Abstract: The present invention relates to compositions and methods to modulate &agr;-secretase and/or to improve cognitive ability. The invention further relates the improved/enhanced cognitive ability in diseased individuals, particularly Alzheimer's Disease patients, and treatment thereof through increased sAPP production. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are compounds preferred for use with the present composition. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP comprising the activation of protein kinase C (PKC) by administering an effective amount of PKC activator(s).

Abstract: Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.

Abstract: The invention encompasses novel compounds which are inhibitors of matrix metalloproteinase, ADAM or ADAM-TS enzymes, and which are useful for the treatment of diseases mediated by those enzymes, including degenerative diseases and certain cancers.

Abstract: The present invention relates to methods for treating multidrug resistant cells, preferably multidrug resistant cancer cells with discodermolide. Discodermolide is found to be effective in limiting the growth of otherwise growth unregulated cells having tubulin mutations and in promoting phosphorylation of the oncogene RAF-1.

Abstract: Low concentrations of gossypol and related phyllophage toxins from cotton improve the effectiveness of insecticidal agents against social insects, including cockroaches, and particularly termites and ants. Levels of gossypol and other cotton phyllophage toxins which are sufficiently low as to be non-biocidal to social insects alone, will significantly increase the control efficacy of other insecticidal agents. Consequently, use of these low levels of these cotton phyllophage toxins allows the levels of insecticidal agents necessary for effectively controlling the insects to be significantly reduced relative to applications without cotton phyllophage toxins. Furthermore, insecticidal agents which are normally ineffective for control of social insects when used alone, may be effective when used in conjunction with the cotton phyllophage toxins.

Abstract: Urea-containing, substituted 4-phenyl-[1,3]-dioxanes, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, obesity or a sleep/wake disorder mediated by orexin-2 are described.

Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

Abstract: Compounds of Formula 1: wherein the variables are defined in the specification have cytochrome P450RAI-1 and P450RAI-2 inhibitory activity, and are suitable for treatment of mammals with conditions which are treatable with retinoids, or which are controlled by or responsive to the organism's native retinoic acid. Formulations containing the compounds of the invention can also be co-administered with retinoids and/or Vitamin A to enhance or prolong the effects of medications containing retinoids, Vitamin A, or of the organism's native retinoic acid.

Abstract: Methods of treating a bacterial infection and of killing or inhibiting bacteria are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.

Abstract: Methods for inhibiting cancer, scar formation, disrupting the cellular cytoskeleton, and conferring resistance from infection are disclosed. Such methods comprise the administration of oleuropein and/or the products of its hydrolysis in therapeutically effective amounts. To that end, a variety of pharmaceutical formulations and routes or administration are disclosed and may be utilized to treat a wide variety of diseases.

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

Abstract: Systems and methods for radiographic imaging of tissue using a radio-opaque imaging agent that in one embodiment accumulates intracellularly in tissue in proportion to its functional, or physiological, activity. In one embodiment, the imaging agent is a cell membrane-permeable, radio-opaque, high affinity ligand for an intracellular target. The imaging agent is administered to a patient, and after an accumulation interval, radiographic images are acquired. The imaging agent preferentially accumulates in certain types of tissue and increases its radio-opacity. The tissue being examined is transilluminated by X-ray beams with preselected different mean energy spectra, and a separate radiographic image is acquired during transillumination by each beam. An image processing system may perform a weighted combination of the acquired images to produce a single displayed image. The system and method thus provides a functional image displayed with the anatomical detail and spatial resolution of a radiographic image.

Abstract: Chemical compositions having superior nematicidal properties are formulated. The compositions contain one or more selected aldehydes as the major component and one or more aliphatic or cyclic isothiocyanates as a minor component. Preferred mixtures contain furfural and one or both of methyl isothiocyanate and allyl isothiocyanate. Plant-parasitic nematodes are controlled by contacting the nematodes with the nematicidal compositions, by, for example, applying the compositions to soil or other plant growth media containing the nematodes.

Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: A compound of formula (I): wherein: R1 represents hydrogen, halogen, alkyl or alkoxy, X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.

Abstract: Compounds having therapeutic utility are of formula (I) B—X—(CH2)n—CR2R3—CR4R5—COY  (I) wherein n=0-1; X is S(O)0-2; Y is OR1 or NHOH; R2 and R4 are independently H or a group (optionally substituted with R10) selected from C1-6 alkyl, C2-6 alkenyl, aryl, C1-6 alkyl-aryl, heteroaryl, C1-6 alkyl-heteroaryl, heterocycloalkyl, C1-6 alkyl-heterocycloalkyl, cycloalkyl and C1-6 alkyl-cycloalkyl; and R1, R3 and R5 are independently H or C1-6 alkyl, provided that not more than two of R2, R3, R4 and R5 are H; or any of CR2R3, CR4R5 and CR2—CR4 is a cycloalkyl or heterocycloalkyl ring optionally substituted with R10 or a group (optionally substituted with R10) selected from C1-6 alkyl, aryl, C1-6 alkyl-aryl, heteroaryl and C1-6 alkyl-heteroaryl; B is heterocycloalkyl (optionally substituted by R6 or R7) bonded through carbon to X, or C1-6 alkyl-heterocycloalkyl (optionally substituted with R6 or R7), or a group (substituted with R6) selected from C1-8 alkyl

Abstract: Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.

Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Abstract: The present invention relates to novel compositions based on hydrated lipidic lamellar phases or liposomal compositions, prepared by combining different lipid molecules, synthetic and/or from natural sources, said compositions comprising at least one of a) labd-13-ene-8&agr;, 15-diol and/or derivatives thereof; b) labd-14-ene-8, 13-diol or derivatives thereof; c) 3&bgr;-hydroxy-labd-14-ene-8, 13-epoxy and/or derivatives thereof, d) a plant extract containing the aforementioned labdenes or derivatives thereof. The compositions of the invention exhibit cytotoxicity against cancerous cells and are utilized for the treatment of tumors and leukemias.

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: This invention relates to compounds containing a trioxane moiety, especially certain artemisinin derivatives, which have cytotoxic and antitumour activity and their use in the treatment of cancer. Some of these compounds comprise a ligand which is capable of binding to a nucleic acid and a group containing a trioxane moiety which is capable of acting as source of free radicals which are capable of chemically interacting with a nucleic acid. Processes for the preparation of such compounds and pharmaceutical compositions containing such compounds are also provided.

Abstract: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.

Abstract: A method of treating plant and animal systems and inanimate surfaces for the purposes of controlling plant pests, introducing pesticides and nutrients into plants, mitigating frost damage to plants, increasing crop yields, controlling certain plant diseases, controlling arthropod, bacterial, fungal, mycoplasma, rickettsia, and viral pests of animals and humans, and disinfecting inanimate surfaces. The method utilizes the unique multi-directional dispersion property of the tannate complex of picro ammonium formate and the tannate complex of picro cupric ammonium formate, in aqueous solution, combined with a minor amount of a surfactant sufficient to prevent formation of ammonium picrate, to penetrate plant and animal systems and inanimate surfaces and travelling multidirectionally therein. The method is carried out by introducing a small but effective amount of the tannate complex to the plant or animal system or inanimate surface.

Abstract: The present invention provides a novel bioactive substance having an antiangiogenic effect. The chemical compound represented by the formula (1) (wherein, R1 represents hydrogen atom, aldehyde group or a lower acyl group, R2 and R3 are the same as or different from each other and represent hydrogen atom or a lower alkoxy group or are combined to represent oxygen atom, R4 represents a lower alkyl group and R5 represents hydrogen atom or a lower alkyl group, provided that compounds in which R1 is aldehyde group, R2 and R3are different from each other and are hydrogen atom or methoxy group, R4 is ethyl group and R5 is hydrogen atom are excluded), a salt thereof or a hydrate thereof was isolated from the culture broth of genus Streptomyces and the structure thereof was analyzed.

Abstract: The present invention relates to new compounds of the formula (I) 1

Abstract: A method for treating neurodegenerative diseases in a warm-blooded animal comprising administering to a warm-blooded animal in need thereof an amount of a compound of the formula wherein A selected from the group consisting of hydrogen and wherein the substituents are defined as set forth in the specification.

Abstract: Compounds represented by the formula: 1

Abstract: An antibiotic SF2487 substance having the formula (I) 1

Abstract: The invention concerns a compound of formula (I), wherein, for example: R1 is of the formula —NHC(═O)(1-4C)alkyl; R2 and R3 are hydrogen or fluoro; R4 and R5 are hydrogen or methyl; >A-B- is of the formula >C═CH—, >CHCH2, or >C(OH)CH2—(> represents two single bonds); D is O, S, SO, SO2 or —NR7; wherein R7 is hydrogen, R10CO—, R10SO2—, RaOC(Rb)═CH(C═O)—, RcC(═O)C(═O)—, RdN═C(Re)C(═O)—, RfNHC(Rg)═CHC(═O)— or R14CH(R13)(CH2)m—; wherein R10 is (1-6C)alkyl [optionally substituted by, for example, hydroxy or (1-6C)alkanoyl], R11C(O)O(1-6C)alkyl or R12O—; wherein R11 is optionally substituted (1-6C)alkyl; R12 is optionally substituted (1-6C)alkyl; Ra, Rb, Rc, Rd, Re, Rf, Rg are (1-6)alkyl; m is 0 or 1; R13 is cyano; R14 is hydrogen or (1-4C)alkyl; >X—Y— is of the formula >C═CH— or >CHCH2—; and pharmaceutically acceptable salts thereof

Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.

Abstract: The present invention relates to novel Pyrrole-Type compounds, compositions comprising Pyrrole-Type compounds, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a composition comprising a Pyrrole-Type compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for treating or preventing a viral infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the replication and/or infectivity of a virus.

