Abstract: A composition for application to exterior surfaces, such as trees, so as to prevent animal damage to the exterior surface, has asphalt and denatonium benzoate mixed together. The denatonium benzoate is 1% to 50% by weight of the total composition. The asphalt is between 50% and 60% of the total composition. Naphtha and dimethyl ether are further components of the total composition. The composition is sprayable onto the exterior surface.

Abstract: There is provided a compound of formula (I) wherein R1a, R2a, R3, X1 to X6, a, b and c have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, inhibitors of HDAC enzyme activity, and thus, in particular, in the treatment of conditions where inhibition of HDAC enzyme activity is required.

Abstract: The present invention relates to polymorphic forms of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester, processes therein, pharmaceutical compositions thereof, and uses therewith.

Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as heart failure.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: The present invention relates to insecticidal compositions comprising compounds having an inhibitory activity versus acyl CoA: cholesterol acyltransferase (ACAT) or salts thereof as effective ingredients. The compounds having inhibitory activity versus ACAT have an excellent insecticidal effect by inhibiting sterol metabolism in noxious insects. Therefore, the compounds of the present invention can be used as safe and effective insecticides.

Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

Abstract: A method for treating coronavirus infection by administering to a subject in need of the treatment an effective amount of one or more of the following compounds: aklavin, sanguinarine, amiodarone, chlorpromazine, clomiphene, dihydroergotamine, dipyridamole, emetine, ephedrine, prochlorperazine, promazine, propiomazine, aminacrine, fluphenazine, fenoterol, peruvoside, proglumide, atenolol, nerifolin, nefopam, cycloheximide, avermectin B1, bepridil, cinnarizine, ethisterone, pararosaniline, methylbenzethonium, niclosamide, pipobroman, homidium, calcimycin, anisomycin, metergoline, amodiaquine, danazol, danthron, ethopropazine, eucatropine, nortriptyline, resorcinol, mebhydrolin, mebeverine, trimipramine, triflupromazine, chlorprothixene, cyclobenzaprine, enoxacin, sulfanitran, monensin, nigericin, perphenazine, methoxamine, astemizole, trifluoperazine, acriflavinium, rotenone, acebutolol, quabain, methiothepin, convallatoxin, halcinonide, cyclosporin, pimethixene, mycophenolic acid, promethazine, mesoridazine,

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.

Abstract: This invention relates to hydroxamic acid derivatives having a carbamate linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.

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 present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

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: A compound comprised of a hydrophilic polymer covalently yet reversibly linked to a amine-containing ligand through a dithiobenzyl linkage is described.

Abstract: The present invention is a method for the treatment of Pervasive Developmental Disorders (PDDs) including; Autistic Disorder, Asperger's Disorder, Childhood Disintegrative Disorder (CDD), Rett's Disorder, and PDD-Not Otherwise Specified (PDD-NOS) comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and/or Formula 2 as herein defined and shown below. The present invention is directed to a method for the treatment of Pervasive Developmental Disorders (PDDs) including; Autistic Disorder, Asperger's Disorder, Childhood Disintegrative Disorder (CDD), Rett's Disorder, and PDD-Not Otherwise Specified (PDD-NOS), which includes mono-therapy and alternatively, co-therapy with at least one additional psychoactive medication.

Abstract: A compound having formula (I) and a process for the preparation thereof are described.

Abstract: Disclosed is a stable aqueous gel formulation suitable for topical use comprising water, an anesthetic (e.g., lidocaine hydrochloride), a viscoelastic polymer, and a tonicity modifier, wherein the aqueous gel formulation is free of preservatives and phosphate buffer, is isotonic with physiological fluids, and is sterile and has low particulate count. Also disclosed is a method of inducing topical anesthesia on a tissue or organ, e.g., the eye, of an animal comprising providing a stable aqueous gel formulation comprising water, an anesthetic, a viscoelastic polymer, and a tonicity modifier, wherein the aqueous gel formulation is free of preservatives and phosphate buffer, is isotonic with physiological fluids, and is sterile, and topically administering an effective amount of the aqueous gel formulation to the tissue or organ of the animal.

