Abstract: This invention discloses that memantine (MMT) protects dopamine (DA) neurons damage through its potent anti-inflammatory effect by inhibiting microglial over-activation and the protection on DA neuron is a dose-dependent response. This invention also discloses that NADPH oxidase plays a critical role of neuroprotection of MMT and MMT therapy for neurodegeneration diseases acts in part through an alternative novel mechanism by reducing microglia-associated inflammation. In addition, this invention reveals that MMT is neurotrophic to DA neurons through the release of neurotrophic factors from astroglia.

Abstract: This invention relates to Applicant's discovery that Metabolic Syndrome, a cluster of disorders stemming from a resistance to insulin, contributes directly to dementia, particularly Alzheimer's disease. Applicant's invention includes a screening method to determine susceptibility and diagnosis of dementia based on the risk factors for Metabolic Syndrome. Applicant's invention further includes methods for the prevention or treatment of dementia and other neurological conditions based on (1) minimizing insulin resistance, thereby preventing excess biosynthesis of insulin; (2) modulating the activity of IDE such that insulin competes less efficiently with ?-amyloid protein for the IDE; and (3) blocking the consequences of NMDA receptor activation, such as by minimizing the generation of NO and other harmful free radicals.

Abstract: A method for treating autism comprising the step of administering an effective amount of a medicament characterized as a NMDA-receptor antagonist or a pharmaceutically acceptable salt thereof.

Abstract: Methods and uses of RNAi-inducing agents for medicaments and treating or preventing a viral infection.

Abstract: Functional polymer compositions and methods of forming such compositions are provided. The functional polymer compositions include at least 50 wt % of one or more polymer components; from 0.1 to 50 wt % of one or more fluids; and from 1 to 50 wt % of one or more active substrates. The combination of one or more fluids and one or more active substrates provides an article from such polymer composition with one or more special functional effects selected from moisturizing, anti-bacterial, disinfecting, anti-viral, anti-mildew, anti-mold, anti-fungal, anti-microbial, moisture/odor absorbing, fragrancing, insect repelling, anti-static and combinations thereof. The one or more fluids and one or more active substrates are released to the surface of polymer based articles. The functional polymer compositions are suitable for a wide range of end use applications including woven and non-woven fabrics.

Abstract: An object of the present invention is to provide, for the case of implementing a therapeutic method in which at least two kinds of anti-dementia drugs are used together, a composition that has a good therapeutic effect on dementia, and also gives excellent compliance. Another object of the present invention is to provide a composition containing at least two kinds of anti-dementia drugs, in which release of the anti-dementia drugs from the composition is controlled, whereby a combined effect of the anti-dementia drugs can be achieved well. Still another object of the present invention is to provide a composition for which the frequency of administration and the amount taken are reduced and hence compliance can be improved, and a method of manufacturing such a composition.

Abstract: Aminocyclohexane and aminoalkylcyclohexane compounds, which are systemically-active as NMDA receptor antagonists, are effective in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau, method of treating disorders resulting from or associated with abnormal hyperphosphorylation of microtubule associated protein tau, and pharmaceutical compositions comprising the same.

Abstract: This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.

Abstract: A method for treating autism comprising the step of administering an effective amount of a medicament characterized as a NMDA-receptor antagonist or a pharmaceutically acceptable salt thereof.

Abstract: A composition and its use for local percutaneous delivery of a drug, in particular a muscle relaxant, more particularly cyclobenzaprine present in an amount of about 1 to about 10% by weight of the composition in an organogel cream are disclosed. The composition is applied directly to the skin over accessible muscles of mastication from which it is rapidly absorbed through the skin to provide control of conditions such as bruxism and tooth clenching. The composition can also be applied to the skin overlying these muscles to control muscle hyperactivity (spasm) and/or trigger points, from other causes. The composition can be formulated to include another active agent such as a non-steroidal anti-inflammatory, for example ketoprofen.

Abstract: The present invention provides novel methods and compositions for the treatment and prevention of demyelinating conditions. One demyelinating condition treated by the methods and compositions of the invention is multiple sclerosis. Also treated are symptoms associated with multiple sclerosis.

