Abstract: The present invention relates to fatty acid esters of polyols or sulfonated fatty acid esters or sulfonated fatty acid amides containing at least one group Y, where Y stands for CF3—(CH2)a—O—, SF5—, CF3—(CH2)a—S—, CF3CF2S—, [CF3—(CH2)a]2N— or [CF3—(CH2)a]NH—, where a stands for an integer selected from the range from 0 to 5, or formula (I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)t— or [CF3—(CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, to processes for the preparation of these compounds, and to uses of these surface-active compounds.

Abstract: The present invention relates to compounds of the formula I wherein R3 is C1-6-alkyloxy, C1-6-acyloxy or aroyloxy; R6 is hydrogen or C1-6-alkyloxy; R7 is C1-6-alkyloxy, C1-6-acyloxy, aroyloxy or arylacyloxy; R8 is hydrogen or C1-6-alkyloxy; or R7 and R8 form together a group O-L-O with L being (CR1R2)n, with R1 and R2 being independently from each other hydrogen or C1-5-alkyl and n being an integer from 1 to 3; R10 is hydrogen or N—C1-4-acyl, N—C1-5-alkyl-x-Cx-alkyl with x being an integer from 1 to 5, for use as medicament for the treatment of a disorder connected to impaired glucose metabolism and impaired insulin action such as syndrome X and diabetes type 1 and 2, especially for the treatment of (non-autoimmune) diabetes type 2.

Abstract: Novel ligand antagonists of the RAR receptors have the following structural formula (I): in which A is a CH2, CHOH, C?O or C?N—OH radical or a sulfur or selenium atom; B is a radical selected from among those of formulae (a) to (f): and Ar is a radical selected from among those of formulae (g) to (i):

Abstract: The use of fibrates, particularly clofibrate, is described for the preparation of a medicament useful in the treatment of congestive heart failure.

Abstract: Compositions are described in which certain thyroid hormone receptor-binding compounds are formulated together with either an enteric coating, an antioxidant, or both an enteric coating and an antioxidant. Such formulation acts to prevent the formation of undesired reaction products in vivo.

Abstract: The invention relates generally to the field of treatment of headache, post-laminectomy syndrome, and other disorders associated with localized pain. The compositions and methods described herein are useful for alleviating both the disorders and the pain associated therewith.

Abstract: Aspirin (ASA) triggers a switch in the biosynthesis of lipid mediators, inhibiting prostanoid production and initiating 15-epi-lipoxin generation, through the acetylation of cyclooxygenase II.

Abstract: The present invention relates to compounds of the formula (I); wherein R1 is H, CH3 or OCH3; R3=H, OH, CH3, OCH3, O-glucose or benzoyloxy; R4=H; R5=H or OH; R6=H or OCH3; R7=H, CH3, OCH3, cinnamoyloxy or (3,4,5-trimethoxy)-benzoyloxy; R8=H, OH, CH3 or OCH3; or R7 and R8 form together a group 0-CH2—O; R9=H or OCH3; R10=H or N-acetyl, N-methyl-2-aminoethyl; to their use as medicament for the treatment of non-autoimmune type 2 diabetes mellitus and/or syndrome X, to dietary and pharmaceutical compositions containing them and to a method for the treatment of non-autoimmune type 2 diabetes mellitus and/or syndrome X in animals including humans, said method comprising the step of administering an effective dose of a compound of the formula (I) to animals including humans which are in need thereof.

Abstract: The invention provides methods for treating beta-Amyloid protein-induced disease, pharmaceutical compositions and compounds useful for the same, and the use of these compounds for the manufacture of a medicament for treating the same. More particularly, the invention relates to the use of natural product compounds isolated from turmeric, gingko biloba, and ginger, and synthetic chemical analogues thereof, for the treatment of a beta-Amyloid protein-induced disease.

Abstract: There is provided a means of applying a heated medicament to the skin and concurrently hydrating the skin thus raising the efficacy of administration.

Abstract: The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, and R10 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of ?-secretase activity.

Abstract: This invention relates to micellar compositions comprising at least one pharmaceutically active substance and a mixture of n-alkyl dimethyl benzyl ammonium chlorides, wherein the mixture comprises more than 30% n-alkyl dimethyl benzyl ammonium chlorides having a chain length superior or equal to C16. This invention also relates to ophthalmic compositions containing such micellar compositions and methods of using these ophthalmic compositions for the treatment of eye conditions.

