Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.

Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.

Abstract: Compositions and methods of treating a neurodegenerative disorder are disclosed herein.

Abstract: The present invention provides a method of reducing body weight in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I: In Formula I, R1 is H, C1-6 alkyl, or C1-6 alkyl-aryl. Each of R2 and R4 of Formula I are independently H, halogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkoxy, —OR2a, —SR2a, —C(O)R2a, —C(O)OR2a, —C(O)NR2aR2b, —NR2aR2b, C1-6 alkyl-NR2aR2b, —N(R2a)C(O)R2b, —N(R2a)C(O)OR2b, —N(R2a)C(O)NR2aR2b, —OP(O)(OR2a)2, —S(O)2OR2a, —S(O)2NR2aR2b, —CN, —NO2, cycloalkyl, heterocycloalkyl, aryl or heteroaryl. Each of R2a and R2b of Formula I are independently H, C1-6 alkyl, C1-10 heteroalkyl or C1-6 alkyl-aryl. R3 of Formula I is absent, C1-6 alkyl or N-oxide. The compounds include the salts, hydrates and isomers thereof. The present invention also provides methods for the treatment of obesity and disorders related to obesity and higher than recommended percentage body fat, such as type II diabetes.

Abstract: The present invention relates to a pheophorbide-? conjugate or its salt, solvate or hydrate. The pheophorbide-? conjugate of the present invention exhibiting fluorescence upon its introduction into cells and degradation inhibits the survival of various cancer cells. Especially, the conjugate of pheophorbide-? and doxorubicin shows higher fluorescence intensity at lower pH (cancer environment). Therefore, the present composition for photodynamic therapy (PDT) of cancers is also very useful in detecting cancers. Interestingly, the anticancer effects of the present composition are dually exerted with help of both the photosensitizer and the anticancer drug of the present conjugates.

Abstract: The present invention provides means for identifying or classifying breast tumors based on the levels of nuclear cathepsin-L (CTSL) and nuclear p53 binding protein (53BP1), and methods of treating thereof.

Abstract: The present invention relates to methods of treating hematological malignancies, including acute myeloid leukemia (AML), comprising the combination of a compound that inhibits the binding of the Smac protein to IAPs (“IAP inhibitor”) and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; and a commercial package comprising said combination. The present invention also relates to the use of IAP inhibitors in combination with one or more pharmaceutically active agents for the preparation of a medicament to treat hematological malignancies, including AML.

Abstract: The present invention relates to method of enhancing the absorption of migraine medications and thereby treating migraines by co-administering to a subject in need thereof an effective amount of a ghrelin mimetic or pharmaceutically acceptable salt, hydrate or solvate thereof and at least one migraine medication selected from a serotonin 5-HT1B/1D receptor agonist, a tryptamine derivative, an ergoline derivative, a non-steroidal anti-inflammatory drug, or an analgesic, or any combination thereof.

Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.

Abstract: A highly moisturizing cosmetic composition having firmness/elasticity-improving effect, wrinkle-improving effect, and texture-improving effect can be provided by blending a metal phthalocyanine derivative or salt thereof in a cosmetic material. For the metal phthalocyanine derivative, iron phthalocyanine tetracarboxylic acid is particularly favorable.

Abstract: The invention relates to pyrrolo[2,3-a]carbazole derivatives, to a method for preparing the same, and to the use thereof as PIM kinase inhibitors. The invention can particularly be used in the pharmaceutical field.

Abstract: Methods of treating cancer by administering a DNA damaging agent and a CHK1 Inhibitor on a dosing regimen are provided.

Abstract: Novel Uses of an aromatic ester isolated from Armillaria mellea, particularly, armillaridin, are disclosed herein. The armillaridin is useful for manufacturing a medicament or a pharmaceutical composition for suppressing the growth of cancerous cells or for enhancing susceptibility of esophageal cancerous cells to a radiation treatment, in a subject.

Abstract: The invention relates to the use of 20-(4-carboxyphenyl)-2,13-dimethyl-3,12-diethyl-[22] pentaphyrine as antibacterial agent in photodynamic treatment. This expanded porphyrin derivatized in position 4 with a carboxyphenyl group proved very active after photo-oxidation both against S. aureus and E. hirae. Its high antibacterial activity and its low toxicity make this pentaphyrine particularly useful as antimicrobial agent both for photodynamic therapy against bacterial infections and in the disinfection of microbiologically contaminated liquids.

Abstract: The present invention relates, in one embodiment, to a method of preventing or treating diabetes using low molecular weight antioxidants. In a further embodiment, the invention relates to a method of protecting and/or enhancing viability of cells/tissues/organs during isolation (harvesting), preservation, expansion and/or transplantation. In yet another embodiment, the present invention relates to a method of inducing immune tolerance. The invention also relates to compounds and compositions suitable for use in such methods.

Abstract: The present invention relates to a compound of formula (I) where T, Q1, R1 to R6 and R30 are each as defined in claim 1, to their preparation and to their use.

