Abstract: The invention relates to dimeric aryl-sulphonamido compounds endowed with inhibitory activity against metalloproteases MMP, having formula (I) below (M)-L-(M?) (I), wherein M and M?, the same or different from each other, represent the residues of the metalloproteases inhibitors of formula (II), wherein R, R1, R2, R3, G and n have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.

Abstract: The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.

Abstract: The present invention relates to compositions including porous biomolecule-containing metal-organic frameworks and methods for their preparation. The porous biomolecule-containing metal-organic frameworks can include a metal component and a biomolecule component. The pores located within the frameworks have a pore space and said pore space is capable to adsorb materials therein. These compositions of the present invention are useful in a wide variety of applications, such as, but not limited to, hydrogen and carbon dioxide sequestration, separation and storage; carbon dioxide uptake; and drug storage and release.

Abstract: Described is a new cooling agent represented by Structure I and compositions with known coolers having cooling properties and the application of Structure I in foodstuffs and chewing gum:

Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.

Abstract: A medicament for the treatment of the phantom phenomena of acute tinnitus and/or phantom pain, a method for the production of such a medicament, and a method for the treatment of such phantom phenomena

Abstract: A method and composition for treating osteoarthritis with ion-channel regulators is disclosed. The ion-channel regulators are used alone or in combination with other osteoarthritis treatment agents, including but not limited to injectable agents such as viscosupplements and steroids. A composition comprising one or more ion-channel regulator(s) and one or more osteoarthritis treatment agent(s) is also disclosed.

Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

Abstract: Disclosed are compositions and methods related to powder and granular emulsifiable concentrate pesticide formulations. As disclosed, emulsions from non-aqueous based liquid or solvent soluble pesticide actives may be prepared using a high purity, high molecular weight sulfonated lignin as the emulsion stabilizer. The resulting emulsions may then be dried to obtain a powder or granular emulsion concentrate where the high molecular weight sulfonated lignin acts as a solid matrix for the pesticide active. The powder or granular emulsifiable concentrate formulations thus formed have high loading rates, good storage properties and are easily reconstituted when added to water.

Abstract: Compositions containing neurogenic agents for inhibition of neuron death and inducing proliferation of neural cells are disclosed

Abstract: Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning—X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.

Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: Treatment of lymphangioleiomyomatosis with the MEK1/2 inhibitor CI-1040 delayed the development of primary tumors and blocked the estrogen-induced lung metastases in treated animals. Such treatment also reduced the number of circulating ELT3 cells and decreased their lung colonization after intravenous injection.

Abstract: The present invention relates to the field of life needs and more particularly to the therapeutic field. The invention relates more particularly to pharmaceutical compositions for helping the takers of addictive drugs to return to abstinence, in the form of a combination of two medicaments constituted of a partial or complete ligand of dopaminergic receptors—in particular of the D1, D2 and D3 receptors, and having direct prodopaminergic activity, and of an indirect prodopaminergic product, in the form of a pharmaceutical composition for oral, parenteral or transdermal administration. The invention also relates to a method for combating the various forms of addiction to licit or illicit drugs.

Abstract: The present invention is directed to transdermal compositions and the uses thereof. These compositions include at least one of the following components: a C1-C6 dialkyl, C12-C30 dialkyl quaternary ammonium salt, a C12-C30 fatty acid, a nitrogenous organic base, C12-C30 fatty alcohol, monoglyceride or the reaction products thereof.

Abstract: The present invention consists of an extended-release metoclopramide hydrochloride pharmaceutical composition, in 30 mg drug substance 5 tablets, for use in gastrointestinal disorders. The formulation is mainly composed of a hydrophilic polymer, a hydrophobic polymer, a hydrophilic component and metoclopramide hydrochloride. The hydrophilic polymer is swollen by hydration when contacting water, forming a gel coat which controls drug substance release. The water inside the matrix dissolves the drug substance and this is diffused outside through the gel coat. The hydrophobic polymer shows plastic deformation properties under compression, tending to surround the drug substance particles reducing the pore quantity and dimensions in the matrix structure, delaying as a consequence the drug substance release. The hydrophilic component is part of the gel coating structure providing support thereto. Drug substance is the metoclopramide hydrochloride or a pharmaceutically acceptable salt thereof.

Abstract: Embodiments of the invention relate to methods and compositions for treating symptoms related to inflammatory conditions and to methods and compositions for treating inflammatory components of common cold, utilizing various method of administration of X-ray contrast media (CM).

