Abstract: A cyclic polycarboxylic acid anhydride, a polycarboxylic acid, or a mixture of them is allowed to react with hydroxylamine or a salt thereof in an organic solvent under dewatering conditions to yield a corresponding cyclic N-hydroxyimide compound. The cyclic polycarboxylic acid anhydride can be, for example, succinic anhydride or glutaric anhydride. The polycarboxylic acid can be, for example, succinic acid, glutaric acid, or adipic acid. In this process, the reaction is preferably carried out using an organic solvent capable of undergoing azeotropy with water as all or part of a reaction solvent while removing water from the reaction system by azeotropy with the organic solvent. This process produces a cyclic N-hydroxyimide compound in a good yield from any of a cyclic polycarboxylic acid anhydride and a polycarboxylic acid.

Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses in pharmaceutical formulations for the treatment of pain.

Abstract: The present invention pertains to the discovery that B. anthracis possesses a luxS gene that encodes a functional LuxS polypeptide, and that B. anthracis synthesizes a functional AI-2 quorum-sensing molecule. The invention provides mutant B. anthracis bacteria lacking the function of the luxS gene, which do not produce a functional AI-2 molecule and have growth defects compared to wild-type B. anthracis. The invention also concerns methods for inhibiting the growth of B. anthracis, or for preventing or treating B. anthracis infection, by inhibiting the activity of the B. anthracis LuxS polypeptide, or by exposure of the B. anthracis to furanone. In particular, the invention concerns the use of furanone, a compound that inhibits AI-2-mediated quorum-sensing, to inhibit the growth of B. anthracis, to inhibit B. anthracis toxin production, particularly that of protective antigen, and to prevent or treat B. anthracis infection. The invention also provides methods to prevent B.

Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.

Abstract: Disclosed herein are isolated compounds or pharmaceutically acceptable salts thereof, which exhibit immunostimulatory or anti-inflammatory effects. The compounds are isolated from the fruiting body of A. camphorata in a solid culture. Also disclosed are methods of stimulating immune responses and/or treating an inflammatory disorder with these compounds and pharmaceutical compositions including the compounds or pharmaceutically acceptable salts thereof.

Abstract: The present invention provides an antimalarial compound 3-[2-(2-Hydroxymethyl-1,4a,5-trimethyl-7-oxo-1,2,3,4,4a,7 8,8a-octahydronaphthalen-1-yl)-ethyl]-5H-furan-2-one of the formula 1 given below or pharmaceutically acceptable derivatives thereof, isolated from Gomphostema niveum and also provides a method for the extraction thereof as well as methods for the treatment of malaria using said compound.

Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.

Abstract: Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a fatty acid metabolism inhibitor, a glycolytic inhibitor, and/or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherapeutic agents. In preferred embodiments, the invention combines an oxirane carboxylic acid, represented by etomoxir, with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose, and/or an antibody against UCP and/or Fas antigen. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.

Abstract: The present invention is directed to the use of EP2 and/or EP4 agonists as therapeutics for the treatment of diseases associated with influenza A viruses, such as for example H5N1 and mutations thereof.

Abstract: Disclosed are a composition for reducing beta amyloid-induced neurotoxicity by inhibiting ?-secretase activity, comprising a dibenzofuran derivative, and a method for preparing the same. Further disclosed is that the combination of the dibenzofuran derivative with a ?-secretase inhibitor or an anti-inflammatory agent shows higher activity with respect to reducing beta amyloid-induced neurotoxicity.

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 disclosure provides copolymers including a first monomer including at least one phospholipid possessing at least one vinyl group and a second monomer including a furanone possessing vinyl and/or acrylate groups. Compositions, medical devices, and coatings including such copolymers are also provided.

Abstract: Methods of stimulating immune response or treating an inflammatory disorder with one of a number of the compounds disclosed herein or a pharmaceutically acceptable salt thereof.

Abstract: A method for inhibiting formation of adhesions following abdominal surgery which involves application of an anti-static fatty acid ethoxylated amide (Cocamide DEA) in a matrix that is placed in the peritoneal cavity at the conclusion of an abdominal surgery and which releases this anti-adhesive chemical over a predetermined time in a range up to seven days. Tests conducted on laboratory rats established that the method reduced the incidence of adhesions from 100 percent (100%) in a test model to near zero in the majority of treated animals. In an alternative embodiment, andrographalide was delivered via a pump with similar results. In still another embodiment, an effective amount of 50% phosphatidylchorene and propylene glycol was delivered, via a pump, into the abdominal cavity, again with similar results.

Abstract: A method of obtaining one or more fractions from one or more plants is disclosed. The method includes subjecting one or more parts of the one or more plants to hydro-alcoholic extraction in presence of a water-insoluble solvent to obtain one or more extracts. The method further includes subjecting the one or more extracts to one or more of de-pigmentation, de-fatting and detoxification process to obtain the one or more fractions. The one or more fractions thus obtained contain a desired pharmacologically active ingredient in concentration greater than concentrations of other pharmacologically active ingredients present in the at least one fraction. Further, the one or more fractions are less toxic as compared with corresponding one or more fractions obtained by conventional methods. In addition, the one or more fractions are therapeutically more effective in various diseases as compared to one or more fractions obtained by conventional methods.

