Abstract: A compound represented by the formula: [wherein R1 is methoxy, methylthio, ethyl, etc.; R5 and R6 are each independently cyclopropylmethyl, (4-tetrahydropyranyl)methyl, etc.; and two of R40, R41 and R42 are C1-6 alkoxy while the remaining one is methoxymethyl, etc.], a salt thereof, or a hydrate of the foregoing. This compound has excellent antagonism against corticotropin-releasing factor receptor.

Abstract: An azabicyclo compound (I) or a salt thereof in accordance with the present invention has an excellent inhibiting action on matrix metalloproteases (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions. wherein R is H, alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, acyl, COOR1, carbamoyl or SO2R2 (wherein R1 and R2 each are alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl); X is methylene, ethylene or propylene; and is a single bond or a double bond.

Abstract: There is provided an acid addition salt of (?)-(3R)-quinuclidin-3-yl(1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate with an acid selected from the group consisting of (?)-(2S,3S)-tartaric acid, (+)-(2S,3S)-di-O-benzoyltartaric acid, (+)-(2S,3S)-di-O-(4-methylbenzoyl)tartaric acid, (?)-L-phenylalanine, benzenesulfonic acid, cyclohexanesulfamic acid, hydrobromic acid, naphthalene-2-sulfonic acid, sebacic acid, (+)-camphor-10-sulfonic acid, p-toluenesulfonic acid, ethanesulfonic acid, methanesulfonic acid and methyl phosphate, which has little hygroscopicity that affects the use as a drug or its drug substance, and is very useful as a drug or its drug substance.

Abstract: A process for the catalytic epoxidation of olefins in the presence of a titanium containing zeolite catalyst and a polar solvent whereby the deactivation of the catalyst upon recycling of the solvent has been considerably reduced. In the process one or more nitrogen containing compounds are introduced at some stage, a solvent stream is recovered, treated to contain less than 50 wppm nitrogen in the form of organic nitrogen compounds and at least a part of it is recycled to the epoxidation step. Also disclosed is a process for the catalytic epoxidation of propene which integrates the treatment and recycle of the solvent into the workup of the reaction mixture.

Abstract: New compounds of general formula I

Abstract: This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] [in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease, drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.

Abstract: The invention relates to compounds of formula (I): wherein: B represents a hydrogen atom, a COOR group, a CONRR? group, or a (C1–C6)alkyl group substituted by a COOR, CONRR? or OR group, G1 represents a —X?—(CH2)n—X—(CH2)m—X?— chain wherein X, X?, X?, n and m are as defined in the description, Cy represents a grouping of formula (II) or (III): G2 represents an alkylene chain as defined in the description, and A represents a NRCOR?, NRCSR?, CONRR?, CSNRR?, NRCONR?R? or NRCSNR?R? group.

Abstract: Compositions comprising bis-tetrahydrofuran benzodioxyolyl sulfonamide compounds that are surprisingly effective protease inhibitors and a second antiretroviral compound are disclosed. Methods of inhibiting retrovirus proteases, in particular multi-drug resistant retrovirus proteases, methods of treating or preventing infection or disease associated with retrovirus infection in a mammal, and methods of inhibiting viral replication are also disclosed.

Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, SO2NH, NHCO or NHCONH; m is either 0 or 1; n is an integer from 2 to 6; q is an integer from 0 to 3; and Y is hydrogen or an aromatic substituent, or a pharmaceutically acceptable derivative thereof; methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection

Abstract: The invention provides novel apoptosis-inducing compounds that include isolated, purified isoapoptolidin, and selectively functionalized isoapoptolidin derivatives and stereoisomers thereof; selectively functionalized apoptolidin derivatives and stereoisomers thereof; and deglycosylated isoapoptolidin and selectively functionalized derivatives and stereoisomers thereof. The isoapoptolidin, apoptolidin, and deglycosylated isoapoptolidin derivatives may be functionalized by substituting any or all of the methoxyl or hydroxyl groups of the parent molecule. Pharmaceutical compositions and methods for using the compounds are also provided.

Abstract: The present invention relates to novel pyrazolo[1,5-a]pyridine derivatives of general formula I: that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety disorders, and depression and stress related disorders.

Abstract: 4-Thio substituted coumarin derivatives, 4,5-dithio substituted coumarin derivatives, and coumarin dimers are provided, as well as processes for their preparation. The invention also provides a method and composition for the treatment of hepatitis C virus (HCV) by adiministering 4-thio substituted coumarin derivatives, 4,5-dithio substituted coumarin derivatives, and coumarin dimers.

Abstract: The invention relates to a process for preparing 5-bromo-2,2-difluorobenzo-1,3-dioxoles and to the use thereof for preparing medicaments and crop protection agents.

Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

Abstract: The present invention pertains to methods for preparing a compound of Formula (I), wherein A is O or N-L; each L is independently H or an acyl group; K is, together with the two contiguous linking carbon atoms, a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system wherein each ring or ring system is optionally substituted; R1 is H, C1 to C4 alkyl or CO2R3; R2 is H or C1 to C4 alkyl; and R3 is C1 to C4 alkyl; comprising hydrogenating a compound of Formula (II), wherein n is 0, 1 or 2 in the presence of a catalyst comprising palladium to form the compound of Formula (I). This invention further pertains to methods for preparing compounds of Formula (II) useful for preparing compounds of Formula (I).

Abstract: Process and a plant to extract and concentrate tannins from wood and from other solid natural products containing it characterized in that the solid products are subjected to an extraction (1) by percolation with water and/or steam and the thus obtained tannin solution is subjected to nanofiltration (5).

Abstract: Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein

Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, for use as therapeutically active substances. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors including obesity.

Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.

Abstract: The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent-moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1–C5) alkyl group, (C2–C5) alkenyl, or a (C2–C5) alkynyl, (C1–C5) alkoxy, (C2–C5) alkenyloxy, or (C2–C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1–C5) alkyl, (C2–C5) alkenyl, or (C2–C5) alkynyl, or a cyclo