Abstract: The present invention relates to the preparation of cyclopropane derivatives, in particular 2-amino-9-[[(1S,2R)-1,2-bis(hydroxymethyl)cyclopropyl]methyl]-4,8-dihydro-1H-purin-6-one, especially via the [(1S,7R)-4-phenyl-3,5-dioxabicyclo[5.1.0]octan-1-yl]methanol intermediate.

Abstract: The invention relates to specific benzodioxepin-3-one compounds, to a process for the preparation thereof and to the use thereof as dyes or as fluorescent emitters for organic electroluminescent devices (OLEDs) or for organic light-emitting electrochemical cells (OLECs), and to corresponding electronic devices.

Abstract: The present invention is directed to co-therapy for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, co-therapy with a therapeutically effective amount of a benzo-fused heterocycle sulfamide derivative and a therapeutically effective amount of one or more anticonvulsant and/or anti-epileptic agents.

Abstract: The invention relates to specific benzodioxepin-3-one compounds, to a process for the preparation thereof and to the use thereof as dyes or as fluorescent emitters for organic electroluminescent devices (OLEDs) or for organic light-emitting electrochemical cells (OLECs), and to corresponding electronic devices.

Abstract: The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Abstract: The present invention relates generally to the field of lipids and in particular aims at improving lipid absorption, for example under conditions of lipid maldigestion or malabsorption. One embodiment of the present invention relates to a composition comprising a sn-2 monoacylglycerol derivative, wherein the sn-1 and sn-3 positions are blocked by protective groups. The acyl group may be a fatty acid, for example one with anti-inflammatory properties.

Abstract: The present invention is a method for the treatment of alcohol abuse and/or addiction comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and/or formula (II) as herein defined.

Abstract: The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.

Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Abstract: Substituted selenophene monomers, and polymers and copolymers having units derived from a substituted selenophene are disclosed. Also provided are methods of making and using the same.

Abstract: A compound of the formula I n which R1 is H or methyl, R2 is H, methyl or ethyl, R3 and R4 are independently hydrogen, methyl, ethyl, n-propyl or iso-propyl, and the dashed lines representing the alternative possibilities of there being present either an additional double bond or an additional group R5, which is H or methyl. The compounds possess a marine odour with sweet character, and are useful in fine and functional fragrances.

Abstract: Substituted selenophene monomers, and polymers and copolymers having units derived from a substituted selenophene are disclosed. Also provided are methods of making and using the same.

Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

Abstract: Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes.

Abstract: The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.

Abstract: This invention is directed to selenophene compounds, selenophene-based polymers (polyselenophene), processes for the preparation of the same and uses thereof. The polyselenophenes of this invention have high conductivity and can be used as electrodes in various devices such as in electrochromic devices, batteries, solar cells, optical amplifiers, organic light emitting diodes, and the like.

Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.

Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

Abstract: The present invention is a method for the treatment of anxiety and related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined. The present invention is directed to a method for the treatment of anxiety and related disorders, which includes mono-therapy and alternatively, co-therapy with at least one anxiolytic.

Abstract: This invention relates to compounds of the formula wherein B, X, Y, Z, R1 and R2 are as defined in the description, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by ACC? inhibitors.

Abstract: The invention relates to a process for the preparation of compounds containing at least one —CF2—O— bridge in the molecule, in which a) an acid is added onto at least one ketene dithioketal, b) the resultant bis(alkylthio)carbenium salt is reacted with at least one compound having at least one hydroxyl group in the presence of a base, c) and subsequently, preferably in situ, the resultant dithioorthoester is subjected to oxidative fluorodesulfurisation using a fluorinating agent and an oxidant to give the compound containing at least one —CF2—O— bridge in the molecule.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein m, n, p, Ar, X, R1, R2, R3, R4, R5 and R6 are as defined herein. Also provided are compositions comprising, methods of preparing, and methods of using the subject compounds.

Abstract: Novel 7,7-disubstituted (5H,9H)-6,8-dioxabenzocycloheptene compounds having the structural formula (I): are useful intermediates in the synthesis of non-steroidal derivatives of vitamin D.