Abstract: A method is disclosed for treating and inducing the regression of established atherosclerotic plaques. A method is disclosed for treating asthma, including treatment of an ongoing asthma attack. In both cases, treatment with PARP inhibitors, such as the PARP inhibitor TIQ-A (Thieno[2,3-c]isoquinolin-5-one), can lead to regression of existing disease and symptoms.

Abstract: The present invention provides a method for preventing or repairing damage to a fetal membrane. In one embodiment, the method comprises contacting a fetal membrane with a composition comprising a four-armed catechol-terminated polyethylene glycol (cPEG) and a biocompatible oxidant. In one embodiment, the four-armed cPEG and the biocompatible oxidant are initially contained in separate solutions, and the solutions are mixed to form the composition just prior to or at the same time that the composition contacts the fetal membrane.

Abstract: Disclosed is an emulsifiable concentrate composition characterized by containing not less than 0.5% by weight but not more than 50% by weight of a hydrophobic agrochemically active compound, not less than 5% by weight but not more than 15% by weight of a surfactant, not less than 2% by weight but not more than 60% by weight of an aromatic hydrocarbon solvent, not less than 2% by weight but not more than 40% by weight of methyl oleate, and not less than 12% by weight but not more than 90% by weight of 1,3-dimethyl-2-imidazolidinone. The emulsion composition is also characterized in that the weight ratio of 1,3-dimethyl-2-imidazolidinone to methyl oleate is within the range from 1:0.03 to 1:2.

Abstract: Topical suspension compositions of nepafenac are disclosed. The compositions are especially suitable for topical ophthalmic administration.

Abstract: The efficacy of light activated therapy treatment is enhanced by use of additional therapeutic agents. Abnormal tissue is destroyed by light activated therapy, and the associated administration of one or more additional therapeutic agents can synergistically enhance the therapy. For example, the concepts disclosed herein encompass the use of the following agents in combination with light activated drug therapy: (1) agents that selectively inhibit heat shock protein 90 (Hsp90); (2) agents that inhibit the Hedgehog pathway (which is believed to play a central role in allowing the proliferation and survival of certain cancer-causing cells, and which is implicated in many of the most deadly cancers); and, (3) agents for reducing the anti-apoptotic effects of Bcl-2 or Bcl-xL. These agents can be used with light activated drug therapy individually, or in various combinations and permutations.

Abstract: This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.

Abstract: The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.

Abstract: This invention features methods and compositions for treating cancer and modulating signal transduction and metabolism pathways. For example, the methods and compositions of the invention can be used to kill or inhibit the growth or spread of cancer cells. The invention also features a method of identifying a compound that modulates a signal transduction or metabolic pathway.

Abstract: The use of benzophenones of the formula I in which R is hydrogen or C1-C4-alkyl and Hal is fluorine, chlorine or bromine for controlling Pseudocercosporella herpotrichoides in crop plants is described.

Abstract: The present invention provides methods of ameliorating or reducing the extent of cardiac arrhythmia disorders, by administering an inhibitor of histone deacetylase enzyme (HDAC).

Abstract: The invention disclosed a total synthesis process of novel ethoxy combretastatins and their prodrugs. Combretastatins are chemically modified by ethoxy substituted on the 4?-position of their B aryl ring and are converted to be their soluble prodrugs of phosphate or their inner salt of phosphorylcholine by modifying the hydroxyl on the 3?-position of their B aryl ring. Similarly, 3?-amino combretastatin is 4?-ethoxy chemically modified and further side chain of amino acid can be introduced to the amino to form soluble prodrug of amino acidamide. The structure of the said compound is showed as formula (I). Ethoxy combretastatins possess potent tubulin polymerization inhibitory activity and can be used for the treatment of inhibiting tumor or neovascular.

Abstract: The present application is directed to the use of X-ray contrast media that act as universal antigens that are labeled herein as “pseudoantigens.” X-ray contrast media have the potential to exist in an aggregated state that is greater in increased concentrations. In this aggregated state, contrast media assume the role of multivalent antigens and can successfully compete with any other antigens involved in antibody-antigen reactions that lead to anaphylaxis. In this competition, the large quantity of contrast media serves to inhibit the adverse effects of antibody-antigen reactions without the contrast media itself creating antibodies or creating toxicity problems.

Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of 4-phenyl-4-hydroxy-butyric acid and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.

