreign enzymes of the organism and enhanced by the addition of various anti-quenchers and wavelength-shifting compounds. The methods described herein feature light-sensitive compounds with known antiviral activity exhibited in the presence of light.

Abstract: The present invention is directed to the use of antiviral compounds having the following generalized structure: wherein R is 2H or ═O; R′ is OH, H, or COOH (single substitution); and R″ is OH, H, or alkyl; and pharmaceutically acceptable salts thereof as therapeutic substances having antiviral activity against human cytomegalovirus (“HCMV”) and for treating diseases caused by HCMV. Dimeric forms of the forgoing antiviral compounds having antiviral activity against HCMV are also disclosed. Pharmaceutical compositions containing the disclosed antiviral compounds are disclosed for topical and systemic administration.

Abstract: The present invention provides novel phenalenone derivatives of formula (I) which are formed by the microorganism Penicillium herquei Bainer & Sartory, DSM 14142, during fermentation. A process for their preparation, their use as pharmaceutical compositions, and their use for the treatment or prophylaxis of bacterial infections, mycoses, oncoses and rheumatic diseases are also disclosed and claimed.

Abstract: Disclosed are methods to lower blood cholesterol levels or inhibit ileal apical sodium co-dependent bile acid transport (ASBT) protein using coumarin and anthracene dione derivatives. Pharmaceutical compositions are also disclosed.

Abstract: The invention relates to compositions and methods for treating and/or preventing lower gastrointestinal (GI) disorders in mammalian patients, more particularly for alleviating and/or preventing the lower GI symptoms associated with such disorders.

Abstract: The invention relates to compositions and methods for treating and/or preventing lower gastrointestinal (GI) disorders in mammalian patients, more particularly for alleviating and/or preventing the lower GI symptoms associated with such disorders.

Abstract: The present invention provides methods of inhibiting metastasis of a tumor and methods of treating a tumor using a combination of an inhibitor of the activation of nuclear factor NF-&kgr;B and a cancer chemotherapeutic agent. In one embodiment of the present invention, combination of curcumin and paclitaxel (taxol) can be used to treat and inhibit metastasis of breast tumor.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo.

Abstract: The invention provides therapeutic antimicrobial compositions comprising natural phenolic compounds and essential oil alcohols and methods of use. The therapeutic antimicrobial compositions are useful to treat internal and external bacterial, fungal, and protozoan infections, as well as antibiotic resistant and secondary opportunistic infections.

Abstract: The present invention provides an agricultural fungicidal composition containing active compounds selected from perylenequinonoid derivatives or salts thereof. The invention also relates the application of the composition against fungal plant infections.

Abstract: Hypericin has been shown to specifically inhibited T-type calcium channel activity. Hypericum extract containing hypericin also inhibited T-type calcium channel activity. Moreover, other chemicals in Hypericum extract showed a synergistic effect to hypericin. In view of this, hypericin or hypericin-containing Hypericum extract can be used as T-channel blockers. Hypericum extract, extract of other species of the Hypericum genus, extract of other plants containing hypericin, hypericin, hypericin derivatives, hypericin analogs, such as pseudohypericin, and other hypericum extract constituents can be used as therapeutics targeted at T-type calcium channels for treatment of diseases associated with T-channel abnormality. Methods for administering hypericin and hypericum extract are disclosed.

Abstract: Substituted phenanthrene-9,10-diones in accord with structural diagram I, 1

Abstract: Anticancer agents containing, as an active ingredient, at least one compound selected from the group consisting of &ohgr;-hydroxy fatty acids and salts or esters thereof, hydroxy oxo-fatty acids and salts or esters thereof, lactones, macrocyclic ketones, and macrocyclic diesters having specific chemical structures.

Abstract: The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.

Abstract: The invention is perylenequinones that are both sonosensitizers and photosensitizers, and their therapeutic use.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1

Abstract: The present invention provides the combined use of acryloyl distamycin derivatives, in particular &agr;-bromo- and &agr;-chloro-acryloyl distamycin derivatives of formula (I), as set forth in the specification, and an antineoplastic topoisomerase I or II inhibitor, in the treatment of tumors. Also provided is the use of the said combinations in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.

Abstract: The present invention provides compounds that are effective in treating disorders caused by the enzymatic activity of matrix metalloproteinases. These disorders include, but are not limited to, rheumatoid arthritis, osteoarthritis, periodontal disease, aberrant angiogenesis, tumor invasion and metastasis, corneal ulceration, and in complications of diabetes. The present invention is also is useful for treating wounds.

