Abstract: A composition suitable for use in a transdermal delivery patch for administration of an opioid, the composition comprising a phosphate compound of tocopherol and a polymer carrier.

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.

Abstract: A method for preventing hyperpigmented skin, undesired pigmentation disorder of skin, or undesired darkening of skin using coumarin compounds, the use of such compounds, and compositions and formulations thereof are disclosed. In a particular embodiment, the coumarin compounds are selected from robustic acid methyl ether, scandenin, and coumophos. The compounds may be prepared as additives to pharmaceutical and cosmetic compositions, and in personal care products such as antiperspirants. In a particular embodiment extends to an antiperspirant product containing a skin darkening inhibitory amount of a compound of the invention. Also, the present skin darkening compounds may be prepared in combination with each other.

Abstract: A dermatological anti-wrinkle agent and an anti-wrinkle cosmetic are stable and satisfactorily effective against wrinkles. The dermatological anti-wrinkle agent includes a tocopherol phosphate represented by the following formula (1): and/or a salt thereof, wherein R1, R2, and R3 represent a hydrogen atom or a methyl group. The anti-wrinkle cosmetic includes the anti-wrinkle agent.

Abstract: The present invention relates generally to new chemical combinations and methods for their use in the treatment of proliferative diseases and in particular cancer.

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: 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: The present invention relates to a sesamol derivative or its salt, and a skin external composition containing the same. More particularly, the invention relates to a sesamol derivative or its salt, which consists of sesamol and 3-aminopropane phosphoric acid, linked with each other by a phosphoric acid diester bond, and can be degraded into sesamol and 3-aminopropane phosphoric acid by enzymes present on the skin so as to simultaneously show the physiological activities of sesamol and 3-aminopropane phosphoric acid, as well as a preparation method thereof and a skin external composition containing the same.

Abstract: Autotaxin (ATX) is a prometastatic enzyme initially isolated from the conditioned media of human melanoma cells that stimulates a myriad of biological activities including angiogenesis and the promotion of cell growth, survival, and differentiation through the production of lysophosphatidic acid (LPA). ATX increases the aggressiveness and invasiveness of transformed cells, and ATX levels directly correlate with tumor stage and grade in several human malignancies. To study the role of ATX in the pathogenesis of malignant melanoma, we developed antibodies and small molecule inhibitors against recombinant human protein. Immunohistochemistry of paraffin embedded human tissue demonstrates that ATX levels are markedly increased in human primary and metastatic melanoma relative to benign nevi. Chemical screens identified several small molecule inhibitors with binding constants ranging from nanomolar to low micromolar.

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: Novobiocin analogues are useful in methods of treating, inhibiting, and/or preventing cyst formation in autosomal dominant polycystic kidney disease (ADPKD) in a subject. The disclosure provides methods of treating ADPKD comprising administering a therapeutically effective amount of a coumarin-3-carboxamide novobiocin analogue. Accordingly, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of mTOR pathway phosphoproteins P-mTOR, P-Akt and P-S6K, or combinations thereof. Further, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of Hsp-90 client proteins CFTR, ErbB2, c-Raf and Cdk4, or combinations thereof.

Abstract: Microparticle compositions comprising metal ion-lipid complexes for drug delivery are described including methods of making the microparticle compositions and methods of treating certain conditions and disease states by administering the microparticle compositions. The metal ion-lipid complexes can be combined with various drugs or active agents for therapeutic administration. The microparticle compositions of the present invention have superior stability to other microparticle compositions resulting in a microparticle composition with longer shelf life and improved dispersability. The microparticle compositions of the present invention have a transition temperature (Tg) of at least 20° C. above the recommended storage temperature (Tst) for drug delivery.

Abstract: A process for the synthesis of bisfuran intermediates of formula (0) useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed. Furthermore disclosed is a HIV protease inhibitor of formula (IV) as well as various intermediates thereof.

Abstract: Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.

Abstract: The invention encompasses methods of decreasing the lumenal diameter of a blood vessel by contacting the vessel with a myosin light chain phosphatase inhibitor.

Abstract: This invention relates with the gambogic acid glycoside derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: X1, X2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted glycosyl, optionally substituted multi-hydroxyl, optional substituent oxy, optional substituent containing carbon, oxygen, sulfur, nitrogen or phosphorus element. Compounds of the present invention are useful as therapeutically effective agents of anti-cancer, anti-virus and anti-bacterial. This invention also relates with their preparative methods and applications.

