Abstract: Disclosed herein is an antioxidant that is an alkylated iminodibenzyl of the general formula: 1

Abstract: The present invention relates to dosage forms of oxcarbazepine for oral administration and to the process for the preparation of such dosage forms.

Abstract: The invention relates to a combination which comprises a P-glycoprotein (P-gp) inhibitor and an antiepileptic drug selected from phenyloin (5,5-diphenyl-2,4-imidazolidinedione), carbamazepine, lamotrigine, gabapentin, oxcarbazepin, valproic acid, and topiramate, and its use for the prevention, delay of progression or treatment of diseases, in particular epilepsy, especially epilepsy which is resistant to antiepileptic drugs.

Abstract: The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating pain etc.

Abstract: Dosage forms and methods for providing a modulated release of cyclobenzaprine are provided. The sustained release dosage forms provide therapeutically effective average steady-state plasma cyclobenzaprine concentrations when administered once per day. The composition of the delay layer and the composition of the drug layer are characterized by the viscosity of the hydrated delay layer remaining higher than the viscosity of the hydrated drug layer during operation in one embodiment. The result is greater uniformity in the release rate from the core providing a more optimal ascending release rate. In other embodiments, the hydrated delay layer has a viscosity that is lower than the viscosity of the hydrated drug layer as well as a hydrated delay layer that is substantially similar to the hydrated drug layer.

Abstract: An efficient and high-yielding method for the preparation of optically pure (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide and (R)-(−)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide by resolution of racemic (±)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide using a tartaric acid anhydride.

Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.

Abstract: Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.

Abstract: The present invention relates to pharmaceutical compositions, in particular oral ions, with therapeutically active content of oxcarbazepine, which have a sustained of the active ingredient. The compositions have a characteristic in vitro release profile.

Abstract: Piperidine derivatives of formula (I) as disclosed in the specification have interesting pharmaceutical properties e.g. as CCR5 inhibitors.

Abstract: The invention features a method for treating a patient having a cancer or other neoplasm by administering to the patient two compounds simultaneously or within 14 days of each other in amounts sufficient to treat the patient.

Abstract: Disclosed is a method for treating pulmonary hypertension using a vasopressin antagonist.

Abstract: Stable tablets comprising benazepril hydrochloride are prepared by employing zinc stearate as the lubricant.

Abstract: Base on the anatomy and neurophysiology described in the Neurophysiologic Basis of Idiopathic Diseases, the categories of oral and parenteral medications can be used to manage and treat fibromyalgia and related diseases, disorders, syndromes and sequelae in a human. The target neurons involve in the genesis and perpetuation of fibromyalgia and related syndromes, diseases and disorders and sequelae in the peripheral nervous system and central nervous system are affected and modulated by the anticonvulsants, antidepressants and opioids.

Abstract: The invention relates to new drug combinations based on sodium channel blockers 1 and magnesium salts 2, processes for the preparation thereof as well as the use thereof for preparing pharmaceutical compositions for the treatment of ischaemic conditions.

Abstract: Methods of treating, preventing, modifying and managing various types of pain are disclosed. Specific methods comprise the administration of a selective cytokine inhibitory drug, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent and/or surgery, psychological or physical therapy. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: Treatment of pain syndromes utilizes a topical polypharmaceutical preparation of phenoxybenzamine, ketamine, gabapentin, nifedipine, carbamazepine, or combinations of them. Other suitable components are blockers of sympathetic alpha 1, 2 and other receptors, NMDA receptor blockers, GABA receptor blockers, AMPA receptor blockers, nitric oxide synthase receptor blockers, calcium channel blockers, ACDP receptor blockers, prostaglandin and leukotriene blockers, substance P blockers, bradykinin and neurotenin as well as other peptide blockers, and TNF alpha blockers. Recommended delivery is by locating a predetermined neurodermal point and locating a gel patch over the predetermined neurodermal point. Iontophoresis then delivers the pharmaceutical agent from the gel patch.

