Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of cytopathic diseases. Cytopathic diseases may be caused by a variety means such as viral infections like HIV and AIDS, or the development of neoplasms in a mammalian subject. The methods and compositions of the invention are effective for inhibiting de novo HIV infection, upregulating viral expression from latent provirus, inhibiting HIV-induced cytopathic effects, down regulating the HIV receptor, increasing Th1 cytokine expression, decreasing Th2 cytokine expression, increasing ERK phosphorylation, inducing apoptosis in malignant cells, inducing remission, maintaining remission, as chemotherapeutic agents, as well as for decreasing symptoms of cytopathic diseases and opportunistic infections that may accompany such diseases.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: The compound is used in pharmaceutical compositions and in a method of treatment of a disease or medical condition which benefits from inhibition of gap junction activity by administering to a subject suffering from such disease or condition.

Abstract: The present invention discloses esters of 4,9-dihydroxy-naphtho[2,3-b]furans and methods of making and using the same. The present invention also discloses conversion of the esters into therapeutically active 4,9-dihydroxy-naphtho[2,3-b]furans in vivo. The present invention furthermore discloses pharmaceutical compositions comprising the esters of 4,9-dihydroxy-naphtho[2,3-b]furans for the treatment of various indications including proliferative diseases.

Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.

Abstract: This invention relates to anti-cancer compounds and to methods for treating or preventing cancer. In one aspect the invention concerns mitochondrially delivered pro-oxidant anti-cancer compounds that generate reactive oxygen species and induce apoptosis of cancerous cells. The delivery moiety can be a lipophilic cation and the pro-oxidant vitamin E analogue, such as ?-tocopheryl succinate, ?-tocopheryl maleate, ?-tocopheryl maleyl amide, or 2,5,7,8-tetramethyl-2R-(4R,8R,12-trimethyltridecyl)-chroman-6-yloxyacetic acid (?-tocopheryloxyacetic acid).

Abstract: The disclosure provides novel trioxane sulfur dimers having Formula I: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer, proliferative disorders, and/or malaria using these compounds and/or compositions.

Abstract: One object of the present invention is to provide a biosensor and a production method therefor, by which hydrogel that enables immobilization of a physiologically active substance can be conveniently produced using safe raw materials. The present invention provides a biosensor which comprises a substrate having a metal layer on its surface, wherein a hydrophilic polymer having a reactive functional group capable of reacting with a hydroxyl group or an amino group of a physiologically active substance is bound to the metal layer directly or indirectly via an intermediate layer.

Abstract: The present invention relates to a cosmetic composition, which comprises a combination of at least two osmolytes chosen from the group comprising taurine or a derivative thereof, inositol, betaine and trehalose. This composition is intended for restoring, maintaining or reinforcing the moisturization of the skin and/or for protecting it against different types of stress and/or for preventing or retarding the appearance of the signs of aging of the skin, or for attenuating the effects thereof, or alternatively for promoting cell or tissue longevity.

Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.

Abstract: Disclosed is an insecticidal composition comprising by weight based on the total weight of the composition: (a) from about 9 to about 91% of one or more anthranilic diamide insecticides; and (b) from about 9 to about 91% of an acrylate/methacrylate-based diblock copolymer component having a water solubility of at least about 5% by weight at 20° C., a hydrophilic-lipophilic balance value of at least about 3, and an average molecular weight ranging from about 1,500 to about 50,000 daltons; wherein the ratio of component (b) to component (a) is about 1:10 to about 10:1 by weight. Also disclosed is a geotropic propagule coated with the insecticidal composition. Further disclosed is a liquid composition comprising the insecticidal composition, and a method for protecting a geotropic propagule and plant derived therefrom from a phytophagous insect pest.

Abstract: The present invention discloses a method of treating, reducing the occurrence of, or improving the symptoms associated with a skin condition by topical application of a compound of formula (I) or a salt thereof, wherein said skin condition is selected from the group consisting of melanogenesis, oxidative damage, inflammation, skin irritation from inflammation, loss of cell adhesion, loss of desquamation, extra-cellular including connective tissue matrix breakdown and skin tone loss thereof, loss of keratinization, cellular senescence, skin aging from cellular senescence, loss of skin whiteness, loss of skin barrier function, loss of skin firmness, rosacea, skin wrinkles and fine lines from cellular senescence, cellular oxidation, loss of skin collagen, topical wounds, and combinations thereof.

Abstract: The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed.

Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed

Abstract: An emulsion concentrate for spontaneous emulsion preparation is described, comprising at least one ectoparasiticidal active ingredient. Moreover, a process for the preparation of a corresponding emulsion concentrate, and also its use for producing emulsions are described. An emulsion which is obtained starting from the emulsion concentrate, and also its use, are also described.

Abstract: The present invention relates to a novel delivery system for delivering therapeutic agents into living cells, and more particularly, to novel chemical moieties that are designed capable of targeting and/or penetrating cells or other targets of interest and further capable of binding therapeutic agents to be delivered to these cells, and to delivery systems containing same.

