Abstract: Disclosed is an amino acid/soluble polysaccharide coacervate that provides modified release of amino acid in the digestive system. A method is also disclosed for forming amino acid coacervate compositions to provide increased delivery and release of one of more amino acids, such as leucine, for example, to the intestine of a human and/or animal.

Abstract: The present invention is directed to a compound for use in the prevention or treatment of a neurodegenerative disease, in particular of a synucleinopathy. The present invention further is directed to a pharmaceutical composition containing an effective amount of said compound and one or more pharmaceutically acceptable auxiliaries.

Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.

Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.

Abstract: Complexes of agomelatine and sulphonic acids of formula (I): Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.

Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: A method of treating a cellular injury in a subject comprising administering to a subject in need thereof, a therapeutically effective amount of a compound of formula I: wherein at least one of R1-R8 is a sulfonic acid, a carboxylic acid, a phosphonic acid, a pharmaceutically acceptable salt of a sulfonic acid, a pharmaceutically acceptable salt of a carboxylic acid, a pharmaceutically acceptable salt of a phosphonic acid, a sulfonate ester, a carboxylate acid ester, or a phosphonate ester; and the remaining R1-R8 are each independently selected from hydrogen, halo, hydroxyl, nitro, nitroso, amino, substituted amino, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoy, alkenyloxy, substituted alkenyloxy, alkynyloxy, substituted alkynyloxy, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, cycloalkynyl, substituted cycloalkynyl, cycloalkyloxy, substituted cycloalkyloxy, heterocyclyl, substituted heterocyclyl, heterocyclyl

Abstract: Methods and compositions are described for reducing airway reactivity and the susceptibility to asthmatic bronchoconstriction that involve increasing sphingolipid content in airways and lungs of a mammalian subject.

Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.

Abstract: The present invention relates to a pharmaceutical combination for the treatment of renal failure in pets, caused by various diseases or ineffective to traditional renal therapy or renal replacement therapy thereby incapable of restoring health. The pharmaceutical combination of the present invention is administered by subcutaneous injection to pets in need thereof, with various advantages including simple use, no requirement for surgery, hospitalization and/or fluid infusion, faster recovery of health status, reduced medical costs, significantly improved recovery rate, reduced mortality and the likes. The pharmaceutical combination of the present invention can also be used for the continuous care treatment of pets with renal failure.

Abstract: A method for treating viral infection includes administering to a subject in need thereof a composition containing P2X receptor antagonists. The methods may achieve preventive or therapeutic effect on hand foot and mouth disease by inhibiting viruses. The P2X receptor antagonists can inhibit infection by a positive-sense single-stranded RNA picornavirus. The virus may be an enterovirus or a Coxsackie virus, such as human enterovirus 71. The P2X receptor antagonist may be PPADS, iso-PPADS, PPNDS, Suramin, NF023, TNP-ATP, NF279, NF157, Evans Blue, an analog thereof, a derivative thereof, or a pharmaceutically acceptable salt thereof.

Abstract: Dermatological disorders having an inflammatory or proliferative component, notably common acne, are treated with topically applicable pharmaceutical compositions containing about 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously formulated into topically applicable gels, preferably aqueous gels, creams, lotions or solutions.

Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.

Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomer solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: A drug screening method is disclosed. The drug screening method includes steps of screening a compound library to obtain a first group of compounds capable of binding to a wild type target; screening the first group of compounds to obtain a second group of compounds capable of binding to a mutant site of a mutant target; analyzing characteristics of binding sites of the wild type target and the mutant type target to obtain physico-chemical properties of the binding sites; identifying a candidate from the second group of compounds according to the physico-chemical properties of the binding site; and performing a bio-assay on inhibitory activity of the candidate.

Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.

Abstract: A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.

Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.

Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.

Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.

Abstract: A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.

Abstract: Disclosed herein are compositions and methods for promoting the repair and regeneration of injured tissues, such as injuries resulting from ischemic damage.

Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: The present invention is directed to methods of inhibiting STDs by topically administering suramin or a derivative thereof to actual or potential sites of infection, and methods of preventing pregnancy by topically applying suramin or a derivative thereof intravaginally. Suramin compositions that include an antimicrobial agent and/or a sperm-function inhibitor are also provided and may advantageously be used in the methods of the invention. A method of simultaneously inhibiting STDs and preventing pregnancy is also provided. Devices impregnated or coated with the topical suramin compositions are further disclosed and may be used to apply the compositions described herein.

Abstract: The present invention provides methods for the local pulmonary treatment of lung metastases and/or primary lung cancer, such as squamous lung cancer and/or small cell lung cancer, using local deposition of one or more agents capable of inhibiting angiogenesis and/or an agent that acts as an active anti-cancer agent and/or an active anti-metastatic agent. The agent capable of inhibiting angiogenesis and/or which acts as an active anti-cancer agent and/or an active anti-metastatic agent is administered to a patient with cancer as a treatment of said metastasis and/or cancer or to extend the lifespan for said cancer patient with reduced systemic side-effects compared to other treatment forms. The agent capable of inhibiting angiogenesis and/or which acts as an active anti-cancer agent and/or an active anti-metastatic agent is administered intratracheal, intrabronchial, intraalveolar or broncioalveolar.

Abstract: Provided herein are compositions and methods for targeted ablation of mutational escape in the face of cancer therapeutic agents. Compositions comprising the yeast-based vehicles are used in combination with other cancer therapeutic agents.

