Abstract: The present invention describes [1,2,4]thiadiazine 1,1-dioxide compounds and pharmaceutically acceptable salts thereof, which are useful in lowering serum uric acid in a patient in need thereof comprising administering to the patient a therapeutically or prophylactically effective amount of a [1,2,4]thiadiazine 1,1-dioxide compound.

Abstract: A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.

Abstract: The invention is directed to deuterated 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.

Abstract: Methods for treating cancer comprising administering a DLL4 antagonist and one or more anti-hypertensive agents are described. Also described are pharmaceutical compositions comprising a DLL4 antagonist and one or more anti-hypertensive agents, and kits comprising the same.

Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.

Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.

Abstract: A pharmaceutical composition for treating or preventing one or both of neural anoxia and reperfusion injury, which includes a pharmacological activator of the PKG pathway, and methods of treating or preventing medical conditions using a pharmacological activator of the PKG pathway.

Abstract: The invention relates to a pharmaceutical composition comprising (i) a renin inhibitor, (ii) a calcium channel blocker (CCB), and a diuretic and to a method of using such composition for the treatment of cardiovascular disease.

Abstract: The present invention includes a method of treating or preventing a CNS white matter injury in a patient in need thereof. The invention also includes a method of stimulating proliferation of a CNS cell in a patient in need thereof.

Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of formula: wherein R is C1-C6 alkyl or (Aryl)CH2-,and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: Methods for treatment of depression-related mood disorders in mammals, particularly humans are disclosed. The methods of the invention include administration of compounds capable of enhancing glutamate transporter activity in the brain of mammals suffering from depression. ATP-sensitive K+ channel openers and ?-lactam antibiotics are used to enhance glutamate transport and to treat depression-related mood disorders and depressive symptoms.

Abstract: The invention is directed to [1,2,4]thiadiazine 1,1-dioxide compounds of formula I wherein A is B is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: The present invention relates to an improved process for the preparation of Chlorothiazide and pharmaceutically acceptable salts thereof. The present invention relates to novel polymorphs of Chlorothiazide and Chlorothiazide salts, in particular Chlorothiazide sodium. The present invention further relates to pharmaceutical compositions comprising Chlorothiazide and Chlorothiazide salts, in particular Chlorothiazide sodium and process for preparation thereof.

Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.

Abstract: The application describes treatment of motoneuronal dysfunctions or disorders using AMPA receptor modulators. Examples of a motoneuronal dysfunction or disorder include obstructive sleep apnea, snoring, multiple sclerosis, spinal cord injury, e.g., crush, partial or complete transection, motor neuron diseases, motor weakness due to aging, stroke, tumor, hemorrhage, degenerative or wasting diseases, and spasticity. One example of an AMPA receptor modulator is a benzothiadiazide compound. Another example of an AMPA receptor modulator is an ampakine. Yet another example of an AMPA receptor modulator is aniracetam.

Abstract: The embodiments provide compounds of the general Formula I and compound 105S, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract: Coagglomerates of mannitol, whose laser volume-average diameter D4,3 is between 1 and 200 ?m, and of granular starch, are characterized in that they have a disintegration behaviour determined according to a test A such that the relaxation time measured is between 30 and 100 seconds and the swelling force is between 0.8 and 3.0 N.

Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.

Abstract: A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, O-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.

Abstract: The invention is directed to 4-hydroxy-5,6-dihydro-1H-pyridin-2-one compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus: wherein R6 is X is N, Ring A is a 5- or 6-membered aryl, optionally substituted by 1-3 R8 moieties, n is 2, and R1-R6 and R8 are defined herein.

Abstract: The present invention relates to cyclopropyl derivatives of formula (I) and salt thereof. These compounds are NK3 receptor antagonists and may therefore be useful for treatment of diseases where the NK3 receptor is implicated, e.g. psychotic disorders.

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

Abstract: The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C.

Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.

