Abstract: Disclosed are methods useful for the topical therapeutic treatment of skin malignancies including skin cancers and cutaneous metastases using compositions containing nanoparticles of paclitaxel or other taxanes.

Abstract: The present invention relates to novel aromatic thio 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 compounds of formula (I) or pharmaceutical acceptable salts, wherein A, B, R1, R2, R3, R4a, R5, and Z are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora.

Abstract: A method of assessing growth hormone deficiency in a human or animal subject, the method comprising administering orally to the subject EP 1572 (Formula I) or EP 1573 (Formula II), obtaining a post-administration sample from the subject, determining the level of growth hormone in the sample and assessing whether the level of growth hormone in the sample is indicative of growth hormone deficiency in the subject. Preferably, the GH level in the sample is measured by immunoassay. Also disclosed is a kit of parts constituting a diagnostic kit comprising: (a) EP 1572 or EP 1573 formulated for oral administration; and (b) means for determining the level of growth hormone in a sample.

Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.

Abstract: The present invention provides a method for reducing the occurrence and progress of intestinal polyps that may develop into colon cancer, and a carboxylic acid amide compound as an active component to reduce intestinal polyps, represented by the following Formula: wherein R is a lower alkyl group and X is a halogen an example being 4-diethoxyphosphinoylmethyl-N-(4-bromo-2-cyanophenyl) benzamide.

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.

Abstract: The invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more organophosphoric acid ester-type compounds and to a method for controlling insecticidal or miticidal pests which have acquired resistance to commercial insecticidal and miticidal agents.

Abstract: The invention provides a compound of formula I: 1

Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.

Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0, 1, 2, 3 or 4; R1 and R2 are each independently selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each of the aforementioned C1-12alkyl groups may optionally and each individually be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl; and each R4 independently is hydroxy, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is —X—R5 or —X-Alk-R6; wherein R5 and R6 each independently are indanyl, indolyl or phenyl; each of

Abstract: Methods and compositions for treating or preventing inflammatory diseases such as psoriasis or multiple sclerosis are provided, comprising the step of delivering to the site of inflammation an anti-microtubule agent, or analogue or derivative thereof.

Abstract: A pesticidal composition comprising (a) 1 to 50% by weight of a lipophilic compound as a pesticidally active ingredient, (b) 0.1 to 10% by weight of at least one nonionic surfactant, (c) 0.3 to 4% by weight of at least one anionic surfactant selected from the group consisting of alkylarylsulfonic acid salts and alkylbiphenylsulfonic acid salts, (d) 15 to 40% by weight of a fatty acid ester represented by the formula: RCOOR′  [1] wherein R is an alkyl group having 2 to 21 carbon atoms or an alkenyl group having 2 to 21 carbon atoms, and R′ is an alkyl group having 1 to 6 carbon atoms, and (e) 20 to 80% by weight of an aromatic hydrocarbon solvent, which shows a good emulsion stability when diluted with water, has a good low-temperature storage stability, and is only slightly irritant.

Abstract: The present invention provides an agent for preventing and curing fatty liver containing, as the effective ingredient compound, a carboxylic acid amide derivative represented by the general formula (1), (wherein R is a lower alkyl group; and X is a halogen atom), and a method for curing fatty liver by administering said agent.

Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.

Abstract: A class of chemical compounds comprising a pyrrolo[2,3-b]pyridine moiety and a halo-substituted heterocyclic moiety, linked via the 3-position of the pyrrolo[2,3-b]pyridine moiety by a methylene group, are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia.

Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.

Abstract: The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.

Abstract: Unsaturated aminodicarboxylic acid derivatives of formula I ##STR1## wherein A is a divalent aliphatic hydrocarbon radical containing 2 carbon atoms and R.sub.1 and R.sub.2 are each independently of the other free or esterified carboxyl groups, and salts thereof, have a pronounced and selective antagonistic action against N-methyl-D-aspartic acid (NMDA)-sensitive excitatory amino acid receptors. These compounds are prepared, for example, by converting, in a formula of formula II ##STR2## wherein Z.sub.1 and Z.sub.2 are hydroxy or protected hydroxy and Z.sub.3 is protected amino, Z.sub.3 into amino and, if present, converting protected hydroxyl groups Z.sub.1 and/or Z.sub.2 into hydroxy and, if desired, converting a resultant compound into another compound of formula I, resolving a resultant mixture of isomers into the individual components and separating the desired preferred isomer and/or converting a resultant free compound into a salt or a resultant salt into the corresponding free compound.

Abstract: N-(3-hydroxy-4-piperidinyl)substituted benzamides, their N-oxide forms and pharmaceutically acceptable acid-addition salts having gastro-intestinal motility stimulating properties, compositions containing the same, and methods of treating warm blooded animals suffering from a decreased peristalsis of the gastrointestinal system.

Abstract: Physically and chemically stable insecticidal preparation in the form of aqueous emulsion or suspension is provided wherein active ingredients which are oily or solid and hardly soluble or insoluble in water are mixed in water with nonionic surfactants having an HLB value of 11 or less and thickeners.

Abstract: A method of making, without use of a solvent, insecticidal pellet compositions of N-hydrocarboyl phosphoroamidothioates and phosphoroamidodithioates is provided.

Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.

Abstract: A composition which comprises (a) at least one insecticide selected from the group consisting of organic phosphorous insecticides, carbamate insecticides and pyrethroid insecticide, (b) crystalline cellulose and (c) crop product powders evaporated with (d) an essential oil and (e) a saccharide respectively in amounts of 0.1 to 10.0% by weight and 10.0 to 40.0% by weight based on the total weight of the composition, which is useful as a bait for the control of noxious insects.

Abstract: Invented are phosphinic acid substituted analogues of steroidal synthetic compounds, pharamaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size.

Abstract: Invented are phosphonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.

Abstract: The invention pertains to novel, potent anticonvulsants, analgesics and cognition enhancers achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to .omega.-[2-phosphonoalkyleneyl)phenyl]-2-aminoalkanoic acids having general formula: ##STR1## Wherein R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, halogen, --CH.dbd.CH--CH.dbd.CH.dbd., amino, nitro, trifluoromethyl or cyano; n and m=0, 1, 2, or 3; and the pharmaceutically acceptable salts and derivatives thereof.

Abstract: The invention relates to novel urease inhibited fertilizer compositions containing urea and a urease inhibiting amount of one or more diaminophosphinyl compounds having oxidized sulfur functions, and methods and composition for inhibiting the activity of urease through use of such compounds.

Abstract: The invention relates to novel urease inhibited fertilizer compositions containing urea and a urease inhibiting amount of one or more o-diaminophosphinyl derivatives of oximes, and methods and composition for inhibiting the activity of urease through use of such compounds.

Abstract: This invention relates to phosphoroamidothioate and phosphoroamidodithioate compounds, to compositions thereof which are useful as pesticides, for example, as athropodicides (that is, insecticides and acaricides), nematocides, and fungicides, and to a method of controlling pests, such as insects, acarids, nematodes, and fungi. The compounds of the invention are effective against soil insects, especially the corn rootworm, when applied by soil application techniques and are also effective when applied to agricultural plants and other plants by foliar application techniques.

Abstract: Dihalovinylphenyl phosphates of the formula I ##STR1## where A and B are each halogen or trihaloalkyl, X is oxygen or sulfur, Y and Z are each oxygen, sulfur or --NH--, R.sup.1 is alkyl, R.sup.2 is alkyl, haloalkyl, alkoxyalkyl or alkylthioalkyl, and R.sup.3, R.sup.4 and R.sup.5 independently of one another are each hydrogen, halogen, nitro, alkyl, cyano, alkoxy, alkoxyalkoxy, alkylthioalkylthio, alkoxyalkyl, alkylthioalkyl, alkylthio, trihaloalkyl or trihaloalkoxy, and pesticides containing these compounds.

Abstract: This invention describes a composition of matter and a method of treating agricultural substrates in which an active ingredient selected from the group consisting of fungicides, bactericides, insecticides, insect repellents, herbicides and plant growth regulators and mixtures thereof is utilized in conjunction with an amount of a glycoside dispersing agent selected from the group consisting of fructoside, glucoside, mannoside, galactoside, taloside, guloside, alloside, altroside, idoside, arabinsode, xyloside, lyxoside and riboside and mixtures thereof which is sufficient to form an emulsion or dispersion of the active ingredient.