Abstract: The present invention provides compositions for extended release of an active ingredient, comprising a lipid-saturated matrix formed from a biodegradable polymer. The present invention also provides methods of producing the matrix compositions and methods for using the matrix compositions to provide controlled release of an active ingredient in the body of a subject in need thereof.

Abstract: The present invention provides compositions and methods for detecting carboxymethyl-lysine (CML) and circulating receptor for advanced glycation end (RAGE) products, and methods for correlating CML and RAGE levels with age-related disease. In particular, serum CML and/or circulating receptor for advanced glycation end (RAGE) products can be used as a clinical biomarker in diagnostics to identify people who are at a higher risk of developing adverse ageing-related outcomes.

Abstract: Nitrated and non-nitrated compounds capable of protecting brain tissue from injury and useful as therapeutic agents to treat neurodegenerative diseases and conditions are disclosed. Methods of using the compounds in therapeutic treatments, and methods of preparing the compounds, also are disclosed.

Abstract: The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.

Abstract: A therapeutic agent or prophylactic agent has an analgesic effect on both nociceptive pain and neuropathic pain and is effective in treatment of fibromyalgia. The agent includes as an effective ingredient a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof.

Abstract: Briefly described, embodiments of this disclosure include compositions, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of identifying a candidate agent for the treatment of hepatitis C virus (HCV) infection, and the like.

Abstract: The present invention relates to pharmaceutical compositions comprising ritonavir premix, a water soluble polymer and a surfactant and process for preparing the same. More particularly, the present invention relates to hot-melt extrusion process for preparing solid oral compositions of ritonavir premix.

Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.

Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.

Abstract: The present invention relates to a high-density lipoprotein (HDL)-like particle composite which is a drug-encapsulating apoA-I comprising apoA-I and a drug encapsulated in the apoA-I capable of releasing the drug encapsulated in the apoA-I under acidic pH conditions, and a preparation method thereof. Since the HDL-like particle composite of the present invention can release the encapsulated drug under acidic conditions, while remaining stable under non-acidic conditions over a wide temperature range, it can be widely used for the development of target-specific drugs.

Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.

Abstract: A therapeutic agent or a prophylactic agent for neuropathic pain provides a synergistically-enhanced analgesic effect at a dose at which a calcium channel ?2? ligand does not produce any side effects as well as which agent does not produce any new side effects on the central nervous system. The therapeutic agent or a prophylactic agent for neuropathic pain includes as effective ingredients a cyclohexane derivative, represented by the following formula, or a pharmaceutically acceptable salt thereof or a prodrug thereof, and a calcium channel ?2? ligand.

Abstract: The present invention relates to crystalline form I of Febuxostat as well as to pharmaceutical compositions comprising crystalline form I as an active pharmaceutical ingredient. Furthermore the present invention relates to a further polymorphic form of Febuxostat designated as form II and to a novel solvate of Febuxostat. The present invention also relates to methods of making crystalline form I, form II and the novel solvate of Febuxostat.

Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.

Abstract: A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.

Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.

Abstract: A mold-resistant paper is provided. The paper is coated on at least one surface with an anti-microbial coating which includes polymerized siloxane and a fungicide. An antimicrobial paper coating and related methods are provided as well. A gypsum panel with improved resistance to mold and mildew is provided as well.

Abstract: The present invention provides a solid dispersion of febuxostat, processes for its preparation, pharmaceutical compositions comprising it and its use for the chronic management of hyperuricemia in patients with gout.

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more benzamide fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. group (A): a group consisting of flutolanil, mepronil, and zoxamide.

Abstract: A pest controlling composition comprising tolclofos-methyl and a neonicotinoid compound represented by the formula (1) as active ingredients.

Abstract: The present invention is directed to a method of enhancing visual acuity in a subject, comprising intravitreally administering to the subject in need of such enhancement, a therapeutically effective amount of an extrasynaptic GABAA receptor antagonist. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the extrasynaptic GABAA receptor antagonist.

Abstract: Disclosed herein are methods and pharmaceutical compositions for reducing the pain associated with parenterally administering a therapeutic agent. The methods and compositions comprise a dispersion comprising microparticles of an analgesic agent in an amount effective to reduce the pain, inflammation, and/or immunological reaction associated with parenterally administering a primary therapeutic agent, wherein the microparticles of the analgesic agent have an effective particle size of less than 20 micrometers.

