Abstract: Prodrugs of ion channeling modulating compounds, including, for example, prodrugs of the ion channel modulating compound of the following formula: are described herein, as well as methods of making and using such prodrugs and pharmaceutical compositions containing such prodrugs.

Abstract: The invention relates to novel substituted 1H-pyrrole-2,5-diones of the formula (IA) in which A?, Ar? and R? are as defined in the description, to novel compositions for controlling animal pests based on substituted 1H-pyrrole-2,5-diones of the formulae (I) and (IA) in which A, A?, Ar, Ar?, R and R? are as defined in the description, and to processes for their preparation.

Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:

Abstract: The present invention features maleiimide compounds, pharmaceutical compositions of maleiimide compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more maleiimide compounds of the invention.

Abstract: A method of treating a patient suffering from a condition or disorder selected from chronic pain, neuropathic pain, fibromyalgia, migraine, bipolar disorder and depression comprises the administration of a pharmacologically effective amount of 3-(phenylmethylamino-methylene)pyrrolidine-2,4-dione (I) or a pharmaceutically acceptable salt or prodrug or solvate thereof. Also disclosed is the use of (I) for the manufacture of a pharmaceutical composition for treatment of such condition or disorder.

Abstract: Tetramic acid analogues of Formula I and Formula II have antibacterial activity, primarily against gram-positive bacteria, and are iron chelators.

Abstract: The present invention relates to novel compounds from Antrodia camphorata and the use thereof.

Abstract: The present invention relates to the use of at least one compound capable of cleaving the diketone crosslinking bonds between two proteins, in a composition applied topically to the skin, as an agent for preventing or treating the signs of ageing of the skin or the orange-peel appearance. The above compound is preferably a N-hydroxy imide of formula (I). These N-hydroxy imides have inhibitory properties on the glycation of proteins and also antioxidant properties. The invention also relates to novel N-hydroxy imides included in formula (I) above.

Abstract: The presently disclosed subject matter relates generally to the fields of molecular biology and medicine. More particularly, it concerns methods involving the use of GSK3 inhibitors in combination with radiation therapies. In some embodiments, administration of a GSK3 inhibitor to a subject results in an amelioration of cognitive decline, toxicity to vascular endothelial cells, and/or neuron death associated with radiation therapy alone.

Abstract: The present invention relates to pharmaceutical agents which are agents for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia or osteoporosis; the pharmaceutical agents frailty suppressants, muscle strength enhancers, muscle increasing agents, cachexia suppressants, body weight decrease suppressants, agents for the prophylaxis or treatment of prostate hypertrophy, amyotrophy or muscle loss caused by a disease or an agent for reducing the prostate weight.

Abstract: The present invention relates to the use of PDE1C as a novel target for the identification of compounds, which can be used for the treatment of pulmonary hypertension, fibrotic lung diseases or other fibrotic diseases outside the lung. The present invention further relates to the use of PDE1C inhibitors in the manufacture of pharmaceutical compositions for use in the therapy of those diseases.

Abstract: The present invention relates to the use of tetramic acid derivatives of the formula (I) in which A, B, G, W, X, Y and Z are as defined above for controlling insects from the suborder of the plant lice (Sternorrhyncha).

Abstract: The use of vacuolar ATPase inhibitors in the prevention and/or treatment of septic shock is herein described. Vacuolar ATPase inhibitors are selected among products of natural, semi-synthetic or synthetic origin.

Abstract: The present invention is to provide a composition for preventing plant diseases which comprises at least Component I and Component II, is capable of obtaining a synergic effect that cannot be expected with each single component, is capable of markedly increasing a control effect in a much smaller amount of chemicals against various plant pathogens, and causes no phytotoxicity suffering. A composition for preventing plant diseases comprises Components I and II as active ingredients. The Component I is (RS)—N—[2-(1,3-dimethylbutyl)thiophen-3-yl]-1-methyl-3-tri fluoromethyl-1H-pyrazole-4-carboxamide.

