Abstract: The present invention relates to a novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof, a production method therefor and a pharmaceutical composition for preventing and treating central nervous system disorders which contains the same as an active component. The novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof according to the present invention can beneficially be used to prevent and treat central nervous system disorders since it exhibits an equivalent biological and pharmacological activity to venlafaxine and salts thereof which are known in the field, it has very little toxicity, and, in particular, it is outstandingly soluble in water as compared with prior-art venlafaxine derivatives.

Abstract: The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type, which alter lymphocyte trafficking. The compounds of the invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.

Abstract: The invention relates generally to methods of influencing central nervous system cells to produce progeny useful in the treatment of CNS disorders. More specifically, the invention includes methods of exposing a patient suffering from such a disorder to a reagent that modulates the proliferation, migration, differentiation and survival of central nervous system cells via S1P or LPA signaling. These methods are useful for reducing at least one symptom of the disorder.

Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a group of formula COR4, or R1 represents a group of formula (A): R2 represents a group of formula NR5R6, or R2 represents a nitrogen-containing heterocyclic group, an aryl group or a heteroaryl group, R3 represents a hydrogen atom or an alkyl group, m represents an integer between 1 and 6 inclusive, n represents 0, 1 or 2, their optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating and/or preventing thrombotic events.

Abstract: An objective of the present invention is to provide a new substance having a cerebral nerve cell neogenesis effect. Another objective is to provide a cerebral nerve cell neogenesis agent that is effective in treating and/or preventing neurological disorders utilizing the substance. With the present invention, a cerebral nerve cell neogenesis agent containing a plasmalogen as an active ingredient is provided. In particular, a preferable cerebral nerve cell neogenesis agent contains, as an active ingredient, a biological tissue (preferably, an avian tissue) extracted plasmalogen mainly including an ethanolamine plasmalogen and a choline plasmalogen.

Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

Abstract: A composition to be used as a permeation enhancer is provided. The composition may be added to topical cosmetics or pharmaceutical formulations that are topically applied. The composition comprises about 10-50% of Pracaxi oil, 15-40% of Patauá oil, 10-30% of Inaja oil, and 10-30% of one of more emollients.

Abstract: The invention generally relates to compositions and methods of their use. More specifically, the invention relates to the use of a compound in modulating erythropoiesis in a subject by mediating the activity and/or quantity of a member present in the LPA3-mediated signaling pathway, such as lysophosphatidic acid receptor subtype 3 (LPA3).

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: S1P receptor modulators are administered following a dosage regimen providing a positive benefit-risk profile.

Abstract: The present invention relates to novel phenyl 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: The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.

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: Endosseous implant to be applied to a human or animal bone, wherein the surface of the implant is made from titanium or a titanium alloy, said implant having a smooth or rough surface texture, which is characterized in that said surface has been treated with at least one selected organic phosphonate compound or a pharmaceutically acceptable salt or ester or an amide thereof; process for producing said implants.

Abstract: Use of an S1P receptor modulator in the treatment or prevention of a disease or condirion dependent on brain-derived neurotrophic factor (BDNF) expression.

Abstract: The invention is directed to a composition and associated method for the treatment of musculoskeletal related disorders and diseases. In particular, the present invention provides a class of citrate compounds that can be used to for the treatment of diseases/disorders characterized by the degeneration of musculoskeletal tissues including menisci, bone, articular cartilage, and soft tissues. Examples of suitable citrate and citrate analog compounds include citrates having the following base formula (I): where X may be one of the following: wherein Y, Y?, and Y? are independently a citrate moiety, O, O—Y, OH, NH, NH—Y, R and R—Y, with R being an alkyl, alkyene, ester, aryl, or phenyl group having from 1 to 6 carbon atoms.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: Methods for treating an individual to improve cognitive function are provided. In the subject methods, an effective amount of a GABAB antagonist, or a blocker of Kir3.2 potassium channels, is administered to the individual, resulting in an improvement in cognitive function of the host. The subject methods find use in a variety of different applications.