Abstract: The present invention describes 1-aminoadamantane derivatives and 3-aminoadamantane-1-carboxylic derivatives in which the 5- or 7-position of the basic adamantane structure can be optionally substituted, methods for the production of the compounds based on the present invention, and methods for the coupling of the monomeric 3-aminoadamantane-1-carboxylic derivatives thus obtained to oligomers. The compounds based on the present invention are suitable for the utilisation as antiviral active ingredients, artificial ion channels, as well as for the therapy, diagnostics and prophylaxis of diseases in which a dysfunction of the GABA system occurs.

Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.

Abstract: A titration package and method for enabling compliance with a regime of changing dosage of medication over a period of time includes a backing having an array of receivers with the array including a plurality of columns and a plurality of rows. A plurality of sets of tablets are provided with each tablet in set having a common dose of medication and a different dose than a tablet of a different set. Each set of tablets is disposed in receivers of one having an adjacent row and an adjacent column. Indicia is provided and disposed adjacent to the columns and rows for displaying common days and successive weeks.

Abstract: A composition for influenza treatment includes an immune enhancer and an anti-viral agent

Abstract: Biocompatible intraocular implants include an anti-excitotoxic agent and a biodegradable polymer that is effective to facilitate release of the anti-excitotoxic agent into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy.

Abstract: The present invention provides for the use of an NMDA receptor antagonist, preferably memantine or neramexane or a pharmaceutical acceptable salt or a prodrug of said antagonists, in the preparation of a pharmaceutical composition for the prevention, amelioration and/or treatment of disorders of metabolism influencing body weight, in particular obesity, an eating disorder and/or in the regulation of appetite. Furthermore, the present invention provides for a method for the prevention, amelioration and/or treatment of disorders of metabolism influencing body weight, in particular obesity, an eating disorder and/or in the regulation of appetite comprising the step of administering to a subject in need thereof a therapeutically effective amount of an NMDA receptor antagonist, preferably memantine or neramexane or a pharmaceutically acceptable salt or prodrug of said antagonists.

Abstract: Biocompatible intraocular implants include an anti-excitotoxic agent and a biodegradable polymer that is effective to facilitate release of the anti-excitotoxic agent into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy.

Abstract: A method for the treatment of disturbance of visual function which comprises administering a pharmaceutically effective amount of memantine to a patient in need of treatment of said disturbance.

Abstract: A titration package and method for enabling compliance with a regime of changing dosage of medication over a period of time includes a backing having an array of receivers with the array including a plurality of columns and a plurality of rows. A plurality of sets of tablets are provided with each tablet in a set having a common dose of medication and a different dose than a tablet of a different set. Each set of tablets is disposed in receivers of one having an adjacent row and an adjacent column. Indicia is provided and disposed adjacent to the columns and rows for displaying common days and successive weeks.

Abstract: The present invention relates to pharmacological methods for the prevention or amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess glutamate-related and/or glycine-related pharmacological activity or that modulate the release of glutamate, glycine, or both from nerve terminals with the central nervous system.

Abstract: This invention relates to an oral dosage form containing between 1 mg and 100 mg of memantine, wherein said dosage form does not contain 10 mg of memantine or 20 mg of memantine, and wherein said dosage form is not prepared by the patient or a person administering the drug to the patient who divides the dosage form containing a larger dose of memantine. Other aspects of this invention relate to pharmaceutical products comprising said dosage forms and methods of administering memantine and treating disease with said dosage form.

Abstract: Pharmaceutical compositions and methods of use thereof for the acute, chronic and prophylactic treatment of neurologic and neurodegenerative diseases, attenuation of acute or chronic neuronal damage in neurological disease (“neuroprotection”), and prophylaxis of neurological diseases, where the neurological diseases may involve excessive stimulation of the NMDA receptor, hypofunction of the NMDA receptor, up- or down regulation of the NMDA receptor, and abnormal subunit structure or function of the NMDA receptor. The pharmaceutical compositions are open-channel antagonists of the NMDA (N-methyl-D-aspartate) receptor complex, and include memantine (a 1-amino-3,5-dimethyl-adamantane hydrochloride), felbamate, acamprosate, and MRZ 2/579. The invention relates to oral, controlled or sustained release, intravenous, rectal, transcutaneous or other preparations such as lipid emulsion or crystal technology.

