Abstract: This invention relates to compositions, and related compounds and methods, of conjugates of immunomodulatory agents and polymers or unit(s) thereof. The conjugates may be contained within synthetic nanocarriers, and the immunomodulatory agents may be released from the synthetic nanocarriers in a pH sensitive manner.

Abstract: Compounds of the formula I in which R, X, L2 and A1-A6 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.

Abstract: The present invention provides pharmaceutical compositions and therapeutic methods for treating diseases such as multiple endocrine neoplasia type IIA, multiple endocrine neoplasia type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract. The therapeutic methods and pharmaceutical compositions use a RET kinase inhibiting substance, such as 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and pharmacologically acceptable salts thereof, and involve a step of administering the RET kinase inhibiting substance to a patient.

Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.

Abstract: This present disclosure is related to the field of N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.

Abstract: The present invention relates to certain spirocyclic compounds that are inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 (11?HSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases.

Abstract: The invention relates to a perylene diimide derivative and to an in vitro method for preparing the same. In addition, the invention relates to a method for detecting heparin in a sample using perylene diimide derivatives, wherein the interaction of the perylene diimide derivative with heparin modulates the intensity of the fluorescent signal of the mixture compared to the solution. The invention also comprises a diagnostic kit for detecting heparin in a sample in vitro, comprising the perylene diimide derivative, as well as the use of the perylene diimide derivative for neutralizing the anticoagulant activity of heparin.

Abstract: A therapeutic or prophylactic agent for cachexia includes as an effective ingredient a compound having a specified morphinan skeleton represented by a compound of the following structure: or a pharmacologically acceptable acid addition salt thereof.

Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.

Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.

Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

Abstract: Pharmaceutical compositions and single unit dosage forms of thalidomide and pharmaceutically acceptable stereoisomers, prodrugs, salts, solvates, hydrates, or clathrates are disclosed. Also disclosed are methods of treating, managing, and preventing diseases and conditions such as, but not limited to, leprosy, chronic graft-vs-host disease, rheumatoid arthritis, sarcoidosis, an inflammatory condition, inflammatory bowel disease, and cancer using the novel dosage forms disclosed herein.

Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

Abstract: The present invention relates to specific solid forms of (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-(4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl)-amide, and its solvates. The present invention further relates to processes for preparing said solid forms, pharmaceutical compositions comprising said solid forms, and methods of using said solid forms and pharmaceutical compositions to treat disease.

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.

Abstract: Novel transdermal preparations combining a non-steroidal anti-inflammatory drug (NSAID) such as flunixin, are disclosed. Methods for using and administering such preparation in the treatment of inflammatory conditions in bovines, including bovine respiratory disease, are also disclosed.

Abstract: Compounds having an excellent hypoglycemic effect and ? cell- or pancreas-preserving effects or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.

Abstract: The invention relates to the use of derivatives of thiazoles having general formula (I) for the preparation of a medicament for the treatment or prevention of dyskinesias caused by a chemical treatment. The invention also relates to a combination of thiazole derivatives having general formula (I) and at least one compound selected from among neuroleptics or products that act on the dopaminergic system for the treatment or prevention of dyskinesias caused by a chemical treatment.

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Abstract: Controlled release systems release at least one pluribioactive antifungal drug exhibiting at least one additional bioactivity from the group consisting of spermiostatic, antineoplastic, antibacterial, antirestenotic and antiviral activities. The drug release system is designed for use as a spermiostatic contraceptive, intravaginal ringed-mesh which may also exhibit antiviral activity, an in situ-forming implant for treating different forms of cancer and topical film for treating or preventing bacterial and fungal infections.

Abstract: The present disclosure relates to therapeutic compositions comprising substituted imidazoliums having multiple acidic groups. The compounds may be used to treat diseases or conditions such as those associated with bone, cancer, or pain. Compositions, dosage forms, methods of treating diseases or conditions, methods of preparation, and other related embodiments related to the substituted imidazoliums are also described herein.