Abstract: The present invention is directed to a dry composition which allows delivery of active agents with good bioavailability. These compositions are prepared by emulsifying the active agent using liposome technology known in the art and then encapsulating with a modified starch. The modified starch is prepared by enzymatic hydrolysis of starch after the preparation of a starch derivative containing a hydrophobic group or both a hydrophobic and a hydrophilic group. The resultant composition is a dry powder with excellent bioavailability. Further, the composition has good load levels and stability.

Abstract: To perform large-scale multiplex analysis of lipid-specific binding, lipid microarrays were developed. Lipids identified as disease associated, or analogs there, can be tolerogenic to patients suffering from autoimmune disease. Lipid array analysis has revealed anti-lipid antibodies in patients with immune disorders, and may contribute to the pathogenesis of disease.

Abstract: The present invention provides for methods of preventing or improving cardiometabolic disorders/metabolic disorders, compositions and pharmaceutical compositions comprising therapeutically effective amount of therapeutic phospholipid compositions and therapeutically effective amount of one or more lipid modifying agents, including statins.

Abstract: The invention provides compositions and methods useful for treating wounds and enhancing wound healing. The present invention discloses a continuous polymer coating system to provide sustained localized delivery of bioactive agents. The data demonstrate the efficacy of a bioactive coating comprising the polymer PLAGA and the agent FTY720, a selective agonist for sphingosine 1-phosphate receptors, and biologically active derivatives and analogs thereof, for use in wound healing. In vitro drug release studies validated 64% loading efficiency with complete release of compound following 14 days. Mechanical evaluation of healing bone showed significant enhancement of mechanical stability in FTY720 treatment groups. Superior osseous integration across the host-graft interface, significant enhancement in smooth muscle cell investment, and reduction in leukocyte recruitment were evident in FTY720 treated groups. The present invention is useful for enhancing angiogenesis for wound healing.

Abstract: Described herein are the use of peripheral blood derived germline stem cells and their progenitors, methods of isolation thereof, and methods of use thereof.

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer or a mixture in all proportions of stereoisomers thereof, in particular a mixture of enantiomers, such as a racemic mixture, wherein R represents a (C1-C6)alkyl or (C1-C6)alkenyl group, optionally substituted by one or more groups chosen among an halogen atom, ORa, SRb, NRcRd, PO(ORe)(ORf), CO2Rg, SO2Rh SO3R1, P0(0H)(CH(0H)Rk), CN, N3 and NH—C(?NH)NH2, with Ra, Rb, Rc and Rd, representing, independently of each other, an hydrogen atom, a (C1-C6)alkyl group or a —CO—(C1-C6)alkyl group, Re, Rf, Rg, Rh and R1 representing, independently of each other, an hydrogen atom or a (C1-C6)alkyl group, and Rk representing an aryl or heteroaryl group, said group being optionally substituted by one or more groups selected from an halogen atom and NO2, as well as to the use thereof and to a process for preparing such a compound, to a pharmaceutical composition containing it and to synthesis intermediates.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: Methods for hydrolyzing solid ungranulated lysophosphatidylcholine with phospholipase A2 are provided. Also disclosed are methods for making a lipid matrix of lysophosphatidylcholine, monoglyceride and fatty acid, and lipid matrices of particular structure.

Abstract: The present invention provides an HDL comprising an agent selected from the group consisting of antiproteases, antixoxidants, antimitotics, anti-apoptotic agents and agents involved in the iron metabolism for use as a medicament.

Abstract: Compositions comprising melatonin and one or more carotenoids and methods for using such compositions for enhancing cognitive and related functions such as reducing or preventing a decline of social interaction, reducing or preventing age-related behavioral changes, increasing trainability, improving attention, maintaining optimal brain function, facilitating learning and memory, reducing memory loss, and preventing or treating cognitive decline caused by dementia in an animal. Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.