Abstract: The novel active compound combinations of certain cyclic ketoenols and ethiprole have very good insecticidal and acaricidal properties.

Abstract: A proliferation of cells can be reduced by contacting the cells with a compound having formula (I) where R and R? are each alkyl groups, R? is hydrogen or an alkyl group and X3, X4 and X5 are each independently selected from the group consisting of hydrogen, benzyl, t-butyldimethylsiloxy radical and triphenylmethyl. Accordingly, compounds of formula (I) can be used for treatment of tumors including melanoma. Also a secretion of a matrix metalloproteinase (MMP) enzyme by cells can be reduced by contacting the cells with the compound having formula (I). Accordingly, compounds of formula (I) can be used for treatment physiological conditions associated with an elevated MMP level, such as tumors.

Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.

Abstract: Compounds having a hydrophobic group with a group and capable of reacting with the cysteine residue for the binding to protein MD-2 are disclosed. The compounds are capable of covalently binding to MD-2, which can be either free or in the complex with other molecules. The compounds are capable of replacing other ligands or preventing a binding of other ligands, especially bacterial endotoxin (lipopolysaccharide-LPS), which can otherwise lead towards unwanted activation of the immune response and acute or chronic inflammatory diseases.

Abstract: The invention relates to novel 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) in which A, B, D, G, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant tolerance promoter compound.

Abstract: Compounds of the Formula I, wherein A1 is O or NH; A2 is O or S; each of R1 and R2 is independently hydrogen, a methyl or C2-C8-saturated or mono- or doubly unsaturated, branched or linear hydrocarbon group; and R3 is a C1-C18-saturated or mono- or doubly unsaturated, branched or linear hydrocarbon group wherein, each of R1, R2 and R3 comprises a heteroatom selected from the group consisting of O and S in the chain and/or is mono- or multiply-substituted by a substituent selected from the group consisting of halogen, hydroxy, C1-C6-alkyl, trifluoromethyl, C1-C6-alkoxy, C6-C10-aryl, and C1-C6-alkyl-C6-C10-aryl are useful for controlling the interaction process between microorganisms such as in the development and/or maturation of biofilms; multicellular swarm behavior; the concerted development of antibiotic resistances; the concerted synthesis of antibiotics; the concerted synthesis of pigments; the concerted production of extracellular enzymes; or the concerted production of virulence factors.

Abstract: The present invention relates to the use of selective insecticidal and/or acaricidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising (a) at least one substituted cyclic dicarbonyl compound of the formula (I) in which W, X, Y and Z are as defined in the description and CDC is one of the dicarbonyl radicals mentioned in the description, and (b) at least one crop plant compatibility-improving compound from the group of compounds given in the description. for controlling insects and/or arachnids, and also to a method for controlling insects and/or arachnids using the compositions.

Abstract: Metal chelators of formula (I) and formula (II) are disclosed or a farmaceutically acceptable salt thereof. Also disclosed are metal chelator-targeting moiety complexes, metal chelator-targeting moiety-metal conjugates, kits, and methods of their preparation and use in diagnosis and/or treatment of diseases and conditions, including, inter alia, cancer and thrombosis.

Abstract: Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.

Abstract: The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis of diseases in people or animals, especially diseases of bacterial infection.

Abstract: The invention relates to novel 3-phenyl-substituted, 3-substituted 4-ketolactams and -lactones of the formula (I) in which Q, W, X, Y, A, B and G are as defined in the disclosure, to processes and intermediates for their preparation and to their use as pesticides and herbicides.

Abstract: The present invention provides novel cationic amphiphiles capable of facilitating transport of biologically active molecules into cells wherein the said amphiphiles contain cyclic head group having polar functional groups and pharmaceutical composition useful for delivering biologically active therapeutic molecules into body cells.

