Abstract: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

Abstract: The invention relates to the use of one or several synthetic or natural furan alkyls for preparing a drug preventing and/or treating obesity or overweight. The use of one or several synthetic or natural furan alkyls for cosmetically treating local excessive weight is also disclosed. Said furan alkyls preferably correspond to formula (I), wherein identical or different R1, R2, R3et R4 are independently of each other a hydrogen atom, a C1-C35alkyl radical, C1-C35 alcenyl radical or a C1-C35 alcynyl radical, preferably C10-C22, wherein said alkyl, alcenyl and alcynyl radicals are substitutable and R1, R2, R3 are preferably a hydrogen atom.

Abstract: The invention features methods, compositions, and kits for the treatment of attention deficit hyperactivity disorder and related behavioral disorders by administering an organic cation 3 (hOCT3) inhibitor.

Abstract: A multi-stage process to control the particle size of a pharmaceutical substance comprising the steps of: passing the pharmaceutical substance through a first stage of a particle size reduction process with a first set of particle size control parameters to obtain a feedstock of reduced median particle size and lesser distribution of median particle size for a second stage of a particle size reduction process; passing the feedstock, through a second stage of a particle size reduction process with a second set of particle size control parameters; optionally, using the product of the second stage or subsequent stages as a feedstock in further stages of a multi-stage particle size reduction process with a set of particle size control parameters for each stage; and collecting a pharmaceutical substance with a median particle size greater than 10 ?m and with a narrow, reproducible distribution of median particle sizes.

Abstract: This invention is directed to a method of treating sexual dysfunction in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, CI, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.

Abstract: This invention relates to the use of 5H-dibenz/b,f/azepine-5-carboxamide derivatives in the manufacture of various medicaments for treating neuropathic pain and for treating neurological disorders which involve both motor impairment and neuropathic pain.

Abstract: The invention relates to compounds according to general formula (1) and/or their enantiomers, diastereomers, and their pharmaceutically compatible salts, and their use to manufacture a medication as well as medications. The compounds are suited for treatment of diseases connected with misfolded proteins.

Abstract: The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to an activity) as well as to alleviate some of the symptoms experienced during menopause or associated with the menstrual cycle. Regardless of the precise formulation, the compositions of the invention can include at least one active ingredient that targets the hypothalamo-pituitary-adrenal (HPA) axis and at least one active ingredient that targets the prefrontal cortex. Either or both of these types of agents can be combined with an agent that inhibits activity in the sympathetic nervous system. Thus, the compositions or combination pharmacotherapies can also include an agent that inhibits a beta-adrenergic receptor or that otherwise acts as an anti-hypertensive or anxiolytic agent.

Abstract: The present invention relates to dosage forms of oxcarbazepine for oral administration that contain oxcarbazepine having a median particle size of from about 14 ?m to about 30 ?m and to processes for the preparation of such dosage forms. The dosage form may be a solid or a liquid dosage form. The solid dosage form may be in the form of a tablet, a capsule, or a granulate. The liquid dosage form may be in the form of a solution or a suspension.

Abstract: The present invention relates to the use of a compound of formula (I) wherein R1 and R2 together form an oxo group, or a pharmaceutically acceptable salt thereof, for the treatment of agitation, in particular behavioral agitation, especially in dementia patients diagnosed with Alzheimer's disease; pharmaceutical compositions comprising a compound of formula I; in combination with at least one compound selected from the group consisting of nootropic plant extracts, calcium antagonists, cholinesterase inhibitors, dihydroergotoxin, nicergoline, piracetame, purine derivates, pyritinol, vincamine and vinpocetin; and a kit including instructions for us of the combination.

Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: A selective kappa opioid receptor antagonist useful for treating ethanol use disorder withdrawal and anxiety, and/or depression, or schizophrenia as independent comorbid conditions.

Abstract: The present invention provides a PPAR ? agonist comprising, as an active ingredient, a tricyclic compound represented by the formula (I) (wherein R1 represents lower alkyl optionally having substituent(s) or the like, R2 and R3 are the same or different and each represents lower alkyl optionally having substituent(s) or the like, R4 and R5 are the same or different and each represents a hydrogen atom or the like, Q1-Q2-Q3 represents CH?CH—CH?CH or the like, Y represents a single bond or the like, Z1-Z2 represents C?CR13 (wherein R13 represents a hydrogen atom or the like), or the like, and A represents —COOH or the like), or a pharmaceutically acceptable salt thereof and the like.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.

Abstract: Extended release pharmaceutical dosage forms of carbamazepine for oral administration to maintain a patient's blood concentration for at least a 12 hour period, methods of administering dosage forms and processes for the preparation of such dosage form.

Abstract: The invention features methods of treating visceral pain in humans by administering an effective amount of a 5HT1B or 5HT1D receptor agonist, (e.g., a triptan). These methods can be used, for example, to treat a human suffering from visceral pain secondary to an underlying disease of a visceral organ, such as pancreatitis. Visceral pain treatable by the methods of the invention may also be secondary to a disease of the liver, kidney, ovary, uterus, bladder, bowel, stomach, esophagus, duodenum, intestine, colon, spleen, pancreas, appendix, heart, or peritoneum.

Abstract: The present invention relates to the use of tarenflurbil and/or a pharmaceutically tolerable salt or derivative thereof in enantiomerically-pure and/or essentially enantiomerically-pure form or a form that is enriched with respect to flurbiprofen racemate and/or a racemate of said salt or derivative, for the production of a drug for the treatment of pain-associated neuropathy, pain-associated neuropathy that is simultaneously accompanied by states of nociceptive pain, peripheral and/or predominantly peripheral neuropathic pain or central and/or predominantly central neuropathic pain.

Abstract: A particle having a rounded shape and characterized by a substantially smooth surface is disclosed. The particle can be made of a food substance (e.g., nutritional substance or nutraceutical substance), a pharmaceutical (pharmaceutically active ingredient or pharmaceutically acceptable carrier) or a cosmetic substance.

Abstract: The disclosure is directed at least in part to compositions and methods comprising nicotinic agonists for treating e.g., nervous system disorders, in particular, to combination therapies that include a nicotinic agonist (for example, nicotine) and a nicotinic acetylcholine receptor desensitization inhibitor (for example, opipramol).

Abstract: The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula I, including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula I.

Abstract: The present invention relates to novel uncoated, color-stable tablet formulations comprising oxcarbazepine, a disintegrant and iron oxide pigments. The oxcarbazepine of the present invention has a particle size of about 14 to about 30 microns with a maximum residue on a 40 micron sieve from about 10% to about 35%. The present invention further provides for a process of preparing the tablet formulations, and a method of treating mammals in need of oxcarbazepine with the novel formulation.

Abstract: The present invention relates to a process for preparing a pharmaceutical composition comprising carbamazepine that has a constant release profile.

Abstract: The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical compositions which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating central nervous system disorders, obesity, and metabolic disorders.

Abstract: The present invention relates to a pharmaceutical composition comprising gaboxadol or a pharmaceutically acceptable salt thereof and one or more inhibitors of PAT1 and/or one or more inhibitors of OAT. The present invention further relates to a pharmaceutical composition comprising from about 0.5 mg to about 50 mg gaboxadol or a pharmaceutically acceptable salt thereof, wherein the composition provides an in vivo plasma profile comprising a mean Tmax which is longer than about 20 minutes.

Abstract: This invention relates to a spray for sublingual administration, used in the treatment and management of pain, especially acute pain. Also provided are methods of treatment and management of pain, a metered dosage system for administration of the spray, and combination therapies.

Abstract: Novel compositions and methods which utilize an erection-enhancing agent and an ejaculation-delaying agent, such that these agents provide an overlapping and/or synergistic effect, are provided. These composition and methods can be beneficially utilized for treating sexual dysfunction and/or for enhancing sexual function.

Abstract: Disclosed in certain embodiments is a method for relieving pain at a site in a human or animal in need thereof, comprising administering by injection or infiltration, a dose of a capsaicinoid and coadministering a tricyclic antidepressant.

