Abstract: Granulates have particles of metformin and particles of a fibrate. Pharmaceutical compositions contain such granulates. Processes prepare the granulates and the pharmaceutical compositions.

Abstract: Disclosed are coumarin derived compounds of formula I as skin lightening agents alone or in combination with other skin benefit agents and together with a cosmetic vehicle: Where each or both R1 and/or R2 represents hydrogen (H); linear or branched, saturated or unsaturated C1-C12 alkyl, alkenyl, acyl, or heteroalkyl (preferably, alkoxy) groups; and R3 represents linear or branched, cyclic or acyclic, saturated or unsaturated C1-C12 alkyl, alkenyl, cycloalkyl, cycloalkenyl, or heteroalkyl group; and R4 represents a hydrogen atom (H); straight or branched, cyclic or acyclic, saturated or unsaturated, containing or not containing a heteroatom C1-C22 alkyl, alkenyl, cycloalkyl, cycloalkenyl, heteroalkyl, aryl, or heteroaryl group.

Abstract: Provided are methods for manufacturing compounds of Formula I wherein all substituents are described herein.

Abstract: Therapeutic substituted cyclopentane compounds, and compositions, medicaments, and therapeutic methods related thereto are disclosed herein.

Abstract: This invention provides methods and compositions for treating a condition associated with phosphorylation of TASK-1 in a subject comprising administering to the subject an amount of an agent effective to overcome the phosphorylation dependent loss of TASK-1 function so as to thereby treat the condition. In a specific embodiment of the invention the agent is a TREK-1 agonist.

Abstract: A compound having a structure is disclosed herein. Compositions, medicaments, and therapeutic methods related thereto are also disclosed.

Abstract: Prodrugs of propofol, methods of making prodrugs of propofol, pharmaceutical compositions of prodrugs of propofol and methods of using prodrugs of propofol and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting are disclosed herein.

Abstract: According to the invention, there is provided a novel 3,4-dihydroxyhydrocinnamic acid derivative, designated DHH105, having blood glucose lowering effects in vivo as a result of the enhancement of glucose transport mediated by the increase of insulin receptor signaling. This invention thus relates to a 3,4-dihydroxyhydrocinnamic acid derivative useful as an anti-diabetic agent, represented by the following formula I: or pharmaceutically acceptable salts thereof, to a method for preparing the compound, and to a composition for treating diabetes comprising the same as an active ingredient.

Abstract: Novel compounds of the general formula (I), wherein Ar, R1, R2, X1, X2, Y1, Y, and Z are as defined in the specification, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.

Abstract: The present invention provides piperine and analogues or derivatives thereof for the treatment of skin conditions treatable by stimulation of melanocyte proliferation, such as vitiligo, and also for treating skin cancer. The piperine and analogues or derivatives thereof may also be used to cosmetically promote or enhance the natural coloration of the skin.

Abstract: The present invention relates to novel hydroxyphenylundecane derivatives of the formula (I), a method for the preparation of said compounds by cultivation of the fungus Cryphonectria parasitica, DSM 14453, and their use as pharmaceuticals, i.e. for the treatment of Alzheimer's Disease, Parkinson's Disease, Huntington's Diseases, stroke, psychosis and/or depressions.

Abstract: The use of compounds of the formula and pharmaceutically acceptable salts thereof, alone or in combination for the treatment of transplant rejection, wherein the substituents are further defined in the application.

Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.

Abstract: Pharmaceutical compositions and dosage forms for administration of hydrophobic drugs, particularly fenofibrate, are provided. The compositions comprise a therapeutically effective amount of an active agent and a solubilizer. The solubilizer is selected to effectively solubilize active agent in the composition. The solubilizers employed as part of the invention include: a vitamin E substance; monohydric alcohol esters such as trialkyl citrates, lactones and lower alcohol fatty acid esters; nitrogen-containing solvents; phospholipids; glycerol acetates such as acetin, diacetin and triacetin; glycerol fatty acid esters such as mono-, di- and triglycerides and acetylated mono- and diglycerides; propylene glycol esters; ethylene glycol esters; and combinations thereof. The pharmaceutical dosage forms contain the compositions in a suitable dosage form unit such as a capsule. Methods of treating patients comprising administering the compositions are also provided.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? suptype.

Abstract: Disclosed are anti-viral compositions containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients), and a pharmaceutical carrier. Also disclosed are methods of treating lesionous symptoms of a viral infection involving applying an effective amount of the anti-viral composition to the lesions.