Abstract: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.

Abstract: The invention relates to an antibiotic substance of microbial origin, arbitrarily denominated GE23077 complex and the individual factors which constitute it, a mixture of said factors in any proportion, the pharmaceutically acceptable salts and compositions thereof, and their use as an antibacterial agent having a selective inhibitory activity against E. coli RNA polymerase.

Abstract: The invention concerns a composition capable of being hydrolyzed by a cutaneous enzyme, glucocerebrosidase. The active precursor is advantageously a gluco-conjugate derived from phenol whereof the two &agr; carbons are free. The invention also concerns the use of such compositions against light-induced skin ageing or for making a medicine for treating certain skin diseases. The invention further concerns novel glucosylated compounds.

Abstract: Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.

Abstract: Sesquiterpene epoxide compounds (trichothecenes) and methods for administering such compounds to achieve apoptotic ablation of internal organs or internal non-malignant cell populations are disclosed.

Abstract: Disclosed is a pharmaceutical composition, comprising a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxcodone or a pharmaceutically acceptable salt thereof, said combination in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising administering to the patient a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxycodone or a pharmaceutically acceptable salt thereof such that the dosing interval of the rofecoxib overlaps with the dosing interval of the oxycodone, said combination in an amount sufficient to provide an analgesic effect in a human patient.

Abstract: A method of potentiating the effects of blood pressure reducing agents in warm-blooded animals, said method comprising administering to said warm-blooded animals of an effective amount of a blood pressure reducing agent and a 2,2′-iminobisethanol derivative.

Abstract: A method for treating wood, characterized by impregnating wood with a metal-containing treating agent containing lignin and/or lignin derivatives and a metal, a metal compound, and/or a metal ion and oxidizing and/or macromolecularizing of the lignin and/or lignin derivatives in the wood to fix the metal component in the wood, and wood and woody materials obtained by the treating method. According to the method of the present invention, while effectively utilizing lignins, lignosulfonic acids, or lignosulfonic acid salts, leaching of the metal component can be suppressed to a low level to thereby retain the effects due to the incorporation of the metal components for a prolonged period.

Abstract: The present invention involves a method for slowing heart valve degeneration in which an inhibitor of hydroxymethylglutaryl CoA reductase is administered.

Abstract: Compounds expressed by the following general formula (1), The compounds can be used as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension; alopecia, acne, psoriasis, dermatitis, hypercalcemia, hypoparathyroidism and metabolic disorder of cartilage.

Abstract: The use of a medium-chain fatty acid triglyceride as the dispersant in the preparation of a medicinal aerosol composition comprising tricyclic compound (I) dispersed in a liquefied hydrofluoroalkane propellant is described. When a liquefied hydrofluoroalkane is added to a kneaded premix of the tricyclic compound (I) and a medium-chain fatty acid triglyceride, the active ingredient is evenly dispersed in the liquefied hydrofluoroalkane. Therefore, by distributing a dispenser first with the kneaded premix and, then, with a liquefied hydrofluoroalkane under cooling or elevated pressure, there can be provided a medicinal aerosol composition an improved uniformity of content of the active ingredient.

Abstract: This invention relates to substituted benzo[1,2-b:5,4-b′]dipyran-4-amines which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and a topic disorders (for example, a topic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzo[1,2-b:5,4-b′]dipyran-4-amines which are CCR5 receptor antagonists. Furthermore, since CD8+T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therpeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.

Abstract: This invention is related to substituted 2-aminoacetamides represented by Formula II: or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1, R2, R3 and R4 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R5, R6 and R7 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R5, is defined as above, and R6 and R7 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR8, CH2, C(O), NR8C(O), C(O)NR8, SO, SO2 or a covalent bond; where R8 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or

Abstract: Compositions which comprise sorbic acid and/or one or more sorbates, and a flavonoid and/or flavonoid derivative, a method for the preparation thereof, and their use.

Abstract: The subject invention relates the use of cembranoids to inhibit nicotine addiction at the behavioral level. The subject host is sensitized to nicotine. Cembranoids are then administered to reduce such sensitization.

Abstract: Novel cyclic ether vitamin D3 compounds having a cyclic ether side chain are disclosed. These compounds were first identified as metabolites of 3-epi vitamin D3 produced via a tissue-specific metabolic pathway which catalyzes the formation of a cyclic ether structure. Also disclosed are 1&agr;(OH) 3-epi vitamin D3 compounds, which are produced via the epimerization of a 3-&bgr;-hydroxyl group of 1&agr;(OH) vitamin D3 precursor in vivo. The vitamin D3 compounds of the present invention can be used as substitutes for natural and synthetic vitamin D3 compounds.

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: Described are methods for treating, preventing, or reducing the risk of the onset of Alzheimer's disease by administering a therapeutically effective amount of an inhibitor of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (“HMG CoA reductase inhibitor”) to a patient who is at risk for a coronary or cerebrovascular event or at risk for Alzheimer's disease.