Abstract: Pesticide strips used to control parasitic mites in honeybees. The pesticide strips are designed to have a lifetime or period of existence, after which the strip no longer exists in its original form. The strip breaks down, such as by disintegration, dissolving, decomposition, being eaten or carrier away, or otherwise degrading over time, so that at the end of the recommended lifetime, the strip is no longer in its original form. In most embodiments, at least 50% of the strip is no longer present, and in other embodiments at least 75% of the strip is no longer present. Preferably, at the end of the recommended lifetime, the strip no longer exists, at least the body of the strip that included the active ingredient. With this design, the strip does not provide extended low-dose pesticide that can be detrimental in treating the mites.

Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases.

Abstract: Artemisinin-derived monomers and artemisinin dimers are shown to exhibit in-vitro anti-cytomegalovirus (CMV) activity. Artemisinin dimers effectively inhibited CMV replication in human foreskin fibroblasts and human embryonic lung fibroblasts with no cytotoxicity at concentrations required for complete CMV inhibition. Artemisinin dimers were found to be potent and non-cytotoxic inhibitors of CMV replication, which indicates their use as therapeutic agents for the treatment of CMV infection in humans.

Abstract: A compound of the formula is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions for inhibiting HIV protease activity and treating HIV infection are also disclosed.

Abstract: The present invention discloses certain chirally correct polyene cyclodextrin acetals and hemiacetals (formula I) that are effective in providing skin clarification, which is useful for the treatment of acne, and skin disfigurements and skin darkening resulting from acne; skin darkening from cancer, diabetes, radiation treatments, chemotherapy, and sun-burn; mitochondrial and DNA dysfunction; age spots; loss of cellular antioxidants; skin changes associated with aging including collagen loss, loss of skin pliability, loss of skin suppleness, skin wrinkles and fine lines, oxidation, damage from radiation, damage from free radicals, and damage from UV; dry skin; xerosis; ichthyosis; dandruff; brownish spots; keratoses; melasma; lentigines; liver spots; skin pigmentation including pigmented spots, dark circles under the eyes, darkened skin, and blemishes; oily skin; warts; eczema; pruritic skin; psoriasis; inflammatory dermatoses; topical inflammation; disturbed keratinization; scalp dryness, and combinations th

Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.

Abstract: A new anticancer compounds of formula (1) Drugs and pharmaceutical compositions to be used in human or veterinary medicine, which include at least one compound of formula (1).

Abstract: The present invention relates to an andrographolide derivative of the formula (I), wherein R1, R2 and R3 are same or different substituents selected from hydrogen, substituted or unsubstituted organic acid radicals, inorganic acid radicals, alkyl, aryl or heteroaryl, and at least one of R1, R2 and R3 is R-lipoic acid, S-lipoic acid or a mixture thereof, or corresponding dihydrolipoic acids thereof, or N-acetylcysteine radical. The derivative has good antitumor effect, can induce apoptosis of tumor cells, can directly kill Gram-positive bacteria (staphylococcus aureus) and drug resistance bacteria (MRSA5676 and MRSA5677), can inhibit the QS-system of Gram-negative bacteria (Pseudomonas aeruginosa), can inhibit and destroy the formation of biofilm of Pseudomonas aeruginosa; and exhibits significant hypoglycemic effect, so that it can be used in manufacture of medicaments for treatment of cancers, inflammation, diabetes, and bacterial and viral infections.

Abstract: The invention relates to methods for improving renal (kidney) function. Methods for decreasing blood urea nitrogen (BUN), for increasing glomerular filtration rate (GFR), and for decreasing serum creatinine are also provided.

Abstract: Described herein are ?9-THC prodrugs, methods of making ?9-THC prodrugs, formulations comprising ?9-THC prodrugs and methods of using ?9-THC. One embodiment described herein relates to the transdermal administration of a ?9-THC prodrug for treating and preventing diseases and/or disorders.

Abstract: A phosphate-containing nanoparticle delivery vehicle includes nanoparticle, an active ingredient, and a phosphodiester moiety connecting the nanoparticle and the active ingredient and forms a prodrug. The nanoparticle delivery vehicle achieves the function of increasing hydrophilicity of the active ingredient and specificity against tumor cells. Advantages of the nanoparticle material include biocompatibility, magnetism and/or controllable drug release.

Abstract: An object of the present invention is to provide a biosensor and a method for immobilizing a physiologically active substance, by which preconcentration effects can be obtained at a pH that is equivalent to or higher than the isoelectric point of the physiologically active substance and the physiologically active substance can be covalently bound to the surface. The present invention provides a biosensor comprising a solid substrate to which a polymer having a primary or secondary amino group is bound, by which a physiologically active substance can be chemically immobilized following preconcentration of the substance at a pH that is equivalent to or higher than the isoelectric point of the substance.