Abstract: The invention relates to 1,2-substituted 2,3-dihydro-1H-5,9-dioxacyclohepta[f]inden-7-ones and 7-substituted benzo[b][1,4]dioxepin-3-ones and to the use of these compounds in fragrance compositions.

Abstract: There is disclosed a method for treating a source of azadirachtin: (a) dissolving said sample in an organic polar solvent; (b) combining the solution of step (a) with an organic non-polar solvent to form a single phase containing the said solvents and dissolved sample; (c) treating said single phase of step (b) with an aqueous salt solution to form an aqueous phase and a phase containing the organic non-polar solvent; and (d) recovering one or other or both of the aqueous phase and the phase containing the organic polar solvent.

Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disorders

Abstract: The invention relates to 1,2-substituted 2,3-dihydro-1H-5,9-dioxacyclohepta[f]inden-7-ones and 7-substituted benzo[b][1,4]dioxepin-3-ones and to the use of these compounds in fragrance compositions.

Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.

Abstract: A compound of the formula whereon R1 is: R5 is: and n, m, Z, R8, R9, R10 and R11 are as defined herein, useful in the treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, and tissue ischemia, particularly myocardial ischemia.

Abstract: The synthesis and study of biological activity of a series of new molecules with potential antimicrobial activity are described. The molecules are bicyclic carbohydrates, based on furanose sugars. Their antimicrobial activity against viruses is demonstrated, next to cytostatic effects. Significantly, a high and selective activity against Cytomegalovirus was observed.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.

Abstract: The present invention relates to oxygen-containing heterocyclic compounds represented by the following formula (I): 1

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.

Abstract: The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient.

Abstract: A preventive and/or therapeutic medicament for circadian rhythm sleep disorders such as jet lag syndrome which comprises as an active ingredient an alkylenedioxybenzene derivative represented by the following formula (I) wherein m represent an integer of from 2 to 5, and n represents an integer of from 1 to 3, such as 5-[3-[(2S)-(1,4-benzodioxan-2-yl-methyl)amino]propoxy]-1,3-benzodioxol, or a pharmaceutically acceptable salt thereof.

Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.

Abstract: Monoesters and macrocyclic diesters of 2,2,4-trimethyl-1,3-pentanediol and phthalic acid or a derivative thereof are described. Methods by which such monoesters and diesters may be prepared are also described. The mono- and diesters according to the invention are useful in the preparation of clear, hard thermoplastic polymers. The thermoplastic polymers are useful in coatings, inks, reinforced plastics and packaging materials.

Abstract: Novel derivatives of benzodioxa alkylene ethers are provided which are useful as melatonergic agents.

Abstract: The invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists of formula I and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LBT.sub.4 antagonists. The compounds of the invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruitus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma and other conditions where marked neutrophil infiltration occurs.

Abstract: The present invention relates to novel biologically-active organic peroxides and to novel uses of both known and new organic peroxides. More specifically, this invention details organic endoperoxides having antiparasitic activity, methods for their preparation and methods for treating malaria and cerebral toxoplasmic encephalitis with the organic endoperoxides.

Abstract: Disclosed are bridge-substituted analogs of tropanes and benztropines as well as methods for: imaging of cocaine receptors; treatment of cocaine abuse; and imaging and treatment of Parkinson's disease.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: The present invention relates to novel biologically-active organic peroxides and to novel uses of both known and new organic peroxides. More specifically, this invention details organic endoperoxides having antiparasitic activity, methods for their preparation and methods for treating malaria and cerebral toxoplasmic encephalitis with the organic endoperoxides.

Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.

Abstract: A novel hydrazine derivative and a pesticidal composition containing the hydrazine derivative as the effecting ingredient. The hydrazine derivative show high pesticidal activity against harmful pests which are resistant to known pesticides such as organophosphorus pesticides, pyrethroids, etc., especially against Lepidoptera harmful pests such as Plutella xylostella, Spodoptera litura, Cnaphalocrocis medinalis, Adoxophyes orana, etc., and is effective for controlling harmful pests in paddy field, upland field, orchard, forest or places to be kept environmentally hygienic.

Abstract: Certain aminomethyl-benzodioxanes and benzopyrans are useful serotonergic agents. They possess anxiolytic properties with few of the side effects often associated with dopaminergic agents.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.