Abstract: The invention relates generally to a system and methods by which a microbiome-based action component may be developed that is useful in order to establish, restore, promote, or maintain subject health. More specifically, the system and methods of the present invention may be used to develop a microbiome-based action component that efficiently summarizes the state of a subject's microbiome along with measures of gut maturity in case of an infant and nutrition readiness in case of an adult subject. Such an efficient summary may be used to render more immediate support or health care to the subject.

Abstract: The present invention describes an approach to increase taurine or hypotaurine production in prokaryotes. More particularly, the invention relates to genetic transformation of organisms with genes that encode proteins that catalyze the conversion of cysteine to taurine, methionine to taurine, cysteamine to taurine, or alanine to taurine. The invention describes methods for the use of polynucleotides that encode cysteine dioxygenase (CDO) and sulfinoalanine decarboxylase (SAD) polypeptides in prokaryotes to increase taurine, hypotaurine or taurine precursor production. The preferred embodiment of the invention is in plants but other organisms may be used. Increased taurine production in prokaryotes could be used as nutraceutical, pharmaceutical, or therapeutic compounds or as a supplement in animal feed.

Abstract: A (meth)acryloyl compound represented by the following formula (A): wherein X is a 2m-valent group having 1 to 60 carbon atoms or a single bond; each Z is independently an oxygen atom, a sulfur atom, or not a crosslink; each R1 is independently a linear, branched, or cyclic alkyl group having 1 to 30 carbon atoms, an aryl group having 6 to 30 carbon atoms and optionally having a substituent, an alkenyl group having 2 to 30 carbon atoms and optionally having a substituent, an alkoxy group having 1 to 30 carbon atoms and optionally having a substituent, a halogen atom, a nitro group, an amino group, a carboxylic acid group, a thiol group, a hydroxy group, or a group in which a hydrogen atom of a hydroxy group is replaced with a vinylphenylmethyl group, wherein the alkyl group, the aryl group, the alkenyl group, or the alkoxy group optionally contains an ether bond, a ketone bond, or an ester bond; each R1A is independently a methyl group or a hydrogen atom; each k is independently an integer of 0 to 2, pr

Abstract: A compound having the formula (I): (I) is disclosed. A method of preparing the compound of formula (I) is also disclosed.

Abstract: This invention relates to methods for improving the quality of the meibum composition of the meibomian glands to enhance or improve the lipid layer of the tear and increase tear breakup time by way of elevating the omega-3 index in patients suffering from symptoms of dry eye, posterior blepharitis, and/or meibomian gland dysfunction. The methods comprise administering a supplementation of omega-3 fatty acids to a patient having an inflamed meibomian gland so as to facilitate an increase in the amount of omega-3's acting as an anti-inflammatory and, respectively, decrease the amount of omega-6's (arachidonic acid) acting as an inflammatory in the composition of the meibum, thereby normalizing the lipid layer of the tear and effectively reducing the associated symptoms. In certain embodiments, the supplementation of omega-3's comprises the esterified or re-esterified triglyceride form.

Abstract: The present invention relates to a pharmaceutical combination comprising a CDK inhibitor and at least one antioxidant enzyme inhibitor for use in the treatment of cancer. The present invention also relates to a method for the treatment of cancer comprising administering to a subject in need thereof, a therapeutically effective amount of a CDK inhibitor and a therapeutically effective amount of at least one antioxidant enzyme inhibitor. The pharmaceutical combination of the present invention exhibits synergistic effect when used in the treatment of cancer.

Abstract: Methods and compositions for inhibiting expression of ASC, expression of NLRP3, and/or formation of NLRP3 inflammasome complex by using diacerein or its analogs are provided. Also provided are methods and compositions for the treatment and/or prevention of a disorder mediated by ASC and/or NLRP3, and/or by formation of NLRP3 inflammasome complex by using diacerein or its analogs.

Abstract: Compositions for use in treating and/or alleviating a symptom of inflammatory bowel disease, colitis, and/or enterocolitis in a subject in need thereof are disclosed. The composition comprises a therapeutically effective amount of an anthraquinone derivative or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable vehicle. In one embodiment, the composition comprises diacerein. Also disclosed is a first composition comprising an anthraquinone derivative selected from the group consisting of diacerein, aloe-emodin, emodin, and rhein, and a first pharmaceutically acceptable vehicle; and a second composition comprising mesalazine, and a second pharmaceutically acceptable vehicle, in combination for use in treating and/or alleviating a symptom of inflammatory bowel disease, colitis, and/or enterocolitis.