Abstract: Compounds of the formula, A-L-B, wherein A is glutamate or a glutamate analog; L is a phosphoramidate or a phosphoramidate analog; and B is serine or a serine analog are described which are potent inhibitors of prostate-specific membrane antigen (PMSA). Such compounds are useful in treatment of prostate cancer; and when chemically attached to a fluorescent dye, can efficiently and selectively label prostate cancer cells for fluorescent imaging.

Abstract: The present invention relates to novel bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed

Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.

Abstract: The present invention relates to the use of a novel class of cancer stem cell pathway (CSCP) inhibitors; to methods of using such compounds to treat refractory, recurrent, or metastatic cancers; to methods of selective killing cancer cells by using such compounds with specific administration regimen; to methods of targeting cancer stem cells by inhibiting Stat3 pathway; to methods of using novel compounds in the treatment of conditions or disorders in a mammal related to aberrant Stat3 pathway activity; and to processes for preparing such compounds and intermediates thereof, and to the pharmaceutical composition of relevant compounds, and to the specific methods of administration of these compounds.

Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.

Abstract: The invention provides compounds of formula (I): or a salt thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using the compounds of formula I.

Abstract: The present inventions provides crystalline forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-(1-{4-[(diethoxyphosphoryl)methoxy]phenyl}-3-hydroxy-4-[4-methoxy-N-(2-methylpropyl)benzenesulfonamido]butan-2-yl)carbamate, methods of preparing the crystalline forms, pharmaceutical compositions containing the crystalline forms, and therapeutic uses thereof.

Abstract: Provided are coumarin compounds of formula I, for example, robustic acid methyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.

Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.

Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.

Abstract: This invention relates to certain chirally-correct mitoprotectant phosphorylated heterocyclic agents [formula (I)], which are useful for the treatment of dermatological disorders that include challenged skin from cancer, diabetes, radiation treatments, chemotherapy, and sun-burn; mitochondrial dysfunction; age spots; acne, loss of cellular antioxidants; skin changes associated with aging including collagen loss, loss of skin pliability, loss of skin suppleness, skin wrinkles and fine lines, oxidation, damage from radiation, damage from free radicals, and damage from UV; dry skin; xerosis; ichthyosis; dandruff; brownish spots; keratoses; melasma; lentigines; liver spots; skin pigmentation including pigmented spots, dark circles under the eyes, darkened skin, and blemishes; oily skin; warts; eczema; pruritic skin; psoriasis; inflammatory dermatoses; topical inflammation; disturbed keratinization; scalp dryness; skin depigmentation, and combinations thereof;

Abstract: A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.

Abstract: A compound of formula (I) is described; wherein the substituents are as defined in the text and wherein the compound is intended for use in the production of a vascular damaging effect in a warm-blooded animal.

Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.

Abstract: Compositions and methods for reducing, preventing, mitigating, and/or delaying the onset of, attenuating the severity of, and/or hastening the resolution of, for example, one or more chemotherapy-associated toxicities in a subject receiving one or more chemotherapeutic agents. In addition compositions and methods for mitigating or preventing a novel form of chemotherapy-induced peripheral neuropathy are disclosed and claimed.

Abstract: Certain 2- and/or 3-substituted 5,6,7 substituted chromones are of use in treatment of treating diseases associated with overproduction of TNF-?, diseases associated with overproduction of superoxide anion radical And the treatment of organ damage. Some of the compounds are novel.

Abstract: The present invention relates to spiroketal compounds that are useful in methods of treating or preventing protozoal infections, parasitic infections, bacterial infections, cell proliferative disorders and anti inflammatory disorders. The spiroketal compounds are also useful as immunosuppressive agents, and also in methods of controlling pests.

Abstract: Provided are: method of producing a sulfur-containing proanthocyanidin oligomer by reducing the molecular weight of proanthocyanidin in plants so that they can be readily absorbed through the intestine of an organism; and a health food composition and a pharmaceutical composition which contain the resultant sulfur-containing proanthocyanidin oligomer as an active ingredient and which are useful for treating and preventing various lifestyle-related diseases and brain diseases caused by generation of active oxygen species as well as for preventing aging.

Abstract: The present invention provides methods and compositions to replace up to 90% of erythropoietin use in the treatment of anemias and hypoxias. The method employs acid and salt forms of inositol-tripyrophosphate (ITPP) isomers to shift the P50 value of hemoglobin, thereby improving the rate and efficiency of oxygenation by blood even when red blood cell counts are low. Indications for the new method include anemias and hypoxia arising from infection, chemotherapy, premature birth, altitude change, compromised lung or heart function, aplastic anemia and anemia associated with a myelodysplastic syndrome, and other causes.

Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.

Abstract: The present invention relates to compounds of the formula (I), where R1 to R3 each, independently of one another, denote H, hydroxyl or alkoxy having 1 to 8 C atoms, R4 denotes alkyl having 1 to 4 C atoms, H, hydroxyl or alkoxy having 1 to 8 C atoms, R5 denotes H or hydroxyl, and R6 denotes H or alkyl having 1 to 18 C atoms, or salts thereof, but where all R1 to R4 together cannot be equal to H, to compositions, and to the preparation and use thereof.