Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

Abstract: The present invention relates to a novel compound isolated from Artemisia Sylvatica, expressed by the formula 1, a method of isolation, and its use thereof, and more particularly to a novel compound isolated from Artemisia Sylvatica, a method of isolation, and its use in inhibiting farnesyl transferase activity, which is essential for activating Ras oncogene, and repressing cancer cell growth.

Abstract: Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.

Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

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: The present invention relates to new compounds of the formula (I): in which X, Y and Z have the meanings given in the description and Het represents one of the groups: in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation, and to their use as pesticides and herbicides.

Abstract: The invention relates to insecticidal mixtures comprising compounds of the formula (I) in which X′, Y′, Z′, n, G′, A′ and B′ are as defined above and agonists and/or antagonists of nicotinic acetylcholine receptors, for protecting plants against attack by pests.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I): in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenalkyl, halogeno-alkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenyl-alkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups: in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: The present invention relates to a novel compound isolated from Artemisia Sylvatica, expressed by the formula 1, a method of isolation, and its use thereof, and more particularly to a novel compound isolated from Artemisia Sylvatica, a method of isolation, and its use in inhibiting farnesyl transferase activity, which is essential for activating Ras oncogene, and repressing cancer cell growth.

Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

Abstract: The invention relates to semicarbazides of the general formula I 1

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, W and Y independently of one another each represent hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups  in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: The invention relates to compounds of formula (I): wherein R1 represents alkyl or ureido, R2 represents alkyl or hydrogen, or R1 and R2 together form a 5- or 6-membered ring, R3 represents CN, NO2, NRaR′a, NRaSO2R′a, NRaCZR5 or CZNRaR′a, R4 represents hydrogen or R3, and medicinal products containing the same which are useful in treating or preventing epilepsy and neurodegenerative diseases.

Abstract: 2,3-Dihydrobenzofuran derivatives of general formula (1): wherein R1 represents a hydrogen atom or an acyl group; R2, R3 and R4 represent a hydrogen atom, a lower alkyl group or a lower alkenyl group; R5 and R6 combine to form a cycloalkyl group or a saturated heterocyclic group containing one or more oxygen atoms or sulfur atoms, provided that R2 and R3 can not simultaneously represent a t-butyl group, or optically active isomers or pharmaceutically acceptable salts thereof are useful as therapeutic or prophylactic agents for various renal diseases and as organ preservatives.

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

Abstract: A method for treating an inflammatory or obstructive disease of the respiratory tract which comprises administering therapeutically effective amounts of both an anticholinergic and a compound of the formula (2) 1

Abstract: The use of compounds that block complement component or its active fragments C5a and/or C5b (such compounds collectively referred to as “C5 blockers”) to treat established joint inflammation (arthritis) is disclosed. Administration of such C5 blockers has been found to: 1) arrest and/or reduce inflammation in joints which are already inflamed, and 2) inhibit the spread of inflammation to unaffected joints.

Abstract: This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): 1

Abstract: There are described new active compound combinations of a compound of the formula (I) 1

Abstract: The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.

Abstract: The invention relates to novel spirocyclic phenylketoenols of the formula in which Het represents one of the groups  in which Q represents and X, Y, Z, m, n, R6, R9, R10 and R11 are each as defined in the description, to a plurality of processes and intermediates for their preparation and to their use as pesticides and herbicides.

Abstract: The present invention provides combinations of cyclic ketoenols of the formula (I) and the active compounds listed herein. The combinations have very good insecticidal and acaricidal properties.

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: Microbicide composition for plants, containing at least two active ingredient components in an amount producing synergistic activity, together with an appropriate filler, characterized in that

Abstract: The invention involves methods and materials for treating and preventing non-invasive fungus-induced mucositis. Specifically, the invention involves administrating an antifungal agent such that it contact mucus in an amount, at a frequency, and for a duration effective to prevent, reduce, or eliminate non-invasive fungus-induced rhinosinusitis. This invention also provides methods and materials for diagnosing non-invasive fungus-induced rhinosinusitis and culturing non-invasive fungus from a mammalian mucus sample as well as specific antifungal formulations and medical devices for treating and preventing non-invasive fungus-induced rhinosinusitis. In addition, the invention provides methods and materials for treating and preventing other non-invasive fungus-induced mucositis conditions such as chronic otitis media, chronic colitis, and Crohn's disease. Further, the invention involves methods and materials for treating and preventing chronic asthma symptoms.

