Abstract: A compound of formula (I-1) wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a —O—R12 group, wherein R12 is a C1-C7 alkyl, a group —CH2—O—CO—R5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group —O—R13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a —CH2— amine, R?1 represents a group chosen among hydrogen and —O—R14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.

Abstract: Derivatized coumarin-based pharmaceutical compositions and methods to use them are provided. The compositions are characterized in that they inhibit the activity of tumor-related CAIX and CAXII to a greater degree than they inhibit the activity of CAI and CAII. The compositions can be used to suppress tumor growth and/or suppress tumor metastases in a mammal.

Abstract: The present invention relates to self-emulsifying formulations based on an active ingredient component and a formulation base with a lipid component and with a binder component and to the use of this formulation as dosage form in the life science sector. The invention also describes a process for producing self-emulsifying formulations by mixing the formulation components to form a plastic mixture and, where appropriate, to manufacture the formulations as dosage form advantageously by use of melt extrusion. The formulations spontaneously form emulsions in water or aqueous media.

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 venous thrombosis). For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents 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 for their detection.

Abstract: The present invention is based upon the identification of regions within the NOTCH-1 receptor that, when mutated, lead to increase receptor signaling. The mutations are associated with uncontrolled cellular growth and this growth may be arrested using agents that interfere with NOTCH-1 activity, such as inhibitors of gamma-secretase. Assays for the NOTCH-1 mutations may be used diagnostically or as part of a treatment regimen for cancer patients.

Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.

Abstract: The present invention provides an enzymatic and a chemical synthesis of melanins and novel melanins.

Abstract: A skin care product comprising from about 0.001% to about 10% of a retinoid, in combination with 0.0001% to about 50% of a combination of retinoid boosters.

Abstract: The present invention provides a novel therapeutic combination comprising one or more anti-androgen agents and one or more antibiotic/anti-inflammatory agents or pharmaceutically acceptable salts or hydrates thereof, useful for the treatment of a dermatological disorder.

Abstract: The present invention provides a biocompatible composition that comprises a bioactive material and a method for using the same. In particular, the composition of the invention is useful for spatio and/or temporal release of the bioactive material. Specifically, the composition of the invention comprises at least one polymeric mixture layer comprising a plurality of biodegradable polymers. The polymeric mixture layer comprises a first biodegradable polymer and a second biodegradable polymer. The relative amount of the first biodegradable polymer or the second biodegradable polymer increases within the polymeric mixture layer in one direction, and the relative amount of the other biodegradable polymer decreases in the polymeric mixture layer in the same direction. The rate of degradation of the first biodegradable polymer is different from the rate of degradation of the second biodegradable polymer. In this manner, the composition allows spatio and/or temporal release of the bioactive material.

Abstract: A stent is provided in combination with delivery of a tocopherol agent, and in particular a des-methyl tocopherol agent, and further beneficially a gamma-tocopherol agent, so as to reduce restenosis along the vessel or other lumenal wall where the stent is implanted. In particular applications, the stent is an endolumenal stent, and more specific beneficial applications is an endovascular stent, and the gamma-tocopherol elutes from a coating or carrier coupled with the stent. Certain combinations are provided with the des-methyl-tocopherol or phytyl substituted chromanol, e.g. gamma-tocopherol, combined with an additional agent such as an anti-restenosis agent, e.g. sirolimus, tacrolimus, everolimus, or paclitaxel, in order to provide synergistic benefit to tissues along the stented or recanalized regions. Other forms of tocopherol or tocotrienol, or other phytyl substituted chromanols, and other compounds such as palm oil, are ailso contemplated. for use to treat restenosis.

Abstract: There is disclosed a combination of inhibitors of Tissue Transglutaminase (TG2), inhibitors of reactive oxygen species (ROS) and CFTR channel activators (potentiators) for separate, sequential or simultaneous administration to CF patients carrying the ?F508-CFTR mutation, and pharmaceutical compositions thereof.

