Abstract: Pyrazine compounds of the formula as well as stereoisomers thereof, N-oxides thereof, prodrugs thereof, and pharmaceutically acceptable salts thereof, wherein the variables in the formula are as defined in the specification. The compounds are useful as potassium channel modulating agents. Also, pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, and methods of using the pharmaceutical compositions.

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hyd

Abstract: Disclosed herein is a pharmaceutical composition comprising Hydroxychloroquine or its pharmaceutically acceptable salt and at least one antidiabetic compound, useful in the treatment of diabetes mellitus.

Abstract: This disclosure concerns antimicrobial compositions and methods for immunoenhancement, for example methods of increasing production of a type I interferon (IFN) in response to pathogen infection, by administration of a TAM receptor inhibitor. In certain embodiments, the disclosure concerns methods of using a TAM receptor inhibitor to treat a viral or bacterial infection in a subject.

Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines of Formula I: that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Abstract: Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.

Abstract: The present invention relates, in general, to glaucoma and, in particular, to a method of preventing or treating glaucoma using statins.

Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.

Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

Abstract: Novel compounds of structure Formula I: or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein n1, R1, R2, R3 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.

Abstract: A compound of the formula (I) wherein the substituents are as defined in the claims, is useful as a pesticide.

Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract: The invention features methods and kits employing bromolysergide in therapies for the treatment of cluster headache disorders.

Abstract: A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; G4 represents hydroxyl group, or —N(R1)(R2) (R1 and R2 represent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, or a saturated heterocyclic group); G5 is a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits Rho kinase.

Abstract: Isoquinolone derivatives of the general formula (I) are NK3 antagonists.

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit Hepatitis C virus (HCV), compositions comprising such compounds, and methods for treating Hepatitis C using such combinations.

Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy; each of U and V represents CH and W represents CH or N, or U represents N, V represents CH and W represents N, or each of U and V represents N and W represents CH; R2 represents hydrogen or fluorine when W represents CH or R2 represents hydrogen when W represents N; A represents O or CH2; Y represents CH or N; Q represents O or S; and n represents 0 or 1; and salts of such compounds.

Abstract: The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein Q, X1, X2, R1 and Z are as defined herein.

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: or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally compris

Abstract: The present invention is concerned with isoxazole-pyridines of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as pharmaceuticals. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.

Abstract: The present invention relates to compounds of formula (I) wherein A, B, Q, X, Y, R1, and R2 are as defined herein; pharmaceutical compositions containing them; a process for their manufacture; and methods for treating CNS disorders with the same.

Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.

Abstract: New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Abstract: Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ?C(H)— or ?N—; R3 is a radical of formula -(Alk1)m-(Z1)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z1 is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(—O)—, —0—(C?O)—, —C(?O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, Or —N(CH2CH3)—; and Q is hydrogen, halogen, nitrile, or hydroxyl, or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; R

Abstract: Embodiments of the invention are directed to methods of treating reperfusion or resuscitation injury in an individual in need of such treatment, comprising the step of administering to the individual who has had, having, or is at immediate risk of having an ischemic event an amount of a composition comprising a protein kinase A (PKA) activator and a ?1-adrenergic receptor antagonist sufficient to reduce reperfusion injury to an ischemic tissue.

Abstract: Derivatives of Sydnonimine and its analogues, which bind selectively to dopamine transporter (DAT) proteins are useful for treating and delaying the progression of disorders and illnesses that are alleviated by inhibiting dopamine reuptake.

Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein all of the variables are defined herein.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: This invention is related to orotic acid compounds of taxane cytotoxic agents and in particular to the conversion of the taxanes to their orotate esters. More particularly the pharmaceutical compositions of paclitaxel orotate and docetaxel orotate provide a strategy to minimize body weight loss during primary chemotherapy and improve patient outcomes and quality of life.

Abstract: A system for preparing a polyphenol containing formulation includes a first component which is a polyphenol and a second component which is the solvent system for the polyphenol. The solvent system includes water and a surfactant which is an ester of a dicarboxylic acid. The components are maintained separately from one another and are mixed prior to use. Specific compositions prepared through the use of the system include polyphenols and a solvent system based upon diaryl sulfosuccinate salts, water and optional glycols together with ancillary ingredients such as buffers, preservatives, coloring agents, fragrances, and thickeners.

Abstract: Administration of Oxybutynin directly to a patient's lungs for treating urinary incontinence, respiratory disease or IBD.

Abstract: The present invention pertains to a method of counteracting a malodor by introducing a malodor counteracting effective amount of a novel 3.2.1-bicyclo-octene or -octane compound represented by formula: wherein R is selected from the group consisting of hydrogen, acetate, carbonate monomethyl ester, and allyloxy; and wherein the broken line represents a single or double bond.

Abstract: L-carnitine, acetyl L-carnitine and propionyl L-carnitine inner salts, or their pharmaceutically acceptable salts, are used in combination to treat oligoasthenoteratosperia including oligospermia, asthenospermia, and teratospermia.