Abstract: The present invention discloses a medicament useful for treating aseptic inflammations, containing anemonin as an effective ingredient, and use of an anemonin compound in treating aseptic inflammations. The effective ingredient in the present medicament, anemonin, can be extracted and separated from natural plants containing anemonin or its precursor. The present invention also discloses a method for preparing anemonin extract. The present medicament can be formulated into preparations for oral administration, injection and topical application, especially liquid extract, plaster, suppository, liniment, and paint etc., which can be transdermally absorbed.

Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: 1

Abstract: Combinations of an ACE inhibitor, an aldosterone antagonist, and a loop diuretic are described for use in treatment of circulatory disorders. Of particular interest are therapies using captopril, enalapril or lisinopril co-administered with spironolactone. This co-therapy would be particularly useful to reduce the death rate or the number of non-fatal hospitalizations or prevent the progression of congestive heart failure in patients with cardiovascular disease.

Abstract: The present invention is directed to compounds effective for increasing the water solubility of poorly soluble drugs. Hydrotropic agents are identified, such as for increasing the solubility of paclitaxel. Polymerizable monomers of the hydrotropic agents are prepared and hydrotropic polymers formed from such monomers are generated. Both the monomers and resulting polymers increase the solubility of poorly soluble drugs. In some cases, the hydrotropic polymers are more effective at increasing solubility at low concentrations relative to a corresponding amount of the hydrotropic agent precursor. Additionally, the hydrotropic polymers (hytrops) can be crosslinked to yield hydrotropic hydrogels (hytrogels) capable of solubilizing a drug. The hytrogels can further be employed to generate micro- and nano-particle suspensions of a poorly soluble drug. The water solubility of paclitaxel can be increased by four orders of magnitude using compounds of the invention.

Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents C

Abstract: Fungicidal mixtures, comprising A) an amide compound of the formula I in which R1, R2 are identical or different and are halogen, nitro, cyano, C1-C8-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, C1-C8-haloalkyl, C2-C8-haloalkenyl, C2-C8-haloalkynyl, C1-C8-alkoxy, C1-C8-haloalkoxy, C1-C8-haloalkylthio, C1-C8-alkylsulfinyl or C1-C8-alkylsulfonyl; x is 1, 2, 3 or 4; y is 1, 2, 3, 4 or 5; and B) the amino compound of the formula II in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compounds I and II and the use of the compounds I and II for preparing such mixtures are described.

Abstract: A means and method for treating malaria using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl or spiropiperidyl ring on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably functionalized or substituted at the 4-position or a spiropiperidyl ring that is functionalized or substituted at the nitrogen atom. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

Abstract: Compounds represented by the formula: 1

Abstract: A method for treating a cardiovascular disorder, which involves administering to a patient in need a therapeutically effective amount of a compound of formula (I): wherein Ar1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, nitro, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, cyclo(lower) alkyl, lower alkenyl, lower alkoxy, halo(lower) alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, hydroxy, lower alkoxy, halo(lower) alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl: n represents 0 or 1; Q represents a single bond or carbonyl; T, U, V and W each independently re

Abstract: 1) Fungicidal compositions comprising a compound (I) which is (4S)-4-methyl-2-methylthio-4-phenyl-1-phenylamino-2-imidazolin-5-one and a compound (II) chosen from the group comprising:

Abstract: Microbicide composition for plants, containing at least two active ingredient components in an amount producing synergistic activity, together with an appropriate filler, characterised in that component I is the compound 2-[&agr;-{-[(&agr;-methyl-3-trifluoromethyl-benzyl)imino]-oxy-}-o-tolyl] -glyoxylic acid-methylester-O-methyloxime, and component II is a compound selected from the group IIA) 5,7-dichloro-4-(4-fluorophenoxy)quinoline (“Quinoxyfen”); IIB) 4-cyclopropyl-6-methyl-N-phenyl-2-pyrimidinamine (“Cyprodinil”); IIC) benzo(1,2,3)thiadiazole-7-carbothio-acid-S-methylester (“Acibenzolar-S-methyl”); lID) 3-anilino-5-methyl-5-(4-phenoxyphenyl)-1,3-oxazolidine-2,4-dione (“Famoxadone”); IIE) 8-(1,1-dimethylethyl)-N-ethyl-N-propyl-1,4-dioxaspiro[4.

