Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.

Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract: The present invention relates to a hard capsule composite formulation comprising a capsule having a hemispherical closure at each end and an interior space; and one or more tablets encapsulated in the capsule, wherein the tablet or the tablets as a whole have a shape conforming to the internal space of the capsule. The hard capsule composite formulation can efficiently charge pharmaceutical compositions inside the limited interior space of the capsule, and hence, it allows packing a high-dose of pharmaceutical composition in a relatively small-sized capsule, which increases productivity and patient compliance. Also, the composite formulation exhibits good dissolution rate because pharmaceutically active ingredients contained in the capsule are separated from one another, and thus, the ingredients are less affected by the dissolution rate of one another, allowing good storage stability which can optimize the therapeutic effects.

Abstract: Therapeutic compositions and methods for treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) include dosage forms that deliver a therapeutic amount of active drug in a delayed and controlled release formulation. The dosage form can be administered at night and drug release is delayed for from 4 to 6 hours or longer, followed by an ascending release rate.

Abstract: Therapeutic compositions and methods for treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) include dosage forms that deliver a therapeutic amount of active drug in a delayed and controlled release formulation. The dosage form can be administered at night and drug release is delayed for from 4 to 6 hours or longer, followed by an ascending release rate.

Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.

Abstract: This application describes compositions of receptor inhibitors, including antipsychotic agents, for example haloperidol, and methods of use for alleviating clinical depression, improving cognition and/or treating other syndromes, conditions or diseases for which anti-depressant agents are prescribed. Furthermore, this application describes compositions and methods to induce supersensitivity in dopamine D2 and other receptors involved in depression and/or cognition as a means of alleviating clinical depression or improving cognition.

Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract: Described herein are enhanced N-methyl-D-aspartate (NMDA) receptor antagonists, pharmaceutical compositions thereof, and their methods of use and treatment, e.g., of Formula (I): wherein one or more of R1, R2, R3, R4, R5, or the ring formed by the joining of R1 and R2, is a hydrophobic moiety which confers enhanced antagonist activity as compared to existing NMDA receptor antagonists, e.g., ifenprodil. Compounds described herein are designed based on the discovery that ifenprodil binds within the allosteric domain of the GluN1/GluN2B NMDA receptor, particularly at the interface between GluN1 and GluN2B subunits. In silico methods are further described herein.

Abstract: A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.

Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt or enantiomer thereof, for use in the treatment of hypertrophic cardiomyopathy, as well as to a method of treating HCM, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt or enantiomer thereof, to treat said HCM. The invention further relates to a treatment programme for treating HCM, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HCM or the symptoms thereof.

Abstract: A drug-containing patch allows transdermal administration of a drug. The patch features a hydrophobic reservoir containing the drug, where the reservoir has a first surface and a second surface. A drug-impermeable backing overlies the first surface of the reservoir. A release sheet may overlie the second surface of the reservoir. The hydrophobic reservoir contains a drug and a hydrophobic matrix, where the hydrophobic matrix includes a hydrophobic filler in an amount which is effective to adsorb said drug; and a mixture of polyisobutylene and mineral oil. The hydrophobic matrix may contain hydrophobic colloidal silica as the hydrophobic filler. The hydrophobic reservoir layer may serve as a skin-contacting adhesive layer. Alternatively, a release-controlling adhesive layer may serve as the skin-contacting adhesive layer. The release-controlling adhesive layer may contain hydrophobic colloidal silica and a mixture of polyisobutylene and mineral oil.

Abstract: A pharmaceutically delivery system is described comprising a pharmaceutically active agent and acidified nitrite as an agent to produce local production of nitric oxide at the skin surface. The dosage form may be in any pharmaceutically acceptable carrier means and comprises an acidifying agent adapted to reduce the pH at the environment. In one embodiment, a barrier consisting of a membrane allows diffusions of the anaesthetic and nitrite ions while preventing direct contact of the skin and acidifying agent.

Abstract: Piperidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.

Abstract: The invention relates to a method of treating Attention Deficit Disorder (ADD) and Attention Deficit/Hyperactivity Disorder (ADHD) and compositions for topical application of methylphenidate comprising methylphenidate in a flexible, finite system wherein the methylphenidate is present in an amount sufficient to achieve substantially zero order kinetics for delivery to the skin or mucosa of a patient in need thereof over a period of time at least 10 hours.