Abstract: The present invention is related to a complexating system comprising a tannin immobilised on a solid support by means of a bifunctional spacer which is covalently bound from one hand to said solid support by a first function and from the other hand to said tannin by a second function, wherein the tannin is a naturally occurring tannin and exhibits at least six hydroxyl groups. Said complexating system can be used in particular for chelating metals and proteins, as an antioxidant, as a radical scavenger or as an antibacterial. More specifically, applications can be found in the clarification and stabilisation of beverages, the treatment of textiles, or the separation and/or purification of proteins and/or metals.

Abstract: A probe solution composition containing a probe capable of binding specifically to a target substance and a moisturizer, which is utilized for spotting the probe to be fixed on a substrate, is provided. As a result, an increased detection sensitivity of a reaction chip, a higher spot shape stability and a simplified manufacturing process can be achieved.

Abstract: The present invention relates to novel antidiabetic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel 3-aryl-&agr;-oxy substituted propanoic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs and pharmaceutically acceptable compositions containing them. Formula (I) where R1 represents t-butyldimethyl silyl, trimethyl silyl or alkoxyalkyl group; R2 represents hydrogen or substituted or unsubstituted (C1-C6)alkyl group.

Abstract: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoicacid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.

Abstract: This invention relates to novel resveratrol analogs of the formula given below; wherein R, R1, R2 and R3 are: 1. R=OH, R1=R2=R3=H; 2. R=OH, R1=Br, R2=R3=H; 3. R=R1=OH, R2=R3=H; 4. R=R1=R3=H, R2=3,4,5-trihydroxybenzoyl; 5. R=R1=H, R2=R3=3,4,5-trihydroxybenzoyl; 6. R=R1=R3=H, R2=3,4-dihydroxycinnamoyl; 7. R=R1=R3=H, R2=3,4,5-trihydroxycinnamoyl; 8. R=R1=R3=H, R2=—CH2CH2N(CH3)2; 9. R=R1=R3=H, R2=—COCH2NH2.HCl. These compounds exhibited high antioxidant properties and are useful in food industry and in cosmetics. The compounds may be used in pharmaceutical composition as an antioxidant or free radical scavenger.

Abstract: Compounds of the formula 1

Abstract: Products and compositions for preventing or reducing the severity of hypertension. These products contain (a) ferulic acid or a ferulate ester, and (b) caffeic acid and/or a chlorogenic acid. The preventive or remedy can suppress a rise in blood pressure and alleviate hypertension, and is usable as a food.

Abstract: Provided is a method of treating hypertension, which comprises administering an effective amount of a compound represented by the following formula (1) or (2): 1

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: The present invention relates to the use of hydroxydiphenyl ether compounds as antimicrobially active substances, to certain new compounds of this type and to processes for the preparation of these compounds.

Abstract: The invention relates to a class of compounds, and analogs thereof, which are effective in protecting cells of the central and peripheral nervous system from deterioration and cell death arising from degenerative disease, trauma, aging or like condition, disease or disorder. The methods utilize novel anti-apoptotic and neuroprotective effects for a group of natural polyphenols in cells of the central and peripheral nervous system.

Abstract: A new and improved cosmetic composition and method of using the same to prevent and treat chemically induced skin irritation and discoloration and protect from the adverse effects of tyrosinase containing a small but effective amount of ethyl p-methoxycinnamate derived from Kaempferia Galanga roots.

Abstract: The present invention relates to stilbene and quinone 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 BOC 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 art stilbenes.

Abstract: The invention relates to an agent for preventing, improving or treating hypertension, which exhibits a hypotensive effect, inhibits the rise of blood pressure and improves hypertension, and food for preventing or improving hypertension, which does not become a burden in daily intake, has a higher antihypertensive effect and is useful as a diet during treatment for patients of hypertension.

Abstract: The present invention relates to novel hydroxyphenylundecane derivatives of the formula (I), 1

Abstract: The present invention relates to a preparation for stimulating or enhancing an immune system comprising one or more agents that stimulate T-lymphocytes in vivo. Such a preparation can be sued in the prophylaxis and/or treatment of a medical condition. The invention further relates to a preparation for use in a pharmaceutical or food product and to a preparation for medical use.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The present invention relates to a pharmaceutical composition useful for treating chronic myeloid leukemia where Bcr-Abl kinase is constitutively expressed in animals and humans, said composition comprising an effective amount of analogs of chlorogenic acid such as neochlorogenic acid (5-O-caffeoyl quinic acid), cryptochlorogenic acid (4-O-Caffeoyl quinic acid), 3-O-(3′-methylcaffeoyl) quinic acid and 5-O-(Caffeoyl-4′-methyl) quinic acid and/or its salts such as sodium, potassium and ammonium together with pharmaceutically acceptable additives.