Abstract: The present invention provides methods for the design and identification of novel antimicrobial compounds, and provides antimicrobial compounds identified using these methods. These antimicrobial compounds inhibit the binding of a prokaryotic single-stranded DNA binding protein to a polypeptide that binds to the prokaryotic single-stranded DNA binding protein. In some examples, the prokaryotic single-stranded DNA binding protein is prokaryotic Exonuclease I. In one embodiment, the antimicrobial compound has the structure wherein Y is selected from the group consisting of CH2, O, and NH, R1 is selected from the group consisting of H, F, Cl, Br, and I, R2 is selected from the group consisting of H and CF3, R3 is selected from the group consisting of H and CO2H, R4 is selected from the group consisting of H and OH, and R5 is selected from the group consisting of H, alkoxy, and NO2.

Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.

Abstract: Stable ultrapure colchicine compositions comprising ultrapure colchicine and a pharmaceutically acceptable excipient are described. The compositions can be tablets. Methods for preparing such compositions and methods of use are also disclosed. Methods of treating gout flares with colchicine compositions are also disclosed.

Abstract: Stable ultrapure colchicine compositions comprising ultrapure colchicine and a pharmaceutically acceptable excipient are described. The compositions can be tablets. Methods for preparing such compositions and methods of use are also disclosed. Methods of treating gout flares with colchicine compositions are also disclosed.

Abstract: The present invention is directed toward particles for delivery of epinephrine to the respiratory system and methods for treating a patient in need of epinephrine. The particles and respirable compositions comprising the particles of the present invention described herein comprise the bioactive agent epinephrine, or a salt thereof, as a therapeutic agent. The particles are preferably formed by spray drying. Preferably, the particles and the respirable compositions are substantially dry and are substantially free of propellents. In a preferred embodiment, the particles have aerodynamic characteristics that permit targeted delivery of epinephrine to the site(s) of action.

Abstract: The subject invention provides materials and methods for treating various health conditions, including the prevention and/or treatment of a viral infection. In a preferred embodiment, a cysteamine compound is administered to a subject to treat an influenza virus infection. More preferably, a cysteamine compound is administered to a subject to treat influenza A, influenza B, influenza C virus infections, including avian influenza virus subtypes (such as H5N1 avian influenza virus).

Abstract: An infection inhibitor of retrovirus, particularly human immunodeficiency virus, comprising, as an active ingredient, at least one compound selected from the group consisting of a compound represented by the formula (I) (GGA) or a salt thereof, a compound represented by the formula (II) (NIK-333) or a salt thereof, and derivatives thereof.

Abstract: The present invention provides polymer micelles with cross-linked ionic cores as delivery vehicles for therapeutics, diagnostics, nucleic acids, proteins, small molecules and the like. The present invention provides additionally methods of synthesis and uses for such micelles.

Abstract: Abuse-resistant oral dosage forms suitable for administration of pharmacologically active agents are provided.

Abstract: A method for separating a polymer from carbon black in devulcanized rubber, the method comprising steps of inserting devulcanized rubber into a bath of a solvent, dissolving a polymer out of the devulcanized rubber and into a solution of the solvent and the polymer, removing the solution from the bath without disturbing an un-dissolved residue comprising carbon black, and recovering the un-dissolved residue.

Abstract: The invention relates to a process for manufacturing porous materials, which comprises the following steps: preparation of a solution of at least one structuring agent, having at least two structuring parts linked by at least one type of reversible non-covalent interaction; formation of the structured or porous material; separation of the at least two parts of the structuring agent at low temperature; and recovery of at least 50% by weight of the two non-degraded structuring parts and the porous material.

Abstract: An ophthalmic lens suited for extended-wear periods of at least one day on the eye without a clinically significant amount of corneal swelling and without substantial wearer discomfort. In one embodiment, an ophthalmic lens is a copolymerization product of at least one oxyperm, at least one ionoperm, and a crosslinker. In one embodiment, a lens has a tensile modulus of less than about 3.0 MPa, yet in another embodiment, the tensile modulus is between about 0.5 to about 1.5 MPa.

Abstract: The present invention relates to a silicone (meth)acrylamide monomer, and this silicone (meth)acrylamide monomer is particularly suitable for use in contact lenses, intraocular lenses, artificial cornea, and the like.

Abstract: A bone cement has a liquid acrylic monomer component, a powdered acrylic polymer component and yellowish beta-carotene (Pro-vitamin A) mixed into one of the liquid or powdered component and FDC blue No. 2 Lake powder mixed into the powdered component. The beta-carotene and FDC blue adds a greenish (yellow plus blue) color to the combined liquid and powdered component. The yellowish color disappears on setting of the bone cement leaving the cement blue.

Abstract: A bone cement comprising a first component and a second component, wherein contacting the first component and the second component produces a mixture which attains a high viscosity an initial period and the viscosity of the mixture remains relatively stable for a working time of at least 5 minutes after the initial setting period, and the mixture is suitable for in-vivo use.