Abstract: The present invention is the synthesis of a series of 1,5-dichloro-9(10H)-anthracenones bearing O-linked and N-linked substituents in the 10-position. These compounds were evaluated for their ability to inhibit the growth of the human oral epidermoid carcinoma cells (KB cell line), human cervical carcinoma cells of ME 180 (GBM 8401) and Chinese hamster ovary cells (CHO), respectively. In addition, redox property of the compounds for inhibition of lipid peroxidation in model membranes was determined.

Abstract: Methods and compositions regarding the prevention of ER-positive cancer and the treatment of ER-positive HER-2/neu-negative breast cancer are disclosed. Compositions exhibiting both tyrosine kinase inhibitor activity and anti-estrogen receptor activity are useful in the cancer treatment.

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: Compounds that inhibit 5-alpha-reductase are provided. The compounds are used to treat prostate cancer, breast cancer, obesity, skin disorders and baldness.

Abstract: A method of controlling target aquatic microorganism pest populations by exposing the target population to a toxic amount of an aquacidal compound comprising an anthraquinone. The method is particularly effective for treating ballast water of ships or other enclosed volumes of water subject to transport between or among geographic areas to control the relocation of plants, toxic bacteria, and animals contained in the water.

Abstract: Pharmaceutical compositions and methods for treating androgen related disorders. The pharmaceutical compositions may include a 5&agr;-reductase inhibitor, such as natural and synthetic flavanoids, catechols, curcumin-related substances, quinones, catechins, particularly epigallocatechin derivatives, fatty acids, and the salts, esters, analogues, pro-drugs, isomers, racemic mixtures, or derivatives of any of the foregoing. The use of testosterone (or DHT) combinations with the aforementioned 5&agr;-reductase inhibitor compounds is also contemplated.

Abstract: Beta-lapachone, which is poorly soluble in most pharmaceutically acceptable solvents, has demonstrated significant antineoplastic activity against human cancer lines. The present invention overcomes this significant limitation by teaching novel pharmaceutical compositions comprising a therapeutically effective amount of Beta-lapachone, or a derivative or analog thereof, and a pharmaceutically acceptable solubilizing carrier molecule, which may be at water-solubilizing carrier molecule such as hydroxypropyl-&bgr;-cyclodextrin, or an oil-based solubilizing carrier molecule, for enhancing the solubility of Beta-lapachone in aqueous solution. The therapeutically effective amount of Beta-lapachone, or a derivative or analog thereof, may be complexed with the pharmaceutically acceptable solubilizing carrier molecule in aqueous solution. The novel pharmaceutical compositions may be administered with a second anticancer agent or in combination with radiation therapy.

Abstract: The present invention provides novel broad spectrum antiseptic compounds that further have properties that allow them to be coated/impregnated into polymer surfaces. Methods for coating these antiseptic compounds onto medical devices especially in-dwelling medical devices to prevent the growth of pathogens in such devices and hence, to prevent infection to patients via such devices are provided. The invention also provides antiseptics that are useful as general surface disinfectants and sterilizers, fluid disinfectants and biocide preservatives.

Abstract: Cytoprotective compounds, many of which are phenolic derivatives characterized by a substituted phenol having certain conjugated bonds, are useful in the treatment of certain ischemic or inflammatory conditions, including but not limited to stroke, myocardial infarction, congestive heart failure, and skin disorders characterized by inflammation or oxidative damage. They are also useful in the manufacture of pharmaceutical and cosmetic formulations for the treatment of such conditions.

Abstract: The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds (including chemokine receptor ligands such as chemokine receptor agonists or antagonists), such as tricyclic phenanthrene derivatives, including uses in the treatment of disease states mediated by chemokines. The relevant chemokines may for example be monocyte chemoattractant protein-one (MCP-1) or interleukin-8 (IL-8), and the relevant chemokine receptors may for example be corresponding chemokine receptors (CCR-2, CCR-4, CXCR-1, and CXCR-2). In other aspects, the invention provides corresponding pharamaceutical compositions and therapeutic methods. In one aspect, for example, the invention provides for the use of phenanthrene-9,10-dione in the treatment of multiple sclerosis.

Abstract: The present invention provides a treatment for mammalian diseases characterized by aberrant cell proliferation. The treatment consists of administering therapeutically active dosages of antibiotic inhibitors such as efrapeptin oligopeptides or mycotoxin derivatives including those comprising a-zearalenol structural motifs resulting in inhibition of cell mitosis.