Abstract: Methods, compositions and systems for preventing an adverse reaction of the skin to the presence of a skin-sensitizing and/or skin-irritating agent by administering an effective amount of phenoxyacetic acid and/or a lower alkyl ester thereof to a warm blooded animal.

Abstract: The use of compounds of the formula and pharmaceutically acceptable salts thereof, alone or in combination for the treatment of transplant rejection, wherein the substituents are further defined in the application.

Abstract: The present invention provides non-peptide organic compounds that have a structure analogous to or reminiscent of the TMOF structure and have pesticidal activity. Thus the present invention concerns pesticidal compounds that inhibit digestion in pests by terminating or otherwise blocking synthesis of digestive enzymes by activating a TMOF receptor (collectively referred to herein as “pesticidal compounds”). The pesticidal compounds and other compounds of the present invention are usefully employed in the control of pests, particularly insect pests such as mosquitoes, which ingest blood.

Abstract: Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers are provided.

Abstract: The present invention provides a low-irritant pesticidal emulsifiable concentrate comprising (a) 1 to 60% by weight of at least one pesticidal active ingredient compound selected from the group consisting of pyriproxyfen and a pyrethroid compound, (b) 2 to 15% by weight of at least one surfactant and (c) 15 to 90% by weight of at least one aromatic ester solvent represented by the formula: Ar—X—COOR  [1] or the formula: RCOO—X—Ar  [2] [wherein R represents non-aromatic group having 1 to 6 carbon atoms; Ar represents an aromatic group; and X represents a single bond or an alkylene group having 1 to 6 carbon atoms]. The pesticidal emulsifiable concentrate of the present invention can be used as an emulsion which is superior in emulsion stability when using after diluting with water, and has low irritation.

Abstract: The present invention is directed to methods for the prevention or inhibition of angiogenesis. The method is accomplished by the administration of an effective amount of 15-epi-16-(para-fluoro)-phenoxy-lipoxin A4, LXA4, 15-epi-LXA4 or 15-R/S-methyl, LXA4 and pharmaceutically acceptable salts, esters, amides, carboxylic acids, or prodrugs thereof, to a subject in need thereof. As a consequence of the action of the therapeutic agent, angiogenesis is prevented or inhibited in the subject.

Abstract: The use of fibrates, particularly clofibrate, is described for the preparation of a medicament useful in the treatment of congestive heart failure, and particularly the states of heart failure unrelated to dyslipidaemic conditions.

Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.

Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include a fibric acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.

Abstract: A pharmaceutical composition comprising as its active ingredients one or more drugs selected from the group consisting of angiotensin II receptor antagonists and angiotensin converting enzyme inhibitors, and one or more insulin resistance improving agents exhibits excellent arteriosclerotic progress inhibitory effects, and is useful as a drug, particularly as a drug for the prevention or treatment of arteriosclerosis. The invention also provides a method for the treatment or prophylaxis of arteriosclerosis by administering in combination (i) at least one of said angiotensin II receptor antagonists or angiotensin converting enzyme inhibitors and (ii) one or more insulin resistance improving agents to a mammal suffering from or susceptible to arteriosclerosis.

Abstract: The present invention provides a new use of an agent that inhibits bile acid reabsorption. An agent that inhibits bile acid reabsorption is useful for the prevention or treatment of obesity or fatty liver.

Abstract: It has been newly found out that ascochlorin, which is a publicly known fat-soluble antibiotic, and its homologues serve as a ligand of retinoid X receptor and react in vivo with the amino group of serum protein to form Schiff bases without showing any side effect of retinoid. Ascochlorin and its homologues are usable in treating and/or preventing a disease or condition which can be relieved by the retinoid X receptor ligand-dependent gene transcriptional regulation (for example, diseases caused by the expression of insulin resistance, hypertension, cerebrovascular diseases, rheumatoid arthritis, autoimmune disease, Ca metabolic disorder, complication of diabetes, arteriosclerosis, etc.). Moreover, they can inhibit denaturation and/or necrosis of pancreatic Langerhans islet &bgr;-cells and, therefore, are usable in making these cells to sustain the insulin productivity.

Abstract: A method of inducing the viral resistance of plants comprises treating the plants, the soil or seeds with an effective amount of the compound of the formula I 1

Abstract: O-medium alkyl esters of diflunisal and related compounds are disclosed having anti-platelet activity, hydroxy radical scavenging properties, enhanced hepatic clearance and low ulcerogenic potential. These compounds have general formula (I) wherein n equals 3-13.

Abstract: The invention relates to the use of trimebutine [2-dimethylamino-2-phenylbutyl-3,4,5-trimethoxy-benzoate hydrogen maleate] or its corresponding stereoisomers for the preparation of a medicament to prevent and/or treat inflammatory somatic pain as well as chronic pain.

Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.