Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.

Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of compounds of formula (I) given below, in particular as anti-ageing actives. wherein A denotes wherein X, Y and Z independently of one another denote hydrogen, C1-C4-alkyl or C2-C4-alkenyl, wherein optionally two of the radicals X, Y and Z are covalently bonded to one another under formation of a bicyclic ring system, in such a bicyclic ring system two of the radicals X, Y and Z together preferably form a radical having 1 to 4 carbon atoms, preferably a hydrocarbon radical having 1 to 3 carbon atoms, B denotes NR1R2, wherein R1 denotes hydrogen or an organic radical having 1 to 14 carbon atoms, R2 denotes an organic radical having 1 to 14 carbon atoms, and wherein optionally R1 and R2 are covalently bonded to one another, preferably so that B is a 3 to 8 membered ring.

Abstract: A method of treating an ocular surface disorder in a subject in need of such treatment is provided. The method includes exposing conjunctival tissue of the subject to an effective amount of a vasopermeability agent that increases conjunctival vascular permeability. In some embodiments, the agent is a nitric oxide donor, which may be in a sustained release form. A method of screening a substance for treating an ocular surface disorder is also provided.

Abstract: The present invention relates to a method for preparing microspheres and microspheres prepared thereby, more particularly to a method for preparing a polymeric microsphere, including preparing an emulsion including a polymer compound, a drug, a water-insoluble organic solvent and a dispersion solvent and adding to the prepared emulsion a base or an acid to remove the water-insoluble organic solvent from the emulsion, a polymeric microsphere prepared thereby, and a composition for drug delivery including the microsphere. According to the present invention, a drug-containing polymer microsphere may be prepared quickly and simply without the solvent evaporation or solvent extraction process, thereby reducing water consumption and minimizing wastewater generation.

Abstract: The present invention relates to an injectable pharmaceutical composition with gelling properties containing:—an active principle; a hydrophobic and bio-compatible organic liquid; and an organogelling substance, the molecules of which have the capacity to bind together via bonds of low energy, wherein said organogelling substance is chosen among L-tyrosine derivatives responding to the following formula (I) wherein: R1 is an alkyl group containing 1 to 3 carbon atoms, linear or branched; and R2 is a hydrophobic group chosen among aliphatic saturated or unsaturated fatty chains or aryl or arylalkyl groups, Its use as a vector for the release of active principles, as well as its process of preparation.

Abstract: Provided herein is a method for identifying a genetic variant that is associated with development of a condition of interest (e.g., Alzheimer's disease), and genetic variants so identified. Methods of treatment with an active agent (e.g., with a particular active agent and/or at an earlier age) is also provided, upon detecting a genetic variant described herein. In some embodiments, the genetic variant is a deletion/insertion polymorphism (DIP) of the TOMM40 gene. Kits for determining if a subject is at increased risk of developing late onset Alzheimer's disease is also provided. Kits for determining if a subject is responsive to treatment for a condition of interest with an active agent are further provided.

Abstract: Provided herein, inter alia, are solid forms of geldanamycin analogs, pharmaceutical compositions comprising a geldanamycin analog and a crystallization inhibitor, methods of making and using such compositions. Additionally, provided are methods for the treatment of cancer, a neoplastic disease state and/or a hyperproliferative disorder, and methods of inhibiting Heat Shock Protein 90 (“Hsp90”).

Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes compositions and methods based on modulating angiotensin activity to stimulate or activate the formation of new nerve cells.

Abstract: The invention relates to methods and compositions for improving cognitive function by using a combination of valproic acid and analogs and derivatives thereof (“valproate”) and an acetylcholinesterase inhibitor (AChEI). In particular, it relates to the use of a combination of a valproate and an AChEI in treating age-related cognitive impairment in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for Mild Cognitive Impairment (MCI), Age-Associated Memory Impairment (AAMI) or Age-Related Cognitive Decline (ARCD).

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: 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: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.

Abstract: The invention discloses the use of cholinesterase inhibitors in treating vascular depression.

Abstract: Compounds, pharmaceutical compositions, and their methods of use in raising serum HDL levels in subjects in need thereof are provided. Also provided are compounds, pharmaceutical compositions, and their methods of use in increasing reverse cholesterol transport in subjects in need thereof. Finally, methods for treating disease by raising serum HDL levels and increasing reverse cholesterol transport are provided.

