Abstract: The present invention provides compounds inhibiting eIF4E activity, and compositions and methods of using thereof.

Abstract: The present invention provides a compound of formula (I) or a stereoisomer thereof, or an atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a stereoisomer thereof, or a pharmaceutically acceptable salt of an atropisomer thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

Abstract: A main object of the present invention is to provide new crystals of (S)-N2-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine maleate (hereinafter, referred to as “compound A”). A Form-I crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2?: 6.9 degrees, 9.4 degrees, 12.5 degrees, 15.1 degrees, 16.4 degrees, 18.3 degrees, 19.0 degrees, 24.9 degrees, 25.4 degrees, 27.3 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu K? radiation (?=1.54 ?). A Form-II crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2?: 6.9 degrees, 9.2 degrees, 12.4 degrees, 14.8 degrees, 16.5 degrees, 18.1 degrees, 18.5 degrees, 19.8 degrees, 23.6 degrees, 24.9 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu K? radiation (?=1.

Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound which compound is useful in the treatment of a psychiatric disorder and their combined use as a medicament, in particular for the treatment of psychiatric and/or cognitive disorders.

Abstract: Described herein are methods of increasing meat quantity and/or improving meat quality of domesticated meat animals using treatments of nicotinamide riboside. The nicotinamide riboside may be in the form of a chloride salt mixed or dissolved in a biologically-acceptable carrier. The treatments may be provided as an in ovo injection or orally administered to the live domesticated meat animal. The methods described herein advantageously increase the size and weight of the domesticated meat animals, reduce the incidences of transportation fatigue, and decrease meat discoloration over time.

Abstract: A quaternary lactam compound of formula (I). The compound is used in the manufacture of a medicament for the treatment and/or prevention of thrombotic or thromboembolic disorders.

Abstract: The invention relates to a compound of formula (I) wherein R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: Compounds, and compositions, methods, and uses thereof, are described herein for treating neurodegenerative diseases and disorders. In particular, vasopressin receptor modulators, and compositions, methods and uses thereof, are described herein for treating neuropsychiatric aspects of neurodegenerative diseases such as Huntington's Disease, Parkinson's Disease, and Alzheimer's Disease.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1 or a salt thereof, wherein q, r, s, Q, R1, R2?, R2?, R3 and R4 are as defined herein.

Abstract: A nitrogen-containing heterocyclic organic compound and an organic electroluminescent device are provided. The nitrogen-containing heterocyclic organic compound has a structure represented by the following general formula (I): and X is N or CH; Y is a single bond, O, S, an imino, a methylene, a methylidenesilane group, a substituted imino, a substituted methylene, or a substituted methylidenesilane group, the substituents in the substituted imino, and the substituted methylene; L, Ar1, and Ar2 are each independently selected from one of a C6-C30 aryl, a C3-C30 heteroaryl, a substituted C6-C30 aryl, and a substituted C3-C30 heteroaryl; n is an integer from 0 to 3; R1 to R8 are each independently selected from one of a hydrogen, a deuteron, a halogen, a C1-C30 alkyl, a C1-C30 alkyl substituted with a heteroatom, a C6-C30 aryl, and a C3-C30 heteroaryl.

Abstract: The present invention relates to new methods for crosslinking a polysaccharide with a bifunctional poly(ethylene glycol). The invention further includes the polymer hydrogels which can be produced using these methods, compositions comprising the polymer hydrogels and methods of use thereof.

Abstract: The present invention relates to HDM2-p53 interaction inhibitors for use in the treatment of cancer, wherein the drug is administered by a high dose intermittent dosing regimen. The present invention relates in particular to the HDM2-p53 interaction inhibitor HDM20I and the dosing regimen di, d8 of a 4 week cycle.

Abstract: Compounds and compositions are described herein for treating post traumatic stress disorder.

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Abstract: Disclosed is a method of preparing ezetimibe, including cross-metathesis using a Grubbs 2nd catalyst and deprotection using a Pearlman's catalyst, and an intermediate thereof. The method of preparing ezetimibe is useful as an efficient ezetimibe synthesis technique in pharmaceutical fields using ezetimibe as a raw material.

Abstract: Provided is a method for detecting impurities in ammonium hydroxide. The method for detecting impurities in ammonium hydroxide includes preparing a potassium permanganate solution, preparing ammonium hydroxide, and adding the potassium permanganate solution several times to the ammonium hydroxide so as to detect impurities in the ammonium hydroxide. Potassium permanganate contained in the potassium permanganate solution is added for each time in the range of 0.0001 mol to 0.01 mol per 1 g of ammonia contained in the ammonium hydroxide.

Abstract: Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.

Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: Disclosed are methods of treating cancer, which include administering a therapeutically effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt or ester thereof, to a subject in need thereof. Also disclosed are methods of inhibiting growth and proliferation of cancer cells in vitro or in vivo, which include contacting the cells with an amount of the compound of formula (I) effective to inhibit the growth or proliferation of the cancer cells. Further disclosed are methods of inhibiting tumor growth, which include contacting the tumor with an amount of the compound of formula (I) effective to inhibit the growth of the tumor.

Abstract: Disclosed are 4-substituted-2-(5-substituted-1H-indol-2-yl)phenol derivatives for controlling the proliferation and migration of kinase-overexpressed cells. The phenol derivatives are represented by Formula 1: wherein X is selected from the group consisting of hydrogen, halogen, a cyano group, a trifluoromethyl (CF3) group, an amidine (C(?NH)NH2) group, and a 5-methyl-1,2,4-oxadiazole group, Y is selected from the group consisting of hydrogen, halogen, a phenyl group substituted with one or two substituents selected from the group consisting of halogen, methoxy, nitro, trifluoromethyl, and aminomethyl, CO—R?, COOR?, OH, O—R?, and NH—R?, each R? is independently selected from the group consisting of C1-C18 alkyl, alkenyl, alkynyl, and —Z-alkyl (wherein Z is a heteroatom selected from the group consisting of O, S, and N or is —(CH2)m—), and m is an integer from 0 to 5.

Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: Compounds and compositions are described herein for treating post traumatic stress disorder.

Abstract: The invention relates to a method of treating or preventing a condition in a subject, comprising administering to the subject an acceptable composition comprising meglumine or a salt thereof. The invention further relates to a method of improving a physiological function in a subject, comprising administering to the subject an acceptable composition comprising meglumine or a salt thereof.

Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: The invention disclosed herein relates to novel Peribysin E analogs of general formula-I. Further the invention provides simple, economical and short synthesis of Peribysin E and its analogs of Formula I, in good yield and purity leading to the identification of more potent cell adhesion inhibitors.

Abstract: Functionality for estimating characteristics of an on-chip noise signal can be implemented on a processing module. An on-chip noise signal is determined at an on-chip determination point of a computer chip. The on-chip noise signal is converted to a frequency-varying signal using a voltage-controlled oscillator implemented on the computer chip. The frequency-varying signal is measured at an off-chip measurement point and frequency information is extracted from the frequency-varying signal. The frequency information is converted to a voltage level associated with the on-chip noise signal based on the relationship between an input voltage provided to the voltage-controlled oscillator and an output frequency generated by the voltage-controlled oscillator.

Abstract: This invention discloses a radiation curable barrier coating composition for application to paper or paperboard substrates that can be applied using a conventional flexographic printing process. The coating composition includes one or more hydrophobic cycloaliphatic radiation curable monomers, one or more alcohol-functional waxes or sterols, and one or more other hydrophobic wax materials. The incorporation of these materials together lowers the MVTR of the coating compared to other radiation curable compositions while also generating improved, higher gloss. This invention also discloses a method to manufacture the coating composition and a preferred method to print the coating composition.

Abstract: In various embodiments, the present invention provides methods of reducing the risk of a cardiovascular event in a subject on statin therapy and, in particular, a method of reducing the risk of a cardiovascular event in a subject on statin therapy having a fasting baseline triglyceride level of about 135 mg/dL to about 500 mg/dL, and administering to the subject a pharmaceutical composition comprising about 1 g to about 4 g of eicosapentaenoic acid ethyl ester or a derivative thereof.

Abstract: In various embodiments, the present invention provides methods of reducing the risk of a cardiovascular event in a subject on statin therapy and, in particular, a method of reducing the risk of a cardiovascular event in a subject on statin therapy having a fasting baseline triglyceride level of about 135 mg/dL to about 500 mg/dL, and administering to the subject a pharmaceutical composition comprising about 1 g to about 4 g of eicosapentaenoic acid ethyl ester or a derivative thereof.

Abstract: In various embodiments, the present invention provides methods of reducing the risk of a cardiovascular event in a subject on statin therapy and, in particular, a method of reducing the risk of a cardiovascular event in a subject on statin therapy having a fasting baseline triglyceride level of about 135 mg/dL to about 500 mg/dL, and administering to the subject a pharmaceutical composition comprising about 1 g to about 4 g of eicosapentaenoic acid ethyl ester or a derivative thereof.

Abstract: The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.

Abstract: The invention in this document is related to the field of preparation of 1,3-(substituted-diaryl)-1,2,4-triazoles and certain intermediates derived therefrom, where said intermediates are useful in the preparation of certain pesticides disclosed in U.S. Pat. No. 8,178,658.

Abstract: The present invention provides aminohydantoin anti-malarial agents. In some embodiments, these agents have the property of functions of targeting malarial aspartic proteases while at the same time having low activity against human BACE. Methods of employing such agents are also provided.

