Abstract: Provided are methods of treating obesity and effecting desired weight loss or preventing undesired weight gain by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The preferential muscarinic acetylcholine receptor M1 antagonist, optionally can be administered with an anti-obesity agent, for example, an anorexiant. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.

Abstract: The present invention relates to pharmaceutical compositions to be used, in a solid galenic form, for oral administration, and primarily including dronedarone and/or at least one of the derivatives thereof, as well as to solid galenic forms manufactured as such from said compositions, preferably in the form of tablets or capsules. The present invention also relates to a method for preparing such solid galenic forms using a hot-melt process.

Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

Abstract: C3-functionalized-cyclopentanyltetrahydrofuranyl carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are described. Compositions comprising the disclosed compound and methods of using the compounds and/or compositions for treating patients infected with HIV are also described.

Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.

Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.

Abstract: Inhibitors of EYA tyrosine phosphatase are provided herein, as well as pharmaceutical compositions and methods relating thereto.

Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.

Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

Abstract: The present invention embraces compounds that modulate the activity of Epstein-Barr Nuclear Antigen 1 (BBNA1) protein and use thereof in methods for treating latent Epstein-Barr virus infection. R7 is a substituted or unsubstituted phenyl, pyridyl, or pyrimidinyl group. A pharmaceutical composition comprising a compound of the invention in admixture with a pharmaceutically acceptable carrier is also provide as are methods for modulating the activity of Epstein-Barr Nuclear Antigen 1 (EBNA1) protein and treating a latent EpsteinBarr virus infection with a composition of the present invention.

Abstract: The invention provides, in part, methods and compositions for treating psychiatric disorders, for example, apathy, dementia, or depression, using combination therapies such a monoamine oxidase inhibitor or a selective serotonin reuptake inhibitor in combination with an anti-psychotic agent.

Abstract: The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.

Abstract: The subject invention relates to a skin cream that can be used to moisturize and rejuvenate skin that has been damaged by exposure to sunlight or which has simply been affected over the years by intrinsic aging. It inhibits the formation of wrinkles and in some cases reduces the depth of existing wrinkles or eliminates them entirely. This invention is based upon the discovery that alkyl lactates, such as ethyl lactate, can be used to improve the penetration of active ingredients in skin care formulations deep into lower layers of the skin tissue. The present invention more specifically discloses a topical formulation comprising ascorbic acid, an amino acid selected from the group consisting of phenylalanine and tyrosine, a non-toxic zinc salt, an alkyl lactate, and a pharmaceutically acceptable carrier.

Abstract: The disclosure relates to a method for managing the risk of dronedarone/beta-blockers interaction by using dronedarone or pharmaceutically acceptable salts thereof in patients with paroxysmal or persistent atrial fibrillation (AF) or atrial flutter (AFL), with a recent episode of AF/AFL and associated cardiovascular risk factors, who are in sinus rhythm or who will be cardioverted to reduce the risk of cardiovascular hospitalization, said patients also expecting to receive a beta-blockers treatment, by performing the following steps: a—initiate beta-blockers treatment at a low dose; b—performing a electrocardiogram (ECG) verification of good tolerability; c—increase of beta-blockers dose only if results in step b) are satisfying.

Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.

Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.

Abstract: Disclosed herein are parenteral solutions containing 3-diethylaminoethoxy benzoyl-benzofurans, such as amiodarone, in a diluent NNDMA (N,N-Dimethylacetamide) useful in the treatment of cardiac arrhythmias both supraventricular, ventricular as well as, the condition of cardiac arrest.

Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.

Abstract: We have identified classes of kallikrein inhibitors as compounds that are useful in the reduction of vascular permeability (e.g., retinal vascular permeability and cerebral vascular permeability) and astrocyte activation. Diseases and conditions associated with increased vascular permeability include diabetic retinopathy, hemorrhagic stroke, and macular edema. Diseases and conditions associated with astrocyte activation include Alzheimer's disease, multiple sclerosis, Parkinson's disease, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, stroke, epilepsy, and brain trauma.

Abstract: There is provided a compound which is a histone deacetylase (HDAC) inhibitor, or a pharmaceutically acceptable ester, amide, solvate or salt thereof, for use in: (I) treating or preventing a pathological condition associated with excess fibrin deposition and/or thrombus formation; and/or (II) potentiating the degradation of fibrin deposits and preventing such deposits associated with pathological conditions or which may lead to such conditions, wherein the HDAC inhibitor, and the dose thereof, is as described in the description. There is also provided valproic acid, or a pharmaceutically acceptable salt thereof, for use in improving or normalizing endogenous fibrinolysis impaired by local or systemic inflammation.

Abstract: The present invention relates to the novel use of prostacyclin analogs for prevention and/or treatment of capillary leakage during surgery. The treatment of the present invention mediates discrete or minimal effects on haemostasis and vasodilation. Thus the present invention provides prostacyclin and analogs thereof for treatment which prevents capillary leakage while minimizing the risk of bleeding. The present invention further provides pharmaceutical compositions and kits of parts comprising prostacyclin or analogs thereof, and methods for treatment.

Abstract: Provided are: a composition containing scirpusin B, which is a composition derived from a natural material and contains scirpusin B at a high content; and a process for producing the composition containing scirpusin B.A composition containing scirpusin B is produced by the extraction from a passion fruit seed. In the extraction of scirpusin B, the passion fruit seed is crushed, and subsequently at least one solvent selected from a hydrous alcohol solvent and a hydrous ketone solvent is added to the crushed product to thereby extract scirpusin B into the solvent.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.

Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.

Abstract: Disclosed is a composition comprising scirpusin A and scirpusin B and anti-obesity potential thereof. Also disclosed are methods of inhibiting adipogenesis using a composition comprising scirpusin A and scirpusin B. The present invention also disclosed methods of therapeutically managing obesity in mammals using a composition comprising scirpusin A and scirpusin B. Still further, the present invention also relates to a method of obtaining compositions comprising A. scirpusin A and scirpusin B and B. piceatannol and its dimers scirpusin A and scirpusin B through bioactivity guided fractionation of the rhizomes of Cyperus rotundus.

Abstract: This invention relates to the use of pterosin compounds of formula I for treating diabetes including type I and type II. Also disclosed is the use of the pterosin compounds for treating obesity.

Abstract: The present invention is directed, inter alia, to methods of treating NUT midline carcinoma (NMC) by administering compounds that promote increased histone acetylation. The invention also includes assay methods for determining the responsiveness of NMC to specific histone deacetylases and other compounds.

Abstract: Amiodarone inhibits the invagination during zebrafish heart development and makes the defect on valves development. The present invention demonstrates that Amiodarone inhibits cancer metastasis and provides a method for inhibiting cancer metastasis in a subject in need thereof comprising administering to the subject a pharmaceutically effective amount of an Amiodarone or its salt.

Abstract: The present invention identifies the cholesterol biosynthetic pathway, including the enzyme oxidosqualene cyclase, as new protein targets for anti-tumor therapeutics. The present invention further provides a class of oxidosqualene cyclase inhibitors containing a tertiary amine linked with aromatic ring structures, as a new class of anticancer agents. Compounds disclosed herein have been tested in 19 cell lines including breast cancer, prostate cancer, lung cancer (including drug-resistant lung cancer H69AR), colon cancer, ovarian cancer (including drug-resistant OVCAR-3), and pancreatic cancer cells, as wells as in human breast and prostate xenograft tumor growth in nude mice, and have been shown to be active.

Abstract: This disclosure relates to a composition that may include frankincense resin and various combinations of essential oils, which combinations may be effective in promoting weight loss. The present disclosure further relates to a weight loss and satiation composition that may include frankincense resin and a flavorant. In some embodiments, the composition may include a gum base.

Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.

Abstract: The invention relates to a method for preventing, attenuating or treating pulmonary hypertension in an individual in need thereof, comprising administering at least one 5-HTT inhibitor to said individual.

Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.

Abstract: Disclosed herein are methods of and systems for predicting recurrence of atrial fibrillation comprising protease and protease inhibitor profiling.

Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.

Abstract: The disclosure relates to a method for managing the risk of dronedarone/beta-blockers interaction by using dronedarone or pharmaceutically acceptable salts thereof in patients with paroxysmal or persistent atrial fibrillation (AF) or atrial flutter (AFL), with a recent episode of AF/AFL and associated cardiovascular risk factors, who are in sinus rhythm or who will be cardioverted to reduce the risk of cardiovascular hospitalization, said patients also expecting to receive a beta-blockers treatment, by performing the following steps: a—initiate beta-blockers treatment at a low dose; b—performing a electrocardiogram (ECG) verification of good tolerability; c—increase of beta-blockers dose only if results in step b) are satisfying.

Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Abstract: According to the embodiments described herein, a SUMOylation inhibitor compound comprising a singleton scaffold is provided. In some embodiments, a method for inhibiting a SUMOylation enzyme in a cell is provided. Such a method may include administering a SUMOylation inhibitor compound to the cell. In some aspects, the SUMOylation enzyme is SUMO E1 or SUMO E2. In some aspects, the method may be used to inhibit a cancer cell in vitro (e.g., grown in culture) or in vivo (e.g., as part of a tumor in a subject). In other embodiments, a method for treating a cancer, degenerative diseases and viral infection is provided. Such a method may include administering an effective amount of a pharmaceutical composition to a subject having the cancer. The pharmaceutical composition may include a singleton SUMOylation inhibitor compound.

Abstract: The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.

Abstract: The present application relates to novel alpha, beta-unsaturated imines, to processes for their preparation, to their use for controlling animal pests including arthropods and in particular insects and to their use in the control of vectors.

Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.

Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.

Abstract: The present invention relates to the novel benzofuran derivatives, the preparation thereof and the composition comprising the same. The benzofuran derivatives of the present invention showed potent inhibiting activity of beta-amyloid aggregation and cell cytotoxicity resulting in stimulating the proliferation of neuronal cells as well as recovering activity of memory learning injury caused by neuronal cell injury using transformed animal model with beta-amyloid precursor gene, therefore the compounds can be useful in treating or preventing cognitive function disorder.

Abstract: A medical device for implantation into vessels or luminal structures within the body is provided, which stimulates positive blood vessel remodeling. The medical device, such as a stent and a synthetic graft, is coated with a pharmaceutical composition consisting of a controlled-release matrix and one or more pharmaceutical substances for direct delivery of drugs to surrounding tissues. The coating on the medical device further comprises a ligand such as a peptide, an antibody or a small molecule for capturing progenitor endothelial cells in the blood contacting surface of the device for restoring an endothelium at the site of injury. In particular, the drug-coated stents are for use, for example, in balloon angioplasty procedures for preventing or inhibiting restenosis.

Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.

Abstract: Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer compris