Abstract: Compounds and pharmaceutical compositions containing such compounds having formula I are provided: where R1, R2a, R2b, R3, R4, and R5 are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including anxiety and mood disorders such as depression.

Abstract: The invention relates to the improvement of visual performance, particularly of visual performance in the darkness, by administration of a colorant that is capable of being incorporated into eye tissue and/or causing yellowing of eye tissue, especially carotenoids, such as lutein and zeaxanthin.

Abstract: Methods and compositions for the treatment or prophylaxis of a disorder associated with platelet activation or enhanced thrombin activity are provided, that include the administration of an effective amount of a compound of the formula: or its pharmaceutically acceptable salt, ester or prodrug, wherein the substituents are defined herein, optionally in the appropriate pharmaceutically acceptable carrier for the route of administration selected.

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: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.

Abstract: Aspects of the present application relate to pharmaceutical formulations comprising a nonsteroidal anti-inflammatory drug, together with a proton pump inhibitor drug, to reduce the incidence of gastrointestinal complications associated with chronic therapy with a nonsteroidal anti-inflammatory drug. Specific aspects of the application relate to fixed dose combinations comprising aspirin, or a derivative thereof, and omeprazole or esomeprazole, or pharmaceutically acceptable salts, solvates, or hydrates thereof.

Abstract: The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK.

Abstract: Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.

Abstract: The present invention provides a glycolipid-containing liposome. In such a glycolipid-containing liposome, the glycolipid includes a plant ceramide portion and a sugar chain portion. The present invention also provides a method of producing a glycolipid-containing liposome. This method includes the following steps of: A) providing a glycolipid in which the glycolipid includes a plant ceramide portion and a sugar chain portion; and B) mixing the provided glycolipid with a liposome raw material and subjecting the mixture to conditions in which a liposome is formed.

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: 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 provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.

Abstract: Based on the discovery that celastrol and gedunin are Hsp90 inhibitors, the present invention provides novel inhibitors of Hsp90. and pharmaceutically acceptable salts, derivatives, and compositions thereof. The invention provides two classes of compounds. One class includes celastrol and its derivatives. The other class includes gedunin and its derivatives. The present invention further provides methods for treating disorders wherein Hs?90 inhibition is desired (e.g., proliferative diseases, cancer, inflammatory diseases, fungal infections, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. Celastrol, gedunin, and derivatives thereof are particularly useful in the treatment of prostate cancer, breast cancer, ovarian cancer, lung cancer, and leukemia.

Abstract: The present invention discloses certain novel prodrugs of chloramphenicol or thiamphenicol, or of an analog of either, including prodrugs of pharmaceutically acceptable salts of chloramphenicol or thiamphenicol or of their analogs, including nitrogen-containing esters of both alcohol groups of such compounds. In certain embodiments these novel prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol or thiamphenicol or of an analog of either. In one embodiment, a certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing the active compound in question.

Abstract: This invention provides compounds having the structural formula: wherein: R1 is an acyl or sulfonyl group, R2 is an acyl group selected from the group consisting of acyl groups derived from cycloaliphatic, aromatic or heterocyclic monocarboxylic acids, imidazolylcarbonyl and triazolylcarbonyl, and R3 is hydrogen or an amino-protecting group, a stereoisomer thereof, a solvate thereof, or a salt thereof, being useful as anti-inflammatory agents and anti-cancer agents.

Abstract: The presently disclosed subject matter provides compounds of the formula, formula (Ia): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, and n are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting acid ceramidase and ceramidase-related activity, and their use as drugs and prodrugs in the treatment and/or prevention of diseases associated with undesirable ceramidase or sphingosine kinase activity, including, but not limited to, cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, asthma, and atopic dermatitis.

Abstract: The present invention provides methods of treating type II diabetes using combinations of diacerein or its derivatives with other antidiabetic agents. The methods may also allow improving glycemic control of type II diabetes patients and/or reducing side effects and/or cardiovascular risks of antidiabetic agents.

Abstract: The present invention relates to methods and compositions of treating or preventing inflammatory diseases or conditions in a patient comprising administering to the patient a therapeutically effective amount of a composition comprising a glutathione donor, 5-amino 4-imidazolecarboxamide ribotide (AICAR), a 3-hydroxy-3-methylgluatryl-coenzymeA (HMG-CoA) reductase inhibitor, D-threo-1-Phenyl-2-decanoylamino-3-morpholino-1-propanol HCl (D-PDMP), and/or 1,5-(butylimino)-1,5-dideoxy-D-glucitol (Miglustat), or derivatives thereof.

Abstract: The present invention is directed to a process for producing non-genotoxic Diacetylrhein (Diacerein), comprising: i) transformation of raw Diacerein (or raw Rhein), into a water-soluble salt; ii) adsorption of the salt Diacerein (or Rhein) solution on a hydrophobic resin; iii) washing with an appropriate solvent to eliminate the impurities (in particular the genotoxic impurities); iv) elution to recover Diacereinor Rhein; v) if the process is applied to Rhein, its transformation to Diacerein by acetylation; vi) acidification of purified Diacerein and its recovery, and drying. The invention is also directed to non-genotoxic Diacerein obtained by the process of the invention, in which the total content of genotoxic impurities is below 1 ppm, and suitable for the preparation of pharmaceutical formulations, in particular capsules, for human and veterinary use, in agreement with the current Health Authorities request.

Abstract: This present invention provides methods and kits for identifying patients at risk of suffering from a drug induced liver injury, particularly for an antioxidant drug, or for identifying patients who are suffering from early stages of a liver disorder by assessing the levels of apolipoprotein in a sample of the patient and comparing that to a reference value. The reference value is predetermined by identifying a population sample and determining an upper limit of normal value. This value is then used as a reference point for comparison of apolipoprotein levels from patient samples. In one embodiment, apolipoprotein levels are combined with ATL and/or total bilirubin levels for predicting liver damage, hepatotoxicity or hepatic events after drug administration.

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, rosacea.

Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the biphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular biphenyl-substituted cyclic ketoenols through the addition of ammonium or phosphium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or nematicides and/or acaricides and/or fungicides and/or for preventing unwanted plant growth.

Abstract: This invention discloses drug-delivery compositions, methods of making prodrugs, and methods of drug delivery using a self-assembled gelator. The backbone of the gelator can contain a drug or prodrug, such as acetaminophen or salicin. Additional drugs or agents can be encapsulated in the gelator. Enzymatic or hydrolytic cleavage can be used to release the drugs.

Abstract: This invention provides compound having a structure of Formula I or Formula II. 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: The present invention relates to a method for treating and screening for compounds for the treatment of sepsis. More specifically, the treatment and screening methods are based on the discovery that granzyme B containing platelets (GzmB-platelet) causes apoptosis by direct contact with cells.

Abstract: There is described a pharmaceutical composition for controlled release of an active compound wherein the active compound is selected from the group comprising tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth subsalicylate, enofelast, triflusal, ketorfanol, indriline, furofenac, cizolirtine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof for the treatment or alleviation of depression. More particularly, there is described an abuse resistant pharmaceutical composition for the treatment of inter alia, depression and controlled release pharmaceutical compositions of related thereto.

Abstract: The invention provides a long acting curcumin derivative, preparation method and pharmaceutical use thereof, wherein said long acting curcumin derivative having the general structural formula disclosed herein, wherein R1 and R2 are hydrogen or methoxyl; R3 and R4 are each independently selected from C1-C50 alkyl. Compared with cuminoids, the inventive long acting curcumin derivative has a better release effect, a higher bioavailability and pharmaceutical activity, and thus can be useful for the treatment of diseases such as depression and cancer.

Abstract: A novel therapy regime/regimen for the treatment of acne related diseases includes administering a topical fixed-dose combination of a retinoid and an anti-bacterial agent, such as BPO, to a course of oral antibiotic therapy.

Abstract: Cancer patients, patients with cognitive dysfunction, or patients with pulmonary hypertension are treated with parenterally administered therapeutic doses of statins. Particularly, transdermal, injection employing liquid infusion or particles are employed. For cancer, the statins may be used by themselves or in conjunction with a chemotherapeutic regimen. Liver cancer is treated orally with super doses of statins.

Abstract: Diabetes consists of a worldwide public health concern that leads to high levels of morbidity and premature mortality and affects millions of people in countries of any level of development. It is estimated that there are more than 150 million people with diabetes in the world, wherein projections from the World Health Organization (WHO) for 2025 such amount may get to 300 million cases. The present invention refers to a process for obtaining an extract rich in rosmarinic acid (RA) from the plant Origanum vulgare and its use as a possible oral hypoglycemic agent for the treatment of diabetes.

Abstract: The invention relates to liquid pharmaceutical compositions for oral administration comprising rhein or diacerein, or salts or esters or prodrugs thereof and processes for preparing such compositions.

Abstract: The subject matter of the invention is a cosmetic and/or dermatological composition for use in the treatment of skin and/or hair disorders. More particularly, the invention relates to a cosmetic and/or dermatological composition comprising an inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, an inhibitor of farnesyl pyrophosphate synthase, or an inhibitor of one of the physiologically acceptable salts thereof and a cosmetic and/or dermatological product. The present invention finds, for example, a very advantageous use in the treatment of the effects of early ageing, in particular in terms of the skin and the hair system.

Abstract: The present invention provides compositions having, as active ingredients, a stilbene derivative and a platinum coordination compound which is highly efficacious and highly safe for treating tumors, particularly for the treatment of solid or malignant tumors and thus methods of cancer and tumor treatment using the composition are also provided.

Abstract: The unexpected expression of tryptophan 2,3-dioxygenase (TDO2) in cancer cells and tumors has been established. Methods for diagnosing cancer based on the expression of TDO2 are provided, as are methods for treating cancer and inhibiting the growth of cancer cells by inhibiting TDO2, as well as pharmaceutical compositions.

Abstract: The present invention relates to the use of a compound of Formula (I??) or pharmaceutically acceptable salt or solvate, isomer or prodrug thereof in the manufacturing of a medicament for the treatment and/or prophylaxis of arthritis and pain.

Abstract: The present invention relates to a compound of the formula: R-AR—O—Y—R? Wherein R represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid, —NO2, —NH2, —NHCOCH3, and —NH—Y—R?, which is attached directly to AR or attached through an aliphatic chain. The carboxylic acid moiety in R includes but is not limited to the following carboxylic acids: benzoic acids, cinnamic acids, ferulic acid, caffeic acid, syringic acid, salicyclic acid, vanillic acid, phenylacetic acids, phenylpropionic acids, and sinapinic acid. -AR—O— is a biologically active phenolic moiety comprising 1 to 6 substituted or unsubstituted aryl rings that are directly bonded to each other, fused together, or joined through a linking group.

Abstract: The invention discloses a compound of formula (I) wherein, at least one of R1, R2, R3 and R4 is —C(?O)Rn and R1, R2R3 and R4 are H or CH3 and Rn is alkyl or alkenyl group. The alkenyl group have one or more number of double bonds either in cis form or trans form or both. In Rn, where n is 12 to 30 carbons; and pharmaceutically acceptable salt thereof. The said alkenyl groups are preferably selected from the group consisting of eicosapentaenoic acid (EPA) or DHA (docosahexaenoic acid). This invention further discloses processes for their preparation of compounds of formula I and pharmaceutical compositions that contain these compounds.

Abstract: The use of HMG-CoA reductase inhibitors (e.g., statins) to treat glaucoma, control intraocular pressure, preserve the trabecular meshwork, protect against ocular neurodegeneration and/or protect against glaucomatous retinopathy is described. The preferred HMG-CoA reductase inhibitors, which are statins having an RI value of 0.2 to 0.7 (e.g., pravastatin), are administered via topical application to the affected eye(s) of the patient.

Abstract: Embodiments of the present invention concern methods, compositions and uses thereof, relating to at least one of vitiligo, or vitiligo-associated autoimmune/autoinflammatory disease (VAAAD). In particular embodiments, genetic variations in the NALP1 gene are of use to detect, diagnose, predict the risk of or treat at least one of vitiligo or VAAAD. In more particular embodiments, the presence of genetic variations such as single-nucleotide polymorphisms (SNPs) in NALP1 genetic region are of use to detect, diagnose or predict the risk of VAAAD. In other embodiments, inhibitors targeted to NALP1, caspase-1 or caspase-5, ASC (PYCARD), interleukin-1?, interleukin-1? receptor, or interleukin 18 may be administered to a subject to treat VAAAD.

Abstract: Disclosed is a cooling sensation agent composition or sensory stimulation agent composition which contains at least one of diester compounds of dicarboxylic acid represented by the formula (1) wherein A represents CH2 or CH?CH, n represents an integer of 0 to 4 when A is CH2, or 1 when A is CH?CH, B is an alcohol residue having 10 to 18 carbon atoms and containing a para-menthane skeleton, which may have a substituent, and C is an alcohol residue having 6 to 18 carbon atoms, which may have a substituent as well as a flavor or fragrance composition, a beverage, a food product, a perfume or cosmetic product, a toiletry product, daily utensil products or groceries, a fiber, a fiber product, clothes, clothing or a medicine, wherein the cooling sensation agent composition or the sensory stimulation agent composition is compounded.

Abstract: Dietary supplement compositions are disclosed. Methods of making and using dietary supplement compositions are also disclosed.

Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.

Abstract: Described herein are microneedle drug delivery systems comprising a pharmaceutical compositions comprising pharmaceutically active agents (e.g., cannabidiol and prodrugs of cannabidiol) and microneedle arrays suitable for local and systemic delivery of the active agent to a mammal. Also described herein are methods of using a microneedle transdermal or topical drug delivery systems comprising pharmaceutical compositions, comprising cannabidiol and prodrugs of cannabidiol, and microneedle arrays in the treatment disease, including pancreatitis and pancreatic cancer.

Abstract: Compositions and methods for modifying biologically active substances to achieve multi-day delivery of such substances, particularly through oral or parenteral administration, are disclosed. The compositions include the biologically active substance conjugated to a carrier having a suitably long half life, typically more than one day, wherein the conjugate optionally contains a spacer linking the carrier to the biologically active substance. Pharmaceutical formulations of the conjugates are also disclosed, as are methods of extending delivery of a single dose of a biologically active substance for more than one day.

Abstract: Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing pulmonary arterial hypertension and/or stable angina. More particularly, aspects of the present invention are related to therapeutic combinations comprising a Rho-kinase inhibitor, such as fasudil, and one or more additional compounds selected from the group consisting of prostacyclins, such as iloprost, endothelin receptor antagonists, PDE inhibitors, calcium channel blockers, 5-HT2A antagonists, such as sarpogrelate, selective serotonin reuptake inhibitors, such as fluoxetine, statins, and vascular remodeling modulators, such as Gleevec.

Abstract: The present invention provides methods and compositions for preventing platelet aggregation and for treating individuals suffering from conditions or undergoing procedures that may result in unwanted platelet aggregation. In particular the invention provides to methods and compositions for arterial vessel pacification. The methods are based on the administration of a therapeutically effective amount of a glycoprotein IIb/IIIa receptor antagonist, e.g., xemilofiban. The treatment may commence prior to a medical or surgical procedure or an outbreak of a condition, either of which results in the activation of platelets that may lead to thrombus formation, and may continue thereafter.

Abstract: A process is described for the preparation of a pharmaceutical comprising an active pharmaceutical ingredient capable of existing in multiple polymorphic forms, wherein the process comprises a step of preparation of a wet phase comprising the active pharmaceutical ingredient and microcrystalline cellulose and a liquid, wherein in the wet phase has a weight ratio of active pharmaceutical ingredient to microcrystalline cellulose above 1.0 or a weight ratio of active pharmaceutical ingredient to liquid above 1.0.

Abstract: The invention concerns a new process for the preparation of high purity diacerein, by oxidisation of the protected aloe-emodin in the presence of an oxidising system and radical catalyst and subsequent substitution of the protector groups with acetyl groups.

Abstract: Novel ester derivatives of ascorbic acid and 2-keto-acid saccharides are provided wherein the ester is introduced by ester bond formation between at least one hydroxy-functionality on the ascorbic acid or 2-keto-acid saccharide and a carboxy-functional organosiloxane, or between a 2-keto-gulonic acid and a hydroxy-functional organosiloxane, as well as methods for their synthesis. Treatment, cosmetic, and personal care formulations comprising the novel esters are also provided, including controlled release forms thereof.

Abstract: Methods and systems are provided for diagnosing male infertility relating to inadequate production of phosphatidic acid and are complementary to the routine tests, assessing sperm count, motility, viability, head morphology, and white blood cell count. Additional therapeutic methods, compositions and dosage forms are provided for treating male infertility that is related to inadequate production of phosphatidic acid. Such therapeutic approaches involve the use of phosphatidic acid or at least one of its precursors in the sperm intracellular signaling pathway.