Abstract: A method of treatment for epilepsy and other disease states is described, which comprises delivery of gabapentin in a gastric retained dosage form.

Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

Abstract: Disclosed are compounds of Formula 1, N-oxides and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, EC(?X1); a is 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).

Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 0, 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

Abstract: Disclosed are compositions comprising (a) at least one compound selected from compounds of Formula 1, N-oxides, and salt thereof, wherein R1 is phenyl optionally substituted with up to 5 substituents independently selected from R3, or pyridinyl optionally substituted with up to 4 substituents independently selected from R3; R2 is C1-C4 haloalkyl; or thiazolyl, pyridinyl or pyrimidinyl, each optionally substituted with up to 2 substituents independently selected from the group consisting of halogen and C1-C4 alkyl; each R3 is independently halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C(R4)?NOR4 or Q; each R4 is independently C1-C4 alkyl; Z is CH?CH or S; and each Q is independently phenyl or pyridinyl, each optionally substituted with up to 3 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy; and (b) at least one invertebrate pest control agent.

Abstract: An assay for a GCH1 allele and associated genotype for the screening, prediction, diagnosis, prognosis, treatment and treatment response of psychiatric, neuropsychiatric, and neurological disorders, such as schizophrenia, schizoaffective disorder and bipolar disorder, and for defining treatments of such disorders. The presence of a variant in the GCH1 gene, alone or in conjunction with a measurement of low or altered biopterin, or altered BH4 system measures, is used to screen or diagnose subjects at risk for developing a psychiatric, neuropsychiatric, or neurological disorder. The genetic assay, with or without a biopterin or BH4 system assay, may also be used to determine treatment regimens. For subjects with an impaired BH4 system, treatments to increase or normalize biopterin, BH4, or the BH4 system can also be used, such as BH4 supplementation, lithium treatment, phenylalanine treatment, or other treatments and therapies.

Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.

Abstract: The invention provides methods of extracting a biodegradable polyester with a supercritical fluid effective to obtain a purified biodegradable polyester, such as a purified biodegradable poly(lactide-glycolide) (PLG). The supercritical fluid can be carbon dioxide at an elevated pressure, or can be carbon dioxide with one or more cosolvents. Methods for carrying out stepwise purification of the biodegradable polyester at multiple pressures or multiple temperatures, or both, are also provided. When the polyester is PLG, a purified PLG copolymer is obtained having a narrowed molecular weight distribution with respect to the unpurified polyester. The purified PLG copolymer can have a polydispersity index of less than about 1.7, less than about 2% monomers, and less than about 10% oligomers. The purified PLG copolymer can exhibit a reduced initial burst effect when incorporated into a controlled release formulation such as a flowable implant adapted to be injected into body tissues.

Abstract: Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.

Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.

Abstract: Provided herein are solid state forms of paliperidone salts, processes for preparation, pharmaceutical compositions, and method of treating thereof. Paliperidone is represented by the following structural formula (I): More particularly, provided are solid state forms of paliperidone acid addition salts, wherein the acid counter ion is provided by an acid selected from the group consisting of L-(+)-tartaric acid, p-toluenesulfonic acid, maleic acid, oxalic acid, fumaric acid, acetic acid and malic acid. Provided also herein is a process for preparing substantially pure paliperidone free base using the solid state forms of paliperidone salts.

Abstract: Oral dosage forms for poorly soluble amine drugs are provided. Such dosage forms include an ionizable compound such as an organic acid, an amphiphilic polymer and a release rate-controlling membrane. Such dosage forms allow for the consistent release of the active agent in both gastric pH conditions and in the intestine. Methods of making such dosage forms are also provided.

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, Sjoegren'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: A method of treatment for epilepsy and other disease states is described, which comprises delivery of gabapentin in a gastric retained dosage form.

Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.

Abstract: The present invention provides methods of treating epilepsy and other neurological disorders. The methods generally involve administering to an individual in need thereof an effective amount of an agent that blocks a transforming growth factor-beta pathway.

Abstract: Delivery of drugs in association with PLGA polymers which have crystallinity resulting from the presence of long chain alkyl groups in terminal units.

Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).

Abstract: The present invention relates to prodrugs of parent drug compounds containing heteroaromatic NH groups.

Abstract: The present invention relates to a composition comprising ocaperidone as an active substance and an effective amount of water-soluble polymers to increase solubility of ocaperidone. The present invention further relates to a therapeutic system for ocaperidone with a compartment for the drug formulation comprising said composition, and to a process for the preparation thereof as well as to the therapeutic use of said composition as antipsychotic drug. The present invention also relates to the solubilisation of ocaperidone in an aqueous medium with the aid of water soluble swellable polymers.

Abstract: The invention relates to use of substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. More specifically, the invention relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of GSK3?, such as Pick's disease among various other diseases as claimed herein.

Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula (I) wherein R1, R2, R3, and RN are as defined herein. Compounds of Formula (I) are useful in the prevention and/or treatment of neurological and psychiatric disorder, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the disclosure and methods of treating the aforementioned conditions using such compounds.

Abstract: The invention provides methods of extracting a biodegradable polyester with a supercritical fluid effective to obtain a purified biodegradable polyester, such as a purified biodegradable poly(lactide-glycolide) (PLG). The supercritical fluid can be carbon dioxide at an elevated pressure, or can be carbon dioxide with one or more cosolvents. Methods for carrying out stepwise purification of the biodegradable polyester at multiple pressures or multiple temperatures, or both, are also provided. When the polyester is PLG, a purified PLG copolymer is obtained having a narrowed molecular weight distribution with respect to the unpurified polyester. The purified PLG copolymer can have a polydispersity index of less than about 1.7, less than about 2% monomers, and less than about 10% oligomers. The purified PLG copolymer can exhibit a reduced initial burst effect when incorporated into a controlled release formulation such as a flowable implant adapted to be injected into body tissues.

Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.

Abstract: A method of treating the intraluminal disease in a coronary artery by injecting therapeutic agents perivascularly into the myocardium near the site of disease.

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.

Abstract: The compositions and methods disclosed herein are of use for the treatment and prevention of weight gain and obesity. In particular, the compositions and methods include treatment of weight gain and obesity with berberine and/or berberine analogs alone or in combination thereof to cause a reduction in an individual's weight or prevent weight gain or obesity. In certain embodiments, the weight gain and obesity are associated with administration of anti-psychotic drugs. In an alternative embodiment, the compositions and methods provide berberine or berberine analogs alone or for coadministration with an anti-psychotic agent. In an additional embodiment, the compositions and methods further include a natural product. The usefulness of the present invention is that berberine and berberine analogs do not have synergistic effects with other drugs and administration results in few side effects.

Abstract: The present invention relates to combination therapies and methods for treating, preventing and/or delaying the onset and/or development of schizophrenia, wherein the combination therapies comprise a hydrogenated pyrido[4,3-b]indole or a pharmaceutically acceptable salt thereof, such as dimebon, and an antipsychotic.

Abstract: The invention relates to compounds for the treatment of dermatological diseases where inflammation, matrix metalloproteinases (MMPs) and peroxisome proliferator-activated receptors (PPARs) play a role in mediating the disease, such as the treatment of acne with Pemirolast or a closely related compound thereof.

Abstract: The present invention relates to a solid, orodispersible and/or dispersible composition comprising (a) from 0.1 to 59% by weight of at least one active substance with particle size no exceeding 50 ?m; (b) from 40 to 99% by weight of at least one diluent without known effect, non water-soluble; (c) from 0.1 to 15% by weight of at least one disintegrating agent; and (d) from 0.05 to 10% by weight at least of one sweetening agent with particle size not exceeding 50 ?m, percentages by weight being expressed compared to the total weight of the aforementioned composition. The present invention also relates to the use of said composition as a drug, a food supplement or in cosmetics and a method of preparation of an orodispersible and/or dispersible compound implementing said composition.