Abstract: The invention concerns a process for producing a preserved customised consumer composition, preferably from a Vending machine, wherein a plurality of ingredient streams are mixed together in predefined relative amounts, characterised in that At least two streams consist of water and preservative only, at least two of which having different concentrations of preservative. The Invention permits the final preservative mix to be independently variable to the formation.

Abstract: Synergistic and residual pesticidal compositions containing synergistic and residual mixtures of plant essential oils and/or their constituents, plant essential oils and/or their constituents in admixture with known active pesticidal compounds or plant essential oils and/or their constituents in admixture with other compounds not previously used as active ingredients in pesticidal formulations, such as, for example, so called signal transduction modulators. In addition, the present invention is directed to a method for controlling pests by applying a pesticidally effective amount of the above synergistic and residual pesticidal compositions to a locus where pest control is desired.

Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6alkyl or C1-C6alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R8 and R9 are each independently hydrogen atom, C1-C6alkyl, —CON(R18)(R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

Abstract: It is an object of the present invention to provide a nanoparticle containing a microbicide and a biodegradable polymer, which is safe and excellent in terms of dispersion stability and has high transparency and good absorbability due to its small particle size. The present invention provides a water-dispersible nanoparticle, which comprises a microbicide and a biodegradable polymer.

Abstract: Synergistic and residual pesticidal compositions containing synergistic and residual mixtures of plant essential oils and/or their constituents, plant essential oils and/or their constituents in admixture with known active pesticidal compounds or plant essential oils and/or their constituents in admixture with other compounds not previously used as active ingredients in pesticidal formulations, such as, for example, so called signal transduction modulators. In addition, the present invention is directed to a method for controlling pests by applying a pesticidally effective amount of the above synergistic and residual pesticidal compositions to a locus where pest control is desired.

Abstract: The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R1 is hydrogen or C1-6-alkyl; R2 is hydroxy, C3-5-acyloxy, hydroxymethyl, 1,3-dihydroxypropyl or C1-6-alkyl; R3 and R4 independently from each other are hydrogen, hydroxy, hydroxymethyl, C1-5-acyloxy or C1-6-alkoxy; R5 is C1-6-alkyl, hydroxymethyl carboxy or methoxycarbonyl; R9 is hydrogen, hydroxymethyl, methoxy, oxo or C1-5-acyloxy; R10 is hydrogen, or R5 and R9 taken together are —CH2—O— or —O—CH2—; or R5 and R10 taken together are —CO—O—, —O—CO—, —CH2—O— or —O—CH2—; R6 is hydrogen, or R5 and R6 together form a bond; R7 and R8 independently from each other are C1-6-alkyl, carboxy, x-hydroxy-Cx-alkyl (with x being an integer from 1 to 6), or C1-6-alkoxycarbonyl with the proviso that at least one of R7 and R8 is C1-6-alkyl; R11 and R12 are both hydrogen or R11 and R12 together are oxo, with the further proviso for formula (I) that if R2 is hydroxy R1 is C1-6-alkyl, for use as medicaments for the t

Abstract: A method and composition for treating, preventing or ameliorating heart failure, cardiac hypertrophy, and/or myocardial dysfunction includes administering a therapeutically effective amount of a HDAC inhibitor, such as phenylbutyrate, in combination with an ACE inhibitor, such as captopril.

Abstract: The present invention discloses methods of using of compounds for the enhancement of the innate immune system of a patient. In particular, the active compounds of the present invention include at least one calcineurin inhibitor, mTOR inhibitor or non-immunosuppresive derivative, or a derivative, isomer, or pharmaceutically acceptable salt thereof; and optionally, at least one calciferol or LMW inhibitor, or a derivative, isomer, or pharmaceutically acceptable salt thereof. Pharmaceutical formulations comprising same are also disclosed.

Abstract: A UGT2B inhibitor capable of increasing the bio-availability of a drug, is a compound in a free base or a pharmaceutically acceptable salt form that is selected from the group consisting of: capillarisin, isorhamnetin, ?-naphthoflavone, ?-naphthoflavone, hesperetin, terpineol, (+)-limonene, ?-myrcene, swertiamarin, eriodictyol, cineole, apigenin, baicalin, ursolic acid, isovitexin, lauryl alcohol, puerarin, trans-cinnamaldehyde, 3-phenylpropyl acetate, isoliquritigenin, paeoniflorin, gallic acid, genistein, glycyrrhizin, protocatechuic acid, ethyl myristate, umbelliferone, PEG (Polyethylene glycol) 400, PEG 2000, PEG 4000, Tween 20, Tween 60, Tween 80, BRIJ® 58, BRIJ® 76, Pluronic® F68, Pluronic® F127, and a combination thereof.