Abstract: The present invention relates to the use of a potassium channel activator in the manufacture of a medicament for suppressing the fasting plasma insulin level and/or postabsorptive insulin level in a mammal in need thereof, wherein the fasting and/or postabsorptive plasma insulin level is reduced to about 5 mU/l or less. The present invention also relates to the use of a potassium channel activator in the manufacture of a medicament for suppressing the fasting plasma insulin level and/or postabsorptive insulin level in a mammal in need thereof for treating or preventing obesity, obesity related disorders and conditions and other disorders and conditions related to weight gain in a mammal in need thereof, said method comprising orally administering to said mammal in need thereof a daily dosage of about 5 mg to about 1200 mg, calculated on a Diazoxide active weight basis.

Abstract: A method of preparing porous microparticles comprises the steps of combining one or more organic compounds with a volatile system, and drying the system thus formed to provide substantially pure porous microparticles of the organic compound or composite porous microparticles of combinations of organic compounds. Organic compounds used in the method may be one or more of a bioactive, a pharmaceutically acceptable excipient, a pharmaceutically acceptable adjuvant or combinations thereof. The invention also relates to porous microparticles produced by such a method, and pharmaceutical compositions comprising such porous microparticles.

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

Abstract: Methods for treatment of depression-related mood disorders in mammals, particularly humans are disclosed. The methods of the invention include administration of compounds capable of enhancing glutamate transporter activity in the brain of mammals suffering from depression. ATP-sensitive K+ channel openers and ?-lactam antibiotics are used to enhance glutamate transport and to treat depression-related mood disorders and depressive symptoms.

Abstract: Compounds of formula (I): wherein: RCy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group, R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.

Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: The present invention provides HCV polymerase inhibiting compounds having the formula (I): where R1 is cyclobutyl-N(Ra)—, n is 1, 2, 3 or 4, and at least one R5 is RaSO2N(Rj)alkyl-. In a non-limiting example, a compound of the present invention is N-[(3-{1-[(cyclobutyl)amino]-4-hydroxy-2-oxo-1,2-dihydro-quinolin-3-yl}-1,1-dioxo-1,4-dihydro-1?6-thieno[2,3-e][1,2,4]thiadiazin-7-yl)methyl]methane-sulfonamide. The present invention also features compositions comprising the compounds of the present invention or pharmaceutically acceptable salts, stereoisomers or tautomers thereof, and methods of using the same to treat or prevent HCV infection.

Abstract: A method of preparing porous microparticles comprises the steps of combining one or more organic compounds with a volatile solvent system, and spray drying the system thus formed to provide porous microparticles of the organic compound or composite porous microparticles of combinations of organic compounds. Organic compounds used in the method may be one or more of a bioactive, a pharmaceutically acceptable excipient, a pharmaceutically acceptable adjuvant or combinations thereof.

Abstract: Sheet-like dosage forms that quickly dissolve or disintegrate in an aqueous environment, for the application of active agent combinations for the treatment of hypertension. The dosage forms contain at least two active agents that are suitable for the treatment of hypertension. The antihypertensive agents are selected from the group that encompasses beta receptor blockers, alpha receptor blockers, calcium antagonists, ACE inhibitors, AT1 antagonists, centrally acting antihypertensive agents, direct vasodilators, and diuretics. The use of active agent combinations according to the invention for the production of an oral dosage form for the treatment of high blood pressure, a method for the therapeutic treatment of hypertension, and a method for the production of a sheet-like dosage form are also disclosed.

Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: The present invention relates to compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by apomorphine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders.

Abstract: Compounds of formula (I): wherein: RCy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group, R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.

Abstract: Compounds, pharmaceutical compositions, kits and methods useful for inhibiting HDAC, thereby treating a disease state for which HDAC possess activity that contributes to the pathology and/or symptomology of the disease state. The compound is selected from the group consisting of: wherein the variables are as defined herein.

Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.

Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract: Pharmaceutical compositions comprising a plurality of formulated particles containing at least one active ingredient and at least one pharmaceutically acceptable excipient, granulated with a granulating composition containing at least one pharmaceutical excipient.

Abstract: The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia.

Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating hepatitis C virus infections: wherein Z is X is N or CR9; Y is —(CR4R5)n—; n is 2, 3, 4, or 5; and R1 through R9 are defined herein.

Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.

Abstract: Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering KATP channel openers with other drugs to treat diseases of humans and animals.

Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.

Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.