Abstract: The present invention relates to regulation of lymphocyte activation and migration. More particularly, the present invention is directed to nucleic acids encoding EDG family GPCR proteins, e.g., EDG-1, 2, 3, 4, 5, 6, 7, or 8, which are involved in modulation of lymphocyte activation and migration. The invention further relates to methods for identifying and using agents, including small organic molecules, antibodies, peptides, cyclic peptides, nucleic acids, antisense nucleic acids, sphingolipid analogs, and ribozymes, that modulate lymphocyte activation or migration via modulation of EDG GPCRs and EDG related signal transduction; as well as to the use of expression profiles and compositions in diagnosis and therapy related to lymphocyte activation and suppression, and lymphocyte migration.

Abstract: D-(threo)-1-aryl-2-disubstitutedacylamido-3-fluoro-1-propanol compounds compounds and analogues thereof (“Fenicol Compounds”), compositions comprising an effective amount of a Fenicol Compound, and methods for treating or preventing a bacterial infection in an animal comprising administering to an animal in need thereof an effective amount of a Fenicol Compound are disclosed.

Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.

Abstract: Pesticide formulations with a crystallization risk are provided. Also provided are methods of making and using such formulations.

Abstract: Proliferative cutaneous disease states or conditions are treated by administering a polyamine transport inhibitor R-X-L-polyamine wherein R is a straight or branched C10-50 saturated or unsaturated aliphatic, carboxyalkyl, carbalkoxyalkyl, or alkoxy; a C1-8 alicyclic; a single or multiring aryl substituted or unsubstituted aliphatic; and aliphatic-substituted or unsubstituted single or multiring aromatic; a single or multiring heterocyclic; a single or multiring heterocyclic aliphatic; an aryl sulfonyl; X is —CO—, —SO2—, or —CH2—; and L is a covalent bond or a naturally occurring amino acid, lysine, ornithine, 2,4-diaminobutyric acid, or pharmaceutically acceptable salts thereof or prodrug thereof, and a polyamine biosynthesis inhibitor.

Abstract: A method of producing a controlled release form of an agricultural active material includes the provision of an organic liquid composition in which the active is present, but where the liquid composition is free from aromatic solvents and is maintained below the normal melting point of the active. The liquid composition is formed into small droplets and the droplets are enclosed by a non-water soluble shell to provide microcapsules, the shell of which is designed to release the agricultural active at a pre-selected controlled rate when the microcapsule is exposed to natural environmental conditions. Controlled release forms of agricultural actives are also provided.

Abstract: The present invention provides a biofilm stripping agent for removing biofilms already formed. The biofilm stripping agent of the present invention contains, as an active ingredient, an amide compound or salt thereof denoted by General Formula (1), wherein R is a C1-11 alkyl group, and Q is a substituent denoted by the following Formulas (Q1), (Q2) or (Q3), wherein, in Formula (Q1), n is an integer ranging from 0 to 4; in Formula (Q2), R1 is a C1-4 alkyl group, and R2 is a hydroxyl group or carbamoyl group; in Formula (Q3), R3 is a hydrogen atom, hydroxyl group or carbamoyl group.

Abstract: Provide is a method for evaluating test agents as candidates for treating prostatic diseases, including benign prostatic hyperplasia (BPH) and androgen dependent and androgen independent prostate cancer. The method comprises providing a mouse comprising a human prostate primary xenograft, where the xenograft contains blood vessels that include human endothelial cells, initiating androgen deprivation in the mouse, administering to the mouse a test agent within a period of 1-7 days after initiating the androgen deprivation, and determining a reduction in human epithelial cells in the xenografts and/or a reduction in number of the endothelial cells or blood vessels in the xenograft. Also provided is a method for treating an individual for human prostate cancer or benign prostatic hyperplasia.

Abstract: Dicyano alkanoic acid amides of formula (I), wherein R1 is H, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, or haloalkynyl; R2 is H, CN, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, alkoxy, or haloalkoxy; R3 and R4 are H, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, cycloalkenyl, halocycloalkenyl, or R3 and R4 together can be alkylene, haloalkylene, alkenylene or haloalkenylene; X is O or S; R5 and R6 are H, alkyl, optionally substituted with 1 to 3 groups CN, NO2, OH, NR7R8, alkoxy, haloalkoxy, alkylthio, haloalkylthio, cycloalkyl, halocycloalkyl and optionally substituted phenyl; or haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, NR7R8, alkoxycarbonyl, haloalkoxycarbonyl, alkenyloxycarbonyl, haloalkenyloxycarbonyl, alkylcarbonyl, haloalkylcarbonyl, R7R8N—C(?O)—, phenylcarbonyl, benzylcarbonyl or phenyl wherein phen

Abstract: The present invention discloses a method of employing ion channel active compounds to delivery metabolism-enhancing molecules within the cell to promote rapid wound healing. It also develops a delivery kit for meperidine as a local anesthetic and wound healing accelerant for dental surgical use. And meperidine thus serves as a pattern for future design off novel wound healing compounds.