Abstract: Compounds of methamphetamine derivatives having a meta-substituted alkyl linker on the benzene ring and a protective group on the nitrogen of the methamphetamine hapten. Such compounds have the structure wherein R1 is an alkyl linker comprising 2-15 carbon atoms and 0-6 heteroatoms, R2 is a leaving group, and R3 is a protecting group.

Abstract: The present invention provides a compound represented by the formula (I) or a salt thereof: wherein R1 represents a hydrogen atom, a C1-10 alkyl group optionally having a substituent, or a protecting group of N; R2 represents a C1-10 alkyl group optionally having a substituent or a C2-10 alkenyl group optionally having a substituent; R3 and R4 independently represent a hydrogen atom or a protecting group of hydroxyl group; X represents —N(R5)R6 or a residue of amino acid or of an amino group of a peptide wherein R5 and R6 independently represent a hydrogen atom, a C1-10 alkyl group optionally having a substituent, or a C3-12 cycloalkyl group optionally having a substituent; and Y represents a hydrogen atom, —CH2NH2, —CONH2, or —COOH. The compound of the present invention is useful as a specific inhibitor of sugar chain related enzymes such as glycosyltransferase and glycosidase, and is useful as, for example, a medicine for treating or preventing diseases associated with sugar chain related enzymes.

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.

Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.

Abstract: A carbamate compound is disclosed.

Abstract: Novel pyraole derivatives of formula (I), wherein: X is oxygen or sufu, R1 is C1–C3alkyl, C1–C3haloalkyl, C1–C3alkoxy-C1–C3alkyl or C1–C3haloalkoxy-C1–C3alkyl; R2 is C1–C3haloalkyl; and R3 is halogen. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.

Abstract: Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.

Abstract: A compound, method and composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4?-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: The present invention relates to novel mixture and maleic and succinic acid derivatives from mycelium of Antrodia Camphorata and the medical use thereof. The present invention relates to the composition or mycelium comprising the compounds of the invention.

Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (22) listed in the disclosure.

Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (43) listed in the disclosure.

Abstract: The invention provides peptides and compounds that can bind to P2Y2 receptors that are useful for modulating the secretion of mucus within mucosal surfaces.

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: The present invention relates to water-soluble drugs, compositions containing same, and, in particular, a water-soluble analogue of geldanamycin. This invention also relates to a method of producing water-soluble analogues of water-insoluble drugs through derivatization and conjugation with a polar moiety via a thiol ether bond with a heterobifunctional linking molecule.

Abstract: This invention relates to biocidal compositions and methods of using same. Also provided is a process for the manufacturing of a biocidal composition in the form of a tablet and a method of using the biocidal compositions for the disinfection of water that may contain microorganisms and biofilms.

Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.

Abstract: The present invention relates to compounds of the formula (I) which are formed by the microorganism ST 003236 (DSM 14476) during fermentation, to a process for preparing and derivatizing them, to a pharmaceutical which comprises a compound of the formula (I) and to the use thereof for producing a pharmaceutical.

Abstract: The present invention provides methods which may effectively be used in the treatment and prevention of early cardiac and early cardiovascular diseases, for example of ischemic origin, such as left ventricular hypertrophy, coronary artery disease, essential hypertension, acute hypertensive emergency, cardiomyopathy, heart insufficiency, exercise tolerance, chronic heart failure, arrhythmia, cardiac dysrhythmia, syncopy, arteriosclerosis, mild chronic heart failure, angina pectoris, cardiac bypass reocclusion, intermittent claudication (arteriosclerosis oblitterens), diastolic dysfunction and systolic dysfunction, as well as improving the success of heart transplantations, through administration of glycogen phosphorylase inhibitor compounds.

Abstract: Selective androgen receptor modulators (SARMs) having antagonist activity in hormone-dependent tumors while exhibiting no activity or agonist activity against other nontumor tissues containing the androgen receptor as well as methods for identifying, designing and using SARMs are provided.

Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumors

Abstract: A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I with an alkylating agent of structure III in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N?-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.

Abstract: A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is C2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-