Abstract: The embodiments herein provide a composition and a method of synthesizing a composition comprising an aliphatic amino acid biosynthesis inhibitor having an antifungal activity. The composition comprises 2-oxo-2H-chromen-7-yl propiolate, diethyl-hex-2-en-4-yne-dioate and dinonyl-hex-2-en-4-yne-dioate. The composition inhibits a biosynthesis of an aliphatic amino acid in a fungal biological system. The aliphatic amino acid is selected from a group consisting of leucine, isoleucine and valine. The composition is used with a concentration of 0-200 ?g/ml. The method comprises mixing solutions of dicyclohexylcarbodiimide (DCC) and Dimethylaminopyridine (DMAP) with alcohol, acetylene carboxylic acid and dichloromethane to obtain a mixture which is stirred filtered and washed with ether. The solvents are evaporated to obtain a residue that is dissolved in dichloromethane and stirred with a catalyst. The extra solvents are evaporated to obtain the derivative compound and purified by silica gel column chromatography.

Abstract: The present invention relates to compositions for the modulation of inflammation in connective tissues in humans and animals and the modulation of markers of such inflammation, including COX-2, TNF-a, IL-1 (3, iNOS, p38, and chemokines, comprising any or all of anabolic, anti-catabolic, anti-oxidant and analgesic agents, including aminosugars, S-adenosylmethionine, arachadonic acid, GAGs, including pentosan, collagen type II, tetracyclines or tetracycline-like compounds, diacerin, super oxide dismutase, L-ergothioneine, methyl sulfanylmethane, one or more avocado/soybean unsaponifiables, and an analgesic, e.g., acetaminophen, and to methods of treating humans and animals by administration of these novel compositions to humans and animals in need thereof.

Abstract: The embodiments herein provide a composition and a method of synthesizing a composition comprising an aliphatic amino acid biosynthesis inhibitor having an antifungal activity. The composition comprises 2-oxo-2H-chromen-7-yl propiolate, diethyl-hex-2-en-4-yne-dioate and dinonyl-hex-2-en-4-yne-dioate. The composition inhibits a biosynthesis of an aliphatic amino acid in a fungal biological system. The aliphatic amino acid is selected from a group consisting of leucine, isoleucine and valine. The composition is used with a concentration of 0-200 ?g/ml. The method comprises mixing solutions of dicyclohexylcarbodiimide (DCC) and Dimethylaminopyridine (DMAP) with alcohol, acetylene carboxylic acid and dichloromethane to obtain a mixture which is stirred filtered and washed with ether. The solvents are evaporated to obtain a residue that is dissolved in dichloromethane and stirred with a catalyst. The extra solvents are evaporated to obtain the derivative compound and purified by silica gel column chromatography.

Abstract: The present invention is based on the discovery of genetic polymorphisms that are associated with venous thrombosis. 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 present invention discloses a magnetic nanodrug for treating thrombosis, which comprises a core formed of magnetic nanoparticles, a shell enveloping the core and made of carboxyl-functionalized polyaniline, and a thrombosis-treatment drug covalently bonded to the shell. The magnetic nanodrug of the present invention is non-toxic to vascular endothelial cells, has superior stability, features superparamagnetism, and can be uniformly dissolved in water. Therefore, the magnetic nanodrug for treating thrombosis can be guided by an external magnetic field to concentrate on a specified region and increase the effect of thrombosis treatment.

Abstract: New pharmaceutical compositions extracted from Ferula assa-foetida are confirmed to effectively treat influenza A (H1N1) virus. The extraction method of the new pharmaceutical compositions mainly includes steps of: (a) extracting F. assa-foetida with methanol to obtain a crude extract; (b) fractioning the crude extract with n-hexane-methanol to obtain a methanol extract; (c) fractioning the methanol extract with chloroform-water to obtain a chloroform extract; and (d) chromatographing the chloroform extract to obtain the pharmaceutical compositions, which can be further fractioned and chromatographed to obtain various sesquiterpene coumarins.

