Abstract: Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.

Abstract: Disclosed are methods and compositions for treating gliomas that involve quinacrine and other acridine analogs. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Urethral suppositories containing a mixed-activity anti-cholinergic drug and methods of use for treatment of over-active bladder are provided. Buffering drugs to pH near their pKas can result in a desired proportion of uncharged drug and can enhance absorption of the agents into urethral tissues.

Abstract: The present invention provides RecA inhibitors, compositions containing them, systems for identifying or characterizing them, and methods of using them.

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds 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: Disclosed is a percutaneous absorption preparation which enables the stable administration of an antidementia drug over a long period of time. More particularly, the percutaneous absorption preparation of the antidementia drug which is used as a plaster on skin comprises at least an adherent layer, an intermediate membrane, and a drug reservoir layer sequentially from the side which is plastered on skin, wherein the drug reservoir layer comprises at least an antidementia drug, an aminated polymer, a polyhydric alcohol, and one or more carboxylic acid esters, the intermediate membrane enables the controlled permeation of the antidementia drug into the side of skin, the adherent layer enables the plastering of the percutaneous absorption preparation on skin, and is permeable to the antidementia drug.

Abstract: The present invention provides novel methods and compositions for the treatment and prevention of CNS-related conditions. One of the CNS-related conditions treated by the methods and compositions of the invention is Alzheimer's disease.

Abstract: The present invention relates to novel uses for a family of small molecules, Differentiation-Inducing Factors (DIFs). It has been discovered that DIFs surprisingly can alter the metabolic processing of amyloid precursor protein (APP) and in turn reduce the level of secreted A?. The metabolic processing of other ?-secretase substrates normally present in cells (Notch and APLP1) is not affected when treated with DIF. The invention provides methods for reducing A? production in mammalian cells that express APP by administering DIF-I, DIF-2, DIF-3, a functionally equivalent analog and or any combination thereof. The invention also provides methods for treating and/or preventing Alzheimer's disease by preferentially reducing A? production.

Abstract: Methods for treating and preventing mucositis, in particular mucositis following the administration of chemotherapy drugs or a combination of said drugs with radiotherapy, are disclosed herein. More specifically, disclosed herein is the administration of a therapeutically effective amount of at least one of an anthocyanoside, a proanthocyanidin, or an extract containing at least one of an anthocyanoside or a proanthocyanidin for the treatment or prevention of mucositis. The therapeutically effective amount of the anthocyanoside, proanthocyanidin or extract can be administered alone or in combination with a therapeutically effective amount of at least one of an anti-inflammatory agent, immunomodulating agent, analgesic, antimicrobial agent or antifungal agent. Also disclosed herein are pharmaceutical compositions for treating and preventing mucositis.

Abstract: The invention relates to the substituted 1,2-ethylenediamines of general formula (I), wherein the groups R1 to R13, A, B, L and i are defined as in the description and the claims. The invention also relates to the use thereof in the treatment of Alzheimer's disease (AD) and similar diseases.

Abstract: Novel fused ring dicationic anti-protozoan compounds. Representative protozoan species include but are not limited to Trypanosoma brucei rhodesiense (T.b.r.) and Plasmodium falciparum. Prodrugs of these compounds can be used as an oral treatment for malaria and human African trypanosomiasis.

Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease.

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds 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: This invention relates generally to the analytical testing of tissue samples in vitro, and more particularly to aspects of genetic polymorphisms associated with the conversion from Mile Cognitive Impairment to dementia, e.g., Alzheimer's Disease (AD). The invention provides AD-associated mutations which are useful in the diagnosis, prognosis or therapeutic treatment of dementia, e.g., Alzheimer's Disease.

Abstract: This invention relates to novel pharmaceutical compositions comprising therapeutically effective combination of a positive allosteric modulator of nicotine receptors; and a cognitive enhancer selected from the group consisting of a nicotine acetylcholine receptor agonist, an acetylcholine esterase inhibitor, a positive AMPA receptor modulator, an antipsychotic drug, an antidepressant drug and an anti Parkinson drug. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating cognitive disorders.

Abstract: The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.

Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin and/or other active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.

Abstract: The present invention relates to a solid pharmaceutical composition comprising memantine, which dissolves or disintegrates in the oral cavity preferably within about 60 seconds. The present invention further discloses orally disintegrating tablets of taste-masked memantine of optimal mechanical strength comprising memantine along with a taste-masking agent and pharmaceutically acceptable excipients.

Abstract: This invention concerns adamantanamines (e.g. memantine, amantadine, and rimantadine) and neramexane salts of thiomolybdic and thiotungstic acids, including their preparation and pharmaceutical compositions, as dual acting drugs. These salts are used to treat or potentially arrest the neurodegenerative pathophysiology, clinical signs and symptoms of dementia of the Alzheimer's type, Parkinson's, Huntington's, AIDS-related dementia and Schizophrenia and its cognitive deficits. Additional uses of these derivatives include antiviral activity.

Abstract: The invention relates to a pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety, or a tautomer, a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof (1), and at least one acetylcholinesterase inhibitor or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof (2), and a pharmaceutically acceptable carrier or excipient, and optionally one or more other therapeutic ingredients.

Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.

Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.

Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.

Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.

Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.

Abstract: A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.

Abstract: Described are compounds having a thiazolhydrazide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said thiazolhydrazide compounds can be used for prophylaxis and/or treatment of neurodegenerative diseases and conditions.

Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.

Abstract: The invention relates to salts of 1-alkylamino-1-deoxypolyols and 9-oxoacridine-10-acetic acid of the general formula (I): wherein A+ is (II) wherein R is selected from the group consisting of ethyl, propyl, butyl, medicinal preparations comprising as an active ingredient salts of formula (I) and/or a mixture of said salt of formula (I) or 9-oxoacridine-10-acetic acid of the formula: and one or more 1-alkylamino-1-deoxypolyols of the general formula (II): wherein: R is selected from the group consisting of ethyl, propyl, butyl.

Abstract: The present invention relates to new indanone inhibitors of acetylcholinesterase, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.

Abstract: A method and formulation for the delivery of an active substance to the skin (epidermis, including the stratum corneum and viable epidermis, and dermis) of a subject. The formulation comprises oil-based or aqueous droplets comprising the active substance within a coating of nanoparticles, particularly silica nanoparticles. The active substance may be suitable for the treatment of a disease or condition which is localised, or at least partially localised, to the skin (eg skin cancer, psoriasis, eczema, infections including bacterial and fungal infections, acne, dermatitis, inflammation, and rheumatoid arthritis).

Abstract: The invention provides novel compounds of formula I: that are opioid receptor ligands. The invention also provides pharmaceutical compositions comprising such compounds as well as methods for treating diseases associated with opioid receptor function by administering such compounds to a mammal in need of treatment. The invention also provides an improved method for isolating intermediate materials useful for obtaining compounds of formula I.

Abstract: The invention provides methods for treating, preventing, and delaying the onset of dementia and mild cognitive impairments by administering to a patient in need thereof at least one cinnamide compound and one or more second-line active ingredients, such as cholinesterase inhibitors; AMPA receptor antagonists; NMDA receptor antagonists; and the like. The invention also provides pharmaceutical compositions, combinations, and kits.

Abstract: Compositions and methods for modulating an NF-?B-mediated immune response are provided.

Abstract: The present invention provides novel methods of combination therapy of ovarian cancer, pharmaceutical kits and combinations of 9-oxoacridine-10-acetic acid and/or salts and/or esters thereof with one or more chemotherapeutic agents. The proposed combination therapy is useful in enhancing the action of chemotherapeutic agents and their proliferative activity on human ovarian cancer cells.

Abstract: A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.

Abstract: NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time.

Abstract: Novel phototherapeutic methods and compositions are described herein. Nanoparticle-assembled microcapsules as a new type of delivery vehicle for photosensitive compounds may be synthesized through a two-step assembly process. Charged polymer chains and counterions may be combined with a photosensitive compound to form photosensitive aggregates, and then nanoparticles may be combined with the aggregates to form the microcapsules. The shell may be composed of nanoparticles and/or polymer, and the core interior may contain the photosensitive compound. Formation occurs rapidly (on the order of seconds) and the conditions are very mild (at room temperature, in aqueous solution, and at neutral pH). The microcapsule synthesis is highly suitable as an encapsulation method, particularly for a charged photosensitive molecule like ICG.

Abstract: The present invention is directed towards lasonolide derivatives, methods of inducing premature chromosome condensation using lasonolide derivatives, and methods of treating disorders, such as cancer, in a subject, the method comprising administering to the subject a lasonolide derivative.

Abstract: The invention provides compositions and methods for inhibiting cell motility, metastatic cancer and viral infections in a mammal that involve increasing the activity or expression of MxA.

Abstract: The present invention relates to the constitutive activity of the Hedgehog pathway in non-small cell lung carcinoma (NSCLC). A method for diagnosing NSCLC by detecting the level of a component of the Hedgehog pathway is provided, as is a method for identifying subjects that will respond positively to treatment with a Hedgehog pathway antagonist. Methods for treating subjects with cancer or cancers resistant to Hedgehog pathway antagonists are also provided.

Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.

Abstract: The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.

Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.

Abstract: The present invention relates to compounds, compositions, and methods useful for: (i) treating or preventing mild cognitive impairment, or (ii) delaying the progression from mild cognitive impairment to Alzheimer's disease in a subject in need thereof.

Abstract: The invention is directed to 1-nitroacridine derivative(s)/tumor inhibitor(s) compositions as well as methods for using said compositions for inhibiting or preventing tumor growth, particularly, prostate cancer cell growth and metastases.

Abstract: The invention relates to a combination comprising an amount of an NO donor, such as ISDN, and/or an amount of another pharmaceutical agent that enhances neurotransmission or which acts as neuroprotectants such as memantine, clomethiazole and tacrine. These compositions can be used in producing cognition and learning enhancement, whereby the invention also provides for a new method of treatment of Alzheimer's disease and related neurodegenerative disorders.

Abstract: Provided herein are methods and compositions for reducing the invasiveness of cancer cells. Such methods and compositions are particularly useful for cancer cells that express a member of the Toll Like Receptor9 (TLR9) subfamily and are useful in selecting the proper treatment for a subject with cancer.