Abstract: The invention provides methods of synthesizing the purified enantiomers of oleocanthal. The invention further provides methods of using oleocanthals in various formulations including, food additives; pharmaceuticals; cosmetics; animal repellants; and discovery tools for mammalian irritation receptor genes, gene products, alleles, splice variants, alternate transcripts and the like.

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 relates to a composition for the prevention and the treatment of cardiovascular disease containing extracts of T. nucifera or abietane diterpenoid compound or terpenoid compound isolated from the same as an effective ingredient. T. nucifera extracts or abietane diterpenoid compound or terpenoid compound isolated from the same of the present invention not only shows excel lent anti-oxidative activity to LDL but also effectively inhibits ACAT activity. Further, T. nucifera extracts of the present invention reduce blood LDL cholesterol and total cholesterol. Therefore, the composition of the present invention can be effectively used for the prevention and the treatment of cardiovascular diseases including hyperlipidemia and atherosclerosis caused by the LDL oxidation and the synthesis and accumulation of cholesteryl ester.

Abstract: The present invention provides a compound represented by the formula: wherein each symbol is as defined in the specification. Since the compound of the present invention has superior hypoglycemic action and superior hypolipidemic action, it is useful as an agent for the prophylaxis or treatment of diabetes, hyperlipidemia, impaired glucose tolerance and the like.

Abstract: Disclosed are prodrugs of (2R)-2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.

Abstract: A liposome formulation for stably incorporating high content of hydrophobic substance is disclosed. The liposome includes two phospholipids with different phase transition temperatures such as saturated and unsaturated phosphatidyl cholines, hydrophobic substances, cholesterol, cholesterol derivatives, antioxidant and hydrophilic polymer-modified lipids such as MPEG-DSPE.

Abstract: A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient the method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a ? receptor blocker; an imidazoline receptor antagonist; a centrally acting ? receptor antagonist; a peripherally acting ? receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduces SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.

Abstract: The present invention relates to novel thiosulfonates derivatives. The present invention also provides methods for preventing, treating and/or reducing inflammation-associated diseases in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous or cutaneous systems as well as infective and tumoral diseases employing said compounds.

Abstract: The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.

Abstract: The compounds of formula I in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as indicated in the description, are novel effective PDE4 inhibitors.

Abstract: The invention provides a biological dressing for treatment of a dermatological disease comprised of one or more resins or other film-forming agents, a topically acceptable volatile solvent, and a pharmacologically active agent. The combined one or more resins are present in a suitable amount such that the composition, when the solvent evaporates, will dry to form a solid coating that sticks to the skin, nail or mucosal membrane to which the composition is applied, and maintain the pharmacologically active agent over a sustained period of time in contact with sites on the skin or mucosal membranes exhibiting symptoms of the disease. Methods are provided for treating symptoms of dermatological diseases with such a pharmacological composition.

Abstract: This invention is directed to a novel method for the inhibition of ?-glucosidase enzyme and thus treating diabetes, viral infections, fungal infections, autoimmune function disorders and obesity using compounds derived as lichen metabolites; more specifically, this includes the therapeutic applications of methylorsellinate (2,4-dihydroxy-6-methylbenzoate, Compound I), methyl-?-orinolcarboxylate (2,4-dihydroxy-3,6-dimethylbenzoate, Compound II) and zeorin (6,22-hopanediol, Compound III).

Abstract: The invention relates to clear, liquid preservatives, which contain a) one or several 1-hydroxy-4-methyl-6-alkyl-2(1H)-pyridones and/or one or several salts thereof. wherein alkyl represents a linear, branched or cyclic alkyl group having 1-12 carbon atoms, and b) one or several alcohols containing one or several aromatic groups.

Abstract: Method for the preparation of ester compounds for use as skin brightening agents and compositions for brightening skin containing the ester compounds.