Abstract: The invention relates to the use of substances for the manufacturing of a pharmaceutical composition or medicament for the treatment of disturbances or illnesses which are linked to malfunction of an ionotropic acetylcholine receptor and/or a calcium-activated potassium channel functionally associated with said acetylcholine receptor, wherein said substance is at least one adamantane derivative.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: A method for treating a microbial infection or disease in a subject, said method comprising administering to said subject an effective amount of a compound according to the formula (1). Wherein; denotes a single or double bond or an epoxidised bond, and A1 to A13 are independently selected from moieties as depicted in the description. Also claimed are methods for disinfecting surfaces using the above compound, and claims to the above compound.

Abstract: The present invention relates generally to pharmacological methods for the prevention or amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess glutamate-related and/or glycine-related pharmacological activity or that modulate the release of glutamate, glycine, or both from nerve terminals with the central nervous system.

Abstract: The use of a compound of formula (I): wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s) of the substituent groups R1 to R6 may together form a 3, 4, 5, 6, 7 or 8-membered ring containing 0, 1 or 2 heteroatom(s); R7 is selected from alkyl, aryl and non-aromatic heterocyclic groups, and R8 is selected from hydrogen, halogen, alkyl, aryl and non-aromatic heterocyclic groups; and pharmaceutically acceptable salts and prodrugs thereof, in the manufacture of a medicament for use in the treatment of a condition generally associated with abnormalities in glutamatergic transmission; novel compounds of formula (1) per se and for use in therapy.

Abstract: This invention relates to the use of a composition for local percutaneous delivery of a drug such as a muscle relaxant, more particularly cyclobenzaprine in an organogel cream. The composition is applied by the patient directly to the skin over accessible muscles of mastication i.e., masseter and temporalis. The composition is rapidly absorbed through the skin to provide control of harmful habits such as bruxism and tooth clenching. The composition can also be applied to the skin overlying these muscles to control muscle hyperactivity (spasm) and/or trigger points, from other causes. The composition can be formulated to include another active agent such as a non-steroidal anti-inflammatory, for example ketoprofen.

Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.

Abstract: The invention provides conjugates of fatty acids and antiviral agents useful in treating liver disorders.

Abstract: Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-&agr; modulators, and thus are useful in the treatment of various diseases.

Abstract: The use of a compound of formula (1), as disclosed in the specification, wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl and aryl, or pharmaceutically acceptable salts thereof, with the proviso that wherein R1 to R4 and R6 are hydrogen, R5 is not selected from CH2CH2NHSO2CH3, CH2CH2NHSO2CF3 and methyl substituted by SO2NH2, SO3H, PO3H2, CONHOH or a heterocyclic group selected from formulae (a), (b), (c), (d) and (e) in the manufacture of a medicament for use in the treatment of a condition generally associated with abnormalities in glutamatergic transmission.

Abstract: A method and composition for treating patients with viral infection with pharmaceutical agents is disclosed. In one embodiment, the virus is influenza A and the pharmaceutical agent is rimantadine or amantadine. The methods of the present invention can be used as a way of eradicating influenza virus topically by direct administration of a dose—nasally—that is much lower than an oral therapeutic dose. Thereby avoiding the side effects associated with oral administration.

Abstract: The present invention provides a method for treating chronic hepatitis C infections in patients in need of such treatment comprising administering an amount of IFN-&agr; in association with an amount of amantadine effective to treat hepatitis C. In accordance with the invention, IFN-&agr; and amantadine are administered at the same time or sequentially. The present invention also provides a kit for treating a hepatitis C infection containing IFN-&agr; and amantadine in suitable dosage forms for administering the combination therapy.

Abstract: The present invention relates to the delivery of compounds for the treatment of Parkinsons through an inhalation route. Specifically, it relates to aerosols containing antiparkinsonian drugs that are used in inhalation therapy. In a composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of an antiparkinsonian drug. In a method aspect of the present invention, an antiparkinsonian drug is delivered to a mammal through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises at least 5 percent by weight of an antiparkinsonian drug to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles, which is inhaled by the mammal.

Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.

Abstract: The invention concerns the use of 1-adamantane amines (amantadines) or structurally similar compounds for combating borna disease virus infections and for treating affective diseases and disorders associated with borna disease virus infections in humans and animals. The use of these substrates results in rapid and lasting elimination of the symptoms and signs and in the suppression of the virus activity.