Abstract: The invention pertains to a method of determining a statin dosage for an individual in need of treatment with a statin, comprising determining a SLCO1B1 genotype from a nucleic acid sample of the individual, said genotype comprising the presence or absence of the SLCO1B1-056 polymorphism, and determining an ApoE genotype or phenotype identifying an ApoE polymorphism selected from the group consisting of ApoE2, ApoE3, ApoE4, and any combination thereof, wherein the combination of a SLCO1B1 genotype identifying the presence of the SLCO1B1-056 C polymorphism and the ApoE genotype or phenotype identifying one of the ApoE3/4 or ApoE4/4 genotypes indicates the statin dosage.

Abstract: The invention provides derivatives and analogs of triazatetracyclo[7.7.0.01,13.02,7]-hexadeca-2,4,6,10,12-pentaenes, 5,7,11-triazatetracyclo[8.7.0.01,6.012,17]-heptadeca-6,8,12,14,16-pentaenes, pharmaceutical compositions comprising these compounds and methods for treatment of hepatitis C viral infections using these compounds.

Abstract: The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification, or a salt thereof, a prodrug of the compound or a salt thereof, a medicament containing the compound or a salt thereof, the medicament which is a phosphodiesterase 10A inhibitor, and a medicament which is for preventing or treating schizophrenia.

Abstract: A proteinase therapy has been invented to eliminate solid tumors by destroying tumors' solid structure and killing cancer cells by cleaving vital extracellular matrix proteins C-terminally, N-terminally or both with cell membrane intact and limited adverse effects. The micro-scale intratumoral proteinase K therapy is tumor specific but not cancer type specific. Proteinase K therapy can be operated on multiple tumors on multiple occasions, if necessary. It may be employed to eliminate any solid tumor to prolong a cancer patient's life span.

Abstract: An aromatic organic solvent solution of a methanesulfonic acid alkyl ester having high thermal stability is obtained by reacting an alkyl alcohol with methanesulfonyl chloride in an aromatic organic solvent in the presence of a tertiary amine, and washing the resulting aromatic organic solvent solution of a crude methanesulfonic acid alkyl ester with an aqueous alkali metal carbonate solution. The washing is performed using the aqueous alkali metal carbonate solution having a concentration of 1 to 3 mass % in an amount of 4 to 6 parts by mass per 1 part by mass of the alkyl alcohol.

Abstract: The present invention embraces Niemann-Pick C1-like 1 protein antagonists and agents that inhibit hepatic virus infection for use in the prevention and treatment of a hepatic virus infection.

Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.

Abstract: The present invention relates to a pyrazolopyran of the general formula I wherein the variables are defined according to the description, including a tautomer, salt, cleavable prodrug, or mixtures thereof, in particular to said pyrazolopyran for use as a medicament and/or an inhibitor of the enzyme serinehydroxymethyltransferase (SHMT). The invention also relates to a process the preparation of a pyrazolopyran of the formula I, to compositions comprising said compound and processes for the preparation of these compositions. Further it relates to use of the pyrazolopyran of formula I as an herbicide as well as to a method of controlling undesired vegetation.

Abstract: A composition and a method of treatment for the reduction of risk factors for cardiovascular disease utilizing a combination of lipid lowering cholesterol absorption inhibitors, e.g. azetidinones, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught.

Abstract: An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): (wherein all symbols represent the same meanings as described in the specification), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7 R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.

Abstract: Compositions, methods, and kits useful for treating hyperlipidemic conditions are provided herein. Such compositions can contain synergizing amounts of nicotinic acid, nicotinamide riboside and/or nicotinic acid metabolites in combination with leucine and/or a leucine metabolite, with or without resveratrol.

Abstract: A composition and a method of treatment utilizing a combination of lipid lowering cholesterol absorption inhibitors, e.g. azetidinones, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught. EPA+DHA are about 80% of the total formulation and about 89% of the total omega 3 fatty acid content of the composition. The formulation may further contain specific amounts of arachidonic acid (AA), stearidonic acid (SDA), and alpha-linolenic acid (ALA).

Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob

Abstract: The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.

Abstract: A stable ternary solid dispersion composition with enhanced physical stability and/or bioavailability comprising: (a) about 1% wt. to about 50% wt. of one or more poorly soluble active pharmaceutical ingredient (API) which belongs to Biopharmaceutics Classification System (BCS) class II and/or IV; (b) about 11% wt. to about 50% wt. of at least one water-soluble polymer; and (c) about 20% wt. to about 99% wt. of crosslinked polyvinylpyrrolidone (crospovidone, a water-insoluble polymer). The solid dispersion is capable of inhibiting crystallization of API in solid state and/or aqueous gastrointestinal tract (GIT) medium. Also disclosed is a method of preparation of such solid dispersion composition by fusion or solvent or fusion-solvent method.