Abstract: A method for treating the symptoms of multiple sclerosis and related neurodegenerative conditions, using a histamine compound that is methylated in vitro prior to being introduced into the body of the patient. The histamine compound is suitably histamine diphosphate, and may be methylated in vitro by mixing in combination with at least one thiol compound in the presence of at least one methyl group donor compound. The thiol compound is suitably L-reduced glutathione and the methyl group donor is suitably betaine hydrochloride. The compounds are mixed vigorous in an acid environment, to create a shearing force that facilitates exchange of the methyl group from the donor compound to the histamine diphosphate. The resulting methylated histamine compound is suitably administered to the patient by transdermal application. The method also provides a medicament for treatment the symptoms of multiple sclerosis and related neurodegenerative conditions, and a method for preparation of such a medicament.

Abstract: The present invention relates to solid pharmaceutical combinations for oral administration comprising nicotinic acid or a nicotinic acid compound or mixtures thereof in an extended release form and an HMG-CoA reductase inhibitor, which are useful for altering lipid levels in subjects suffering from, for example, hyperlipidemia and atherosclerosis, without causing drug-induced hepatotoxicity, myopathy, or rhabdomyolysis.

Abstract: A composition for treating wood-based material including at least one C1-C7 monocarboxylic acid salt or C1-C7 monocarboxylic acid or a mixture thereof as active agent against deteriation of wood. The composition also includes alkyd emulsion of high unsaturated fatty acid content and/or aluminum ion containing compound in the form of polyaluminum formate in a same aqueous liquid carrier as the C1-C7 monocarboxylic acid salt or C1-C7 monocarboxylic acid or a mixture thereof.

Abstract: A synergistic antimicrobial composition containing a glyphosate compound and diiodomethyl-p-tolylsulfone is provided. Also provided is a method of inhibiting the growth of or controlling the growth of microorganisms in a building material by adding such a synergistic antimicrobial composition. Also provided is a coating composition containing such a synergistic antimicrobial composition, and a dry film made from such a coating composition.

Abstract: The subject of the present invention is the use of aminaphtone for the preparation of a medicament for treating arteriophaties, in particular arteriophaties of a degenerative inflammatory type. Preferably, said medicament is formulated for oral administration.

Abstract: This invention relates to novel compounds that are deuterated derivatives of fingolimod and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a lysophospholipid edg1 (S1P1) receptor agonist, such as fingolimod.

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

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

Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine and a gamma-aminobutyric acid compound at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.

Abstract: The present invention discloses methods for prevention and prophylactic treatment of plant diseases by application of glyphosate to a plant in need of treatment. In certain embodiments, soybean plants in need of treatment at vegetative and reproductive growth stages prior to or subsequent to infection, may be treated with glyphosate in order to prevent infection or suppress disease development, symptomatology, and yield loss. Application of a fungicide (e.g. a strobilurin fungicide such as pyraclostrobin or picoxystrobin) together with glyphosate, is also contemplated. Soybean diseases that may be treated in this manner include Soybean Sudden Death, Brown Stem Rot, Stem Canker, and Charcoal Rot, among others.

Abstract: Compounds of formula wherein the variable are defined in the specification, are used in compositions which stimulate T cell responses.

Abstract: Biocompatible intraocular implants include a steroid and an auxiliary agent, where the auxiliary agent is present in an amount sufficient to lessen the severity of at least one side effect compared to the use of an otherwise identical implant lacking said auxiliary agent. The steroid and the auxiliary agent may be present on the same intraocular implant or on different implants. The steroid and auxiliary agent may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the steroid may be associated with a polymeric coating having one or more openings effective to permit the steroid to be released into an external environment. The implants containing the steroid and an auxiliary agent may be placed in an eye to treat one or more ocular conditions while reducing the side effects otherwise accompanying steroid use.

Abstract: The present invention provides ?-hydroxy-?-aminophosphonates, ?-amino-?-aminophosphonates, and analogs thereof that inhibit carnitine acyltransferases. The invention also provides compositions comprising these ?-hydroxy-?-aminophosphonates, ?-amino-?-aminophosphonates, and analogs, and methods of the use of such compounds and compositions in the treatment, amelioration or prevention of pathological conditions, diseases or disorders that are linked with fatty acid metabolism, such as non-insulin dependent diabetes or obesity. The invention also provides processes for the preparation of such compounds and compositions.