Abstract: The present invention describes an approach to increase taurine or hypotaurine production in prokaryotes. More particularly, the invention relates to genetic transformation of organisms with genes that encode proteins that catalyze the conversion of cysteine to taurine, methionine to taurine, cysteamine to taurine, or alanine to taurine. The invention describes methods for the use of polynucleotides that encode cysteine dioxygenase (CDO) and sulfinoalanine decarboxylase (SAD) polypeptides in prokaryotes to increase taurine, hypotaurine or taurine precursor production. The preferred embodiment of the invention is in plants but other organisms may be used. Increased taurine production in prokaryotes could be used as nutraceutical, pharmaceutical, or therapeutic compounds or as a supplement in animal feed.

Abstract: The present invention belongs to the technical field of organic chemistry, and specifically relates to a method for preparing rosuvastatin sodium.

Abstract: One aspect of the disclosure relates to methods of treating a fibrotic condition in an individual. The methods include administering to an individual having a fibrotic condition an effective amount of a lactic dehydrogenase (LDH) inhibitor, wherein the fibrotic condition involves an internal organ or tissue, or ocular tissue, and said administering is effective to treat the fibrotic condition. Methods of administration and pharmaceutical compositions and systems for practicing such methods are also disclosed.

Abstract: Provided is a pharmaceutical combination preparation including fimasartan and rosuvastatin as active ingredients together with meglumine. The combination preparation exhibits an outstanding effect in treating cardiovascular disease by improving the disintegration and the dissolution which obtained better drug bioavailability and drug safety.

Abstract: The present disclosure provides acyltransferases useful for synthesizing therapeutically important statin compound.

Abstract: The present invention relates to fluorine substituted CBD compounds, compositions thereof and uses thereof for the preparation of medicaments.

Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R4, R5, X1, X2, X3 and X4 are as defined herein, and wherein the compound comprises at least one F, Cl, Br, I or 123I moiety, are provided. Uses of such compounds for imaging diagnostics in cancer and therapeutics methods for treatment of subjects in need thereof, including prostate cancer as well as methods and intermediates for preparing such compounds are also provided.

Abstract: The conjugates of present invention are formed by the combination of rhein or their analogues with the organic bases or amino acids in molecular force between them. The methods for preparing the conjugates and their uses for manufacturing medicines in the treatment of diabetic nephrosis, recovery of gastrointestinal function and prevention of intestinal adhesion, as well as treatment of osteoarthritis, rheumatic arthritis and rheumatoid arthritis are also described. Rhein or their analogues as the left part of general formula (I) is selected from (1) the compounds of rhein or their analogues, in which one or two substituents of R2˜R3 and R6˜R7 are COOH at least two substituents of R1˜8 are —H; or (2) the rhein-containing extract derived from plants. In general formula (I), M represents nitrogen-containing organic bases or basic amino acids.

Abstract: Methods are provided herein for treating cardiac arrhythmias, such as for treating an arrhythmia syndrome, for example Brugada syndrome, in a subject. In some embodiments, the methods include selecting a subject with Brugada syndrome and administering to the subject an effective amount of an agent that increases the expression or activity of SIRT1 in the subject. In some embodiments, the agent increases Nav1.5 activation. In some embodiments, the agent increases the expression or activity of SRIT1 and increases Nav1.5 activation.

Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, and in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. Antiviral activity of enzyme inhibitors is demonstrated.

Abstract: The present invention relates to biodegradable biocide agents against marine woodborers. In particular, the present invention relates to novel slow releasing biocide impregnating solutions against marine woodborers, and methods of creating anti marine woodborer environments.

Abstract: A composition and a method of treatment utilizing a combination of statins (or HMG-CoA reductase inhibitors), a class of drug used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught.

Abstract: The present invention relates to prodrug derivatives of pentamidine, their use in the treatment and/or prophylaxis of diseases such as tumor diseases, as well as leishmaniasis, trypanosomiasis, pneumocystis carinii pneumonia (PcP), and malaria.

Abstract: A method of preventing or inhibiting L-cystine crystallization is disclosed, using the compounds of formula I: R1a—[O]v-(-A-L-)m-A-[O]v—R1b??I wherein A, L, R1a, R1b, m, and v are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to L-cystine crystallization, such as comprising (but not limited to) kidney stones.