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 methods to prevent worsening of and/or to improve cognitive functioning and behavior problems in patients with dementia by means of ApoE genotyping to guide the use of AChEI drugs, including rivastigimine. Also included are kits for determining ApoE4 status and recommended treatment strategy.

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: Prodrugs of tapentadol with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing pain relief with the tapentadol prodrugs are provided herein. Prodrugs having side chains of valine, leucine, isoleucine and glycine amino acids and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with tapentadol administration, as well as increasing the oral bioavailability of tapentadol are provided herein.

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 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: Compounds of formula (I) or formula (II) have dopaminergic activity: wherein: R1 is a carboxyl, carboxyl ester, or carboxamide group; R2 is a group —C(?O)—NR3R4, or —S(?O)2—NR3R4; R3 and R4 are independently selected from hydrogen, optionally substituted C1-C6 alkyl, (C1-C5 fluoroalkyl)-CH2—, -Q, and —CH2Q, wherein Q is an optionally substituted monocyclic carbocyclic or heterocyclic ring of (3) to (6) ring atoms; or R3 and R4 together with the nitrogen to which they are attached form an optionally substituted monocyclic cycloalkyl or non-aromatic heterocyclic ring of (3) to (8) ring atoms; R5 is hydrogen, or a natural or non-natural alpha amino acid residue linked via a peptide bond; R6 is hydrogen or a group R7C(?O)—; and R7 is C1-C6 alkyl, C1-C6 fluoroalkyl or cyclopropyl.

Abstract: A transdermal delivery system (TDS) for administering at least one active agent through the skin. The system has a first electrode, a second electrode, and a matrix located between the first and second electrodes. The TDS contains at least one active agent which is either alkaline or acidic. The system is configured such that when applying a voltage to the electrodes, the pH of the matrix, in the case of an alkaline active agent, does not exceed the pH of the active agent and, in case of an acidic active agent, does not fall below the pH of the active agent.

Abstract: The invention discloses the use of cholinesterase inhibitors in treating vascular depression.

Abstract: A dermal or transdermal therapeutic system comprising a reservoir that contains at least one active substance, an active substance-permeable membrane which delimits the active-substance reservoir, and a closing layer. The closing layer is impermeable to the active substance at a temperature lying below the skin temperature while being permeable at skin temperature and above.

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 catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.

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: The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug.

Abstract: A monolithic device for transdermal administration of an active pharmaceutical ingredient which is selected from propargylamines and rivastigmine and is liquid at 25° C., has an adhesive matrix layer which includes the active ingredient in an acrylic polymer pressure sensitive adhesive without cross-linker agent containing a metal atom, the adhesive having a shear value of between 1.5 and 15 hours, and further includes a non-volatile coadjuvant selected from squalene and triethylcitrate present in the layer in an amount of 1 to 15 wt %. The combination provides good release of the drug in use, reduces loss of the drug during a drying step in manufacture, reduces chemical interaction of the layer with the drug and achieves low level of skin irritation.

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: There have been found novel compositions for the controlled release of agrochemical active substances, containing at least one agrochemical active substance, cellulose ester and calcium carbonate.

Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.

Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing 4-(aminomethyl)cyclohexanamine derivatives as shown in formula (1).

Abstract: The present invention is directed to compositions and methods for the transdermal delivery of a pharmaceutically active compound. In some embodiments, the addition of inert pharmaceutical ingredients in place of a portion of adhesive in a transdermal patch formulation increases the rate of skin permeation of a pharmaceutical compound.

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: The present invention relates to composition comprising at least one L-type calcium channel blocker, particularly the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, in combination with at least one cholinesterase inhibitor, particularly donepezil, and uses thereof in methods of treatment.

Abstract: A method of causing a patient to reduce or cease tobacco use that involves the administration of a cholinesterase inhibitor.