Abstract: Methods of treating or preventing chronic pain or convulsion are disclosed by administering to an animal a sodium channel blocker and at least one of gabapentin and pregabalin. Also disclosed are pharmaceutical compositions and kits for the treatment or prevention of chronic pain or convulsion.

Abstract: Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9-11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.

Abstract: A novel method of vehicle modulated administration of an anticonvulsive agent to the mucous membranes of humans and animals is disclosed. The vehicle system is an aqueous pharmaceutical carrier comprising an aliphatic alcohol (10-80%) or a glycol (10-80%), and their combinations with a biological surfactant such as a bile salt or a lecithin. The pharmaceutical composition provides a means to control and promote the rate and extent of transmucosal permeation and absorption of the medicaments via a single and multiple administration. Nasal administration of the pharmaceutical preparation produces a high plasma concentration of the anticonvulsant nearly as fast as intravenous administration.

Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Abstract: The present invention provides a controlled release device for sustained or pulsatile delivery of pharmaceutically active substances for a predetermined period of time. This invention further provides such device in which sustained or pulsatile delivery is obtained by the unique blend and Inmate mixture of pharmaceutically active substances with a microbial polysaccharide and uncrosslinked linear polymer and optionally a crosslinked polymer and/or lipophillic polymer and/or saturated polyglycolyzed glyceride. The invention also provides a process for the manufacture of such devices and pharmaceutical compositions containing the same.

Abstract: The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

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: The present invention provides a compound of the formula (I) and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. In said formula, X=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Y=O, (CH2)m, S, SO, SO2, NH, NR8; Z=NH, O, NR8, S, SO, SO2. The remaining substituents are described in the specification.

Abstract: Provided are microparticles of active pharmaceutical ingredients, drug delivery vehicles comprising same, and methods for making them.

Abstract: The present invention provides an osmotic device containing controlled release venlafaxine in the core in combination with an anti-psychotic agent in a rapid release external coat. A wide range of anti-psychotic agents can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray-coated rather compression-coated onto the device. The device with spray-coated external core is smaller and easier to swallow than the similar device having a compression-coated external coat. The device is useful for the treatment of depression, anxiety or psychosis related disorders.

Abstract: Purified soy phosphatidylserine is used to make cochleates. The cochleates contain at least about 75% soy phosphatidylserine and optionally a bioactive load. A preferred cochleate contains the antifungal agent amphotericin B.

Abstract: The present invention relates to a method for releasing an active substance from a composition. The active substance is either substantially water-insoluble and/or immobilised on or in nanosized particles. A diffusion gradient is established between the inside and the outside of the composition, which allows the transport of a nanosuspension of the active substance through the pores of the membrane.

Abstract: A method of preventing or treating diabetic retinopathy is disclosed including administering to a mammal a therapeutically effective amount of an inhibitor of retinal pericyte apoptosis. Also disclosed is a pharmaceutical composition which treats and/or prevents diabetic retinopathy comprising as an active agent a therapeutically effective amount of at least one inhibitor of retinal pericyte apoptosis and a pharmaceutically acceptable carrier.

Abstract: NMDA receptor antagonists, especially mirtazapine, can be used to treat tension-type headaches.

Abstract: The present invention provides a method of treating a visceral pain syndromes in a mammal. The method includes administering to the mammal an effective amount of a selective norepinephrine (NE)-serotonin (5-HT) reuptake inhibitor (NSRI), e.g., milnacipran.

Abstract: The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Abstract: The invention relates to formulations, e.g. film-coated tablets containing oxcarbazepine and to processes for the production of said formulations. The film-coated tablets have a tablet core comprising a therapeutically effective dose of oxacarbazepine being in a finely ground form having a mean particle size of from 4 to 12 &mgr;m (median value), and a hydrophilic permeable outer coating.

Abstract: The present invention relates to a controlled release pharmaceutical composition comprising amounts ranging from about 0.1 to about 4.5% w/w, of one or more of rate controlling cellulosic ether polymers.