Abstract: A polyacrylate formulation suitable for delivery of drug to through a body surface of an individual. By loading the drug and permeation enhancers at a high concentration into a polyacrylate proadhesive that has inadequate adhesive properties for typical adhesive application on the skin, a formulation with desirable adhesive characteristics and effective therapeutic properties can be made. The proadhesive has higher glass transition temperature than typical pressure sensitive adhesives.

Abstract: Compositions and methods for the treatment of drug-induced long QT syndrome and other cardiac channelopathies are disclosed herein. The compositions and methods of the present invention comprise binding one or more QT prolonging drugs with a liposome prior to parenteral (intravenous or subcutaneous) administration, or administration of an empty liposome prior to or concomitantly with therapeutic agents known to have a high risk of QT prolongation, or immediately following an envenomation. The results presented show an abrogation of the adverse effects of QT prolonging drugs in a dose-dependent manner by the compositions of the present invention.

Abstract: Cerebral palsy impaired speech in children and adolescents are effectively treated by administration of a psychostimulant. Low doses of the psychostimulant significantly (p=0.0025) increases the percentage of correctly pronounced intelligible syllables or words and the ability to more intelligibly communicate (p=0.0309). The improvement in speech persists after cessation of or prior to continued psychostimulant treatment.

Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.

Abstract: This invention provides methods of identifying agents useful to prevent, ameliorate or treat one or more symptoms of Friedreich's ataxia or other neurodegenerative disease, and methods of employing the identified agents to prevent, reduce, delay or inhibit one or more systems of Friedreich's ataxia or other neurodegenerative disease.

Abstract: The present invention provides a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.

Abstract: The invention relates to compounds of structural formula (Ia): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, X4, X6, X10, R1, Y, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.

Abstract: The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.

Abstract: The invention provides methods for treating or ameliorating cognitive dysfunction, fatigue, energy, concentration, mood, and pain associated with fibromyalgia using compositions containing methylphenidate or pharmaceutically equivalents thereof.

Abstract: The present invention relates to a fentanyl coated tablet and to the method for the preparation thereof.

Abstract: This invention relates to a oral pharmaceutical formulation for methylphenidate or its analogs, derivatives, isomers or enantiomers, including d-threo-methylphenidate.

Abstract: The invention relates to dosage forms that provide prolonged therapy. In particular, the invention relates to dosage forms including various pluralities of drug-containing resin particles. The invention also relates to methods of making these dosage forms and methods of treating using these dosage forms.

Abstract: The invention provides, in part, methods and compositions for treating psychiatric disorders, for example, apathy, dementia, or depression, using combination therapies such a monoamine oxidase inhibitor or a selective serotonin reuptake inhibitor in combination with an anti-psychotic agent.

Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1 and R2 are as described herein, compositions including the compounds, their pharmaceutically acceptable salts and esters and methods of using the compounds.

Abstract: The present invention relates to novel fluorinated piperidine derivatives having antagonistic activity at the 5-HT2B receptor, pharmaceutical compositions comprising these compounds and their use as a medicine.

Abstract: Compositions for the transdermal delivery of methylphenidate in a flexible, finite form are described. The compositions comprise a polymer matrix that includes methylphenidate or a pharmaceutically acceptable salt and at least one acrylic polymer that is non-reactive with methylphenidate. Methods using the compositions to achieve transdermal delivery of methylphenidate or for treating Attention Deficit Disorder (ADD) and/or Attention Deficit/Hyperactivity Disorder (ADHD), postural orthostatic tachycardia syndrome, or narcolepsy also are described.

Abstract: Pharmaceutical compositions and methods for the treatment of Gulf War Illness in human patients comprising administering a central nervous system (CNS) stimulant in a daily low-dosage amount, and micronutrients acetyl L-carnitine, L-tyrosine, N-acetyl cysteine, and alpha-lipoic acid. The CNS stimulant and micronutrient components may be in admixture for convenient daily oral administration of a low dosage CNS stimulant and micronutrients in the range of about 60-250 mg acetyl L-carnitine, 50-200 mg L-tyrosine, 60-250 mg N-acetyl cysteine, and 25-100 mg alpha-lipoic acid per day.

Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of hypertrophic cardiomyopathy, as well as to a method of treating HCM, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said HCM. The invention further relates to a treatment programme for treating HCM, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HCM or the symptoms thereof.

Abstract: A therapeutic method for treating apraxia of speech in children. The child can also be diagnosed with autism, mental retardation, dyslexia. Verbal development stages and nonverbal development stages are tested and observed. If a child demonstrates at least 18 to 24 month development stage of either the verbal development or the non-verbal development, a therapeutic dosage of dopamine agonistic medicine is administered to the child in addition to speech therapy and language training.

Abstract: The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval.

Abstract: This invention provides a method of treating a patient afflicted with a neurodegenerative disorder, e.g., Huntington's disease, comprising administering to the patient rasagiline as an add-on therapy to or in combination with pridopidine. This invention also provides a package and a pharmaceutical composition comprising rasagiline and pridopidine for treating a patient afflicted with a neurodegenerative disorder. This invention also provides rasagiline for use as an add-on therapy or in combination with pridopidine in treating a patient afflicted with a neurodegenerative disorder. This invention further provides use of rasagiline and pridopidine in the preparation of a combination for treating a patient afflicted with a neurodegenerative disorder.

Abstract: The subject of the invention is compounds of formula (I): in which R1-R10 are as defined within, the method of preparation and therapeutic application as cannabinoid CB1 receptor antagonists.

Abstract: A nasal delivery device for and method of delivering a substance, preferably comprising oxytocin, non-peptide agonists thereof and antagonists thereof, preferably as one of a liquid, as a suspension or solution, or a powder to the nasal airway of a subject, preferably the posterior region of the nasal airway, and preferably the upper posterior region of the nasal airway which includes the olfactory bulb and the trigeminal nerve, and preferably in the treatment of neurological conditions and disorders.

Abstract: A method for treating or preventing a disease, condition or state in a subject in need thereof by administering to the subject an effective amount of the (?)-enantiomer of perhexyline or a pharmaceutically acceptable salt, prodrug or derivative thereof, substantially free of the (+)-enantiomer, or pharmaceutical composition containing same. The disease, condition or state may be associated with altered tissue energetics, impaired tissue energetics, altered cardiac tissue energetics, impaired cardiac tissue energetics, altered hepatic tissue energetics, impaired hepatic tissue energetics, and diabetes.

Abstract: Disclosed is an external preparation composition having good transdermal absorbability. An external preparation composition having excellent transdermal absorbability can be produced by dissolving a medicinal substance or a salt thereof in a fatty acid-based ionic liquid to form a composite ionic composition of the medicinal substance. The external preparation composition can be used as a liquid preparation, an ointment, a cream, a plaster or the like, and enables to provide a preparation having excellent transdermal absorbability.

Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: The present invention is directed to a method for treating a patient suffering from a metabolic disorder such as the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, and the metabolic sequale of these diseases including cardiovascular, cerebrovascular, renal and hepatic diseases, comprising the step of: administering to a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes a pharmaceutical composition comprising (1) at least one compound that stimulates an increase in central dopaminergic neuronal activity level in the subject, and (2) at least one compound that stimulates a decrease in central noradrenergic neuronal activity level in the subject.

Abstract: Cerebral palsy impaired speech in children and adolescents are effectively treated by administration of a psychostimulant. Low doses of the psychostimulant significantly increases the percentage of correctly pronounced intelligible syllables or words and the ability to more intelligibly communicate. The improvement in speech persists after cessation of or prior to continued psychostimulant treatment.

Abstract: The treatment of acute pain with a sufficient dosage by intranasal administration of fentanyl results in a time to onset of action comparable to intravenous administration and a significantly faster onset of action than nasal titration of fentanyl. The nasal administration of a sufficient amount of fentanyl to obtain pain relief has lower maximum plasma concentrations comparable to intravenous administration and results in lower rates of adverse events like respiratory depression, nausea and vomiting. Compositions for use in the method are also disclosed.

Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.