Abstract: The composition of the present invention comprises a sodium channel blocking compound which is capable of specifically binding to a site, either on an SS1 region or an SS2 region, on an extracellular region of a sodium channel alpha subunit, and a pharmaceutically acceptable carrier.

Abstract: Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, in which: R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH; R2 is a mono- or bicyclic aromatic ring system or a mono- or bicyclic heteroaromatic ring system; R3 is C1-20alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-5alkyl, C1-10alkoxyC1-10alkyl, or an aromatic or heteroaromatic ring system; W is SO2 or a bond; X is O or S; and Y is a group of the formula A1—A2—A3 in which A1 and A3 each represent a bond or a straight chain or branched alkylene group, said alkylene group(s) containing a total of 1 to 10 carbon atoms and A2 represents a bond or O, S, SO, SO2, CO, C═CH2, CONH, NHCO, CR15R16, CH═CH or C═C, providing that when A2 is O, S, SO, SO2 or CONH, A3 contains at least two carbon atoms linking the A2 group and the CH2 group in formula (I).

Abstract: The invention provides an aqueous SC formulation comprising: a) 50 to 80% w/v pyrimethanil; b) 0.2 to 5% w/v of a polyoxyethylene-polyoxypropylene block copolymer surfactant; and c) 0.2 to 5% w/v of a naphthalene formaldehyde condensate surfactant. We have found that formulations according to the invention surprisingly do not solidify when milled during manufacture and also exhibit a low propensity to crystallise when stored for prolonged periods.

Abstract: Dihydronaphthalene compounds have excellent 17&agr;-hydroxylase/C17-20-lyase inhibiting activity, thromboxan A2 synthesis inhibiting activity, and aromatase inhibiting activity and are thereby are useful as preventive and/or therapeutic agents for various male sex hormone- and female sex hormone-dependent diseases such as prostate cancer, prostatomegaly, masculinization, breast cancer, mastopathy, uterine cancer, endometriosis, and ovarian cancer, as well as myocardial infarction, angina pectoris, and bronchial asthma.

Abstract: A method of preventing or treating an opioid-induced side effect in a patient who has been chronically taking opioids, the method comprising administering a quaternary derivative of noroxymorphone in an amount sufficient to prevent or treat the side effect in the patient, but which amount would be insufficient to treat a patient with the same opioid-induced side effect who had not chronically been administered opioids.

Abstract: Structurally novel kappa opioid receptor antagonists are provided and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.

Abstract: The invention provides compounds and compositions of the formula: wherein the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl; R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl; each R3 is independently a substituent selected from -halogen, —OR′, —OC(O)R′, —NR′R″, —SR′, —R′, —CN, —NO2, —CO2R′, —CONR′R″, —C(O)R′, —OC(O)NR′R″, —NR″C(O)R′, —NR″C(O)2R′, , —NR′—C(O)NR″R′″, —NH—C(NH2)═NH, —NR′C(NH2)═NH, —NH—C(NH2)═NR—, —S(O)R′, —S(O)2R′, —

Abstract: The invention provides compounds of formula (I) wherein R1 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a hydroxy group, an alkoxy group having from 1 to 6 carbon atoms, a halogen atom, a nitro group, an amino group, a monoalkylamino group wherein the alkyl moiety has from 1 to 6 carbon atoms, a dialkylamino group wherein each alkyl moiety may be the same or different and each has from 1 to 6 carbon atoms, a dialkoxyamino group wherein each alkoxy moiety may be the same or different and each has from 1 to 6 carbon atoms, an alkanoyalmino group having from 1 to 20 carbon atoms or an alkanesulfonylamino group having from 1 to 6 carbon atoms; R2 represents a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms; and R3 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an alkoxy group having from 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof.

Abstract: Compounds of formula I, wherein R1, R2, R3 and Ra Rh are as defined in the specification. The compounds are useful in the prophylaxis and in the treatment of arrhythmias, in particular a trial and ventricular arrhythmias.

Abstract: Disclosed are compounds of the formula or pharmaceutically acceptable salts thereof wherein: represents: and A, B, G, D, E, Ra, Rb, W, and Z are defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

Abstract: Disclosed are novel substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are suitable for administration to patients as continuous infusion solution and are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds and methods for the treatment and/or control of cancer.

Abstract: Methods for the prevention, treatment, or management of apnea, apnea disorders, bulimia nervosa, irritable bowel syndrome, urinary incontinence, bradycardia, bradyarrhythmia, syncope, other disorders, or symptoms thereof using (−) norcisapride, or a pharmaceutically acceptable salt thereof, substantially free of its (+) stereoisomer.

Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.

Abstract: Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable arylsulfonyl or heteroarylsulfonyl group attached to the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditions to provide the proton pump inhibitors with a half life measurable in hours, and are capable of providing sustained plasma concentrations of the proton pump inhibitor drugs for longer time than presently used drugs. The generation of the proton pump inhibitor drugs from the prodrugs of the invention under physiological conditions allows for more effective treatment of several diseases and conditions caused by gastric acid secretion.

Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ═C(R1a)— or —[N□(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted bi

Abstract: Compounds of the formula useful for the treatment of depression and other conditions such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, sexual dysfunction, eating disorders, addictive disorders caused by ethanol or cocaine abuse and related illnesses.

Abstract: Compounds of formula (One) wherein A1, A2, A3, and A4 independently H, halogen, or methyl; E is —N═ or —CH═; G is O═ or S═; J is —O—, —NH— or —NT1— wherein T1 is alkyl having 1 to 6 carbon atoms; L1, L2, and L3 are independently H, halogen, cyano, methyl, monohalomethyl, dihalomethyl, or trihalomethyl; M is —S—, —S—(═O), or —S(═O)2—); and Q is aryl, substituted aryl, heteroaryl, or substituted heteroaryl. The compounds are useful as fungicides.

Abstract: The present invention relates to muscarinic receptor modulators, specifically, 7-oxo-2-azabicyclo[2.2.1]heptanes of formula (I) which are useful for the treatment of various diseases and conditions, for example, Alzheimer's disease, glaucoma, psychosis, particularly schizophrenia or schizophreniform conditions, mania, pain, bipolar disorder, depression, sleeping disorders, epilepsy, gastrointestinal motility disorders, urinary incontinence, and cognition enhancement.

Abstract: Novel disubstituted imidazoles are disclosed which are useful in the treatment of bacterial infections, particularly through the inhibition of FAB I.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Abstract: A method of protecting a corn plant from destructive insects which comprises applying to the seed from which it grows or the soil from which the seed grows a composition comprising an insecticidal 1-arylpyrazole and an insect repellent. A composition comprising the insecticidal 1-arylpyrazole and the repellent.

Abstract: The invention provides autoinducer-2 analogs that regulate the activity of autoinducer-2 and methods of using such analogs for regulating bacterial growth and pathogenesis.

Abstract: This invention provides estrogen receptor modulators of formula 1, having the structure wherein X, Y1, Y2, Y3, Y4, Z1, Z2, Z3, and Z4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.

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: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: The strength of a nitroglycerin dosage to be administered to patients suffering from angina can be reduced when a portion of the dosage is replaced with menthol containing substances (MCS). MCS and specifically 1% Menthol has been found to potentate the effect of nitroglycerin. Accordingly, MCS can be used as a substitute for a portion of the nitroglycerin dosage administered to a patient. Side-effects common to nitroglycerin usage such as headache and fainting are significantly reduced when a nitroglycerin/MCS solution is used which has 50% of the nitroglycerin dosage per spray commonly used without sacrificing treatment effectiveness.

Abstract: This invention relates to new antiestrogens of the general formula in which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens). Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.

Abstract: The present invention is directed to the use of jojoba oil esters to treat and prevent envelope virus infections. Jojoba oil esters applied to the skin alone or in combination with other compounds are effective for treating and preventing viral infections.

Abstract: The present invention relates to a composition comprising a nano-emulsion that contains 5-aminolevulinic acid as well as a carrier in an aqueous phase. This invention also relates to a pharmaceutical preparation containing this composition. The nano-emulsions of this type can be used in photodynamic therapy as well as in the photodiagnostic detection of proliferatives cells.

Abstract: Administration of a pharmaceutical composition in the form of a suppository comprising: (a) a prostaglandin vasodilator; (b) 15-hydroxyprostaglandindehydrogenase inhibitor: and (c) a base material that is solid at room temperature and releases components (a) and (b) when inserted in the urethra, is effective for the treatment of male erectile dysfunction.

Abstract: The present invention relates to the compounds of formula: in which R1, R2, R3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.

Abstract: Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an &agr;-1-adrenergic antagonist, &agr;-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

Abstract: The present invention is directed to a liquid formulation of metformin or its pharmaceutically acceptable salts thereof. The liquid pharmaceutical composition comprises a therapeutically effective amount of metformin or its pharmaceutically acceptable salt, in a liquid carrier, which may also include a sweetener that does not increase the blood glucose level of a subject after ingestion thereof. In one embodiment, it may also include alkyl hydroxyethylcellulose, and/or a polyhydroxy alcohol. In another embodiment, the carrier may contain a sweetener, mineral acid, and bicarbonate salt maintained at a pH of 4.0 to 9.0. It is useful for treating hyperglycemia and diabetes.