Abstract: The present invention relates to a pharmaceutical composition for treating wounds or revitalizing skin comprising the Euphorbia kansui extract, the fractions thereof, or the diterpene compound isolated therefrom as an active ingredient. The Euphorbia kansui extract may act on epithelial cells to induce PKD1 activity required for improving the reproduction capability of differentiated epithelial cells, and thus may induce the phosphorylation of lower ERK1 and the generation of Cycline D, thus exhibiting an excellent ability to activate the reproduction of damaged skin. Therefore, the Euphorbia kansui extract may be used effectively as an active ingredient in a pharmaceutical composition for treating wounds or reproducing skin, a health food for recovering skin damage or reproducing skin, or a functional cosmetic for inducing skin cell activity.

Abstract: Pharmaceutical compositions of colchicine for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined or desired release profile. Methods of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are also provided.

Abstract: The invention provides compositions, kits, and methods for treatment of neuronal injury. In one embodiment, the composition comprises a biomembrane sealing agent, such as PEG, and a bioactive agent, such as a magnesium compound. The biomembrane sealing agent and/or the bioactive agent an intravenous administration, an intramuscular administration, an intrathecal administration, a subcutaneous administration, an epidural administration, a parenteral administration, a direct application onto or adjacent to a site of the pathological condition, and any combinations thereof. Alternatively, the biomembrane sealing agent and/or the bioactive agent may be delivered from a pump or an implant.

Abstract: The invention relates to prodrugs of vitamin K2, in particular prodrugs of MK-7 in which the diketone is converted to a monosubstituted or disubstituted ester type derivative. These compounds are shown to give MK-7 in plasma.

Abstract: This invention relates to pharmaceutical compounds and nutritional supplements that are acetylated derivatives of naturally occurring amino acids and acetylated derivatives of peptides derived from naturally occurring amino acids containing hydroxyl groups. They are as useful as anti-platelet drugs, and as nutritional supplements.

Abstract: A method of preventing or inhibiting L-cystine crystallization is disclosed, using the compounds of formula I: R1a—[O]v-(-A-L-)m-A-[O]v—R1b??I, wherein A, L, R1a, R1b, m, and v are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to L-cystine crystallization, such as comprising (but not limited to) kidney stones.

Abstract: The present invention relates to a method of stabilising a tear film in an individual having an ocular surface inflammatory disorder by providing a compound to an ocular surface of the individual to reduce the synthesis of a cholesterol by a meibum-producing tissue.

Abstract: The present invention relates to an injenane-type diterpene compound derived from Euphorbia kansui Liou, and a pharmaceutical composition for treating or preventing viral infectious diseases, a health functional food for preventing or ameliorating viral infectious diseases and a composition for enhancing the production of interferon-gamma, which comprise the injenane-type diterpene compound. Furthermore, the present invention relates to a method for preventing or treating viral infectious diseases including administering the composition to a subject having a viral infectious disease occurrence or a risk thereof with a therapeutically effective dose.

Abstract: The present invention relates to a compound characterized by the following Formula I: or a pharmaceutically acceptable salt thereof, wherein X, Y, and Z are as described herein. Compounds of the present invention are useful for the treatment of HIV.

Abstract: The present invention relates to novel pharmaceutical combinations with synergistic action of diacerein or a pharmaceutically acceptable salt of diacerein and non-steroidal inflammatory drugs, having analgesic, anti-inflammatory, antipyretic, and osteoarthritis-treating activities.

Abstract: Compounds having a structure of Structure I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R1, R2, R3, R4, R5, J1, J2, X, Z, n1 and n2 are as defined herein, and wherein at least one of R1, R2 or R3 is an alkyl, alkenyl, aryl or aralkyl ester, are provided. Uses of such compounds for treatment of various indications, including prostate cancer, as well as methods of treatment involving such compounds are also provided.

Abstract: An aqueous suspension of a hydrophobic nutrient is disclosed. In particular, the nutrient, in ester form, is combined with a selected dispersion aid and a dispersion agent(s), and then dispersed in an aqueous medium to form the suspension.

Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the therapeutic and/or prophylactic treatment of, inter alia, dermatitis.

Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, skin cancer.

Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.