Abstract: The invention relates to the use of a composition comprising at least one volatile molecule specific to the estrus of cows in order to improve the reproductive function of a bull. In particular, the composition according to the invention makes it possible to act on the libido of the bull, but also on the production of semen by the bull. Preferably, the composition used comprises at least one molecule from among coumarin, squalene, 6-amino undecane, 2-butanone, 9-octadecenoic acid and 1,2-dichloroethylene.

Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.

Abstract: The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering budiodarone to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of budiodarone and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of budiodarone may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling.

Abstract: A rodenticidal compound of formula (I): as well as the isomers thereof, in particular enantiomers, diastereoisomers, tautomers or mixtures of isomers in all proportions, where: R1 is: H or (II) or (III) with X?H, OH, Cl, Br, F or N02; R2 is: (IV) or (V) or (VI) with X?H, OH, Cl, Br, F or NO2; R3 is: O or S or (VII) with X?H, OH, Cl, Br, F or N02. Compositions containing such compounds as well as a method of use thereof in controlling harmful rodents are also described.

Abstract: This invention relates to a composition containing quercetin, vitamin B3, and vitamin C. Also disclosed is a method of using the composition for enhancing physical or mental performance or treating various diseases or disorders.

Abstract: A method for treating thrombotic disorders using a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid. Also disclosed is a method of improving the efficacy of a blood thinning medication by co-administering a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid to a subject being treated with a blood thinning medication.

Abstract: There is provided a method of conjugating a polymer containing a free aldehyde group with a flavonoid in the presence of an acid catalyst, such that the polymer is conjugated to the C6 or C8 position of the flavonoid A ring. The resulting conjugates may be used to form delivery vehicles to deliver high doses of flavonoids, and may also be used as delivery vehicles to deliver an additional bioactive agent.

Abstract: This invention relates to novel coumarin derivatives, formulations comprising same, and to methods of making and using these compounds and formulations, which are useful as repellents against insects and/or pests. The compounds also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents. This invention also relates to novel methods for modeling and/or predicting the repellency of unknown compounds.

Abstract: Two crystalline forms of pinocembrin of formula (I): ? and ?, their preparation and their use for manufacture of pharmaceutical compositions. There exists difference between them in bioavailability. They are used for treating and preventing cerebral ischemic diseases by protective action of neurovascular unit, and enhancing blood drug level in vivo.

Abstract: Methods of treating bone cancer are disclosed. The methods comprise administering to a patient a therapeutically effective amount of a compound of formula (Ia) wherein R1, R2, R3, R4, and R5 are described herein, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents is always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts thereof.

Abstract: At least one compound selected from among coumarin and/or derivative thereof, butylated hydroxyanisole, ethoxyquine and mixtures thereof, and admixtures thereof with other active agents selected from among active agents for combating desquamative conditions of the scalp, plant extracts having propigmenting activity and active agents that slow hair loss and/or promote hair regrowth, are useful for preventing and/or limiting and/or stopping the development of canities.

Abstract: This invention relates to novel coumarin derivative, formulations comprising same, and to methods of making and using these compounds and formulations, which are useful as repellents against insects and/or pests. The compounds also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents.

Abstract: The present invention relates to novel 2-oxo-2H-chromene-3-carboxamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to a novel use for the compound of Chemical formula 1 in order to produce drugs or foods for the prevention or treatment of obesity, fatty liver, diabetes, metabolic syndrome or the like, and to a composition for the prevention or treatment of obesity, fatty liver, diabetes, metabolic syndrome or the like which contains the compound of Chemical formula 1 as an active ingredient, and also to a method for the prevention or treatment of obesity, fatty liver, diabetes, metabolic syndrome or the like comprising the administration of the compound of Chemical formula 1 to a mammal in a therapeutically effective dose.

Abstract: The present invention relates to compounds: and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation.

