Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Abstract: The present invention relates to compounds having the general formula (I) with the definitions of A, X, R1-R6 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: The presently disclosed subject matter provides derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) that are characterized by substantially reduced cyclooxygenase inhibiting activity, yet retain the ability to interact with and modulate the activities of other polypeptides such as the class of peroxisome proliferators-activated receptors (PPARs) and ?-secretase. Also provided are methods of using the derivatives to treat pathological disorders.

Abstract: The invention relates to a novel method for treating or reducing the symptoms of schizophrenia, said method comprising administering to a host in need thereof an effective amount of a compound able to selectively increase the ion flow through KCNQ potassium channels. Furthermore the invention relates to the use of selective KCNQ potassium channel openers for the preparation of a pharmaceutical composition for treating or reducing the symptoms of schizophrenia and related symptoms, disorders and diseases. Furthermore the invention relates to a method of screening for a compound, which is a selective KCNQ potassium channel opener and which is capable of having an anti-psychotic potential.

Abstract: The embodiments provide compounds of the general Formulas I-IV, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula 1, the use of the progesterone receptor modulators for the manufacture of medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.

Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.

Abstract: Compounds of formula (I) have been found to be useful as inhibitors of DDAH.

Abstract: The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds.

Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.

Abstract: The present invention relates to fungicidal mixtures comprising, as active components, 1) at least one 2,4-disubstituted N-biphenylpyrazolecarboxamide of the formula I in which X=oxygen or sulfur; R1 and R2=independently of one another cyano, nitro, halogen, C1-C6-alkyl, C1-C6-haloalkyl, methoxy, difluoromethoxy or trifluoromethoxy; R3=halogen, C1-C4-alkyl or C1-C4-haloalkyl; R4=hydrogen or halogen; and 2) at least one active compound II selected from groups A) to F): A) azoles; B) strobilurins; C) carboxamides; D) heterocyclic compounds; E) carbamates; F) other fungicides; in a synergistically effective amount, methods for controlling harmful fungi using mixtures of at least one compound I and at least one active compound II, the use of the compounds I with active compounds II for preparing such mixtures and also compositions and seed comprising these mixtures.

Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The invention relates to fungicide mixtures containing in the form of active componenets: 1) at least one type of 3,5-disubstituted pyrazol-carboxylic acid biphenylamide of (formula I), wherein X=oxygen or sulfur, R1 and R2=cyano, nitro, halogen, C1-C6-alkyl, C1-C6-halogenalkyl, methoxy, difluormethoxy or trifluormethoxy; R3=halogen, C1-C4-alkyl or C1-C4-halogenalkyl; R4=hydrogen or halogen; and (2) at least one type of active substance II selected from A) to F) groups: A) azole; B) strobilurin; C) carboxylic add amides; D) heterocyclic compounds; E) carbamates and F) other fungicides in synergistically active quantity. A method for combating parasitic fungi by means of mixtures consisting of at least one type of compound I and at least one type of active substance II, the use of the compound(s) I with the active substances II for producing said mixtures and substances and seeds containing them are also disclosed.

Abstract: A medicament having inhibitory activity against NF-?B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.

Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.

Abstract: The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: wherein Z is selected from a group consisting of O, C, N, and S; each of Ar1, Ar2, and Ar3 is a moiety selected from a group consisting of an aryl and a substituted aryl; Y is selected from a group consisting of S, O, CH2 and SO2; K is selected from a group consisting CH2, CF2, O, NH, and SO2; each of n1 and n2 is an integer selected from a group consisting of 0, 1, 2, 3, and 4; and each of x, y, m1 and m2 is an integer selected from a group consisting of 0 and 1. Pharmaceutical compositions based on compounds I are also provided for treatment of a neurological disorders, diseases, or pathologies, and for treatment of infectious diseases.

Abstract: Fungicidal mixtures comprising 1) enestroburin of formula I: and 2) dimethomorph of formula II: as active components in a synergistically effective amount, method of controlling harmful fungi using mixtures of compound I with compound II, use of compound I with compound II for the preparation of such mixtures, and compositions comprising these mixtures.

Abstract: A compound represented by the formula (1): wherein each symbol is as defined in the specification, and a salt thereof and a prodrug thereof unexpectedly have superior GPR40 receptor agonist activity, superior in the properties as a pharmaceutical product such as stability and the like, and can be a safe and useful pharmaceutical agent as a drug for the prophylaxis or treatment of GPR40 receptor related pathology or diseases such as diabetes and the like.

Abstract: Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treating related disorders such as body weight gain, elevated free fatty acid, cholesterol and triglyceride levels and other disorder exacerbated by obesity.

Abstract: The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods.

Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.

Abstract: Compounds, compositions, and methods for inhibiting the onset of metabolic syndrome and treating related disorders in a subject in need of such therapy are disclosed.