Abstract: The invention includes aqueous compatibilized pesticidal formulations and methods of making them. In typical embodiments, formulations comprise a first electrolytic pesticide and a second electrolytic pesticide, and about 30 to about 300 g/L of at least one alkyl polyglycoside. The invention also includes methods of preparing pesticidal formulations to increase the concentration of the electrolytic pesticides. The invention also includes storage and transport systems containing formulation embodiments. The invention also includes methods inhibiting pests.

Abstract: The present invention relates to compositions that may alleviate symptoms of ocular stress, as well as methods of their production, use, and storage compositions. The compositions comprise at least one ocular epithelial cell associating group and at least one hydrophilic group. In one embodiment the at least one ocular epithelial cell associating group and at least one hydrophilic group are substituents on a conjugated polyaromatic core. The compositions may be used in ophthalmic compositions and ophthalmic devices.

Abstract: The present invention relates to compounds capable of inhibiting and/or decreasing the activity of one or more cathepsins, thereby treating and/or preventing various disease states associated with one or more cysteine proteases including, but not limited to, cathepsins and papain-like cysteine proteases. Disease states treated and/or prevented by the compounds of the invention include, but are not limited to, mammalian parasitic diseases in which the parasite utilizes a critical cysteine protease from the papain family. Examples of parasitic diseases to be treated or prevented by the compounds of the invention include, but are not limited to, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, coccidiosis, giardiosis, cryptosporidiosis or schistosomiasis.

Abstract: The present is based on the finding that folate targeted liposomal alendronate (FT-AL-L) was significantly more potent against two tested cancer cell lines than the free alendronate (AL) or the non-targeted liposomal alendronate (AL-L), as observed by the increased cytotoxicity of the folate targeted liposomal alendronate. Thus, the present disclosure provides targeted liposomes comprising a membrane and an intraliposomal core, the membrane comprising at least one liposome forming lipid and a targeting moiety, such as folate, exposed at the membrane's outer surface; and the intraliposomal core comprising encapsulated therein least one N-containing bisphosphonate. Also provided by the present disclosure are methods of use of the targeted liposomes such as for the treatment of a disease or disorder.

Abstract: Provided are diphenyl sulfide derivatives which have excellent S1P3 antagonistic activity and are useful as drugs. Intensive studies have been made for the purpose of creating a compound having S1P3 antagonistic activity. As a result of the intensive studies, it has been found that diphenyl sulfide derivatives represented by general formula (1) have excellent S1P3 antagonistic activity. In general formula (1), R1 is a hydrogen atom or the like; R2 is an optionally substituted alkyl group having 1 to 6 carbon atoms, or the like; X is a methylene group which may be substituted with one or two fluorine atoms, or the like; Y is a hydrogen atom or the like; and Z is a halogen atom.

Abstract: Suggested are new non-aqueous agricultural compositions, comprising (a) biocides and (b) alkoxylation products of unsaturated fatty alcohols.

Abstract: Novel synthetic forms of etherified oxidized phospholipids and methods of utilizing same for preventing and treating atherosclerosis and other related disorders, as well as inflammatory disorders, immune mediated diseases, autoimmune diseases and proliferative disorders, are provided. In addition, methods of synthesizing etherified and esterified oxidized phospholipids and of using same for preventing and treating atherosclerosis and other related disorders are also provided.

Abstract: Methods and compositions for enhancing the ability of hypoxia-activated bioreductive agents to kill tumor cells within solid tumors are provided. Local regions of hypoxia are created within a tumor, or within a region containing a tumor, resulting in enhanced activation of hypoxia-activated bioreductive agents (e.g. tirapazamine) within the local region. The activated hypoxia-activated bioreductive agents kill tumor cells in the hypoxic region by catalyzing DNA stand breakage within the tumor cells. Because the activity is localized, side effects that typically occur as a result of systemic administration of bioreductive agents are reduced.

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.