Abstract: The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17?-hydroxy steroid dehydrogenase type 1.

Abstract: The present invention is directed to compounds that are analogues of lipid mediators derived from a fish oil-derived fatty acid, eicosapentaenoic acid [C20:5 ?-3; EPA], but with a longer tissue half-life and enhanced bioactivity. These analogues may be used to treat inflammatory, angioproliferative, cardiovascular, thrombophlebotic, vascular, ocular, dermatologic, neurodegenerative, pulmonary, endocrine, reproductive, rheumatologic and gastrointestinal diseases.

Abstract: This invention relates to a treatment pad which may be used in cosmetic treatment and which produces soothing, relaxing, calming and similar effects in persons. The treatment pad comprises 0.1 to 90% weight (% wt) of a hydrophilic polymer selected from the group consisting of polyvinyl alcohol (PVA), polyethylene glycol (EG), polyacrylamide (PAAm), polyacrylic acid (PAAc), polyhydroxyethyl methacrylate (PHEMA) and polyethylene oxide (PEO); 0.01 to 0.

Abstract: This invention is related to compounds and use of N-Acyl-N?-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 group; R1 is a straight or branched C1-C8 alkyl or C3-C8 alkenylene or C3-C8 alkynylene chain, optionally substituted with CF3, phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C1-C4 alkyl, halogens, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R2, R3 are independently hydrogen, a C1-C3 alkyl chain, halogen, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R4, R5 are independently hydrogen or C1-C6 alkyl; R6 is a hydrogen or a straight or branched C1-C8 alkyl or linked to R5 can form a five to seven membered lactam; R7 is hydrogen or C1-C6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, in

Abstract: The present invention relates to phenyloxyaniline derivatives, to methods of their production and to uses thereof.

Abstract: D-(threo)-1-aryl-2-disubstitutedacylamido-3-fluoro-1-propanol compounds compounds and analogues thereof (“Fenicol Compounds”), compositions comprising an effective amount of a Fenicol Compound, and methods for treating or preventing a bacterial infection in an animal comprising administering to an animal in need thereof an effective amount of a Fenicol Compound are disclosed.

Abstract: The present disclosure provides amide-based, non-nucleoside compounds having an inhibitory activity against endogenous polymerases, such as polymerase alpha and polymerase gamma. This disclosure further provides uses of treating hyperproliferative diseases or disorders, such as benign or malignant neoplasms, and more specifically cancers that are sensitive to inhibition of polymerase alpha and polymerase gamma.

Abstract: Methods of identifying death receptor sensitizing compounds and methods of using death receptor sensitizing compounds are provided.

Abstract: The invention provides methods of treating a diabetic subject comprising administering a glucosylceramide synthase inhibitor to the subject.

Abstract: This disclosure relates to amides, aryl sulphonamides, aryl ureas, and ?,?-diketones derivatives useful as carboxylesterase esterase inhibitors. The disclosure is also directed to the use of these compounds as selective human intestinal carboxylesterase inhibitors and insect carboxylesterase inhibitors. The disclosure is also directed to pharmaceutical compositions and pesticide formulations containing these compounds, and to methods for treating or ameliorating the toxic effects following administration of drugs such as cancer therapy drugs, treating or ameliorating the effects of a drug overdose, and to the use of the compounds for increasing the effectiveness of insecticides and pesticides.

Abstract: Novel florfenicol compounds having the chemical structure: or a pharmaceutically-acceptable salt thereof or a solvate thereof, or prodrug thereof, wherein R1 is CHCl2, CHClF, CHF2, CHBrCl, CH3, CH2N3, CH2CN, CH(R2)NH2 or CH X1X2; where R2 is H, CH3 or CH2OH, and X1 and X2 are independently selected halogens; and R3 is CH2Cl, CH2F, CHF2, CHCl2 or CH2OH are disclosed. The compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.