Abstract: The invention relates to phosphorylated polyphenols, phosphorylated flavonoids, and phosphorylated pyrone analogs. Methods and compositions for the modulation of side effects of substances using such phosphorylated compounds are described. Methods and compositions are described for the modulation of blood-tissue barrier (BTB) transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide lowered side effects when phosphorylated pyrone analogs are coadministered with therapeutic agents.

Abstract: There is provided a method of inhibiting the occurrence of one of more of the following conditions:—the proliferation of monocytes/macrophages; or—the proliferation of smooth muscle cells; or—the expression of CD36 receptors; or—the uptake of oxidized LDL, the method comprising the step of administering an effective amount of one or more phosphate derivatives of one or more electron transfer agents.

Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class. 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: 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: 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: Methods are described for the treatment and prevention of metabolic disorders or other diseases by administering a pyrone analog or a derivative thereof. Methods are also described for the treatment and prevention of metabolic disorders and other diseases by administering a pyrone analog, or a derivative thereof, in combination with one or more additional agents such as, for example, lipid lowering agents or glucose lowering agents. Methods are described for the modulation of lipid transporter activity to increase the efflux of lipid from a physiological compartment into an external environment. Methods disclosed herein may be used to assess treatment or prevention of a metabolic disorder following administration of a pyrone analog or a derivative thereof.

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

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

Abstract: Tocopheryl succinate derivatives according to formula I: are described. These compounds increase the activity of protein phosphatase 2A, can be included in pharmaceutical compositions, and can be used for the treatment of androgen receptor-dependent cancers such as prostate cancer.

Abstract: There is provided an alkaloid formulation comprising the reaction product of one or more alkaloids with one or more phosphate derivatives of one or more electron transfer agents.

Abstract: The invention relates to novel and known substituted phosphonates for use in ameliorating amyloid aggregates, particularly for use in the treatment of Alzheimer's disease.

Abstract: The invention relates to phosphorylated polyphenols, phosphorylated flavonoids, and phosphorylated pyrone analogs. Methods and compositions for the modulation of side effects of substances using such phosphorylated compounds are described. Methods and compositions are described for the modulation of blood-tissue barrier (BTB) transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide lowered side effects when phosphorylated pyrone analogs are coadministered with therapeutic agents.

Abstract: Methods are described for the treatment and prevention of metabolic disorders or other diseases by administering a pyrone analog or a derivative thereof. Methods are also described for the treatment and prevention of metabolic disorders and other diseases by administering a pyrone analog, or a derivative thereof, in combination with one or more additional agents such as, for example, lipid lowering agents or glucose lowering agents. Methods are described for the modulation of lipid transporter activity to increase the efflux of lipid from a physiological compartment into an external environment. Methods disclosed herein may be used to assess treatment or prevention of a metabolic disorder following administration of a pyrone analog or a derivative thereof.

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 instant invention discloses methods of preparing phospholipid delivery systems encapsulating one or more bio-affecting compounds, said methods comprising solubilizing a heterogeneous phospholipid mixture into a suitable organic solvent to form a concentrated formulation of phospholipids, wherein the phospholipids comprise a charged phospholipid species, and mixing the concentrated formulation with an aqueous solution comprising at least one bio-affecting compound. The instant invention also discloses methods of using a phospholipid delivery system encapsulating at least one bio-affecting compound for administration to an individual in need thereof.

Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The invention relates to phosphorylated polyphenols, phosphorylated flavonoids, and phosphorylated pyrone analogs. Methods and compositions for the modulation of side effects of substances using such phosphorylated compounds are described. Methods and compositions are described for the modulation of blood-tissue barrier (BTB) transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide lowered side effects when phosphorylated pyrone analogs are coadministered with therapeutic agents.

Abstract: The present invention provides a 3?,4?,5-trimethoxy flavone derivative and a pharmaceutically acceptable salt thereof, preparation thereof, and a pharmaceutical composition for the treatment and prevention of dry eye syndrome comprising the same as an active ingredient. The 3?,4?,5-trimethoxy flavone derivative and its pharmaceutically acceptable salt inhibit corneal damage through excellent stimulatory action on mucus secretion in the conjunctiva and therefore may be effective as a prophylactic or therapeutic agent for dry eye syndrome.