Abstract: Disclosed herein are methods and compositions for the diagnosis and treatment of Vascular Associated Maculopathy, or a symptom thereof, in a subject. Disclosed herein are methods and compositions for the diagnosis and treatment of one or more symptoms associated with Vascular Associated Maculopathy Disclosed in a subject. Disclosed herein are methods and compositions for the diagnosis and treatment of severe maculopathy or last stage maculopathy in a subject. Disclosed herein are methods and compositions for the diagnosis and treatment of resolving aberrant choriocapillaris lobules in a subject.

Abstract: The present invention relates to novel formulations comprising ezetimibe as active ingredient. In particular the invention relates to a pharmaceutical composition comprising 5 to 20 wt-% ezetimibe, 50 to 85 wt-% diluent, 3 to 25 wt-% disintegrant, 1 to 10 wt-% binder, and 0.5 to 1 wt-% lubricant, characterized in that the ezetimibe has a particle size distribution of d(0.9) of 5 ?m to 35 ?m and d(0.5) of 3 ?m to 20 ?m, as well as methods for preparing said formulations.

Abstract: The present invention relates to stilbene and quinine compounds related to combretastatin A-4 and their use as anticancer compounds and prodrugs. The compounds include those with an alkyl group on the double bond of cis- or trans-stilbenes, compounds with one or more (and preferably 2 or 3) alkyl group substituents on the stilbene A ring, compounds with an alkoxy group other than methoxy at position 3, 4, and/or 5 of the stilbene A ring, compounds (or prodrugs) in which BBOC amino acid esters are formed with the phenolic hydroxyl at the 3-position of the B ring and compounds (or prodrugs) based on a benzoquinone B ring. The present invention further relates to the photochemical reactions of stilbene compounds, either the above compounds disclosed for the first time herein or compounds based on prior stilbenes.

Abstract: Methods for treating abnormal glycosylated hemoglobin (HbA1c) levels in a patient in need thereof, wherein the provided methods comprise administering to a patient in need a therapeutically effective amount of an Interleukin-1? modulator. Also, the invention provides compositions comprising at least one lipid modifying agent and an IL-1? modulator.

Abstract: Compounds, ceramide analogues, having a cyclic structure derived from cyclopropane, cyclobutane or cyclopentane, the ring bearing two chains consisting of an amide function. Each amide function is attached to the ring by the nitrogen atom of the function and carries a hydrocarbon chain derived from a fatty acid. The amide functions can be cis or trans relative to one another. Processes for the preparation of these novel compounds as well as pharmaceutical and/or cosmetic compositions containing them.

Abstract: The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.

Abstract: The present application relates to compositions and methods for treating a proliferative disorder by administering to a subject a pharmaceutical composition of a dual kinase inhibitor. Catecholic butanes cane serve as dual kinase inhibitors for purposes of methods described herein. Subjects can be further treated by co-administering an EGFR inhibitor. The present application also relates to analyzing a sample with respect to levels of IGF-1R and EGFR and comparing levels of IGF-1R and EGFR to a control. Patients can be selected for treatment with a catecholic butane based on the assessment; optionally, patients can be further treated with an EGFR inhibitor, an IGF-1R inhibitor, or both.

Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment, particularly for reducing the risk of cardiovascular disease, especially coronary heart disease (such as myocardial infarction) and stroke. For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents and kits for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents and kits for their detection.

Abstract: The present invention relates to novel substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss, muscle loss, acne and hirsutism.

Abstract: This disclosure relates to novel compounds containing an H2S releasing moiety and a nitric oxide (NO) releasing moiety covalently linked with a core (e.g., a salicylic acid moiety) and the use of such compounds in treating inflammatory diseases, including cancers. Therapeutic potency of these compounds is significantly higher than NSAIDs containing a H2S-releasing moiety alone (HS-NSAIDs) and NSAID containing a NO-releasing moiety alone (NO-NSAIDs). The compounds, in addition, exhibit reduced side effect, e.g., reduced stomach ulcers, upon administration.

Abstract: The present invention is based on the discovery of genetic polymorphisms that are associated with cardiovascular disorders, particularly acute coronary events such as myocardial infarction and stroke, and genetic polymorphisms that are associated with responsiveness of an individual to treatment of cardiovascular disorders with statin. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.

Abstract: The invention provides novel lipophilic dopamine derivatives with improved stability and physiological half-life. The compounds may be used for organ and tissue preservation during storage and transport, or in the pre-treatment of organ and tissue donor or recipients. Moreover, they may be used as therapeutic agents for the prevention or treatment of ischaemia-related pathological conditions.

Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.