Abstract: Methods for reducing autoimmune induced inflammation, including rheumatoid arthritis in a subject in need of such therapy are disclosed.

Abstract: Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.

Abstract: Method for enhancing the fungicidal effectiveness of a) ethaboxam of the formula I, which comprises applying the active compound I simultaneously, that is separately or together, with at least one active compound II from the group consisting of: b) dithiocarbamates, such as maneb, mancozeb, metam or metiram, sulfenic acid derivatives, such as captan or folpet, strobilurin derivatives, such as kresoxim-methyl or pyraclostrobin, cinnamides and analogs, such as dimethomorph or flumorph, or dithianon, famoxadone, cymoxanil, fluazinam, zoxamide, mefenoxam or chlorothalonil, N-(2-{4-[3-(4-chlorophenyl)prop-2-ynyloxy]-3-methoxyphenyl}ethyl)-2-methanesulfonylamino-3-methylbutyramide, N-(2-{4-[3-(4-chlorophenyl)prop-2-ynyloxy]-3-methoxyphenyl}ethyl)-2-ethanesulfonylamino-3-methylbutyramide or 5-chloro-7-(4-methylpiperidin-1-yl)-6-(2,4,6-trifluorophenyl)-[1,2,4]triazolo[1,5-a]pyrimidine in synergistically effective amounts, by spraying or dusting the seeds, the plants or the soils before or after sowing of the

Abstract: The present invention relates to a compound represented by the following formula: (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or a combination thereof, wherein Ro, R1, R1?, R2, R2?, R3 and n are defined herein. The present invention further relates to a method of treating a patient from endometreosis or uterine fibroids.

Abstract: Disclosed herein are novel tricyclic diterpene compounds. These compounds, including their prodrug esters and acid-addition salts, are useful as Interleukin-1 and Tumor Necrosis Factor-alpha modulators, and thus useful in the treatment of various diseases. Pharmaceutical compositions comprising, and uses of, theapeautically effective amounts of the above compounds and their prodrug esters, and pharmaceutically acceptable carrier, are also disclosed, and are useful as, for example, anti-inflamatory analgestics, treatments for immune disorders, anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection, for example. Completley synthetic and semi-synthetic methods of making these compounds and their analogs are disclosed.

Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.

Abstract: Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treating related disorders such as body weight gain, elevated free fatty acid, cholesterol and triglyceride levels and other disorder exacerbated by obesity.

Abstract: Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treating related disorders such as body weight gain, elevated free fatty acid, cholesterol and triglyceride levels and other disorder exacerbated by obesity.

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Method for controlling rust infections in leguminous plants by using orysastrobin, mixtures of orysastrobin and a fungicidally active compound II from the group of the azoles, acylalanines, amine derivatives, anilinopyrimidines, dicarboximides, dithiocarbamates, heterocylic compounds, phenylpyrroles, cinnamides, and analogs, or other fungicides according to the description, and also compositions and seed comprising these mixtures.

Abstract: Fungicidal mixtures, comprising as active components 1) carbamate oxime ethers of the formula I, in which X is N or CH, and 2) at least one active compound II selected from the group of the azoles, strobilurins, carboxamides, heterocyclic compounds, carbamates, guanidines, antibiotics, nitrophenyl derivatives, sulfur-containing heterocyclyl compounds, organometallic compounds, organophosphorus compounds, organochlorine compounds, inorganic active compounds, cyflufenamid, cymoxanil, dimethirimol, ethirimol, furalaxyl, metrafenone and spiroxamine, in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compound I with active compounds II, the use of the compound I with active compounds II for preparing such mixtures and compositions comprising these mixtures.

Abstract: Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.

Abstract: The present invention concerns nematicidal compounds, their formulation as nematicidal composition and their use for controlling nematodes, preferably plant parasitic nematodes.

Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.

Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.

Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed

Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2 I in which A, R1 and R2 are as defined in the description, and b) dimethomorph or flumetover, and/or c) a valinamide of the formula III in which R13 is C3-C4-alkyl and R14 is naphthyl or phenyl, where the phenyl radical is substituted in the 4-position by a halogen atom, a C1-C4-alkyl or C1-C4-alkoxy group, and/or d) benalaxyl, ofurace, metalaxyl, furalaxyl or oxydixyl, and/or e) 1-(2-cyano-2-methoxyiminoacetyl)-3-ethylurea in a synergistically effective amount.

Abstract: The present invention relates to compounds of the formula I in which A1, A2, R2 and R3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention relates to the use of compounds of the formula I for the therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, novel compounds of the formula I, pharmaceutical preparations comprising them and processes for their preparation.

Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.

Abstract: A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:

Abstract: Novel polycyclic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.

Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.

Abstract: The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.

Abstract: Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.