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

Abstract: The invention features compositions and methods that are useful for treating or preventing AAT deficiency and associated conditions. In addition, the invention provides methods for identifying compounds useful for treatment of AAT deficiency and associated conditions.

Abstract: Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include naphthalenesulfones, phenylsulfones, and certain peptides with unnatural amino acids and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.

Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.

Abstract: Methods of treatment or prophylaxis of bacterial vaginosis, prevention of recurrence of bacterial vaginosis and alleviation or prevention of symptoms or diagnostic criteria of bacterial vaginosis are provided. The methods include administration of an effective amount of a macromolecule comprising a polylysine, polyamidoamine, poly(etherhydroxyamine) or poly(propyleneimine) dendrimer and one or more sulfonic acid containing moieties attached thereto.

Abstract: It is an object of the present invention to provide a novel sterilization method capable of killing not only microorganisms in water, but also microorganisms in a gas. Specifically, the present invention provide a method for sterilizing a gas or liquid, comprising contacting a microorganism in a gas or liquid with a material containing an amorphous carbon having a sulfo group introduced therein.

Abstract: Method of treating a tumor in a patient in need thereof by administering to the patient an effective amount of 4-[6-(diethylaminomethyl)naphth-2-ylmethyloxycarbamoyl]benzohydrozamic acid.

Abstract: The present invention relates to the field of therapeutic methods, compositions and uses thereof, that affect, directly or indirectly, the behavior of LRP receptors. These compositions and methods result in the treatment of inflammatory, immunological and metabolic conditions. More particularly, the methods and compositions of the invention are directed to the identification of small molecules, drugs and/or pharmacological agents that affect the Wnt pathway by affecting normal complex formation among various signaling receptors, the LRP5 and LRP6 receptor, and related ligands.

Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.

Abstract: A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.

Abstract: The present invention relates to compositions that may alleviate symptoms of ocular stress, as well as methods of their production, use, and storage compositions. The compositions comprise at least one ocular epithelial cell associating group and at least one hydrophilic group. In one embodiment the at least one ocular epithelial cell associating group and at least one hydrophilic group are substituents on a conjugated polyaromatic core. The compositions may be used in ophthalmic compositions and ophthalmic devices.

Abstract: The present invention is directed to drug dosage forms that release an agent that raises the pH of a patient's gastrointestinal tract, followed by a non-steroidal anti-inflammatory drug. The dosage form is designed so that the NSAID is not released until the intragastric pH has been raised to a safe level. The invention also encompasses methods of treating patients by administering this coordinated release, gastroprotective, antiarthritic/analgesic combination unit dosage form to achieve pain and symptom relief with a reduced risk of developing gastrointestinal damage such as ulcers, erosions and hemorrhages.

Abstract: Small molecules and their derivatives are described for the treatment and/or prevention of intestinal fluid loss. Also disclosed are methods of using said molecules and their derivatives to treat and/or prevent conditions associated with increased levels of 3?,5?-adenosine monophosphate. Specific compositions of the invention are also novel.

Abstract: The present invention provides methods to reduce or inhibit weight gain by administering inhibitors of the SirT1 protein to a subject. Methods to identify such inhibitors are also disclosed.

Abstract: The present invention encompasses compositions and methods that activate P2Y receptors for the increased production of new synapses in the central nervous system. The formulations of the invention may be administered to a healthy subject or to a subject in need thereof to restore synapses.

Abstract: A modification of pharmacokinetics of suramin by use of amino compounds in modification of lipophilicity and protein binding characteristics for tackling the physico-chemical properties of suramin that gives it poor distribution in the body; formulating the resulting product in a form that leads to targeting body fluids like the lymphatic system when administered in a specific way; and determining the route of administration that maximizes targeting with a view to reducing the dosage so as to limit toxicity, hence increase tolerance by patient.

Abstract: Described are a method and a composition for preventing and/or treating a disease related to mitochondrial dysfunction by inhibiting the fatty acid oxidation of one or more cells of an organism. Particularly, the fatty acid oxidation is inhibited by inhibiting the expression and/or activity of the enzyme Camitin-Palmitoyl-Transferase-1 (CPT-1) by means of an arylalkyl- or arlyoxyalkyl-substitued oxirane carboxylic acid or pharmaceutically acceptable salts and derivatives of the arylalkyl-substituted oxirane carboxylic acid.

Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect vesicle-fusing ATPase; a method for assaying pesticidal activity of a test substance, which comprises measuring the activity of a vesicle-fusing ATPase in a reaction system in which the vesicle-fusing ATPase contacts with a test substance, and the like.

Abstract: Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include naphthalenesulfones, phenylsulfones, and certain peptides with unnatural amino acids and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.

Abstract: A method for determining a therapeutically effective amount of suramin for administering to a patient, who is to receive a cytotoxic agent, which comprises the steps of determining the circulating suramin concentration in the patient; administering suramin, if required, to establish a low circulating concentration of suramin in the patient of below about 200 ?M; and administering the chemotherapeutic agent to the patient when the low circulating concentration of suramin is present in the patient. Conveniently a nomogram can be constructed for use in clinical settings with the suramin.

Abstract: The present invention relates to the field of therapeutic methods, compositions and uses thereof, that affect, directly or indirectly, the behavior of LRP receptors. These compositions and methods result in the treatment of inflammatory, immunological and metabolic conditions. More particularly, the methods and compositions of the invention are directed to the identification of small molecules, drugs and/or pharmacological agents that affect the Wnt pathway by affecting normal complex formation among various signaling receptors, the LRP5 and LRP6 receptor, and related ligands.

Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.