Abstract: The invention is in the technical field of vector control and in particular mosquito and bed bug control. The active compound compositions of this invention are used against animal pests such as arthropods which transmit disease pathogens or which annoy the well-being of humans and animals. The active compound compositions of this invention are in particular useful to overcome target-specific and/or metabolic-specific resistance of mosquitos and bed bugs.

Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.

Abstract: The present disclosure is related generally to a method for prevention and/or treatment of infections, e.g., respiratory infections, in a subject before or after the onset of a disease state associated with the infection.

Abstract: The present invention relates to aryloxy substituted phenylamidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions (I).

Abstract: The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a compound of formula I: wherein A, B, and X have any of the meanings defined in the specification; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.

Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.

Abstract: The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.

Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.

Abstract: Provided are cellulose esters useful for inhibiting solution crystallization of drugs. Specific polymers include cellulose esters of formula I: wherein n of the ?-carboxyalkanoyl group, is 3, 4, 6, or 8 to provide a ?-carboxyalkanoyl group chosen from succinoyl, glutaroyl, adipoyl, sebacyl, and suberyl groups; and wherein R is chosen from: a hydrogen atom; and an alkanoyl group chosen from acetyl, propionyl, butyryl, valeroyl, hexanoyl, nonanoyl, decanoyl, lauroyl, palmitoyl, and stearoyl groups; wherein there is a total degree of substitution of the alkanoyl group and the ?-carboxyalkanoyl group of at least 2.0; and wherein the polymer comprises m repeating units where n=1 to 1,000,000, or 10 to 100,000, or 100 to 1,000, such as 1 to 6,000. Embodiments further include compositions comprising cellulose esters and poorly water-soluble drugs, which compositions exhibit greater solubility and stability in solution as compared to the drugs alone.

Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.

Abstract: The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.

Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.

Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.

Abstract: A microcapsule in which a liquid droplet is coated with a resin, wherein in the droplet, a pesticidally active solid ingredient is suspended in a compound of formula (I), wherein R represents a C1-C5 alkyl group, is useful as a formulation of a pesticidally active solid ingredient.

Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.

Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.

Abstract: Compounds of formula I wherein X is O or S(?O)n; n is 0, 1 or 2; R1 is optionally substituted alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, cycloalkenyl, halocycloalkenyl, phenyl, hetaryl, phenylalkyl, hetaryl alkyl, optionally fused to phenyl, hetaryl or heterocyclyl; A is —NRb2, —C(=G)GRb, —C(=G)NRb2, —C(?NORb)Rb, C(=G)[N?SRb2], —C(=G)NRb—NRb2, C2-C6-alkandiyl, C2-C6-alkenediyl, C1-C3-alkyl-G-C1-C3-alkyl, wherein Rb is as defined in the description, or optionally substituted phenyl, hetaryl, heterocyclyl, optionally fused to phenyl or heterocyclyl; B is an optionally substituted saturated or partially unsaturated hydrocarbon chain with 1 to 3 carbon chain atoms; D is an optionally substituted saturated or partially unsaturated hydrocarbon chain with 1 to 5 carbon chain atoms or C3-C6-cycloalkyl; G is oxygen or sulfur; or the enantiomers or diastereomers or salts or N-oxides thereof, processes for preparing the compounds I, pesticidal compositions and synergistic m

Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exhacerbated respiratory disorders and urological disorders.

Abstract: In one aspect, the invention relates to sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.

Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.

Abstract: The invention discloses a method for the separation and purification of epothilones, especially discloses a method for the separation and purification of epothilones B and A using normal phase silica gel chromatography, which comprises loading the sample after dissolving the sample containing epothilones B and A with C1-C7 alkyl halide compounds or mixing the sample with silica gel, then gradient eluting silica gel column by an elution solvent of normal phase silica gel column, and finally obtaining products.

Abstract: Compositions and methods for anti-thrombotic and antiplatelet therapy in a subject are provided. Administration of an MAO-B inhibitor results in reduced platelet aggregation or reversion of platelet aggregation. Methods of administering an MAO-B inhibitor with at least one antiplatelet agent are also disclosed. Such combination therapies result in an additional protective effect, and in some instances a synergistic effect. The compositions and methods of the present invention are useful for treating and preventing recurrence of several cardiovascular, cerebrovascular and peripheral vascular diseases and injuries, and may be applied to subjects displaying traditional drug resistances.