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: Administration of either a tocopherol represented by the general formula (1) or a tocotrienol compound ester derivative before or after exposure to radiation is effective in preventing or treating health disorders caused by the radiation exposure.

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: The present invention relates to compounds of the formula (I), where R1 to 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.

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

Abstract: Methods and compositions are described for the modulation of hyperglycemia and/or one or more symptoms of hyperglycemia. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of calcineurin inhibitors out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity to increase the efflux of calcineurin inhibitor from physiological compartments.

Abstract: The invention provides novel trioxane dimers having formulae III, IV or V: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer and/or malaria using these compounds and compositions.

Abstract: The subject invention concerns platinum complexes that exhibit antitumor cell and/or antiparasitic activity. The subject invention also concerns the use of platinum complexes of the invention to treat oncological and inflammatory disorders. The platinum complexes of the invention can also be used to treat or prevent infection by a virus or a bacterial or parasitic organism in vivo or in vitro.

Abstract: This invention relates to a powder composition comprising a silicone represented by the following formula (1) comprising an alcoholic hydroxyl group, and a powder, to an oil-based powder composition formed by dispersing this powder composition in an oil, and to a cosmetic material containing these materials. R1aR2bR3cSiO(4?a?b?c)/2??(1) where, in formula (1), R1 are identical or different organic groups selected from alkyl groups, aryl, aralkyl or fluorinated alkyl groups having 1-30 carbon atoms, R2 is a substituent having one or more alcoholic hydroxy groups, R3 is a group represented by the following general formula (2), ?and a, b, c, d are integers satisfying the relations: 1.0?a?2.5, 0.01?b?1, 0.001?c?1, 1.5?a+b+c?2.6, and 0?d?500. The powder composition of this invention has little cohesion, excellent dispersibility and excellent stability over time as an oil-based powder composition.

Abstract: There is provided a therapy for lowering the blood levels of a lipid selected from the group comprising LDL cholesterol, triglycerides, overall cholesterol and mixtures thereof, the therapy comprising the step of administering an effective amount of one or more phosphate derivatives of one or more electron transfer agents.

Abstract: The invention relates to the use of a compound of the formula (I) for the treatment of bacterial infections caused by mycobacteria and related microorganisms, such as tuberculosis, leprosy, nocardiosis, diphtheria, pulmonary mycobacterial infection, cutaneous mycobacterial infection, atypical mycobacterial infection and mycobacteriosis.

Abstract: The invention is related to phosphonate substituted compounds having immuno-modulatory activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: A dermatological anti-wrinkle agent and an anti-wrinkle cosmetic are stable and satisfactorily effective against wrinkles. The dermatological anti-wrinkle agent comprises a tocopherol phosphate represented by the following formula (1): and/or a salt thereof, wherein R1, R2, and R3 represent a hydrogen atom or a methyl group. The anti-wrinkle cosmetic includes the anti-wrinkle agent.

Abstract: The present invention relates to a method for topical delivery of trace metals for the modulation of certain metalloenzymes. The method of topical delivery of the present invention comprises; (i) mixing of a trace metal salt of a phosphorylated nitrogen heterocyclic base complexed with a chelating agent [Figure l], and (ii) a carrier, and (iii) topical application of said mixture. The modulation of metalloenzymes such as Superoxide Dismutase, Elastase, Tyrosinase, Matrix metalloproteases, and Ubiquitin-Proteasome pathway by the methods of the present invention is useful for providing anti-inflammatory, skin whitening, wrinkles reduction, skin aging control, cellular antioxidant, acne control, hair growth modulation, and skin damage control benefits.

Abstract: There is provided a dietary or health supplement comprising an effective amount of a micronutrient selected from the group consisting of phosphate derivatives of tocopherol, ubiquinol, ascorbic acid, tocotrienol, retinol and mixtures thereof delivered with an acceptable carrier.

Abstract: 7,8-Bicyclic-chroman derivatives of Formula I: wherein the substituents are defined as in the specification or the pharmaceutically acceptable salts thereof, are disclosed. They are useful for the treatment of inflammatory disorders, neurodegenerative disorders and/or mitochondrial disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.