Abstract: A system and method for reverting the antibiotic tolerance of persister cells. Brominated furanones, which are quorum sensing inhibitors, are used to revert the antibiotic tolerance of persister cells and enhance their susceptibility to antibiotics by up to one hundred fold. Brominated furanones can be used against bacterial persister cells in biofilms or planktonic form.

Abstract: A novel antiseptic agent composition which has a wide antimicrobial spectrum and excellent antiseptic properties is provided. An antiseptic agent composition A contains a glycerin hydroxy fatty acid monoester that is an ester of glycerin and a hydroxy fatty acid having 8 to 18 carbon atoms, and a specific antiseptic agent such as an alkanediol. An antiseptic agent composition B contains the glycerin hydroxy fatty acid monoester and an aromatic antiseptic agent. An antiseptic agent composition C contains the glycerin hydroxy fatty acid monoester and a chelating agent.

Abstract: The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.

Abstract: Benzolipoxin analogs, methods of their preparation and pharmaceutical compositions containing the compounds are provided. The compounds and compositions are useful in methods for treatment of various diseases, including, inflammation, autoimmune disease and abnormal cell proliferation.

Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: The invention relates to compounds derived from betulin, and to the use thereof in plant pest control, particularly as antifeedants for butterfly larvae, beetles and snails. Further, the invention relates to novel betulin derivatives and methods for the production thereof either directly from betulin, or via intermediates derived therefrom.

Abstract: PROBLEM TO BE SOLVED A burdock fruit extract containing arctigenin at high content and its production method are provided, and both of which are used for treatment of pancreatic cancer. SOLUTION The burdock fruit extract containing arctigenin at high content by enzymatically converted arctiin into arctigenin with beta-glucosidase, which is an enzyme occurring endogenously in a burdock fruit, and adding ethanol, extracting, concentrating and then freeze-drying or spray drying.

Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: We describe for the first time that andrographolide derivatives such as DDAG effectively reduced OVA-induced inflammatory cell recruitment into BAL fluid, IL-4, IL-5, IL-13 and eotaxin production, serum IgE synthesis, pulmonary eosinophilia, mucus hypersecretion and AHR in a mouse asthma model potentially via inhibition of NF-?B activity. Moreover, low dose of DDAG and glucocorticoid combination treatment synergistically attenuate inflammation in mouse asthma model. These findings support a therapeutic value for DDAG in the treatment of asthma.

Abstract: The present invention relates to the biosynthetic gene cluster for tautomycetin (TTN) produces tautomycetin. Also provided are engineered micro-organisms for the production of TTN and analogs thereof, as well as methods of screening for compounds for activity.

Abstract: The present invention is directed to compositions and methods for pain management, and for treating inflammation or an inflammation-associated disorder in a subject comprising administering to the subject a therapeutically effective amount of a COX-2 inhibitor and a therapeutically effective amount of a prostacyclin analog, such as treprostinil, a pharmaceutically acceptable salt thereof, or a treprostinil derivative described herein.

Abstract: This invention provides new lipoxin analogs, compositions containing analogs, and methods of using these compounds and compositions for treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease. The invention also provides for methods of treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease with compositions containing COX-2 inhibitors. Further, the invention provides methods for preventing systemic diseases beyond theoral cavity that are related to periodontal disease using the composition containing lipoxin analogs, COX-2 inhibitors, or both.

Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

Abstract: An external preparation containing the following components (A) and (B): (A) a non-steroidal analgesic/anti-inflammatory agent, and (B) an organic amine. The external preparation of the present invention has improved skin permeation and excellent stability of a non-steroidal analgesic/anti-inflammatory agent in the external preparation. The external preparation of the present invention also has excellent appearance.

Abstract: The diterpenic labdane 3-[2-[decahydro-6-hydroxy-5-(hydroxymethyl)-5,ha-dimethyl-2-methylene-1-naphthalenyl]ethylidene]-dihydro-4-hydroxy-2(3h)-furanone, chemically diagrammed as inhibits the synthesis of pro-inflammatory cytokines, activates the PPAR-gamma receptor and diminishes nuclear factor kappa B. The compound is useful to treat auto-immune diseases, for organ and tissue transplantation, and to treat immunodeficiency (e.g., AIDS).

Abstract: A substrate (100) comprising a sol-gel derived coating (101). The coating, is chemically bonded to the substrate (100) and is derived from a polysiloxane to form a network of silicon-carbon and silicon-oxygen bonds. An antimicrobial is releasably captured within the network and is capable of defusing from the coating in vivo in response to introduction of a fluid into the coating.

Abstract: A method for inhibiting formation of adhesions following abdominal surgery which involves application of an anti-static fatty acid ethoxylated amide (Cocamide DEA) in a matrix that is placed in the peritoneal cavity at the conclusion of an abdominal surgery and which releases this anti-adhesive chemical over a predetermined time in a range from about five to seven days. Tests conducted on laboratory rats established that the method reduced the incidences of adhesions from 100 percent (100%) in a test model to near zero percent (0%) in the treated animals. In an alternative embodiment, Andrographalide was delivered through a drug pump with similar results. In still another embodiment, an effective amount of Rapamune was delivered, via a pump, into the abdominal cavity, again with similar results.