Abstract: The present invention relates to a novel process suitable for large-scale production of phenyl propane derivatives as well as to novel intermediates in the process.

Abstract: Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1–C6alkylene bridge; A4 is a C1–C6alkylene bridge; D is CH or N; W is, for example, O, NR7 or S; T is, for example, a bond, O, NH or NR7; Q is O, NR7, S, SO or SO2; Y is O, NR7, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, CN, nitro, C1–C6alkyl, C1–C6haloalkyl, C1–C6alkylcarbonyl or C2–C6alkenyl; R4 is, for example, H, halogen, CN, nitro or C1–C6alkyl; R5 and R6 are, for example, H, CN, OH, C1–C6alkyl, C3–C8cycloalkyl, C3–C8cycloalkyl-C1–C6alkyl, C1–C6haloalkyl, C1–C6alkoxy or C1–C6haloalkoxy; R7 is H, C1–C6alkyl, C1–C6alkoxyalkyl or C1–C6alkylcarbonyl; k, when D is nitrogen, is 1, 2 or 3; or, when D is CH, is 1, 2, 3 or 4; and m is 1 or 2; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds and

Abstract: A compound comprising a target cell-specific portion and human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug, or a polynucleotide encoding said NQO2 or said variant or fragment or fusion or derivative. A recombinant polynucleotide comprising a target cell-specific promoter operably linked to a polynucleotide encoding human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug. The compounds and polynucleotides are useful in a method of treating a patient in conjunction with a suitable prodrug.

Abstract: A fungicidally active compound of the formula: a) wherein Q is —NY—NH—, —N?N—, or X is oxygen, sulfur, sulfoxide, or sulfone; n is 0 or 1; Y is hydrogen, C1–C4 alkanoyl, C1–C4 haloalkanoyl, C1–C6 straight chain or branched alkoxycarbonyl, C1–C4 alkoxy(C1–C4)alkoxycarbonyl, C1–C4 alkyl, or C1–C4 haloalkyl; R1 is C1–C6 alkoxy, C3–C6 branched alkoxy, C3–C6 cycloalkoxy, phenoxy, benzyloxy, C2–C6 alkenyloxy, C2–C6 alkynyloxy, C1–C6 haloalkoxy, silyloxy, (C1–C6 alkoxy)-carbonylmethoxy, C1–C6 thioalkoxy, C1–C6 alkylamino, C1–C6 alkyl, C3–C6 branched alkyl, (C1–C6 alkoxy) C1–C6 alkoxy, or (C1–C6 alkoxy)carbonyl; R2 and R3 are each, independently, hydrogen, halogen, C1–C6 alkyl, C3–C6 branched alkyl, C1–C6 haloalkyl, C1–C6 alkoxy, C1–C6 haloalkoxy, cyano, or (C1–C6 alkoxy)carbonyl; R4 is C1–C6 alkyl; and Z1 and Z2 are each independently, carbon or nitrogen, with the proviso that when Z1 is carbon, X is oxygen, and R2 is hydrogen, then R3 cannot be hydrogen; b) wherein R5 is C1–C6 alkoxy; and R6 and

Abstract: A compound represented by the following formula (1) or a salt thereof: wherein R1 represents a C1-12 alkyl group, phenyl group, 1-naphthyl group and the like, R2 represents a C2-12 alkyl group, (R3)b represents 0 to 4 substituents such as a halogen atom, R4 represents a lower alkyl group, R5 represents hydrogen atom or a lower alkyl group, n represents an integer from 2 to 4, and X represents —NH— or —O—, which has superior hypoglycemic action, hypolipidemic action and total cholesterol reducing action, and is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of diseases including diabetes mellitus, hyperlipidemia and the like.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.

Abstract: A compound comprising a target cell-specific portion and human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug, or a polynucleotide encoding said NQO2 or said variant or fragment or fusion or derivative. A recombinant polynucleotide comprising a target cell-specific promoter operably linked to a polynucleotide encoding human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug. The compounds and polynucleotides are useful in a method of treating a patient in conjunction with a suitable prodrug.