Abstract: Compounds of the general formula and to the use thereof for controlling microorganisms are provided.

Abstract: By providing a reusable support base or carrier which is constructed for being easily held by the user in the person's hand, and incorporating additives, therapeutic agents and/or medicinal components therein, a highly effective and easily employed, multi-purpose hand and/or skin cleaner, sanitizer, drug delivery, and exercise system is realized. Preferably, the support base or carrier is formed from soft, pliable, compressible and/or flexible material which is easily manipulated by the user in the person's hand or on the skin surface of other areas of the person's body. By employing selected additives or combinations thereof, a multi-purpose, highly effective, and unique hand or skin cleaning, sanitizing, and drug delivery system is realized in a system which also improves and enhances the individual's ability to obtain exercising of the hand.

Abstract: Disclosed are prodrugs of (2R)—2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.

Abstract: The purpose of this invention is: new selenohydroxy acid compounds and their derivatives; their process for the preparation; use of the new compounds as precursors of L(+)-selenomethionine and/or source of selenium in human or animal nutrition, in cosmetics and pharmaceutics; and nutritional, cosmetic and pharmaceutical compositions containing them.

Abstract: This invention relates to medicaments and their use in the alleviation of inflammation and pain in joints.

Abstract: The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV, its production method, an intermediate compound useful for its production and a pharmaceutical composition containing these compounds, and the present invention relates to a compound represented by the formula (I): (wherein A represents —(CH2)n—, etc.; B represents —(C?O)—, etc.; D represents —(CH2)m—R?, etc.; E represents a hydrogen atom, etc.; G represents —(CH2)p-J, etc.; bond Q represents a single bond or double bond; and R1, R2 and R3 may be the same or different and each represent a hydrogen atom, etc.), a prodrug thereof or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to compounds that are analogues of lipid mediators derived from a fish oil-derived fatty acid, eicosapentaenoic acid [C20:5 ?-3; EPA], but with a longer tissue half-life and enhanced bioactivity. These analogues may be used to treat inflammatory, angioproliferative, cardiovascular, thrombophlebotic, vascular, ocular, dermatologic, neurodegenerative, pulmonary, endocrine, reproductive, rheumatologic and gastrointestinal diseases.

Abstract: Compositions and methods for treating noninflammatory pain, including but not limited to, neuropathic pain by using peroxisome proliferator activated receptor a (PPARa) agonists to treat a subject having such pain are described. The agonists may be used with additional therapeutic agents such as an inhibitor of fatty acid amide hydrolase or a cannabinoid CB1 or CB2 cannabinoid receptor agonist.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.

Abstract: A stick for the topical or transmucosal application of a skin care or active agent onto and via the nasal mucosa, respectively, is provided, wherein the stick material contains a composition of at least one carrier substance and at least one skin care or active agent, which is capable of acting on the nasal mucosa and/or being resorbed by it or which contains at least one volatile substance that acts on the deeper respiratory tract and/or is being resorbed by the deeper respiratory tract. Furthermore, the use of a medical skin care or cosmetical stick or of a stick material or of a refill cartridge containing said material for the topical or transmucosal application is described.

Abstract: An aqueous ophthalmic composition comprising a branched glycerol compound selected from the group consisting of a branched, glycerol monoalkyl ether, a branched, glycerol monoalkyl amine, a branched, glycerol monoalkyl sulfide, or any mixture thereof, present in a total amount of from 0.05 ppm to 1,000 ppm; a cationic antimicrobial component, and having an osmolality in a range from 200 mOsmol/kg to 400 mOsmol/kg. The presence of the branched glycerol compound enhances the biocidal efficacy of the aqueous ophthalmic composition containing one or more cationic antimicrobial components.

Abstract: The present invention relates to novel compounds, pharmaceutical compositions and methods for treating tumors, cancer and hyperproliferative diseases including psoriasis, genital warts and hyperproliferative cell growth diseases, including hyperproliferative keratinocyte diseases such as hyperkeratosis, ichthyosis, keratoderma or lichen planus.

Abstract: Synergistically enhanced disinfecting solutions comprising sodium chlorite in the range of 10 about ppm to about 5000 ppm and myristamidopropyl dimethylamine in the range of about 0.05 ppm to about 500 ppm for. In addition, synergistically enhanced disinfecting solutions comprising myristamidopropyl dimethylamine in the range of 0.05 ppm to 500 ppm and polyhexamethylene biguanide in the range of about 0.01 ppm to about 100 ppm for.