Abstract: The invention provides anionic water-soluble tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one, preferably two or three, negatively charged groups and/or acidic groups that are converted to negatively charged groups at the physiological pH, preferably Bchls having a group COO<?>, COS<?>, SO3<?>, PO3<2?>, COOH, COSH, SO3H, and/or PO3H2 bound through an ester or amide bond to one or more of the positions 17<3>, 13<3>, and 3<2> of the tetracyclic or pentacyclic Bchl molecule, for photodynamic therapy and diagnosis.

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.

Abstract: A composition which comprises substance represented by Formula (I), [Meanings of the symbols that are included in the formula are given in the specification as definitions] a pharmaceutically acceptable carrier, and a dissolution aid. is useful for improving solubility, oral absorbability and/or absorbability in blood of a poorly water-soluble or water insoluble tetracyclic compounds having an ALK inhibitory activity that are useful as a prophylactic and/or therapeutic agent for cancer, depression, and cognitive function disorder.

Abstract: A material comprising at least one polymer and at least one sensitizer wherein the sensitizer is localised at a surface of the material wherein the sensitizer is an agent or compound able to provide improved anti-bacterial and/or anti-viral activity following exposure of the sensitizer to a particular wavelength or range of wavelengths of electromagnetic radiation.

Abstract: A method for treatment of the symptoms of neurologic dysfunctions, including major depression, an autism spectrum disorder (ASD), and schizophrenia. The patient is administered an amount of a compound that increases the catalytic activity of MAO-A. The effective compound is preferably reserpine, administered in a dosage of less than about 0.03 mg per day. The reserpine may be administered topically or transdermally at a dosage in the range from about 0.002 mg per day to about 0.02 mg per day.

Abstract: The present invention relates to novel fusarisetin compounds separated from Fusarium sp. FN080326 and having an anticancer activity, and to the use thereof. In detail, novel fusarisetin compounds separated and purified from Fusarium sp. FN080326, which is in turn separated from a soil sample, have an inhibitory activity on the proliferation and transfer of cancer cells such as breast cancer cells, liver cancer cells or myeloid leukemic cells. Therefore, the compounds can be effectively used for anticancer compositions containing the compounds as active ingredients.

Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.

Abstract: The present invention relates generally to methods and compositions for targeting of intracellular molecules involved in proliferation and protein synthesis of activated cells using polyanionic multivalent macromolecules. In particular aspect, multiple sulfate groups linked to polyol are specifically targeted to the cytoplasm and nucleus of proliferating and activated cells. The invention further comprises novel polyanionic macromolecular compounds and formulations.

Abstract: The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.

Abstract: Compositions for the promotion of muscle protein synthesis and control of tumor-induced weight loss in patients that are, for example, suffering from cancer cachexia, and methods of administering such compositions.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans.

Abstract: This invention is directed to methods of preventing or treating diseases or conditions associated with alterations in cellular integrity including alterations in endothelial permeability, excessive cell proliferation or tissue remodeling. Particularly, this invention is directed to methods of treating diabetic nephropathy, malaria, or cancer. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel rho kinase inhibitor compound to treat the disease.

Abstract: This invention relates to a method and composition for providing in various health benefits by administering various bioactive compounds derived from the plant Morinda cirtrifolia to individuals. This invention relates to using one or more of the following: Noni Leaf Extract; Noni Leaf Juice; and/or Roast Leaf More particularly this invention relates to administering one or more of the following: Pyro-phorbide a, Pheophorbide a, Purpin 7, and/or Pheophorbide all which may be derived from Noni leaf extract, Noni leaf juice, and/or Roast leaf Moreover, the foregoing formulations result in alleviating pain and inflammation.

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: The invention relates to substituted azaindole derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted azaindole derivatives for producing medicaments.

Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.

Abstract: The present invention relates to two main components, mahanine and mahanimbine (dehydroxy-mahanine) from Murraya koenigii for the treatment of glioblastoma and cervical carcinoma. Mahanimbine exhibited anti-cancer activity against lymphoid leukemia, myeloid leukemia, glioma, cervical carcinoma, pancreatic, colon and lung cancers in nineteen cells of different genetic status. C-3 hydroxy and NH groups are responsible contributing groups for their cytotoxicity. Mahanine reduced the doses of cisplatin and paclitaxel in cervical cancer showing better efficacy and useful as an adjunct chemotherapeutic agent to reduce toxicity these two drugs. A new cheap process for this preparation was established. EtOAc extract containing alkaloids enriched with mahanimbine and mahanine, is active against glioma and cervical cancers.

Abstract: A unique class of N-acyl O-amino phenol prodrugs of CBI-TMI and CBI-indole2 were synthesized and shown to be prodrugs, subject to reductive activation by nucleophilic cleavage of a weak N—O bond, effectively releasing the free drug in functional cellular assays for cytotoxic activity approaching or matching the activity of the free drug, yet remain essentially stable to ex vivo DNA alkylation conditions. Most impressively, assessment of the in vivo antitumor activity of a representative O-(acylamino) prodrug, 8, indicate that they approach the potency and exceed the efficacy of the free drug itself (CBI-indole2), indicating that the inactive prodrugs not only effectively release the free drug in vivo, but that they offer additional advantages related to a controlled or targeted release in vivo.