Abstract: The invention relates to compounds and methods useful in detection and therapy of HPV-associated diseases. The invention is based on the elucidation of a mechanism by which replication of HPVs occurs in naturally infected tissues and cells. Moreover it is based on the identification of distinct epigenetic changes of the viral genome in infected cells that allows promotion of the affected cells to precancerous and cancerous cells. The invention therefore provides methods of diagnosing neoplasias and their precursor lesions as well as methods of preventing the development of malignancies or inhibiting tumor growth.

Abstract: The present invention relates to methods of identifying a disease treatable with PARP modulators by identifying a level of PARP in a sample of a subject, making a decision regarding identifying the disease treatable by the PARP modulators wherein the decision is made based on the level of PARP. The method further comprises of treating the disease in the subject with the PARP modulators. The methods relate to identifying up-regulated PARP in a disease and making a decision regarding the treatment of the disease with PARP inhibitors. The extent of PARP up-regulation in a disease can also help in determining the efficacy of the treatment with PARP inhibitors. The present invention also relates to methods of identifying a disease treatable with PARP modulators by identifying a level of PARP in a plurality of samples from a population, making a decision regarding identifying the disease treatable by the PARP modulators wherein the decision is made based on the level of PARP.

Abstract: Described is a new cooling agent represented by Structure I and compositions with known coolers having cooling properties and the application of Structure I in foodstuffs and chewing gum:

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful inter alia for the treatment of obesity.

Abstract: Cinnamic and phenylpropiolic acid derivatives of formula (I) having antitumour and chemo sensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.

Abstract: The invention relates to 2-amino-3-benzoylbenzeneacetamide, i.e. nepafenac, crystals having reduced chargeability, to processes for the preparation thereof, and to the use thereof for preparing pharmaceutical formulations.

Abstract: Strobilurin derivatives can be employed for the treatment and/or prevention of disorders of iron metabolism in mammals.

Abstract: A method of enhancing progenitor cell differentiation, including enhancing myogenesis, neurogenesis, and hematopoiesis, by contacting a progenitor cell with an effective amount of a deacetylase inhibitor (DI). The progenitor cell can be part of cell culture, such as a cell culture used for in vitro or in vivo analysis of progenitor cell differentiation, or can be part of an organism, such as a human or other mammal. Contacting the progenitor cell with a DI can lead to enhancement of expression of terminal cell-type specific genes in the progenitor cell, such as enhancing expression of muscle-specific genes in myoblasts. Administering a DI to a subject also can provide some prophylactic or therapeutic effect for inhibiting, preventing, or treating associated with a degeneration or loss of tissue. The DI can be administered to a subject as part of a pharmaceutical composition.

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Abstract: The present application refers to methods for cancer diagnosis and treatment, particularly in types of cancers associated with aberrant CpG methylation of the miR-34a promoter.

Abstract: The invention relates to novel aromatic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, b their use as medicaments and to medicaments comprising them.

Abstract: The present invention is directed to transdermal compositions and the uses thereof. These compositions include at least one of the following components: a C1-C6 dialkyl, C12-C30 dialkyl quaternary ammonium salt, a C12-C30 fatty acid, a nitrogenous organic base, C12-C30 fatty alcohol, monoglyceride or the reaction products thereof.

Abstract: A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tmax of 4-10 hours.

Abstract: A composition of matter comprising in combination as component (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and as component (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said composition of matter, and a method of treating pain, e.g. neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.

Abstract: A method for the treatment and/or prophylaxis of a neurological and/or neuropsychiatric disorder associated with altered dopamine function comprising administering to the eye of a patient in need thereof an effective amount of an agent that modulates neurotransmitter production or function.

Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as Parkinson's disease, and the manufacture of medicaments for such treatment.

Abstract: The aim of the invention to provide a less complex method for the production of A-ring aromatized acetyl minocyclines of the formula (I), wherein R1 to R5=acetyl and/or H, which can also be used on an industrial scale, is achieved in that minocycline hydrochloride is reacted with acetanhydride in the presence of a proton catcher, the reaction product is subjected to chromatographic filtration using a carrier material and an eluant, the eluant is distilled off, and the product is subsequently cleaned by recrystallization.

Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).

Abstract: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].

Abstract: The present invention provides compositions of matter, kits, and methods for use in treating cancer and viral conditions. In particular the invention provides for pharmaceutical compositions containing nitrobenzamide compounds that have enhanced solubility in aqueous solutions.