Abstract: The invention relates compositions and methods for treating pathological lung conditions using whole-grain flaxseed or flaxseed lignans. Specifically, the invention relates to the dietary use of flaxseed lignans.

Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.

Abstract: The present invention concerns a method for modulating the enzymatic activity of an enzyme, wherein said enzyme interacts with BMP, said method comprising the step of administering or inducing Hsp70, or a functional fragment or variant thereof, in a form suitable for allowing interaction between BMP and Hsp70, or said functional fragment or variant thereof, and thereby modulating the enzymatic activity of an enzyme interacting with BMP.

Abstract: The present invention relates to tautomycetin (TTN) and analogs thereof. Also provided are methods of using TTN and analogs thereof in the treatment of various diseases relating to SHP2 function.

Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: The present invention relates to therapeutic compounds that are Nrf2-ARE pathway activators suitable for the treatment of diseases known to be mediated by oxidative stress such as motor neurone disease. The invention also includes compounds identified by methods of the invention for treatment of neurogenerative diseases.

Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the biphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular biphenyl-substituted cyclic ketoenols through the addition of ammonium or phosphium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or nematicides and/or acaricides and/or fungicides and/or for preventing unwanted plant growth.

Abstract: This invention relates generally to methods and pharmaceutical formulations useful in treating patients suffering from obstructive sleep apnea syndrome (OSAS). Treatment of OSAS is effected by administering a carbonic anhydrase inhibitor to the patient in combination with at least one additional active agent. Examples of additional active agents include modafinil, eszopiclone, zolpidem, zaleplon, and phentermine.

Abstract: The present invention concerns a method for identifying a compound which inhibits the activation of RAC GTPase by DOCK5 protein comprising the steps of (i) coexpressing the DOCK5 and the RAC proteins in a cell, wherein said DOCK5 protein induces the conversion of inactive RAC, which inactive RAC is bound to GDP, to active RAC, which active RAC is bound to GTP, (ii) contacting or not said cell with said compound, (iii) determining the conversion of inactive RAC to active RAC in the presence or absence of said compound, and (iv) selecting the compound inhibiting the conversion of inactive RAC to active RAC. Said compound is useful for treating disease-associated bone loss.

Abstract: The present invention provides a Cinnamomum subavenium extract for inhibiting melanogenesis. The present invention also provides a composition for inhibiting melanogenesis including compounds inhibit tyrosinase activity.

Abstract: An oral dosage form of a non-steroidal anti-inflammatory drug (NSAID) is rendered safer for extended or chronic use for anti-inflammatory, analgesic or antipyretic therapy by combining it with an antihypertensive drug. The antihypertensive drug acts prophylactically to inhibit or reduce NSAID-induced hypertension and by so doing the adverse cardiovascular side effects of NSAIDs, such as high blood pressure, heart attack, stroke, opththamologic complications, and death, when NSAIDs are used repetitively over an extended period of time for reducing inflammation or in pain management.

Abstract: The present invention relates to compounds from mycelium of Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) infection.

Abstract: The present invention relates to the identification and diagnostic use of biomarkers in primary colorectal cancer tumors whose activation level are predictive of the likelihood of the onset of metastatic disease. These biomarkers may be used to determine the suitability of a patient for aggressive and/or targeted treatments. Kits and compositions of the invention are also provided.

Abstract: The present disclosure provides copolymers including a first monomer including at least one phospholipid possessing at least one vinyl group and a second monomer including a furanone possessing vinyl and/or acrylate groups. Compositions, medical devices, and coatings including such copolymers are also provided.

Abstract: The present invention is directed to methods and compounds for inhibiting bacterial growth and treating a bacterial infection in a subject. These methods involve providing an inhibitor of intrabacterial pH homeostasis, including inhibitors of the Mycobacterium tuberculosis Rv3671c gene encoded membrane protease. Methods for identifying novel compounds that disrupt intrabacterial pH homeostasis and their use for inhibiting bacterial growth and treating a bacterial infection in a subject are also disclosed.

Abstract: The present invention relates to novel methylene furanone derivatives as well as the use thereof as a protective, antioxidant, or depigmentation agent in cosmetic or dermatological compositions. The invention also relates to a method for preparing said derivatives involving a Suzuki-Miyaura coupling reaction from corresponding dibromofuranone derivatives. The invention also relates to a method of preparation involving a coupling reaction of 2-methoxy-furan derivatives with a ketone followed by dehydration.

Abstract: The invention relates to a method of treating with furanone derivatives and the pharmaceutically acceptable salts thereof, one or more conditions of the skin, in particular regulating skin condition, regulating signs of skin aging, treating a number of conditions such as contact dermatitis, skin irritation, rosacea, acne, psoriasis, and preventing and protecting skin tissue against age-related damage or damage resulting from insults such as harmful (UV) radiation or environmental pollution, stress and fatigue.