Abstract: A combination of two drugs, from two different and previously unrelated categories, provides effective and long-lasting relief from neuropathic pain. Both drugs can be taken orally, in a convenient, painless, non-invasive manner that does not require injections. One drug in this combination is an &agr;2 adrenergic agonist, exemplified by clonidine. The other drug in the combination is an adamantane derivative which has NMDA antagonist activity, such as memantine. Tests described herein demonstrate that when memantine is administered together with an &agr;2 adrenergic agonist such as clonidine, these drugs mutually potentiate one another's neuropathic pain-relieving action, and provide potent and sustained neuropathic pain relief, even when each agent is administered at a low dosage that is below its threshold for causing adverse side effects.

Abstract: The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer composition to a mammal, such as a human, whereby bile acids are sequestered. The polymers of the invention comprise spirobicyclic ammonium moieties and optionally, further comprise a hydrophobic substituent, a quaternary ammonium-containing substituent or a combination thereof.

Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.

Abstract: Use of adamantane derivatives of the formula ##STR1## in which R1 and R2 are identical or different and can be hydrogen or straight-chained or branched alkyl groups having 1 to 6 carbon atoms, ortogether with the nitrogen atom can represent a heterocyclic group having 5 or 6 ring atoms,in which R3 and R4 are identical or different and can be hydrogen, straight-chained or branched alkyl groups having between 1 and 6 carbon atoms, cycloalkyl groups having 5 or 6 carbon atoms or a phenyl group, and in which R5 is hydrogen or a straight-chained or branched alkyl group having between 1 and 6 carbon atoms for treating diseases of the inner ear.

Abstract: Stimulating non-amyloidogenic processing by the activation of cell surface serotonin receptors linked to phospholipase and protein kinase C is described. Activation of the cell surface serotonin receptors is accomplished by contacting the cell with an agent which is a serotonin agonist or which increases the intrasynaptic concentration of serotonin. Also described is the activation of cell surface serotonin receptors by dexnorfenfluramine. Agents which cause the activation of cell surface serotonin receptors can be administered to an individual to stimulate non-amyloidogenic processing in the brain of the individual, thereby inhibiting the deposition of amyloid in the brain of the individual.

Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the diterpene- and benzolactam-classes.

Abstract: The migraine-treating effectiveness of a local anesthetic drug is significantly enhanced by coadministering dextromethorphan or dextrorphan.

Abstract: The migraine-treating effectiveness of an antimigraine drug is significantly enhanced by administering a selective 5-HT.sub.1 agonist together with dextromethorphan or dextrorphan.

Abstract: Methods and pharmaceutical compositions in unit dosage form for treating neurodegeneration in a human or non-human animal afflicted therewith wherein the active agent is a therapeutically effective amount of a polyamine having the formula: ##STR1## or a salt thereof with a pharmaceutically acceptable acid wherein: R.sub.1 and R.sub.6 may be the same or different and are hydrogen, alkyl, hydrocarbyl aryl, hydrocarbyl aryl alkyl, cycloalkyl, or any of the foregoing wherein the alkyl chain is interrupted by at least one etheric oxygen atom;N.sup.1, N.sup.2, N.sup.3 and N.sup.4 are nitrogen atoms capable of protonation at physiological pH's;a and b may be the same or different and are integers from 1 to 4;A, B and C may be the same or different and are bridging groups of variable length.

Abstract: A method for treating symptoms of patients diagnosed with tardive dyskinesia (TD) using NMDA receptor antagonists is disclosed. This invention illustrates that certain NMDA-receptor antagonists are effective pharmacologic agents in the treatment of hyperkinesia and cognitive disorders that present in patients diagnosed with TD. The disclosed agents reduce the severity and duration of involuntary movements associated with tardive dyskinesia. Certain of the disclosed agents are also effective in increasing the attention span, concentration span, memory and everyday functional performance as measured both subjectively as well as objectively as demonstrated using standard neuropsychological tests such as those assessing reaction time and short-term memory. The invention also discloses a method of treating tardive dyskinesia that acts in a neuroprotective manner to reduce or prevent glutamate-related excitotoxic damage to the basal ganglia.

Abstract: Pharmaceutical compositions having antiviral, antiinflammatory and other activities are disclosed. The compositions are of compounds derived from diterpene phorboids.

Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from diterpenes of the phorbol-, resiniferonol- and ingenol-classes.