Abstract: The present invention relates to a method of treating, preventing, or delaying the onset of Alzheimer's disease and/or dementia in mammals. More particularly, the invention relates to method of administration of compositions containing defined chemical species useful for treating, preventing, or delaying the onset of Alzheimer's disease and/or dementia in mammals. In some embodiments, a composition used in connection with such methods comprises one or more of 1) thyroid hormone and 2) cyclo(His-Pro) and a zinc salt. Such compositions may also be used to treat metabolic syndrome and cerebrovascular diseases.

Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.

Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.

Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water-soluble oligomer.

Abstract: The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPAR?, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPAR? modulation such as diabetes.

Abstract: The present invention relates to a compound of formula (I) for use as a medicine, in particular for use in the treatment of diseases mediated by the actvation of the protein kinase Erk1/2, such as neurogenerative illnesses like Alzheimer's and related dementia, epilepsy, Parkinson's disease, Huntington's disease, or stroke, and likewise relates to the pharmaceutical compositions containing said compound. The compound of formula (I) effectively inhibits the activation of the enzyme Erk1/2 induced by the tissue plasminogen activator (TPA) and also effectively inhibits the apoptosis generated by the ?-amyloid peptide.

Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).

Abstract: Nutritive proteins are provided. In some embodiments the nutritive proteins comprise a protein digestibility corrected amino acid score (PDCAAS) that exceeds a benchmark protein. Also provided are nucleic acids encoding the proteins, recombinant microorganisms that make the proteins, methods of making the proteins using recombinant microorganisms, compositions that comprise the proteins, and methods of using the proteins, among other things.

Abstract: Disclosed herein are novel motuporamine compounds that act as anti-metastatic agents with low toxicity and high anti-migration activity. The non-toxic, anti-metastatic agents may be given to patients with potential or actual metastatic cancers, such as pancreatic cancers, alone in combination with known and/or new therapies to help block the growth and spread of tumor(s).

Abstract: Campylobacter are the commonest reported bacterial causes of gastroenteritis in the UK and industrialized worlds. This invention relates to a method of preventing or reducing the colonisation of the gastrointestinal tract of an animal with Campylobacter. Accordingly, the present invention provides a method for disinfection of an animal comprising administering to said animal at least one compound that binds to MOMP or FlaA of Campylobacter in an effective amount to reduce the number of Campylobacter present in the gastrointestinal tract of said animal. The present invention also provides a method of preventing or reducing transmission of Campylobacter from one animal to another.

Abstract: A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.

Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

Abstract: Use of an adamantaneamine derivative for the treatment of actinic keratosis.

Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.

Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.

Abstract: The present invention relates to adamantane derivatives that are active as antiviral and anti-microbial agents; antiviral or antibacterial compositions comprising adamantane derivatives or pharmaceutically acceptable salts thereof; and methods of preventing or treating viral or bacterial infections in mammalian hosts through the administration of adamantine derivatives or their salts or pharmaceutical compositions comprising the same. In particular, viral infections prevented or treated by the methods of the present invention may include, but are not limited to, those caused by arenavirus or one or more pox viruses, such as vaccinia and/or variola.

Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).

Abstract: A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.

Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.

Abstract: Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.

Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.

Abstract: The present invention relates to the treatment of an individual afflicted with mast cell mediated diseases comprising administering to the individual an effective amount of a 1-amino-alkylcyclohexane derivative.

Abstract: Pharmaceutical combinations comprising a beta-3 adrenergic receptor agonist and a muscarinic receptor antagonist, and methods for their use are disclosed. Disclosed combinations include solabegron and oxybutynin. Methods of using the pharmaceutical combinations for the treatment of one or more symptoms associated with overactive bladder, for example, frequency of urgency, nocturia, and urinary incontinence, are also disclosed.

Abstract: Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.

Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt of amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.

Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.

Abstract: The present invention relates to pharmaceutical compositions comprising tramadol and celecoxib and their uses as medicaments or analgesics, more particularly for the treatment of severe to moderate pain with an inflammation component.

Abstract: The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and/or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.

Abstract: The invention features compositions, methods, and kits useful for the treatment of filovirus-mediated diseases, e.g., hemorrhagic fever caused by Ebola virus, in an animal.

Abstract: Disclosed is a microcapsule composition for inhibiting an ethylene response in plants, which comprises a plurality of microcapsules, each including an agent for blocking an ethylene binding site in plants in an oil droplet, and a coating encapsulating the oil droplet and the agent for blocking the ethylene binding site in plants. A method for preparing microcapsules of an agent for blocking the ethylene binding site in plants, and a method for inhibiting an ethylene response in plants are also disclosed.

Abstract: The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.

Abstract: A skin care product comprising from about 0.001% to about 10% of a retinoid, in combination with 0.0001% to about 50% of at combination of retinoid boosters.

Abstract: This invention relates to the drugs, derivatives and analogs containing adamantane structures of new indication applications of anti-tumor. The invention also relates to above compounds to treat tumors and other diseases with FIG. 1. These drugs, derivatives and analogs are generated by the modification of the parent or fragment structures and formation of pharmaceutically acceptable salts, complex salts or prodrug. The drugs, derivatives and analogs as described are administered alone or together with at least one known anti-tumor and immune chemotherapeutic agent including treatment of viral, bacterial and fungal diseases, neurological diseases, endocrine system diseases, and immune system diseases.

Abstract: The present invention relates to a compound of formula (I) for use as a medicine, in particular for use in the treatment of diseases mediated by the actvation of the protein kinase Erk1/2, such as neurogenerative illnesses like Alzheimer's and related dementia, epilepsy, Parkinson's disease, Huntington's disease, or stroke, and likewise relates to the pharmaceutical compositions containing said compound. The compound of formula (I) effectively inhibits the activation of the enzyme Erk1/2 induced by the tissue plasminogen activator (TPA) and also effectively inhibits the apoptosis generated by the ?-amyloid peptide.

Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).

Abstract: An excellent potential-dependent cation channel inhibitor or an excellent masking agent is provided.

Abstract: Novel crystalline form of perphenazine 4-aminobutyrate trimesylate and a process of producing the same are disclosed. The novel crystalline form is characterized by a unique XRPD pattern and a DSC that exhibits an endothermic peak at a relatively high temperature (e.g., higher than 209° C.). Also disclosed are a process of preparing perphenazine 4-aminobutyrate trimesylate by in situ deprotection and salification, in a single-step synthesis, and a highly pure perphenazine 4-aminobutyrate trimesylate obtained thereby. Uses of any of the described perphenazine 4-aminobutyrate trimesylate are also disclosed.

Abstract: The invention provides compositions and methods for treating a subject who has suffered from a central nervous system disorder. More particularly, the invention provides sustained polymeric drug delivery systems having a polymer particle, a therapeutic agent, and a buoyancy agent for direct delivery of therapeutic agents into the central nervous system.

Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: The present invention provides regio- and stereoselective oxidation of unactivated C—H bonds using an engineered mutant cytochrome P450 monooxygenase and an engineered substrate.

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: Methods for modulating macrophage proliferation in an individual afflicted with or at risk for an ocular disease such as ARMD are provided. The methods employ a polyamine analog, or salt or protected derivative thereof. Macrophage proliferation has been implicated in a number of serious disorders, including ARMD. The invention also provides methods for aiding diagnosis and monitoring therapy of an ocular disease such as ARMD.

Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention.

Abstract: The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and/or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.

Abstract: Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.

Abstract: The present invention concerns the use of a mixture of enantiomers enriched in the dextrogyral enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts, for the preparation of a drug intended to prevent or to treat disorders that can be managed by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity.