Abstract: Provided herein are compositions and methods that inhibit expression of Adam12 gene products, such as ADAM12 mRNA and/or ADAM12 polypeptides, as a therapeutic approach for the treatment of, or promotion of healing of, wounds.

Abstract: The present invention relates to a new compound of salvianolic acid L, its preparation method, a pharmaceutical composition containing the salvianolic acid L, and its use for preparing a medicament for treating cardio-cerebrovascular diseases.

Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.

Abstract: Biphenyl compounds having the formula (I): are useful for preventing/treating pathologies linked to a deficiency of the activation of the RAR gamma receptor, e.g., for treating a pathology linked to a cell differentiation and/or proliferation disorder, for treating acne, for treating psoriasis.

Abstract: The invention provides a method for determining a dose and dosing schedule, and making dose adjustments of patients taking PBA prodrugs as nitrogen scavengers to treat nitrogen retention states, including ammonia accumulation disorders as well as chronic renal failure, by measuring urinary excretion of phenylacetylglutamine and/or total urinary nitrogen. The invention provides methods to select an appropriate dosage of a PBA prodrug based on the patient's dietary protein intake, or based on previous treatments administered to the patient. The methods are applicable to selecting or modifying a dosing regimen for a subject receiving an orally administered waste nitrogen scavenging drug, and to monitoring patients receiving such drugs.

Abstract: The invention relates a pharmaceutical composition comprising a combination of: (i) the AT 1-antagonist valsartan or a pharmaceutically acceptable salt thereof; and (ii) a NEP inhibitor or a pharmaceutically acceptable salt thereof and optionally a pharmaceutically acceptable carrier and to a method for the treatment or prevention of a condition or disease selected from the group consisting of hypertension, heart failure, such as (acute and chronic) congestive heart failure, left ventricular dysfunction and hypertrophic cardiomyopathy, diabetic cardiac myopathy, supraventricular and ventricular arrhythmias, atrial fibrillation, atrial flutter, detrimental vascular remodeling, myocardial infarction and its sequelae, atherosclerosis, angina (whether unstable or stable), renal insufficiency (diabetic and non-diabetic), heart failure, angina pectoris, diabetes, secondary aldosteronism, primary and secondary pulmonary hypertension, renal failure conditions, such as diabetic nephropathy, glomerulonephritis, scler

Abstract: Provision of a pharmaceutical product, a quasi-drug, a food, a beverage, a pet food, a feed, and others which are highly safe, have excellent action of promoting energy consumption, promoting fat burning, promoting carbohydrate burning, or improving an effect of exercise, and which are effective for the prevention or amelioration of obesity or metabolic syndrome or the improvement of motor functions. An agent for promoting energy consumption, an agent for promoting fat burning, an agent for promoting carbohydrate burning, an agent for improving an effect of exercise, an agent for improving motor functions, an agent for inhibiting acetyl-CoA carboxylase 2, and an agent for inhibiting pyruvate dehydrogenase kinase 4 containing chlorogenic acids or salts thereof as an active ingredient.

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: Provided herein are organoselenium compounds and pharmaceutical compositions thereof. Also provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders using the compounds and pharmaceutical compositions provided herein.

Abstract: This invention generally relates to compositions and methods for treating myelodysplastic syndrome. In one embodiment, this invention relates to methods for treating myelodysplastic syndrome with ezatiostat or a salt thereof and lenalidomide.

Abstract: Methods, compounds, and topical formulations for reduction of skin sagging, creasing and/or wrinkling are disclosed. The methods comprise topically applying a composition comprising an ?2 adrenergic receptor agonist. Amelioration of skin sagging, creasing and/or wrinkling begins within minutes after topical application of a disclosed composition. A single application can significantly reduce skin sagging, creasing and/or wrinkling for at least about 8 hours.

Abstract: The invention relates to the medical field, more precisely in the field of anti-cancer treatment and treatment of Alzheimer's disease, Parkinson's disease or Pick's disease or for ameliorating symptoms of Down syndrome, providing newly synthesised multi-vanilloyl derivative compounds and their use in the treatment of said disorders.

Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

Abstract: Biphenyl compounds having the formula (I): are useful for preventing/treating pathologies linked to a deficiency of the activation of the RAR gamma receptor, e.g., for treating a pathology linked to a cell differentiation and/or proliferation disorder, for treating acne, for treating psoriasis.

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: Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.

Abstract: An improved composition for skin cleansing and protection is disclosed. The composition contains an effective amount of at least one alpha-hydroxyl acid or a pharmaceutically acceptable salt thereof, at least one base, one surfactant and one skin protectant. Various additives and excipients may be included in the formulation. The improved composition disclosed herein achieves a higher bacteria killing rate and shows longer action duration. The disclosed composition is capable of penetrating deep into the skin which allows for delivery of more anti-microbials to sites that are at a higher risk of being infected. Various modifications of the improved composition are also disclosed.

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, actinic keratosis.

Abstract: Said invention refers to a pharmaceutical form for selective colon delivery of drugs or bioactive molecules degraded and/or poorly absorbed in the gastrointestinal tract. The system comprises a core consisting of the active ingredient, and a protease inhibitor layer and/or an absorption enhancer layer, said core being separated from these layers by means of a polymer that swells and/or dissolves and/or is degraded when in contact with the biological fluids present in the gastro-intestinal tract; depending on the thickness of the polymeric layer, the release of the drug can be modulated with respect to the inhibitor and/or promoter.

Abstract: The present invention relates to compositions comprising a combination of PKC activators and PKC inhibitors and methods to modulate ?-secretase activity; improve or enhance cognitive ability; and/or reduce neurodegeneration in individuals suffering from diseases that impair cognitive ability, particularly Alzheimer's Disease. The invention also relates to methods for improving or enhancing cognitive ability. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP (sAPP) comprising the activation of protein kinase C (PKC) in the brain and inhibiting PKC in peripheral tissues. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are preferred PKC activators and Vitamin E is a preferred PKC inhibitor for use in the inventive composition.

Abstract: Disclosed are new colchicine solid complexes, methods of making the solid complexes as well as formulations prepared therefrom and uses thereof.

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: A composition having an agent adapted to affect a multimeric protein by binding to a binding site of the multimeric protein and thereby affecting an equilibrium of units, wherein the multimeric protein has an assembly having a plurality of said units, wherein each of the units has a first complementary surface and a second complementary surface and wherein the first complementary surface of one unit is associated with the second complementary surface of another unit, provided that the assembly is at least one of different quaternary isoforms on a condition that in the multimeric protein (1) a structure of each of the units determines a structure of the different quaternary isoforms, (2) the units are in the equilibrium and (3) the structure of the different quaternary isoforms influences a function of the multimeric protein.

Abstract: The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.

Abstract: The present invention is successful in providing caffeic acid derivatives namely eicosanyl caffeate and docosyl caffeate from Glycyrrhiza. Also, the present invention provides a composition comprising said bio actives and also provides a process to prepare the composition. Ultimately, the invention provides solution for the management of ulcer.

Abstract: Therapeutic compounds, methods, and compositions are disclosed herein for treating glaucoma and baldness in mammals. The specific compounds are described herein and are modified prostaglandin derivates.

Abstract: Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.

Abstract: There is provided an anti-degradation agent capable of exhibiting an excellent deterioration-inhibiting property for foods, cosmetics, etc., showing a good effect even when added in a small amount, having a high heat resistance, and being free from adverse influence due to light. There are provided (1) an anti-degradation agent comprising a water-insoluble antioxidant, a water-soluble antioxidant and an emulsifying agent; and (2) an anti-degradation agent comprising a water-soluble antioxidant, and carnosol and/or carnosic acid wherein a total content of the carnosol and the carnosic acid is not less than 4% by weight.

Abstract: The present invention relates to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, and more particularly, to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, including a first step of dissolving a biodegradable polymer in a non-volatile polar organic solvent, a second step of adding poorly soluble drugs to water and the biodegradable polymer solution to produce a dispersion, and a third step of adding the dispersion to emulsifier solutions in a batch under the condition of low mechanical energy level stirring.

Abstract: (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.

Abstract: Synthetic polyphenolic compounds of formula (I), their modes of synthesis, and pharmaceutical compositions thereof are provided herein. Use of the compounds and compositions described herein for inhibiting proteasomal activity and for treating cancer is also provided.

Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.

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: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.

Abstract: Described is the use of benzotropolone and their derivatives, especially the compounds of formula (1); wherein R2, R3, R4, R5 and R6 independently of one another are hydrogen; OH; C1-C30alkyl, C2-C30al-kenyl, C1-C30alkoxy, C3-C12cycloalkyl or C1C30hydroxyalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C6-C20aryl, which may be substituted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G, C2-C18alkenyl, C2-C18alkynyl, C7-C25aralkyl, CN, or —CO—R17; C1-C30mono- or dialkylamino; COR9; COOR9; CONR9R10; CN; SO2R9; OCOOR9; OCOR9; NHCOOR9; NR9COR10; NH2; *—(CO)—NH—(CH2)n1—(PO)—(OR11)2; —(CO)—O—(CH2)n1—(PO)—(OR11)2; sulphate; sulphonate; phosphate; phosphonate; —(CH2)n2—[O—(SO2)]n3—OR11; —O—(CH2)n4(CO)n5—R11; —(O)n6—(CH2)n7—(PO)—(OR9)2; —(O)n6—(CH2)n7—SO2—OR9; halogen; organosilanyl; organo-siloxanyl; or a sugar residue linked directly in an ?- or ?-mode via the anomeric oxygen to the benzotropolone system or via a linear or branched alkylene, alkenyle

Abstract: The present invention relates to supporting weight management, weight loss and/or to the prevention and/or treatment of metabolic disorders. In particular the present invention relates to preventing and/or treating metabolic disorders by modulating, in particular reducing the amount of proteobacteria and/or deferribacteres in the gut. One embodiment of the present invention relates to the use of a primary composition comprising an agent that reduces the amount of proteobacteria, preferably gamma-proteobacteria, even more preferred enterobacteria; and/or deferribacteres in the gut for the preparation of a composition to treat or prevent metabolic disorders, to support weight loss and/or to support weight management.

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

Abstract: Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

Abstract: Pharmaceutical compositions and oral dosage forms of (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and methods of treating diseases comprising orally administering such pharmaceutical compositions and dosage forms are disclosed.

Abstract: Methods for modulating the level of a chemokine in a cell by administering to a cell an effective amount of a depside or an anthocyanin are provided. More particularly, a method for modulating the level of a chemokine in a cell by administering to a cell an effective amount of a depside having the structure of formula (IV): Formula (IV) wherein R is selected from H or CH3 or an anthocyanin selected from cyanidin 3-glucoside, delphinidin 3-glucoside, or combinations thereof, or an enantiomer, optical isomer, diastereomer, N-oxide, crystalline form, hydrate, or pharmaceutically acceptable salt thereof is provided. Also provided are compounds according to Formulas I-IV, pharmaceutical compositions, unit dosage forms, and food or feed supplements containing such compounds.

Abstract: (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.

Abstract: The invention provides novel compounds of formula (I), wherein: R1 is a radical derived from one of the known ring systems; R2 is a phenyl radical optionally substituted; Xn represents a birradical selected from the group consisting of: —(CH2)1-4—, (C2-C4)-alkenyl, (C2-C4)alkynyl, —S—(CH2)1-3—#, and —(CH2)1-3—O—#; wherein the symbol # indicates the position at which Xn is attached to R1; Yn is a birradical selected from the group consisting of: —(CH2)2-4—, —S—(CH2)1-3#, and —O—(CH2)1-3—#; wherein the symbol # indicates the position at which Yn is attached to R2; and R3 is a radical selected from the group consisting of: —OR4. The compounds of formula (I) are useful in the treatment of cancer.

Abstract: The present invention relates to the use of lipophilic diesters of the chelating agent 1,2-bis(2 aminophenoxy)ethane-N,N,N?,N?-tetraacetic acid (BAPTA) for inhibition of proteolytic activities of certain metalloproteinases, calpain and TACE The invention further relates to methods for preventing, treating or managing TACE-related diseases or disorders in mammals comprising administering to a mammal in need thereof, a pharmaceutical composition comprising a therapeutically effective amount of said lipophilic diesters of the chelating agent BAPTA.

Abstract: The present invention relates to the field of therapeutic methods, compositions and uses thereof, that affect, directly or indirectly, the behavior of LRP receptors. These compositions and methods result in the treatment of inflammatory, immunological and metabolic conditions. More particularly, the methods and compositions of the invention are directed to the identification of small molecules, drugs and/or pharmacological agents that affect the Wnt pathway by affecting normal complex formation among various signaling receptors, the LRP5 and LRP6 receptor, and related ligands.

Abstract: The present invention provides methods and compositions for increasing the rate of nail growth in mammals, especially humans, using thyromimetic compounds.

Abstract: The present invention is related to a family of phenyl-prenyl derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or Parkinson's Disease. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the compounds of formula (I) for medical use, particularly for the use for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder, and to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder.

Abstract: The present invention, in one or more embodiments, comprises water-soluble derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecylcatechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising water soluble urushiol esters of general formula (I) Tolerizing and desensitizing mammals, including humans, to allergens contained in plants of the Anacardiaceae and Ginkgoaceae families is attained by administering a composition containing at least one water soluble urushiol ester compound.

Abstract: The present invention provides a method for treating a cancer in a subject involving administering to the subject a compound of formula (II) or (II?): wherein R1, R2, R3, R4, R5, R6 and R7 are independently H, OH, alkylcarbonyloxy, or a pharmaceutically acceptable salt thereof. Also provided is a compound of formula (II) or (II)?, wherein R1 and R2 are independently OH, alkoxy or alkylcarbonyloxy, R3 and R4 are independently H, OH, alkoxy or alkylcarbonyloxy, R6 is H, alkoxy or alkylcarbonyloxy, R5 is H, OH or alkylcarbonyloxy, R6 is H or alkoxy, and R7 is H, or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed herein are isolated compounds or pharmaceutically acceptable salts thereof, which exhibit immunostimulatory or anti-inflammatory effects. The compounds are isolated from the fruiting body of A. camphorata in a solid culture. Also disclosed are methods of stimulating immune responses and/or treating an inflammatory disorder with these compounds and pharmaceutical compositions including the compounds or pharmaceutically acceptable salts thereof.

Abstract: Sulfur-containing ligands and methods of their utilization for binding metals and/or main group elements and removing them from fluids, solids, gases and/or tissues are disclosed.