Abstract: Compounds of the formulae (1), (2) and selected hindered nitroxyl, hydroxylamine and hydroxylamine salt compounds such as the compound of formula (3), wherein Gi is hydrogen; C1-C22alkyl; C1-C22alkylthio; C2-C22alkylthioalkyl; C5-C7cycloalkyl; phenyl; C7-C9phenylalkyl; or SO3M; G2 is C1-C22alkyl; C5-C7cycloalkyl; phenyl; or C7-C9phenylalkyl; E is oxyl or hydroxyl; V is —O—; or —NH—; a is 0 or 1 or 2; b, c and d and g are each independently of one another 0 or 1; e is an integer from 1 to 4; f, m, n and p are each independently of one another an integer from 1 to 3; q is 0 or an integer from 1 to 3; Q, T and G3 are as defined in claim 1; G4 and G5 are each independently of the other hydrogen; or C1-C22alkyl; exhibit marked antiinflammatory action.

Abstract: Non-nucleoside inhibitors of HIV-1 reverse transcriptase are described. Such inhibitors may be used as part of a combination therapy to treat HIV infection. Compounds described herein exhibit antiviral potency. In addition, compounds described herein exhibit metabolic stability. Also described herein are processes for preparing Non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

Abstract: A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof.

Abstract: An insect repellent composition containing 3,8-p-menthane-diol and benzylbenzoate as active compounds is described. Typically, the active compounds are each present in the composition in an amount which is less than an amount of the compound required to be effective as an insect repellent by itself. The composition may additionally include one or more additional active compounds selected from the group consisting of 2-butyl-2-ethyl-1,3-propanediol, 2-ethyl-1,3hexanediol and 5-N-butylacetanilide. One or more promoters, carriers, diluents, dispersants, solvents, emollients, emulsifiers, colouring agents, fragrances or thickening agents may also be included in the composition.

Abstract: Compounds, compositions, and methods of avoiding edema while treating or preventing PPAR?-mediated diseases, including cancer, using derivatives and prodrugs are provided.

Abstract: The present invention relates to methods of identifying a disease treatable with PARP modulators by identifying a level of PARP in a plurality of samples from a population, making a decision regarding identifying the disease treatable by the PARP modulators wherein the decision is made based on the level of PARP. The method further comprises of treating the disease in a subject population with the PARP modulators. The methods relate to identifying up-regulated PARP in a disease and making a decision regarding the treatment of the disease with PARP inhibitors. The extent of PARP up-regulation in a disease can also help in determining the efficacy of the treatment with PARP inhibitors. The present invention discloses various diseases that have up-regulated or down-regulated PARP and can be treated with PARP inhibitors or PARP activators, respectively.

Abstract: The present invention relates to the use of one or more retinoid agonists and/or antagonists comprising retinoids with selective Retinoid X Receptor (RXR) agonistic or antagonistic activity alone or in combination with one or more peroxisome proliferator activated receptor (PPAR) ligands for the manufacture of a medicament for the (preferably oral or topical) treatment (this term including prevention/prophylaxis and/or therapy) of one or more manifestations of metabolic syndrome (also known as syndrome X), also called diseases hereinafter, especially from one or more manifestations thereof selected from the group consisting of diabetes type II, obesity, dyslipidemia, hypertension and polyneuropathy, each of which can also be linked with a high risk of cardiovascular diseases. Corresponding methods, the compounds and combinations for use in the treatment of the mentioned diseases and comparable invention embodiments are also described.

Abstract: A pharmaceutical composition including therapeutically effective amounts of at least one HMG-CoA reductase inhibitor present as a dyhydroxyacid salt and at least one additional therapeutic agent.

Abstract: This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally.

Abstract: Novel calcilytic compounds and methods of using them are provided.

Abstract: The present disclosure concerns a new class of selective estrogen receptor modulators (SERMs). The disclosure also includes the identification of a previously unknown membrane associated estrogen receptor. Methods for making and using the disclosed SERMs are disclosed, including pharmaceutical formulations of the disclosed novel compounds in useful compositions.

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 relates, inter alia, to a process for preparing a compound of formula (I): which comprises either (a) reacting a compound of formula (II): with 2-cyanophenyl, or a salt thereof, in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane, or (b) reacting a compound of the formula (III): with a compound of the formula (IV): in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane; where W is the methyl (E)-2-(3-methoxy)acrylate group C(CO2CH3)?CHOCH3 or the methyl 2-(3,3-dimethoxy)propanoate group C(CO2CH3)CH(OCH3)2, or a mixture of the two groups. In addition, the present invention relates to a novel precursors of the compound of formula (I) and methods for making them.

Abstract: The present invention relates to novel non steroidal anti-inflammatory compounds (NSAIDs) derivatives of sulindac, for the treatment/prevention, alone or in combination, of cancer.