Abstract: An intimal thickening inhibitory agent comprising, as an active ingredient, a compound represented by formula (1): wherein x represents an oxygen atom or a group of formula (2) —S—(O)n  (2) wherein n represents an integer of from 0 to 2, R1 represents a hydrogen atom or an acyl group; R2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group; R3 represents a lower alkyl group; and R4, R5, and R6, which may be the same or different, each represent a hydrogen atom or a substituted or unsubstituted alkyl group; or R3 and R4 may be taken together to form a 5-membered ring; or R5 and R6 may be taken together to form a cycloalkyl group; provided that R6 is nil when R3 and R4 are taken together to form benzofuran or benzo[b]thiophene.

Abstract: The present application relates to the use of 3-(2,4,6-trimethylphenyl) -4-neopentylcarbonyloxy-5,5-tetramethylene-&Dgr;3-dihydrofuran-2-one for controlling insects of the family Aleurodidae (white fly).

Abstract: Herein disclosed are prophylactic/therapeutic agents for atherosclerosis containing a compound of general formula (1): wherein R1 represents a hydrogen atom or an acyl group, R2 represents a lower alkyl group, R3 represents a hydrogen atom or a lower alkyl group, and R4, R5 and R6 represent a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group or an aryl group, or R2 and R4 together with the oxygen atom may form a furan or dihydrofuran ring, or R5 and R6 may combine to form a cycloalkyl group or a heterosubstituted cycloalkyl group in which one or more methylene groups of the cycloalkyl group are replaced by oxygen, sulfur or alkyl-substituted nitrogen atoms, a possible optically active isomer or a pharmaceutically acceptable salt thereof, as an active ingredient.

Abstract: The present invention relates to novel derivatives of Andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of Andrographolide have the general formula (I) The andrographolide derivatives represented by general formula (I) are useful for treating cancer, HSV, HIV, psoriasis, restonosis, atherosclerosis, other cardiovascular disorders, and can be used as antiviral, antimalarial, antibacterial, hepatoprotective, and immunomodulating agents and for treatment of other metabolic disorders.

Abstract: 8-Acetylarteminolide of the formula (I) having inhibitory activities against farnesyl-protein transferase(FPTase), a progression of the cell cycle and angiogenesis may be useful for the prevention and treatment of various cancers and angiogenesis-related diseases:

Abstract: Anticonvulsant derivatives useful in maintaining weight loss.

Abstract: The present invention relates to new aromatic di-keto derivatives and to their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents. The derivatives are glucose-6-phosphate translocase inhibitors and can be used in the treatment of diabetes mellitus. The present invention further relates to a process for the production of the derivatives, to the use of the derivatives and their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents as pharmaceuticals, in particular to their use in the treatment of diabetes mellitus, and to pharmaceutical compositions comprising the derivatives, pharmaceutically acceptable salts, esters, ethers or other chemical equivalents thereof.

Abstract: The present invention relates to new compounds of the formula (I) in which X represents halogen, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that always one of the radicals Y and Z represents halogen while the other represents alkyl, and Het represents one of the groups  in which A, B, D and G have the meanings given in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: The present invention relates to novel substituted bicyclic lactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, cranial cerebral trauma, states of pain or CNS-mediated spasms.

Abstract: A therapeutic method is provided for treating a mammal afflicted with a herpesvirus infection, comprising administering an effective amount of a compound of formula I: wherein R1-R11, have any of the values disclosed in the specification; or a pharmaceutically acceptable salt thereof. The invention also provides novel compounds of formula I, and pharmaceutical compositions comprising compounds of formula I.

Abstract: The present invention relates to novel derivatives of Andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates.

Abstract: Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents methine; Y represents an optionally substituted imino or oxygen atom. These novel spiro compounds exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.

Abstract: The present invention is directed to methods and compositions for treating cardiac indications, such as heart failure, hypertension and congestive heart failure, in an animal by administration of compositions comprising combinations of at least two or more agents into a single administrative dose. Such compositions and methods provide a means to treat cardiac indications with several agents with out administering multiple individual agents either concurrently or separately. Methods and compositions comprising combinations of at least two or more agents provide a way to administer multiple agents that is easier for patients to use, is more easily administered by caregivers, and that facilitates the physicians determination of drug interactions, patient side effects and dosages.

Abstract: A novel antifungal compound, “CAY-1”, was isolated from the dried fruit of Capsicum frutescens (cayenne pepper), purified to homogeneity, and characterized as a novel sterol glycoside (a saponin) with a molecular mass of 1243.35 Da. CAY-1 demonstrates antifungal activity against a large variety of fungal organisms associated with diseases in plants, animals and humans including, but not limited to, Aspergillus flavus, A. fumigatus, A. parasiticus, A. niger, Pneumocystis carnii and Candida albicans, but has minimal toxic effects on mammalian cells.