Abstract: An optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative represented by the formula 4 is produced by a process including (a) reacting an optically active secondary amine, represented by the formula 1, with an alkylation agent R2—X, in the presence of a base, thereby converting the secondary amine into an optically active tertiary amine represented by the formula 3; and (b) subjecting the tertiary amine to a hydrogenolysis, thereby producing the N-monoalkyl derivative, 1

Abstract: A pharmaceutical formulation is provided for nasal drug administration of a topically administrable decongestant, a topically administrable corticosteroid and a pharmaceutically acceptable carrier, and may optionally include further carriers, therapeutic extenders, and the like. Such formulations may also optionally further include a therapeutically active member selected from the group consisting of a topical antibiotic, a topical antihistamine (preferably a non-sedating antihistamine), a leukotriene D4 antagonist, a 5-lipoxygenase inhibitor, and a FLAP antagonist, or a pharmaceutically acceptable salt thereof. In addition, methods for using the formulation to treat decongestant/corticosteroids-responsive conditions, diseases or disorders such as chronic obstructive nasal congestion and/or obstructive sleep apnea conditions, are provided, as are drug delivery devices and dosage forms for housing and/or dispensing the formulations.

Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF&agr;) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNF&agr; and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNF&agr; and/or one or more other involved cytokines, alone or in combination with other agents.

Abstract: A method for resolving enantiomers of a compound containing the structure of the formula: 1

Abstract: Compositions and methods for the treatment of depressive disorders through the administration of modafinil with antidepressants.

Abstract: The invention features a method for treating a patient diagnosed with, or at risk of developing, an immunoinflammatory disorder by administering an SSRI or analog or metabolite thereof and, optionally, a corticosteroid or other compound to the patient. The invention also features a pharmaceutical composition containing an SSRI or analog or metabolite thereof and a corticosteroid or other compound for the treatment or prevention of an immunoinflammatory disorder.

Abstract: Compositions and methods for the treatment of depressive disorders through the administration of modafinil with antidepressants.

Abstract: Compositions and methods for the treatment of depressive disorders through the administration of modafinil with antidepressants.

Abstract: Compositions and methods for the treatment of disorders through the administration of modafinil with M-drugs.

Abstract: The present invention provides a method of preventing or treating motion sickness by orally or topically administering a halogenated pheniramine.

Abstract: Methods and compositions are disclosed utilizing the optically pure (−)-isomer of bupropion to assist in smoking cessation, for treating smoking and nicotine addiction, and for treating pain, including, but not limited to, chronic pain, neuropathetic pain and reflex sympathetic dystrophy, and other disorders such as narcolepsy, chronic fatigue syndrome, fibromyalgia, seasonal affective disorder and premenstrual syndrome, while avoiding adverse affects associated with racemic bupropion.

Abstract: The present invention relates to novel essentially pure venlafaxine and the process of preparation thereof. The present invention also relates to novel solvate forms of venlafaxine hydrochloride and the process of preparation thereof. Furthermore, the present invention provides a novel process for preparing venlafaxine hydrochloride from venlafaxine; the process comprises the steps of: i) preparing a mixture of venlafaxine with acetone; and ii) exposing the mixture in gaseous hydrochloric acid.

Abstract: A pharmaceutical combination includes an effective amount for a day of amphetamine in base and/or salt form where the molar ratio of l-amphetamine to d-amphetamine released therefrom in a time period later in the day is higher than said ratio released therefrom in a time period earlier in the day.

Abstract: Granules of allylamine- or benzylamine-anti-mycotic or one of its pharmaceutically acceptable salts, characterized in that the granules are coated and that they contain:—microcrystals of an allylamine- or benzylamine-anti-mycotic or one of its pharmaceutically acceptable salts, —at least one binder selected from the group consisting of cellulosic polymers, such as ethylcellulose, hydroxypropylcellulose and hydroxypropylmethylcellulose, acrylic polymers, povidones, polyvinyl alcohols and mixtures thereof—optionally a diluent agent selected from the group comprising cellulosic derivatives, starches, lactose, polyols such as mannitol and/or an antistatic agent selected from the group comprising micronised or non micronised talc and/or a permeabilising agent selected from the group comprising colloidal silica and precipitated silica. Process for obtaining such granules and orodispersible tablets comprising them. Use of said orodispersible tablets.

Abstract: The present invention relates to new substituted carboxylic acid amides of general formula 1

Abstract: The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a CNS-penetrant NK-1 receptor antagonist (e.g., a substance P receptor antagonist) in combination with an antidepressant or an anxiolytic agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a CNS-penetrant NK-1 receptor antagonist and an anxiolytic agent or antidepressant.

