Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract: The present invention relates to thiazolidinedione derivatives, to the processes for preparing same and to the therapeutic use thereof for preventing or treating cancer, and more specifically breast cancer. These compounds are of formula (I) and exhibit, at a concentration of 100 ?M, a hepatocyte viability preferably greater than 60%, preferably greater than 80% and more preferentially greater than 85%.

Abstract: A method of treating a dermatological disorder in a subject includes the step of administering a therapeutically effective amount of at least one PPAR? agonist or derivative thereof to the subject.

Abstract: The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.

Abstract: The present invention relates to a novel monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses to of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.

Abstract: Disclosed are compositions and methods for the inhibition of biofilm formation or reduction of existing or developing biofilms in a patient. These methods also inhibit the aggregation of bacteria that form biofilms in the airways. The methods include administering to a subject that has or is at risk of developing biofilms a compound or formulation that inhibits the formation or polymerization of actin microfilaments or depolymerizes actin microfilaments at or proximal to the site of biofilm formation. Such a compound can be administered in combination with a compound or formulation that inhibits the accumulation or activity of cells that are likely to undergo necrosis at or proximal to the site of biofilm formation (i.e., neutrophils). The methods and compositions can further include the use of anti-DNA and/or anti-mucin compounds, as well as other therapeutic compounds and compositions.

Abstract: The present inventions relate to a number of fields including wound healing, a waterless antibacterial disinfectant, a surgical scrub, insect repellant, and methods of treating traumatic injuries, particularly those on the battlefield where there is a need to stabilize the patient and prevent infection.

Abstract: The present invention provides compositions comprising sugar, cysteine, and/or sugar-cysteine products, methods of preparing the same, and/or using the same.

Abstract: A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus.

Abstract: The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules.

Abstract: The invention relates to novel active substance combinations consisting of heterocyclic trifluorobutenylen of formula (1), wherein X is halogen and n is 0, 1 or 2, and of known insecticide substances. Said novel active substance combinations are suitable for fighting harmful pests like insects and nematodes.

Abstract: Provided are methods for increasing fat locally in a body of a subject in need thereof comprising percutaneously administering to the subcutaneous fat of the subject a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, optionally delivered as a composition comprising a pharmaceutically acceptable carrier, as described herein. In certain embodiments, the pharmaceutically acceptable carrier comprises a percutaneous carrier, as described herein. Further provided are compositions comprising a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, for use according to the invention.

Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.

Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.

Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.

Abstract: The present invention relates to a dosing regimen for a selective S1P1 receptor agonist, whereby the selective S1P1 receptor agonist is administered to a subject in such a way that during the initial treatment phase the selective S1P1 receptor agonist is administered at a dose which induces desensitization of the heart wherein said dose is below the target dose, and at a dosing frequency that sustains desensitization of the heart, until no further acute heart rate reduction occurs, followed by dose up-titration to the target dose of the selective S1P1 receptor agonist.

Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.

Abstract: Novel agents exhibiting anti-biofilm formation activity while being non-cytotoxic are provided, as well as methods of using the same, either per se or conjugated to a polymer, for preventing and/or reducing the formation of microbial biofilms and/or for disrupting microbial biofilms. The novel agents described herein include thiazolidine-2,4-diones (TZDs), pyrrolidine-2,5-diones (PYDs), imidazolidine-2,4-diones or oxazolidine-2,4-diones, substituted by an alkyl having 7-20 carbon atoms in its backbone chain.

Abstract: The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as amino-transferases. The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.

Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.

Abstract: The present invention relates to a dosing regimen for a selective S1P1 receptor agonist, whereby the selective S1P1 receptor agonist is administered to a subject in such a way that during the initial treatment phase the selective S1P1 receptor agonist is administered at a dose which induces desensitization of the heart wherein said dose is below the target dose, and at a dosing frequency that sustains desensitization of the heart, until no further acute heart rate reduction occurs, followed by dose up-titration to the target dose of the selective S1P1 receptor agonist.

Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.

Abstract: The disclosure includes compounds of Formula (1): wherein X1, X2, Q, Z, R1, and R2 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.

Abstract: Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.

Abstract: The invention relates to methods for treating pain disorders including neuropathic and inflammatory pain and to methods to reduce or eliminate nociceptive tolerance induced by opiate analgesic use by administering an agent that suppresses or blocks S1P biological activity.

Abstract: Modified release pharmaceutical compositions of epalrestat are provided. Methods of manufacturing the tablets and treating various diseases and conditions, including diabetes and diabetic complications, by administering the modified release compositions to patients in need thereof are also provided.

Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.

Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.

Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).

Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity. In particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence.

Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing a viral infection comprising administering an effective amount of a Wnt pathway inhibitor optionally in combination with one or more anti-viral agents. In certain embodiments, the subject is diagnosed with a chronic viral infection such as human immunodeficiency virus (HIV).

Abstract: A treatment method for controlling vascularization in a patient's eye or skin includes administering to the patient's eye or skin a pharmaceutical composition having formula (I) or a pharmaceutically acceptable salt, hydrate, enantiomer, diastereomer, racemate or mixtures of stereoisomers thereof. wherein the patient has a disease or disorder associated with vascularization in the eye or skin or wherein said patient is at risk for developing a disease or disorder associated with vascularization of the eye or skin.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract: The invention relates to novel active substance combinations consisting of heterocyclic trifluorobutenylen of formula (I), wherein X is halogen and N is 0, 1 or 2, and of known insecticide substances. Said novel active substance combinations are suitable for fighting harmful pests like insects and nematodes.

Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.

Abstract: Disclosed herein is method of treating glaucoma or ocular hypertension comprising administering a prostaglandin agonist and a second therapeutically active agent to a mammal in need thereof, wherein said second therapeutically active agent is selected from: ?-Blockers, Adrenergic Agonists, non-selective adrenergic agonists, ?2-selective adrenergic agonists, Carbonic Anhydrase Inhibitors, Cholinergic Agonists, direct acting cholinergic agonists, chlolinesterase inhibitors, Glutamate Antagonists, Ca2+ channel blockers, Prostamides, Prostaglandins, Cannabinoids, and combinations thereof. Compositions and medicaments containing a combination of these two active agents are also disclosed.

Abstract: A method of treating a psychiatric or cognitive developmental disorder in a subject, includes administering to the subject a therapeutically effective amount of at least one RXR agonist.

Abstract: This invention relates to compositions, methods for preparing the compositions and methods for treating or preventing diseases, comprising administering the compositions.

Abstract: The invention provides 5-deuterium enriched 2,4-thiazolidinediones and 2,4-oxazolidinediones, such as 5-(4-((6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzo[d]imidazol-2-yl)methoxy)benzyl)-5-deutero-thiazolidine-2,4-dione, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating medical disorders, such as cancer, using the same.

Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic.

Abstract: The invention provides compositions and methods for determining GLP-1 analog and/or DPPIV inhibitor response in a subject. In one embodiment, the composition comprises a solid support comprising probes for measuring a biomarker panel comprising, for example, adiponectin, C-peptide, hsCRP, insulin, proinsulin. The simultaneous use of multiple biomarkers with independent classification power will increase the performance of the biomarker panel in characterizing GLP-1 analog and DPPIV inhibitor response. The invention also provides methods of treating a subject (e.g. one experiencing cardiodiabetes) and determining the efficacy of a therapy through assaying the various biomarkers of a biomarker panel disclosed herein.

Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac

Abstract: A method is described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of an inhibitor of Pmt-mediated O-linked glycosylation and/or in the presence of one or more ?-1,2-mannosidases.

Abstract: The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.