Abstract: The present invention relates to a fluorene derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition comprising the same as an effective ingredient for preventing or treating HCV-related disease. A fluorene derivative according to the present invention is identified to exhibit an antiviral performance against not only HCV, but also highly against HCV mutants, particularly double mutants and thus can be used in a pharmaceutical composition for prevention or treatment of HCV-caused liver disease, such as acute hepatitis C, chronic hepatitis C, liver cirrhosis, hepatocellular cancer, etc., particularly, liver disease caused by mutants of HCV. The derivative can be useful in a pharmaceutical composition for prevention or treatment of HCV-related liver disease by which the problem of resistant mutation against conventional therapeutic agents is solved.

Abstract: The present invention describes a compound of formula (I) which can be used in the diagnosis, treatment or prevention of neurotensin receptor-related conditions such as tumors and hematological malignancies.

Abstract: Compositions, devices and methods employing therapeutic concentrations of a triptan for treatment of migraine are described. Also described are methods and apparatuses for delivery of zolmitriptan for achieving a Tmax as quick as 2 minutes and not later than 30 minutes in the majority of subjects.

Abstract: The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.

Abstract: The present disclosure relates to compounds of Formula I, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms thereof and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis and characterization of aforementioned substances.

Abstract: The present invention relates to methods for treating acne and other skin infections caused or mediated by Propionibacterium acnes, Gardnerella vaginalis, or Staphylococcus aureus in a patient with a safe and effective amount of a topically applied oxazolidinone antibiotic compound.

Abstract: The present invention relates to pharmaceutical compositions useful for administration for treating, preventing, or reducing the risk of microbial infections.

Abstract: The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions.

Abstract: The present invention relates to the field of blood coagulation, more specifically it relates to a method of treating a thromboembolic disorder by administering once daily a direct factor Xa inhibitor in oral dosage form to a patient in need thereof, wherein the factor Xa inhibitor has a plasma concentration half life indicative of a bid or tid administration interval, e.g. of 10 hours or less.

Abstract: Methods are disclosed to treat or prevent at least one disease or condition in a subject in need thereof comprising administering a compound of Formula (I): or a pharmaceutically acceptable salt, or ester thereof, wherein R1 and R2 are independently chosen from a hydrogen atom or linear, branched, and/or cyclic C1-C6 alkyl groups, with the proviso that R1 and R2 are not both hydrogen or a pharmaceutically acceptable salt or ester thereof. Such diseases or conditions may relate to coronary heart disease (CHD), for example atherosclerosis; metabolic syndrome/insulin resistance; and/or a dyslipidemic condition such as hypertriglyceridemia (HTG), elevated LDL-cholesterol, elevated total-cholesterol, elevated Apo B and low HDL-cholesterol. The present disclosure further provides for a method of reducing atherosclerosis development. Pharmaceutical compositions comprising a compound of Formula (I) are also disclosed.

Abstract: The present invention relates to processes for the preparation of triazoles. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.

Abstract: Methods for the efficient synthesis of fatty acid derivatives and their intermediates are provided.

Abstract: The present invention relates to the prodrug of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-morpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, rivaroxaban per se; processes for their preparation, and the application in treatment and/or prophylaxis of diseases, especially of thromboembolic disorders. The prodrug of a compound of formula (B) is chemically designated as 5-chloro-N-formyl-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide.

Abstract: The present invention provides an agent for preventing the increase in a body weight (or for decreasing a body weight) or an anti-obesity agent each comprising at least one component selected from the group consisting of EPA and pharmaceutically acceptable salts, esters and derivatives thereof as an active ingredient for obesity in which the increase in the formation of hepatic lipid or the occurrence of fatty liver is mild, preferably the increase in the formation of hepatic lipid or the occurrence of fatty liver is not observed.

Abstract: A pharmaceutical composition, comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound represented by the following structural formula at least one acidifying agent; and a vehicle base comprising at least one pharmaceutically acceptable non-aqueous solvent. Values and preferred values of the variables in structural formula (I) are defined herein.

Abstract: The present application relates to novel substituted N-phenethyltriazoloneacetamides, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.

Abstract: The present invention relates to oxazolidinone compounds represented by Chemical Formula 1, pharmaceutically acceptable salts thereof or hydrates, a method of preparing the same, and a pharmaceutical composition for preventing or treating Hepatitis C infection: Wherein R1, R7 and X are defined in the detailed description.

Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.

Abstract: (R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.

Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.

Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.

Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH.

Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.

Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protectiong from neuron cell death.

Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.

Abstract: A novel canola variety designated VR 9561 GS and seed, plants and plant parts thereof, produced by crossing Pioneer Hi-Bred International, Inc. proprietary inbred canola varieties. Methods for producing a canola plant that comprises crossing canola variety VR 9561 GS with another canola plant. Methods for producing a canola plant containing in its genetic material one or more traits introgressed into VR 9561 GS through backcross conversion and/or transformation, and to the canola seed, plant and plant part produced thereby. This discovery relates to the canola variety VR 9561 GS, the seed, the plant produced from the seed, and variants, mutants, and minor modifications of canola variety VR 9561 GS. This discovery further relates to methods for producing canola varieties derived from canola variety VR 9561 GS.

Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.

Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.

Abstract: The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors.

Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

Abstract: A method of rapid transbuccal delivery of an active agent into the bloodstream is provided. The method can include providing a pharmaceutical composition comprising the active agent, resin and a volatile solvent and, optionally, water. In some embodiments, the method achieves a Tmax 60 minutes or less, an onset of therapeutic effect of 60 minutes or less, and/or achieves therapeutic serum levels of the active agent within 60 minutes or less. Related compositions also are provided.

Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.

Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.

Abstract: Silicon dioxide free orally disintegrating tablet formulations of zolmitriptan or a pharmaceutically acceptable salt thereof having magnesium carbonate heavy and sodium stearyl fumarate with one or more pharmaceutically acceptable excipients and a process for preparing such a formulation and its use in the treatment of migraines.

Abstract: The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

Abstract: The present invention relates to a composition including at least one C7 sugar, or derivative from esterification of said sugar, and a pharmaceutically acceptable carrier for treating alopecia. The present invention also relates to a method for cosmetically treating hair and nails, said method being intended to stimulate the growth thereof and/or slow the loss thereof. According to said method, a cosmetic composition including at least one C7 sugar, or derivative from esterification of said sugar, is administered. The present invention finally relates to a method for cosmetic care of hair and/or eyelashes and/or nails.

Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.

Abstract: Provided is a pharmaceutical composition for preventing or treating hyperlipidemia comprising (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one or its pharmaceutically acceptable salt; and an angiotensin II receptor blocker as active ingredients.

Abstract: Provided is a pharmaceutical composition for preventing or treating hyperlipidemia comprising (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one or its pharmaceutically acceptable salt; and a calcium channel blocker or a fibrate as active ingredients.

Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.

Abstract: The disclosure relates to diseases in the peripheral nervous system, particularly hereditary neuropathies, such as Charcot-Marie-Tooth (CMT) disease. It is shown that this disease is associated with decreased acetylated tubulin levels, which can be overcome by inhibition of histone deacetylases (HDACs). Using HDAC inhibitors, it is shown herein that the symptoms of the CMT phenotype can be overcome both in vitro and in vivo. Also provided herein are two different mouse models of CMT disease.

Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I).

Abstract: The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalone adipic acid cocrystal, a 1:0.5 metaxalone fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them.

Abstract: A method of treating a disease or condition in which up-regulating GAGs is therapeutically beneficial is disclosed. The method comprises locally administering to a subject a therapeutically effective amount of an agent capable of down-regulating activity or expression of a component of the renin-angiotensin system.

Abstract: A method for treating migraines is disclosed. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent, including small molecules and peptides being administered to a patient in need of treatment. In particular, the drug delivery system is designed for inhalation for delivery of drugs to the pulmonary circulation in a rapid and therapeutically effective manner.

Abstract: Provided is an agent for treating and/or preventing obesity. An agent for suppressing expression of NPC1L1 (Niemann-Pick disease, type C1, gene-like 1) and/or LIPG (Lipase, endothelial) mRNA, and an agent for preventing and/or treating obesity, each comprising, as an active ingredient, a compound having CETP inhibitory activity, or a salt thereof, or a solvate thereof.

Abstract: The present invention relates to methods for producing particles of metaxalone using dry milling processes as well as compositions comprising metaxalone, medicaments produced using metaxalone in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of metaxalone administered by way of said medicaments.