Abstract: The oral controlled drug delivery system of the present invention comprises carbamazepine and one or more hydrophobic polymers in homogenous admixture, wherein the system does not comprise any means capable of preventing the conversion of carbamazepine to its dihydrate form. The present invention provides an oral controlled drug delivery system for carbamazepine having a desirable controlled rate of delivery of carbamazepine, which system is simple, uncomplicated and easy to manufacture.

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: The invention features a method for treating a patient having a cancer or other neoplasm by administering to the patient two compounds simultaneously or within 14 days of each other in amounts sufficient to treat the patient.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.

Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject comprising administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and a greater inhibition of norepinephrine reuptake than serotonin reuptake, and wherein said compound is not administered adjunctively with phenylalanine or tyrosine. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Abstract: Erodible, gastric-retentive dosage forms are provided that are formulated using the in vitro drug release profile obtained with USP Disintegration test equipment rather the USP Dissolution Apparatus. The invention is premised on the discovery that the USP Disintegration Test and modified versions thereof are far more predictive of the in vivo release profile for a controlled release dosage form than is the standard USP Dissolution Test, particularly controlled release dosage forms of the swellable, erodible type. The dosage forms generally comprise particles of a biocompatible, hydrophilic polymer having the active agent incorporated therein, wherein the particles are optionally but preferably compacted into a tablet or loaded into a capsule. The dosage forms can be used to deliver water-insoluble or sparingly soluble drugs as well as water-soluble drugs, providing that the latter are coated with a protective coating or contained in a protective vesicle.

Abstract: The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of the Ca2+-activated potassium channel (Gardos channel) of erythrocytes. The compounds can be used as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation.

Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Abstract: A process for the preparation of 10-methoxycarbamazepine, an important intermediate in the preparation of 10-oxo-10, 11-dihydro-5H-dibenz(b,f)azepine-5-carboxamide(oxcarbazepine) from 10-methoxy-5H-dibenz(b,f)azepine(10-methoxyiminostilbene), is disclosed, which process comprises reacting 10-methoxyiminostilbene with cyanic acid (HOCN) in the presence of a mild acidic reagent in a solvent. Also disclosed is an improved method for the hydrolysis of 10-methoxycarbamazepine to oxcarbazepine, which method comprises carrying out the hydrolysis in a biphasic system chosen such that the oxcarbazepine is substantially insoluble in both phases, whereas the by-products or impurities are soluble in at least one of the phases. The oxcarbazepine thereby prepared is an anticonvulsant, and has been proposed for use as an anti-epileptical agent in the treatment of AIDS-related neural disorders, and for the treatment of Parkinson's disease and/or Parkinsonian syndromes.

Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, A, R1, R2, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.

Abstract: Method for treating multiple sclerosis or encephalomyelitis by administering to a patient a combination of a tricyclic antidepressant drug and tyrosine or phenylalanine or both.

Abstract: Methods and compositions of antidepressants and analogs thereof for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and chronic pain, particularly useful for treating a localized pain.

Abstract: Topical compositions and methods for treating pain. The invention provides oil-in-water emulsions comprising an antidepressant; an NMDA-receptor antagonists; a lipophilic component; water; and a surfactant. The compositions induce a local-anesthetic effect when topically administered to intact skin thereby treating or preventing pain, for example, neuropathic pain.

Abstract: The invention features a method for treating a patient having an inflammatory disorder, by administering to the patient (i) a tricyclic antidepressant (e.g., amoxapine); and (ii) a corticosteroid (e.g., prednisolone) simultaneously or within 14 days of each other in amounts sufficient to reduce or inhibit inflammation.

Abstract: The present invention pertains to methods for reducing the platelet activation state in an individual comprising administering a selective serotonin reuptake inhibitor (SSRI). The platelet activation state is reduced upon administering a SSRI, as measured by one or more platelet activation markers. The invention also relates to methods for treating or preventing an individual at risk for a vascular event, disease or disorder by administering a SSRI.