Abstract: The present invention relates to synergistic mixtures comprising, as active components, one insecticidal compound I selected from the group of insect growth regulators comprising chitin synthesis inhibitors, moulting disruptors and ecdysone receptor agonists; and one fungicidal compound II selected from the group of strobilurine fungicides in synergistic effective amounts.

Abstract: A rodenticidal compound of formula (I): as well as the isomers thereof, in particular enantiomers, diastereoisomers, tautomers or mixtures of isomers in all proportions, where: R1 is: H or (II) or (III) with X?H, OH, Cl, Br, F or N02; R2 is: (IV) or (V) or (VI) with X?H, OH, Cl, Br, F or NO2; R3 is: O or S or (VII) with X?H, OH, Cl, Br, F or N02. Compositions containing such compounds as well as a method of use thereof in controlling harmful rodents are also described.

Abstract: Compounds used to inhibit glycolytic pathway small molecule kinase 6-Phosphofructo-2-kinase/Fructose-2,6-bisphosphatase (PFKFB) are set forth; these inhibitors can be used in the treatment of certain diseases in which cells or tumors rely on glycolytic metabolism, such as many cancer cells.

Abstract: The present invention relates to synergistic mixtures comprising, as active components, one insecticidal compound I selected from the group consisting of carbamates; and one fungicidal compound II selected from the group of strobilurines in synergistic effective amounts.

Abstract: The present invention relates to pharmaceutical composition comprising the naturally occurring compounds selected from (±) Marrnesin, Columbianetin, Dihydroxanthyletin and substituted coumarin derivatives of 7-allyloxy coumarin, 7-benzyloxy coumarin, 7 -methoxycoumarin, 7-acetyloxy coumarin, 4-methyl-7-hydroxy coumarin and 4-methyl-7-acetyloxy coumarin. The said compositions possess a high degree of acetylcholinesterase inhibitory (AChE) property.

Abstract: The present invention is based on the discovery of genetic polymorphisms that are associated with venous thrombosis. 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 disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.

Abstract: The disclosure provides novobiocin analogues with noviose replacements which are useful as Hsp90 inhibitors in the treatment of cancer.

Abstract: Provided are coumarin compounds of formula I, for example, robustic acid methyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.

Abstract: Methods of increasing production, stability or activity of a target polypeptide are provided herein. The method includes increasing the level of an antioxidant in a cell comprising a polynucleotide encoding the target polypeptide. Also provided are cells and transgenic organisms produced using the methods described herein. Methods of treating a subject with a condition treatable by administration of the target polypeptide are also disclosed. Finally methods and compositions for transiently increasing antioxidants in plant cells are provided.

Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.

Abstract: This invention relates to new compounds that can serve as hypoxia mimetics. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one of these compounds.

Abstract: A process for producing micronized dispersed micro-particles and to micro-particles produced by this process.

Abstract: The present invention relates to a method for controlling blood glucose level and a method for the prophylaxis or treatment of diabetes mellitus and/or its complications. The present invention further relates to an anti-diabetic formulation for controlling blood glucose level and/or for the prophylaxis or treatment of diabetes mellitus and/or its complications.

Abstract: 6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules.

Abstract: The present invention relates to pharmaceutical composition comprising the naturally occurring compounds selected from (±) Marmesin, Columbianetin, Dihydroxanthyletin and substituted coumarin derivatives of 7-allyloxy coumarin, 7-benzyloxy coumarin, 7-methoxy coumarin, 7-acetyloxy coumarin, 4-methyl-7-hydroxy coumarin and 4-methyl-7-acetyloxy coumarin. The said compositions posses a high degree of acetylcholinesterase inhibitory (AChE) property.

Abstract: A pharmaceutic composition for treating psoriasis. Ii has an active component and a carrier. The active component has a major active ingredient osthol and a group of minor active ingredients: xanthotoxol, xanthotoxin, isopimpinellin, bergapten, and imperatorine. The major active ingredient osthol accounts for at least 90% by weight of the active component, which accounts for 5-35% by weight of the overall pharmaceutic composition.