Abstract: A pain relief lollipop comprises a candy matrix comprising (a) an opioid agonist, (b) an N-methyl-D-aspartate receptor antagonist different from the opioid agonist, and, optionally, a muscle relaxant, sedative, anxiolytic, and/or antidepressant. A patient can self-administer small amounts of the pain relief drug as needed by simply licking or sucking on the lollipop in response to his subjective experience of pain.

Abstract: Disclosed is the identification of specific molecular targets and cellular pathways involved in the mechanism of action of 2-amino-2-propane-1;3-diols.

Abstract: This invention provides: 1) a method of treating androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 2) a method of preventing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 3) a method of suppressing or inhibiting androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer; and 4) a method of reducing the risk of developing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer, by administering to the subject a pharmaceutical composition comprising an anti-estrogen agent and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof.

Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.

Abstract: Novel polyamines, their synthesis and use in pharmacological, cosmetic or agricultural applications are provided. The polyamines induce antizyme production which in turn down regulates both the production of polyamines by omithine decarboxylase (ODC) and the transport of polyamines by its corresponding polyamine transporter. These compounds will preferably enter the cell independent of the polyamine transporter. As drugs, these compounds are used to treat any disease associated with cellular proliferation including but not limited to cancer.

Abstract: The invention relates to methods of using sodium channel modulators, particularly TTX-R sodium channel modulators and/or activity dependent sodium channel modulators to treat painful and non-painful lower urinary tract disorders, particularly painful and non-painful overactive bladder with and/or without loss of urine.

Abstract: The present invention relates to the use of certain resorcinol derivatives as skin lightening agents.

Abstract: Methods for treating an individual with a psychiatric order with a pharmacologic agent that enhances learning or conditioning in combination with a session of psychotherapy are provided. These methods of the invention encompass a variety of methods of psychotherapy, and psychodynamically oriented psychotherapy, and psychiatric orders including fear and anxiety disorders, addictive disorders, addictive disorders including substance-abuse disorders, and mood disorders. The pharmacologic agents used for the methods of the present invention are ones that generally enhance learning or conditioning, including those that increase the level of norepinephrine in the brain, those that increase the level of acetylcholine in the brain, and those that enhance N-methyl-D-aspartate (NMDA) receptor transmission in the brain.

Abstract: Compositions of matter comprising sertraline and a solubilizing agent which increases the solubility of sertraline in aqueous chloride ion-containing use environments.

Abstract: Pharmaceutical compositions contain a surfactant and one or more active ingredients selected from among anti-infective agents, anti-inflammatory agents, anti-mucolytic agents, antihistamines, antiseptics, combinations of antibiotics and combinations of these agents. The compositions are formulated for aerosol administration to treat chronic sinusitis or nasal polyps.

Abstract: Octopamine salts are disclosed which have powerful metabolic enhancing effects in humans via oral administration. These salts not only have increased stability but also greatly increased bioavailability over the base form. The metabolic enhancing properties include positive blood sugar regulation, increased thermogenesis and fat loss, increased anticatabolism/anabolism, decreased appetite, improved mental focus and psychological outlook and increased energy production and anti-fatigue actions.

Abstract: Compounds useful for treating HIV are disclosed having the general formula 1

Abstract: Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.

Abstract: A pharmaceutical formulation is provided for pulmonary drug administration of a bronchodilator, a corticosteroid and an optional pharmaceutically acceptable carrier. In addition, methods for using the formulation to treat bronchodilator/corticosteroid-responsive conditions, diseases or disorders are provided, as are drug delivery devices and dosage forms for housing and/or dispensing the formulations.

Abstract: The present invention relates to the delivery of stimulants through an inhalation route. Specifically, it relates to aerosols containing stimulants that are used in inhalation therapy. In a method aspect of the present invention, a stimulant is delivered to a patient through an inhalation route. The method comprises: a) heating a coating of a stimulant, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% stimulant degradation products. In a kit aspect of the present invention, a kit for delivering a stimulant through an inhalation route is provided which comprises: a) a coating of a stimulant drug and b) a device for dispensing said coating a stimulant as a condensation aerosol.

Abstract: Pharmaceutical formulations useful for the treatment of pulmonary disorders are described. These compositions are formulated for pulmonary administration and contain a bronchodilator, a vasoconstrictor, a corticosteroid, and an optional pharmaceutically acceptable carrier. Drug delivery devices and dosage forms for housing and/or dispensing the formulations are also described.

Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R′=H or O(═) as well as pharmaceuticals c

Abstract: The present invention is directed to a pharmaceutical composition and method for the treatment of rhinitis and cold-like symptoms which includes a non-steroidal anti-inflammatory drug (NSAID), a decongestant, and an antihistamine. It has been found that an NSAID enhances the activity of a decongestant and an anti-histamine, thus permitting a reduction in either or both in administration of separate dosage forms. The same enhancement can also occur with an anti-tussitive. Thus, the effective amount of the decongestant or the antihistamine or both is less than about 75% of an amount present in an approved dose of the decongestant or the antihistamine, or both, relative to an amount of the NSAID corresponding to about 100% of the amount present in a normal strength dosage form of the NSAID.