Abstract: Polyamines with varying chain-lengths were evaluated for antimicrobial activity in order to test the hypothesis that these bis-cationic amphipathic compounds may also bind to and permeabilize intact Gram negative bacterial membranes. The compounds were found to possess significant antimicrobial activity and mediated via permeabilization of bacterial membranes. Homologated spermine, bis-acylated with C8 or C9 chains was found to profoundly sensitize E. coli to hydrophobic antibiotics such as rifampicin.

Abstract: Substituted propane-1,3-diamine derivatives, methods for producing such derivatives, and medicaments and pharmaceutical compositions containing such derivatives useful for the treatment or prophylaxis of pain, urinary incontinence, itching, tinitus aurium, or diarrhea are provided.

Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

Abstract: N-acylethanolamines (NAEs) that can deliver an ethylene- or cytokinin-like effect to a plant, plant part or fungus are disclosed. Also disclosed are methods of using the NAEs.

Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p

Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

Abstract: A water-free composition for the bleaching and brightening of human hair at the same time with a simultaneous conditioning effect is disclosed. The particularly exceptional effects of the bleaching agent is that improvement of shine and elasticity. The bleaching agent comprises a) at least one compound with a bleaching or brightening effect, in particular a peroxide and/or an ammonium salt, and b) 0.001% to 10% by weight, calculated to the total composition, of at least one ubiquinone of the formula (I) wherein n is a number from 1 to 10, and at least one sphingolipid of the formula II where R1 and R2 are independent from each other alkyl- or alkenyl group mit 10 to 22 carbon atoms, R3 is methyl, ethyl, n-propyl or isopropyl group and n is a number between 1 to 6, preferably 2 or 3.

Abstract: The invention relates to compounds of formula (I): wherein: B represents a hydrogen atom, a COOR group, a CONRR? group, or a (C1–C6)alkyl group substituted by a COOR, CONRR? or OR group, G1 represents a —X?—(CH2)n—X—(CH2)m—X?— chain wherein X, X?, X?, n and m are as defined in the description, Cy represents a grouping of formula (II) or (III): G2 represents an alkylene chain as defined in the description, and A represents a NRCOR?, NRCSR?, CONRR?, CSNRR?, NRCONR?R? or NRCSNR?R? group.

Abstract: Disclosed are compounds of formula X, which are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.

Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.

Abstract: A process for preparing particles of a substance, such as a protein or polypeptide, comprising: (a) preparing a first liquid comprising water, the substance and a modulator, wherein the modulator has a solubility in water which decreases with increasing temperature; and (b) contacting the first liquid with a second liquid comprising a fluid gas and an organic solvent using an anti-solvent fluid gas technique under conditions of temperature and pressure which result in the precipitation of particles comprising the substance, wherein the temperature of the first liquid is at or above the cloud point temperature of the first liquid when the first liquid contacts the second liquid. Also claimed are particles obtained according to the process and compositions containing the particles.

Abstract: The present invention provides an anti-tumor pharmaceutical composition having a high anti-tumor effect with low side-effects. The anti-tumor pharmaceutical composition comprises a N-vanillyl fatty acid amide of formula (1): wherein —CO—R group represents a saturated or unsaturated fatty acid residue containing from 14 to 32 carbon atoms. Accordingly the invention provides an anti-tumor pharmaceutical composition comprising a N-vanillyl fatty acid amide which relates to capsaicin wherein the composition has a low side-effect and a high anti-tumor effect, in particular an anti-melanoma effect and an anti-leukemia cell effect; and is very low pungent, stimulatory and preinflammatory effect.

Abstract: The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I R1 is a methyl or ethyl group; R2 is H, methyl or an ethyl group; R3 is ethyl or a propyl group; and R4 is a hydroxyl or amide group, and the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to. The present invention further relates to a method for the stereoselective synthesis of the 2R stereoisomer of PID and PIA.

Abstract: A method of inhibiting cell proliferation in a patient suffering from such disorder comprising administering to said patient an effective amount of a composition comprising, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, which is a substituted styrene compound which can also be a naphthalene, an indane or a benzoxazine; including nitrile and molononitrile compounds, and pharmaceutical compositions comprising, in admixture with a pharmaceutically acceptable carrier, a pharmaceutically-effective amount of such compound.

Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis. Importantly, these compounds can be administered orally.