Abstract: Pyrazolone derivative formulations are provided. The formulations include a pyrazolone derivative active agent, e.g., edaravone, and an amphiphilic solubilizing agent. Also provided are methods of making and using the subject formulations.

Abstract: The present disclosure is directed to compounds and methods for treating irritable bowel syndrome, chronic kidney disease and end stage renal disease by administering to a subject in need thereof a compound or a pharmaceutically acceptable salt thereof, wherein the compound has the structure

Abstract: This invention relates to the discovery of novel rosuvastatin and atorvastatin analogues.

Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers.

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: Disclosed is a novel therapeutic means against interferon-resistant hepatitis C. Specifically disclosed are: a pharmaceutical composition for treating interferon-resistant hepatitis C, which is characterized by comprising at least one component selected from the group consisting of an ?-3 polyunsaturated fatty acid, a pharmaceutically acceptable salt of the fatty acid and an ester of the fatty acid as an active ingredient; and a method for utilizing the pharmaceutical composition.

Abstract: A disinfecting shower cleaner composition including a medium-chain fatty acid coupled with a nonionic surfactant providing temperature stable antimicrobial compositions. The invention specifically relates to antimicrobial compositions including fatty acid antimicrobial agents coupled with an ethoxylated amine and methods of using the antimicrobial compositions.

Abstract: The present invention provides a composition, such as a food and pharmaceutical agent, which comprises dihomo-?-linolenic acid, and which has the effect of preventing or treating skin diseases; a composition such as a food and pharmaceutical agent which comprises dihomo-?-linolenic acid and which has the effect of preventing or treating skin diseases; and a composition which comprises dihomo-?-linolenic acid and which has the effect of preventing or treating diseases related to increased mast cell count.

Abstract: The present invention relates to a method of treating an incretin related disease such as diabetes, obesity and the like by delivery of long chain fatty acid to the colon by bypassing the upper digestive tract.

Abstract: A levothyroxine composition includes levothyroxine sodium and mannitol. The composition is a solid. The composition may include from 100 to 500 micrograms levothyroxine sodium and from 1 to 5 milligrams mannitol. The composition may include from 100 to 200 micrograms levothyroxine sodium, and the mass ratio of mannitol to levothyroxine sodium in the composition may be at most 40:1. The composition may include about 500 micrograms levothyroxine sodium, and the mass ratio of mannitol to levothyroxine sodium in the composition may be at most 10:1.

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

Abstract: Compositions for application and methods of application of a composition to modify hair. In one embodiment, a composition includes a compound (molecule) represented by: wherein A and B are individually selected from a hydrogen, a hydroxyl group and a halogen, with the proviso that when one of A and B is a hydroxyl group, the other of A and B is a hydrogen and when one of A and B is a halogen, the other of A and B is a halogen or a hydrogen; wherein Z is, for example, an aryl moiety; and wherein X1 and X2 are, for example, individually selected from a hydrogen and an alkyl moiety, wherein R1 and R2 are individually selected from an oxo, a hydroxyl or an ester group; wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, or a salt.

Abstract: The present invention provides methods of regulating physiological and metabolic parameters and of treating diseases by administering metadichol to a subject in need of such regulation and/or treatment. Metadichol can be administered as a liquid or gel formulation.

Abstract: The invention provides compositions comprising xanthohumol/cyclodextrin complexes that are water soluble and that have increased stability relative to xanthohumol alone.

Abstract: Disclosed is an oral pharmaceutical formulation of pelubiprofen which is improved in dissolution rate and stability. As a result of an improvement in the dissolution rate of pelubiprofen, the oral pharmaceutical formulation can show high bioavailability and thus exert pharmacological effects thereof rapidly. It also can be stored with high stability as a result of the minimal generation of related compounds.

Abstract: This invention discloses a process for stabilizing an aqueous mineral preparation comprising a step of adding at least one aldehyde-containing and/or aldehyde-releasing and/or phenolic and/or isothiazoline biocide to said aqueous mineral preparation.