Abstract: The present invention related to the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with critical buccal condition, leading to difficulties in swallowing oral medicine forms and thus difficulties in treating said illnesses. Particularly, the present invention discloses the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with dysphagia and/or odynophagia and/or aspiration risk. Another aspect of the present invention is the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for the treatment of dysphagia and/or odynophagia and/or aspiration risk.

Abstract: The present invention relates to a method for preparing microspheres and microspheres prepared thereby, more particularly to a method for preparing a polymeric microsphere, including preparing an emulsion including a polymer compound, a drug, a water-insoluble organic solvent and a dispersion solvent and adding to the prepared emulsion a base or an acid to remove the water-insoluble organic solvent from the emulsion, a polymeric microsphere prepared thereby, and a composition for drug delivery including the microsphere. According to the present invention, a drug-containing polymer microsphere may be prepared quickly and simply without the solvent evaporation or solvent extraction process, thereby reducing water consumption and minimizing wastewater generation.

Abstract: The present application describes deuterium-enriched risperidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present invention relates to new piperidine modulators of dopamine receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.

Abstract: Disclosed are dosage forms and methods comprising benzisoxazole derivatives. More particularly, disclosed are dosage forms, methods, and new uses of benzisoxazole derivatives that substantially reduce or substantially eliminate certain side effects of the benzisoxazole derivatives when dosed to a patient.

Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.

Abstract: The present invention relates to an extended release composition of paliperidone for oral administration comprising paliperidone and at least one matrixing agent. The said extended release composition maintains desired therapeutic drug effect over a prolonged period of time and thereby reduces the side effects resulting due to excess drug blood plasma concentration. Further, the invention also relates to process for the preparation of an extended release oral composition of paliperidone.

Abstract: A process for preparing microparticles comprising a biologically active material and a polymer and having a mean particle size expressed as the volume mean diameter (VMD) of from 10 to 500 ?m, wherein the biologically active material is substantially insoluble in the polymer, which process comprises: a. contacting a mixture of the biologically active material or a precursor thereof, the polymer or a precursor thereof and a processing aid with a supercritical fluid which is capable of swelling the polymer under temperature and pressure conditions necessary to maintain the fluid in a supercritical state; b. allowing the supercritical fluid to penetrate and liquefy the polymer, whilst maintaining the temperature and pressure conditions so that the fluid is maintained in a supercritical state; c. releasing the pressure to precipitate microparticles comprising the biologically active agent and the polymer.

Abstract: The present invention relates to methods of treating the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability—hypersensitivity—hyperaesthesia—dissociative phenomena— . . . ) using compounds and compositions of compounds having D4 and/or 5-HT2A antagonistic, partial agonistic or inverse agonistic activity. The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and/or (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and/or (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and/or biological compounds.

Abstract: Compounds of Formula I and Formula II and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed.

Abstract: The present invention relates to a new method of treatment for persons meeting diagnoses for major depressive disorder, or other unipolar (non-bipolar, non-psychotic and non-treatment resistant) depression. The method comprises administering a combination of two categories of drugs, antipsychotics or dopamine system stabilizers, in combination with a newer antidepressant such as a selective serotonin reuptake inhibitor, as initial treatment or as soon as possible. The method targets the prevention of suicide, and provides other benefits including preventing disease progression development of tolerance toward the antidepressants. Another aspect of the invention relates to using the method for alleviating cognitive distortion and related functional impairment or health risks, and/or using the method for smoking cessation or nicotine withdrawal.

Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein Y, R1, R2, R3, and R4 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.

Abstract: Pyrimidone derivatives of formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.

Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: Methods are provided for partial aortic obstruction for cerebral perfusion augmentation in patients suffering from global or focal cerebral ischemia. Alternatively, the methods can be used to partially obstruct aortic blood flow to condition the spinal cord to secrete neuroprotective agents prior to abdominal aortic aneurysm repair. Partial obstruction of a vessel can be accomplished by a device comprising an elongate catheter and a distally mounted expandable member. The expandable member may comprise one or two balloons. Other medical devices, such as an angioplasty, stent, or atherectomy catheter, can be inserted distal the expandable member to provide therapeutic intervention.