Abstract: The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide (I) or repaglinide and at least one other antidiabetic compound selected from the group consisting of thiazolidinedione derivatives (glitazones), sulfonyl urea derivatives and metformin for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of diseases, especially metabolic disorders and in particular type 2 diabetes and diseases and conditions associated with diabetes; to a composition, respectively, which comprises nateglinide and a pharmaceutically acceptable carrier and to a process of making such composition; the use of such combination or composition for the preparation of a medicament for the prevention, delay of progression or treatment of metabolic disorders; a method of prevention, delay of progression or treatment of diseases in warm-blooded animals; the use of such combination or composition for

Abstract: The present invention relates to compositions and methods for decreasing the infectivity, morbidity, and rate of mortality associated with a variety of pathogenic organisms and viruses. The present invention also relates to methods and compositions for decontaminating areas colonized or otherwise infected by pathogenic organisms and viruses. Moreover, the present invention relates to methods and compositions for decreasing the infectivity of pathogenic organisms in foodstuffs.

Abstract: Methods for treating mammals for neurointoxication are provided comprising treating the mammal with a xenon-containing gas. Methods of providing neuroprotection in mammals are also disclosed comprising administering therapeutically effective amounts of xenon, preferably in combination with pharmaceutically acceptable carriers, diluents or excipients.

Abstract: A method is disclosed for enhancing the activity of a particulate Dispersed Active Metal (DAM) catalyst during operation of a reactor wherein the hydrogenation of carbon monoxide to produce a mixture of hydrocarbons is being carried out comprising withdrawing a mixture of hydrocarbons and a portion of the DAM catalyst from the reactor, reducing the hydrocarbon content thereof with hydrogen at a temperature above the temperature of the reactor, oxidizing a slurry of the catalyst particles in a suitable fluid at low temperature to form an oxidized precursor, reducing the precursor at elevated temperature to reform the catalyst and returning it to the reactor. The catalyst may be passivated before returning to the reactor.

Abstract: Semipermeable porous membranes having an average pore diameter in the range 0.01-3 &mgr;m, and porosity in the range 30%-90%, based on semi-crystalline fluoropolymers and the respective preparation process, wherein the semi-crystalline fluoropolymers comprise: (a) from 10 to 70% by moles of ethylene, (b) from 30 to 90% by moles of a fluorinated monomer selected from tetrafluoroethylene, chlorotrifluoroethylene, or mixtures thereof, (c) from 0.1 to 30% by moles, with respect to the total amount of monomers (a) and (b), of a hydrogenated monomer of formula: CH2═CH—(CH2)n—R1  (I) wherein R1=—OR2, or —(O)tC(O)pR2 wherein t and p are integers equal to 0.

Abstract: Disclosed is an acrylic sol for a sound insulating underbody coating. It includes acrylic polymer fine particles, a plasticizer, a filler, a plasticizer, a blocking type urethane resin, a curing agent and a foaming agent. Since it includes the acrylic polymer particles as a major constituent unit, it does not generate a hydrogen chloride gas and dioxins when it is burned. Moreover, since the paint film resulting from the acrylic sol has a net-shaped structure by the cross-linkage reactions of the urethane resin, and since the bulkiness of the paint film is increased by the foaming agent, it has a good cold resistance and adhesion property toward automotive steel plates, and effects a superb chipping resistance and sound insulating performance.

Abstract: A process additive for polyolefin films and foams produces products having reduced aging time and reduced greasiness and reduced grease-like transfer as compared to glycerol monostearate (GMS). Carbon dioxide based blowing agents are suitable. The process additive comprises a fatty acid N-aliphatic alcohol amide of the general formula R—CON(R′)R″. R is a fatty hydrocarbon radical having from about 8 to 30 carbons. R′ typically is hydrogen. R′ can also be an alkyl radical of from about 1 to 6 carbons or an alkyl alcohol radical of from about 1 to 6 carbons. R″ is an alkyl alcohol fragment of from about 1 to 6 carbons. The alkyl alcohol fragments can be monohydric or polyhydric. Secondary fatty monoalkanolamides in which R′ is hydrogen are particularly useful, especially stearamide monoethanolamine (MEA).

Abstract: To provide a microporous film having excellent permeability and mechanical strength as well as excellent SD function at low temperatures and film-breaking resistance at high temperatures. A microporous film made of a resin composition at least comprising 1 to 50% by weight of a ring-opening polymer of an unsaturated condensed alicyclic compound, and 1 to 50% by weight of one or more resin components selected from the group consisting of polyolefins having a weight-average molecular weight of 500000 or less, thermoplastic elastomers and graft copolymers.