Abstract: According to the present invention, a metal nanoparticle dispersion suitable to multiple layered coating by jetting in the form of fine droplets is prepared by dispersing metal nanoparticles having an average particle size of 1 to 100 nm in a dispersion solvent having a boiling point of 80° C. or higher in such a manner that the volume percentage of the dispersion solvent is selected in the range of 55 to 80% by volume and the fluid viscosity (20° C.) of the dispersion is chosen in the range of 2 mPa·s to 30 mPa·s, and then when the dispersion is discharged in the form of fine droplets by inkjet method or the like, the dispersion is concentrated by evaporation of the dispersion solvent in the droplets in the course of flight, coming to be a viscous dispersion which can be applicable to multi-layered coating.

Abstract: A method and an apparatus is disclosed that uses a gas lift tubing arrangement to produce synthetic hydrocarbon related products. Using the Fischer Tropsch process as an example, the tubing is packed with a suitable catalyst and then hydrogen and carbon monoxide are injected into the top of the tubing in a fashion similar to a gas lift process. As the gases travel past the catalyst, synthetic hydrocarbons are formed and heat is rejected. The synthetic hydrocarbons and water flow out of the bottom of the tubing and travel up the annulus to the surface. In some embodiments, this process is carried out in a producing well or a in producing riser. In a producing well or a producing riser, the production from the well which flows up the annulus cools the synthetic hydrocarbon derived products. In additional and alternate embodiments, this process can be used in non-flowing wells.

Abstract: The disclosed invention relates to a process for conducting a Fischer-Tropsch reaction, comprising flowing a reactant mixture comprising fresh synthesis gas and tail gas in a microchannel reactor in contact with a catalyst to form at least one hydrocarbon product, the catalyst being derived from a catalyst precursor comprising cobalt and a surface modified catalyst support.

Abstract: The present invention relates to a method for removal of metal ions from an aqueous solution, which comprises contacting the aqueous solution with a phosphazene-formaldehyde resin as well as an ion exchange resin comprising a phosphazene-formaldehyde resin.

Abstract: A method for the production of a mechanically stabilized polyazole polymer membrane or film having the following steps: a) providing a membrane or film containing i.) a polyazole with at least one amino group in a repeating unit except the ones obtained by reacting aromatic and/or heteroaromatic diaminocarboxylic acids, ii.) at least one strong acid and iii.) at least one stabilizing reagent, the total content of stabilizing reagents in the membrane or film being within the range of from 0.01 to 30% by weight, b) performing the stabilization reaction in the membrane, immediately or in a subsequent processing step of the membrane, c) optionally doping the membrane obtained in accordance with step b) with a strong acid or concentrating the present strong acid by removal of present water, wherein the stabilizing reagent contains at least one oxazine-based compound and wherein the polyazole polymer has at least 1.8 dl/g intrinsic viscosity.

Abstract: A formulation for foaming a thermoplastic polymer, for example PVC, comprises a carrier, exothermic and endothermic chemical blowing agents and 1 wt %, preferably less than 0.2 wt % of water. The liquid formulation can readily be used for foaming PVC and other thermoplastics.

Abstract: The present disclosure provides a plurality of glass bubbles having an average true density of up to about 0.55 grams per cubic centimeter and a size distribution including a median size in a range from about 15 micrometers to 40 micrometers. A hydrostatic pressure at which ten percent by volume of the plurality of glass bubbles collapses is at least about 100 megapascals. In some embodiments, the plurality of glass bubbles is a graded fraction preparable by classifying a second plurality of glass bubbles, wherein the second plurality of glass bubbles has a higher percentage of glass bubbles with a size of up to ten micrometers than the first plurality of glass bubbles. Composites including the plurality of glass bubbles are also disclosed.

Abstract: The invention provides a particulate material comprising porous polymeric microparticles having a mesoporous structure. A process for making the particles is also presented. The process comprises impregnating a porous microparticulate template material with a liquid comprising one or more monomers. The one or more monomers are then polymerized in and/or on the template material to form a polymer, and the template material is then removed to produce the particulate material.