Abstract: A compound of the formula (I): wherein R1 represents a C1-C6 alkyl, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and represent hydrogen or a C1-C6 alkyl; Ra represents hydrogen, C1-C6 alkyl or C2-C6 alkenyl or together with R2 represents a C1-C3 alkylene; Arom represents a heteroaryl; A represents a C1-C6 alkylene; E represents a single bond, oxygen, sulphur or R4NR4—, wherein R4 is hydrogen or C1-C7 alkenoyl; X1 and X2 both represent oxygen; X2 is attached at the 3-position or the 4-position; or a pharmacologically acceptable salt or ester thereof. The compound has superior acetylcholinesterase inhibitory action and selective serotonin reuptake inhibitory action, and is useful for treating Alzheimer's disease, depression, Huntington's chorea, Pick's disease, tardive dyskinesia, compulsive disorders or panic disorders.

Abstract: There is disclosed a method for glycemic control of a patient having a disease selected from the group consisting of type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance, hyperglycemia, and postprandial hyperglycemia, said method comprising administering to a patient in need thereof a pharmaceutical composition comprising an acetyl cholinesterase inhibitor compound. There is further disclosed a method for reducing HbA1C concentrations as a measure of glycemic control, comprising administering to a patient in need thereof a pharmaceutical composition comprising an acetyl cholinesterase inhibitor compound. Lastly, there is disclosed a pharmaceutical formulation for daily administration comprising an acetyl cholinesterase inhibitor, from about 5 mg to about 15 mg of loratadine and optionally from about 5 mg to about 16 mg of elemental zinc.

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

Abstract: The present invention includes insecticidal carbamates that are useful, for example, for the control of insects, such as mosquitoes, which can be used in applications where exposure to and/or contact with humans is likely. The insecticides of the present invention include phenyl N-methyl carbamates and compositions comprising them that exhibit species-selective inhibition of acetylcholinesterase (AChE) and are preferably toxic to mosquitoes but not humans. Of particular interest are compounds of Formula (I) and Formula (II): Compounds of Formula (I) and Formula (II) are especially suitable for insecticide treated nets and indoor residual spraying for mosquito control.

Abstract: The present invention provides compositions and methods for preventing, treating or reversing neuronal dysfunction in a mammal resulting from exposure to organophosphate nerve agents, organophosphate insecticides and incapacitating agents of the central nervous system (CNS); CNS injury, including traumatic brain injury, neurologic complications of cardiac surgery, perinatal asphyxia, and stroke, spinal cord injury, and peripheral nerve injury; and neuronal disorders associated with the loss of motor function including post-polio syndrome, amyotrophic lateral sclerosis, myasthenia gravis, Parkinson's disease and Rett syndrome; neurodegenerative disorders including Alzheimer's disease, mild cognitive impairment and schizophrenia; and cognitive impairment associated with aging.

Abstract: The present invention relates to a multiparticulate osmotic delivery system. The system is a modified release composition suitable for oral administration. The composition includes a core that includes at least one drug in combination with at least one pharmaceutically acceptable excipient. The composition further includes an osmotic subcoat surrounding the core, and a modified release overcoat surrounding the osmotic subcoated core.

Abstract: A crystalline rivastigmine hydrogentartrate of Form II and an amorphous rivastigmine hydrogentartrate of Form III.

Abstract: This invention relates to methods to prevent worsening of and/or to improve cognitive functioning and behaviour problems in patients with dementia by means of ApoE genotyping to guide the use of AChEI drugs, including rivastigimine. Also included are kits for determining ApoE4 status and recommended treatment strategy.

Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.

Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and (b) a carrier of at least one mono-C-substituted or di-C-substituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.

Abstract: Microparticles and a method for their production is described. The process of the present invention provides a simple, quick, and efficient one-pot process for the production of microparticles containing a hydrophilic active agent of various and uniform morphologies, including microcapsules, microspheres, and microsponges. The microparticles are preferably used for pharmaceutical applications.

Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they

Abstract: The present invention relates to a novel retinoid derivative compound represented by the formula I: wherein X, R1, R2 and R3 are as defined herein or pharmaceutically acceptalbe salts thereof. Also, the present invention relates to processes for producing the compound of the formula I and to an anti-cancer composition comprising the compound of the formula I. The compound of the formula I according to the present invention exerts high anti-cancer effects while not causing undesirable side effects.