Abstract: The present invention provides methods to obtain biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases, fluorescence diagnosis and PDT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, ophthalmological or urological disorders. An embodiment of the present invention consists of a method to synthesize diketo-chlorins as precursors. In yet another embodiment these precursors are converted to ?-functionalized hydroxy- and dihydroxy-chlorins. Another embodiment is to provide amphiphilic compounds with a higher membrane affinity and increased PDT-efficacy. Another embodiment consists of the formulation of the desired isomer into a liposomal formulation to be injected avoiding undesirable effects like precipitation at the injection site or delayed pharmacokinetics of the tetrapyrrole systems.

Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein Y, R1, R2, R4 and n have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.

Abstract: A method of administering photodynamic therapy includes using a microwave frequency-sensitive light-emitting polymer as a light source to excite a administered photosensitizer to exert cytotoxicity in situ at a site containing undesired or diseased tissue.

Abstract: An anti-hepatitis C virus agent or anti-HIV agent comprising, as an active ingredient, a fullerene derivative which has a nitrogen atom forming a ring together with adjacent bonded carbon atom pairs constituting the carbon cluster skeleton of the fullerene or a quaternary amine salt thereof is provided.

Abstract: The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to certain indolin-2-ones and aza-indolin-2-ones which possess anti-tumor activity and are accordingly useful in methods of treatment of the human or animal body, in particular such compounds are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.

Abstract: The present invention relates to a therapeutic or prophylactic method for treating Parkinson's disease by administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to a pharmaceutical composition for treatment or prophylaxis of Parkinson's disease comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity. Moreover, the present invention relates to a method for enhancing dopamine signal in the brain, which comprises administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to pharmaceutical composition for enhancing dopamine signal in brain comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity.

Abstract: The present invention is directed at methods for preventing or minimizing the intensity of the serotonin syndrome in humans and lower animals which comprises administering proserotonergic agents and serotonin surge protectors. The present invention is also directed to pharmaceutical compositions comprising proserotonergic agents and serotonin surge protectors useful for carrying out the method of the present invention.

Abstract: The invention concerns materials and methods relating to the use of OMD (osteomodulin) and\or PRELP (Proline/arginine-rich end leucine-rich repeat protein) expression, particularly under-expression, to discriminate cancer and non-cancer cells in a variety of cancers. The invention further provides methods and materials based on OMD and\or PRELP for use in therapy e.g. to suppress cancer initiation or development.

Abstract: The present invention provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.

Abstract: Compositions for antagonizing phosphorylation and subsequent degradation of glycogen synthase kinase 3 beta (GSK3?) in epidermal cells are disclosed. GSK3? phosphorylation antagonists include molecules that function to inhibit or reduce the binding activity or enzymatic activity of an upstream signaling molecule leading to GSK3? phosphorylation, or by downregulating the expression of one or more upstream signaling molecules involved in regulating GSK3? phosphorylation. Methods of using the GSK3? phosphorylation antagonists to inhibit or reduce the phosphorylation and degradation of GSK3? in epidermal cells are provided. The methods are useful to promote epithelialization and closure of wounds, such as chronic non-healing wounds.

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: The invention relates to methods and compositions for the treatment of constipation. The method of the invention involves administration of a suppository containing chlorophyll, chlorophyllin copper complex or chlorophyllin. The suppository contains an outer layer to prevent spillage of chlorophyll or chlorophyllin prior or after administration. Other ingredients that may also be effective treatments may be included. This method may be useful as a new and safer treatment for constipation, including constipation-predominant IBS and other functional anorectal disorders. Chlorophyll, or chlorophyll copper complex and chlorophyllin in the suppository form may improve bowel activity by stimulation of secretion and motility, thus relieving symptoms of constipation. This is the first description of this unique method of delivering these safe, natural products to patients suffering from constipation.

Abstract: Provided are compositions and methods for treatment of conditions and diseases of the skin, for example fine lines and wrinkles and rosacea. The compositions include a porphyrin that is a chlorophyllin, a chlorin compound, a complex of a chlorin compound, or a salt or ester of the chlorin compound or its complex.

Abstract: The invention concerns methods of treating suicidal ideation or behavior in a subject in need thereof, comprising decreasing endogenous nicotinic acetylcholine receptor (nAChR) activity in the subject; therapeutic packages for treating suicidal ideation or behavior; and methods for determining the efficacy of a treatment for suicidal ideation or behavior. In some embodiments, the treatment methods comprise administering to the subject an effective amount of an inhibitor of a nAChR, such as a lithium compound, mecamylamine, clozapine, or asenapine.