Abstract: A pharmaceutical composition comprising licarbazepine acetate, especially eslicarbazepine acetate, in combination with suitable excipients, in particular a binder, and a disintegrant. Also disclosed is a granulation process, especially a wet granulation process, for making the pharmaceutical composition.

Abstract: To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.

Abstract: Methods for the prevention or treatment of stress-related disorders by administering a therapeutically effective amount of a dual serotonin/norepinephrine reuptake inhibitor to an individual under stress are described. A triple monoamine reuptake inhibitor for serotonin/noradrenaline/dopamine may also be administered to an individual at risk for a stress-related disorder. In a preferred embodiment the compound is milnacipran and is prophylactically administered at an effective amount to delay or prevent stress-related disorders in an individual at risk.

Abstract: Novel modified release pharmaceutical composition comprising at least one active agent(s); a polymer system in an amount less than about 80% w/w of the composition comprising at least two swellable pH independent polymers wherein at least one is hydrophilic; optionally other pharmaceutically acceptable excipients is provided. Process for preparation of such compositions and methods of using them is also provided. The compositions are formulated into suitable dosage forms that provide therapeutic concentrations of active agent for extended periods of time.

Abstract: Pharmaceutical sustained release composition comprising at least one active agent(s), or its tautomeric forms, analogues, isomers, polymorphs, solvates, or salts thereof; preferably an antiviral active agent is provided. Also provided is a process of preparation of such composition and method of using them. The sustained release compositions of the present invention are able to deliver the active agent in a desired manner for an extended period of time.

Abstract: This invention is directed to a tetrahydro-indazole cannabinoid modulator compound of formula I: and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.

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

Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.

Abstract: The present invention relates to new pharmaceutical formulations comprising pharmaceutically active agents which can induce one or more involuntary coughs in a patient when administered as conventional formulations and/or via conventional routes. Formulations are provided comprising a cough-inducing pharmaceutically active agent, wherein the formulation may be administered by pulmonary inhalation without inducing a cough. Alternatively, formulations are provided for administering the cough-inducing active agent via an alternative route.

Abstract: The present invention relates to the use of a mixture of the enantiomers of a compound of Formula (I) or of pharmaceutically acceptable salts of said enantiomers consisting of at least 55% of the R-enantiomer, most preferably of at least 98% of the R-enantiomer, and not more than 45 % of the S-enantiomer, most preferably not more than 2% of the S-enantiomer, for the manufacture of a pharmaceutical composition for the treatment of neuropathic pain; to a method for the treatment of neuropathic pain; and to a pharmaceutical composition comprising as active agent a mixture of the enantiomers of the compound of formula I or pharmaceutically acceptable salts of said enantiomers consisting of at least 55% of the R-enantiomer and not more than 45% of the S-enantiomer.

Abstract: The present invention relates to methods of promoting wakefulness in an individual by administering a carbamoyl ester or a pharmaceutically acceptable salt thereof.

Abstract: Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the ?4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which ?4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

Abstract: This invention is directed to a cannabinoid modulator compound of formula (I): or a form thereof, and methods for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.

Abstract: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuropsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

Abstract: The present invention provides a prophylactic or therapeutic agent for depression or anxiety disorders, comprising (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide.

Abstract: There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless leg syndrome (RLS) or periodic leg movement in sleep (PLMS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS, dystonia, RLS or PLMS.

Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one nitric oxide enhancing group, 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 cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.

Abstract: The invention features methods, compositions, and kits for the treatment of pain or pruritus in a patient. In one embodiment, the methods, compositions, and kits of the invention provide for a combination therapy including a tricyclic compound and a tetra-substituted pyrimidopyrimidine.

Abstract: Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.

Abstract: The amount of penetration into the skin in adhesive patches generally tends to show a certain peak and trough. An adhesive patch is provided in which the drug shows satisfactory penetrability because of a polymer proportion and drug penetration is constant over a certain period. The adhesive patch for external use has a pressure-sensitive adhesive layer containing a drug. It is characterized in that the pressure-sensitive adhesive layer comprises: polyvinylpyrrolidone and/or a copolymer of monomers including vinylpyrrolidone as the main ingredient; and a (meth)acrylic ester copolymer having a basic nitrogen atom and/or cationic nitrogen atom.

Abstract: Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.