Abstract: The invention relates to a highly active, highly specific urokinase inhibitor which is suitable for therapeutic applications and can be synthesized in an extremely simple manner. Surprisingly, it was found that amidino benzylamine derivatives, especially 4-amidino-benzylamine, with two bonded amino acids represent a new group of highly active and very selective uPA inhibitors. The urokinase inhibitors can be used in medical applications, e.g. in the treatment of malign tumors such as in cases of metastatic spread.

Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

Abstract: The present invention relates to novel active compound combinations of a valinamide derivative of the formula 1

Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as heart failure.

Abstract: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds and compositions of this invention.

Abstract: Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.

Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.

Abstract: It is to provide a novel fungicide having high controlling effects on plant diseases particularly on wheat powdery mildew and cucumber gray mold, without ill effects on crops. A carbamate derivative represented by the general formula [I] {wherein X is a halogen atom, a C1-C6 alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a C1-C6 alkyl group, R2 is a hydrogen atom, a C1-C6 alkyl group or the like, R3 is a hydrogen atom or a C1-C6 alkyl group, G is an oxygen atom, a sulfur atom or the like, Y is a hydrogen atom, a C1-C10 alkyl group, C2-C10 alkenyl group or the like, and Q is a hydrogen atom, a C1-C6 haloalkyl group, a phenyl group or the like} and an agricultural/horticultural fungicide containing the same as the active ingredient.

Abstract: The present invention relates to the use of certain resorcinol derivatives as skin lightening agents.

Abstract: The present invention is concerned with pseudopolymorphic forms of 1-(4-carbazolyloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanole (carvedilol) or of optically active forms or pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them.

Abstract: Non-absorbent articles are disclosed. The non-absorbent articles include an effective amount of an aromatic inhibitory compound to substantially inhibit the production of exotoxins by Gram positive bacteria.

Abstract: This invention is directed to a method for preventing or treating neurodegenerative disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II): 1

Abstract: Pharmaceutical compositions containing organic compounds or salts thereof that serve as modulators for the SDF-1 or I-TAC chemokines are disclosed. The compounds and compositions are useful in the treatment of cancer, especially in the inhibition of cancer proliferation, growth, and metastasis. Methods of interfering with SDF-1 and/or I-TAC binding to the CCXCKR2 receptor and treating cancer using the compounds and pharmaceutical compositions of the present invention are also disclosed.

Abstract: In one aspect, the present invention provides a method of inhibiting an Edg-3 receptor mediated biological activity in a cell. A cell expressing the Edg-3 receptor is contacted with an amount of an Edg-3 receptor inhibitor sufficient to inhibit the Edg-3 receptor mediated biological activity. Preferably, the inhibitor is not a phospholipid.

Abstract: The invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes.

Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of renal failure.

Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.

Abstract: Novel biphenyl derivatives of the general formula (I), in which A, X, R1, R1′, R1″, R2 R2′, R2″ and n are as defined in Patent claim 1, stereoisomers thereof and physiologically acceptable salts or solvates thereof are novel inhibitors of integrin receptors, in particular of the &agr;v&bgr;3, &agr;v&bgr;5 and/or &agr;v&bgr;6 integrin receptors. The novel compounds can be used as medicaments.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR&dgr; suptype.

Abstract: This invention provides compounds of formula I having the structure wherein: B, D, C, and R1 as defined herein.

Abstract: The invention relates to trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and the physiologically acceptable salts and the prodrugs thereof. These compounds are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer, diabetes, immuno-modulation, neurologic degenerative diseases, osteoporosis and infectious diseases. The invention also relates to the use of compounds containing fluoromethyl sulfonyl groups as phosphate mimics. These mimics may be used to inhibit, regulate or modulate the activity of a phosphate binding protein in a cell.

Abstract: Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors.

Abstract: Compositions for controlling diseases caused by protozoans of the genus Neospora, which are characterized in that they comprise one or more active compounds which inhibit the microtubulin system of plants.