Abstract: Disclosed are compounds of the formula: 1

Abstract: A pharmaceutical composition having a gel consistency at room temperature and suitable for the treatment of a vaginal infection comprises, on a total composition weight basis, about 0.1 to about 3 weight percent of benzydamine hydrochloride, about 16 to about 35 weight percent of a polyoxyalkylene block copolymer, and about 2 to about 30 weight percent of propylene glycol, in water having a pH value in the range of about 3.5 to about 7. The weight ratio of water to polyoxyalkylene block copolymer in the composition is less than about 4:1. Optionally, the gel compositions can also contain glycerin, physiologically tolerable preservatives and buffers, as well as other pharmaceutically acceptable excipients.

Abstract: The present invention is directed to methods that can be used in the treatment of wounds, burns, and photodamaged skin. Methods can be used for both humans and animals and involve the administration of compositions containing selegiline and/or desmethylselegiline.

Abstract: Effects of deprenyl or propargylamine compounds (MAO inhibitors) and novel compositions comprising at least one MAO inhibitor and at least one antiinflammatory agent such as nonsteroidal antiinflammatory drugs (NSAIDS), steroids, acetaminophen (COX-3 inhibitors), 5-lipoxygenase inhibitors, leukotriene receptor antagonists, leukotriene A4 hydrolase inhibitors, antihistaminics, histamine 2 receptor antagonists, phosphodiesterase-4 antagonists, cytokine antagonists, CD44 antagonists, antineoplastic agents, 3-hydroxy-3-methylglutaryl coenzyme A inhibitors (statins), estrogens, androgens, antiplatelet agents, antidepressants, Helicobacter pylori inhibitors, proton pump inhibitors, thiazolidinediones, dual-action compounds, combinations of these drugs with other agents, derivatives and metabolites of synthetic and natural antiinflammatory agents.

Abstract: This invention provides pharmaceutically active enantiomers of the venlafaxine metabolite O-Desmethyl venlafaxine, R(−)-4-[2-(Dimethylamino-i-(1-hydroxycyclo-hexyl)ethyl]phenol or R(−)1-[2-(dimethylarinno)-1-(4-hydroxyphenyl)ethyl]cyclo-hexanol, and S(+)-1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclohexanol or S(+)-4-[2-(Dimethylaamino)-1-(1-hydroxycyclohexyl)ethyl]phenol, or one or more pharmaceutically acceptable salts or salt hydrates thereof, as well as pharmaceutical compositions utilizing these enantiomers and methods of using the enantiomers to treat, inhibit or control central nervous system disorders.

Abstract: The invention relates to compounds of formula (I), to salts and stereoisomers thereof, to their production and to their use for producing medicaments used for treating cardiovascular diseases.

Abstract: The present invention provides compositions and methods for the treatment of reduced blood flow to the central nervous system in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition comprising the administration to a subject of an amphetamine in combination with a cyclooxygenase-2 selective inhibitor.

Abstract: A method of preventing or suppressing symptoms of psychosis by treating non-psychotic patients who are at risk of developing psychosis. The method includes determining whether a patient is at risk for developing psychosis; making a diagnosis that the patient is at risk; and administering to the patient a selective D3 antagonist prior to the time the patient is psychotic in an amount sufficient to prevent or suppress symptoms of psychosis.

Abstract: The invention provides improved formulations and methods for the treatment of neurological disorders.

Abstract: The invention provides a solid composition comprising fluoxetine, exhibiting a dissolution profile, as determined in a basket at 100 rpm and a buffer pH 7.5, such that after 15 minutes, from 30 to 70% of the fluoxetine is released, after 30 minutes, from 70 to 98% of the fluoxetine is released, after 45 minutes, more than 90% of the fluoxetine is released.

Abstract: The present invention concerns a tablet comprising two distinct segments. More particularly the invention relates to combinations of two pharmaceutical substances and methods of treatment of allergic disorders.

Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Abstract: The invention relates to substituted 1-aryl-but-3-enylamine and 1-aryl-but-2-enylamine compounds, to a method for the production thereof, to medicaments containing said compounds and to their use in the production of medicaments.

Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: A gelled composition formulated to maintain an active ingredient in association with the nasal membrane for an extended period of time is provided. The gelled composition may be formulated as a decongestant or a sinus discomfort relieving agent. The invention further includes a system and method for applying the gelled composition to the nasal membrane.

Abstract: Invented is paroxetine hydrochloride anhydrate in Form B and paroxetine hydrochloride anhydrate in Form D. Also invented are pharmacetucal formulations comprising these compounds and methods of using these compounds in therapy.