Abstract: Multiple myeloma and other hematologic tumors and/or malignancies can be treated by administration of a G1 and/or S phase drug, which is preferably &bgr;-lapachone, or a derivative or analog thereof, combined with a G2/M phase drug such as a taxane derivative, which is advantageously paclitaxel. This combination of the G1 and/or S phase drug with the G2/M phase drug results in an unexpectedly greater than additive (i.e., synergistic) apoptosis in multiple myeloma cells. The invention includes methods of treating multiple myeloma by administering the combination of the G1 and/or S phase drug and the G2/M phase drug, pharmaceutical compositions comprising the combination of drugs used in these methods, as well as pharmaceutical kits.

Abstract: A compound of formula (I), wherein &agr;X is ═O, ═N—OR6, &bgr;NHR or &bgr;OH wherein R6 is H or C1-C6 alkyl, bond a is oriented &ggr; or &dgr; and R is H, C1-C6 alkyl which is unsubstituted or substituted by C6-C10 aryl, or C3-C6 cycloalkyl; &egr; is a bond when &zgr; and &eegr; are not bonds or, when X is ═O, &zgr; and &eegr; are both bonds and &egr; is not a bond; R1 and R2, which are the same or different, are H or a halogen; R3 and R4, which are the same or different, are H, C1-C6 alkyl, C3-C6 cycloalkyl, a heterocyclic group or an aromatic group; bond e is oriented &ggr; or &dgr;; and R5 is C1-C6 alkyl; or formula (Ib), or formula (II), or formula (III), has activity as a cytokine production inhibitor and an inhibitor and an inhibitor of tyrosine kinase.

Abstract: The present invention relates to the use of rhein or diacerhein compounds to treat and prevent vascular diseases that cause obstruction of the vascular system such as blood vessel restenosis and atherosclerosis.

Abstract: A method of controlling target aquatic microorganism pest populations by exposing the target population to an effective amount of an aquacidal compound. The aquacidal compounds are selected from the group consisting of quinones, anthraquinones, naphthalenediones, quinine, warfarin, coumarins, amphotalide, cyclohexadiene-1,4-dione, phenidione, pirdone, sodium rhodizonate, apirulosin and thymoquinone. The method is particularly effective for treating ballast water of ships or other enclosed volumes of water subject to transport between or among geographic areas to control the relocation of plants, toxic bacteria, and animals contained in the water.

Abstract: This invention relates to a method of inhibiting tumor cell adhesion, pain, and inflammation at a wound during a surgical procedure by delivering an irrigation solution containing a tumor cell anti-adhesion agent and a plurality of additional agents to an operative site during the surgical procedure. In addition, methods of inhibiting tumor cell attachment and implantation during a surgical procedure as well as inhibiting tumor metastasis during a surgical procedure are also provided.

Abstract: The invention is perylenequinones that are both sonosensitizers and photosensitizers, and their therapeutic use.

Abstract: A method for increasing the systemic exposure of cells selected from tumor cells and normal cells to an orally administered pharmaceutically active compound, wherein a bioenhancer comprising an inhibitor of BCRP is orally administered concomitantly with said orally administered pharmaceutically active compound, and in which method the inhibitor is administered simultaneously with the pharmaceutical compound.

Abstract: A product and method for reducing and preventing the ingestion of substrates by avians wherein the substrates are disposed within an avian house. The product is a bird repellent in combination with a substrate disposed within an avian house. As a result of the reduced ingestion of substrates such as litter, healthier avians are achieved.

Abstract: A foam skin cream can be obtained by preparing a phase I by melting at 75° C. a mixture containing fatty acids, especially C12-C22 fatty acids, optionally unsaturated and/or polyunsaturated fatty acids, emulsifiers, coemulsifiers, such as triceteareth-4-phosphate, followed by metering it with stirring to a phase II temperature-controlled at 75° C. obtained from an aqueous mixture containing moisturizers, such as propylene glycol and/or polyhydric alcohols, especially glycerol, emulsifiers, such as alkyl sarcosinates, and skin care additives, such as allantoin; wherein homogeneous mixing of phases I and II is provided and said metering is performed at a temperature of 75° C.; after the metered addition, the temperature is maintained at 75° C. for a period of between 5 and 20 minutes; whereupon the temperature of the thus obtained mixture is lowered to a temperature of between 30 and 40° C. with constant stirring; the pH value is adjusted to from 7.6 to 8.

Abstract: The present invention is based in part on the surprising discovery that Tanshinones from Salvia miltiorrhiza act as allosteric high-potency N-methyl-D-aspartate receptor antagonists. Pharmacological blockade of excessive activation of N-methyl-D-aspartate receptors (NMDARs) greatly reduces ischemic injury of neurons in cell culture and animal models. Tanshinones thus represent a novel class of compounds with NMDA receptor blocking activities with potential for the development of safe neuroprotective drugs for therapy of stroke and other neurodegenerative and neuropsychiatric disorders.