Abstract: Compositions for the formation of temperature resistant, tough, flame retardant polyurethane foams, comprising a low VOC polyisocyanate component wherein the isocyanate is a low functionality isocyanate; a low VOC active-hydrogen containing component substantially reactive with the low functionality isocyanate to form a polyurethane; a surfactant composition; and a catalyst component, wherein the total mass loss of the foam is less than 1% by weight as measured by ASTM E595. The foams are useful as gasketing materials, for example.

Abstract: The invention disclosed includes a coating composition for siliceous surfaces. The coating includes at least one component from the group consisting of poly(alkoxy)silane, poly(halo)silane, alkoxysilane, halosilane, and mixtures thereof and a catalyst compound which generates a proton to hydrolyze the component when exposed to radiation. Preferably, the catalyst is a photo-acid. The invention also includes a method of coating the optical fiber. The aforementioned coating is applied to an exterior surface of the fiber. A proton is generated to promote the hydrolysis of the component. The invention further includes a method of accelerating adhesion between the exterior surface of the article and the coating. The inventive coating is applied to the surface of the fiber and the coating is exposed to a radiation source.

Abstract: Highly comfortable hydrophilic contact lenses are made from a coploymer of an ethylenically unsaturated fluoro-sulfone ester, ethylenically unsaturated fluorosulfone ester monomer of acrylic or methacrylic acid having alkyl hydroxy group and N-Vinyl 2-pyrrolidinone and methods for the manufacturing thereof.

Abstract: An elastomer system having biocide properties is described, useful, in particular, for dental impressions. An efficient system is provided for destroying microbes, without adversely affecting the crosslinking properties and the mechanical qualities of RTV 2 elastomers. Said system comprises an RTV 2 silicone, preferably SiH/SiVi polyaddition product and a biocide selected among active chlorine precursors, preferably among N-chloramines. The system may include functional additives (silicon fillers, alumina, paraffin, vaseline oil). As for the biocide, it can be provided with an antiseptic auxiliary adjuvant along with EDTA-type sequestering agents.

Abstract: To provide a dental alginate impression material composition without the defects of the conventional alginate impression material compositions using a pH indicator, that the confirmation of the completion of the gelation is inaccurate and difficult, and that they are poor in the affinity with water to be used during the mixing, the dental alginate impression material composition containing an alginate, a gelling reaction material, a gelling adjustment material, and a filler as major components further contains 0.001 to 0.1% by weight of one or more pH indicators selected from Cresol Red, &agr;-naphtholphthalein, Tropaeolin OOO, Thymol Blue, and phenolphthalein; 0.1 to 10% by weight of a water-soluble polyether that is a liquid at 25 ° C.; and 0.001 to 5% by weight of an inorganic pigment and/or an organic pigment having a color distinctly different from a color tone caused by color formation of the pH indicator during the gelation upon mixing with water.

Abstract: The antifouling composition of the present invention includes a glassy matrix formed by crosslinking a mixture of a silanol-terminated silicone and an alkoxy functionalized siloxane to provide an interpenetrating polymer network of glass and silicone and at least two materials capable of microphase separation, at least one of which is graftable to the glassy matrix.

Abstract: The invention relates to an antifouling paint having a binder comprising a rosin material and an auxiliary film-forming resin, the paint including an ingredient having marine biocide properties, wherein the binder comprises a blend of the rosin material and an auxiliary film-forming resin in a ratio of 20:80 to 95:5 by weight, the auxiliary film-forming resin comprising 20-100% by weight of an acid-functional film-forming polymer (A) whose acid groups are blocked by groups capable of hydrolyzing or dissociating to leave a polymer soluble in sea water, the blocking groups being selected from divalent metal atoms bonded to a monovalent organic residue, divalent metal atoms bonded to a hydroxyl residue and monoamine groups which form an organic solvent soluble amine salt of the polymer, and 80-0% by weight of a non-hydrolyzing water-insoluble film-forming polymer (B).

Abstract: This invention relates to an organic foundry binder containing an alkyl resorcinol, or preferably a readily available mixture of alkyl resorcinols, and derivatives thereof. Preferably, the organic foundry binder is a furan binder. Foundry mixes are prepared by mixing the binder with a foundry aggregate. Foundry shapes (molds and cores) are prepared by shaping the mix and allowing it to cure to form a workable foundry shape. The invention also relates to the preparation of metal castings using the foundry shapes and the metal castings prepared with the foundry shapes.