Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.

Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.

Abstract: The present invention provides ?-hydroxy benzeneacetic acid derivatives of the formula as defined in the specification which is a precursor indispensable for synthesis of compounds having two 5-membered lactone rings fused to central cyclohexa-1,4-diene nucleus, and a process of easily preparing the same. According to the preparation process of the present invention, the ?-hydroxy benzeneacetic acid derivative can be readily prepared at high purity and yield without using toxic materials or producing toxic by-products. Some novel compounds, synthesized by using such a ?-hydroxy benzeneacetic acid derivative, have excellent fastness properties, dye fixing rate and leveling property to general synthetic fiber materials such as polyester fibers and their blends with other fibers, especially to micro fibers, and also can be used as a coloring agent for plastic resins, color tonors, color filters, etc.

Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of Ru complexes with bidentate ligands, having one amino or imino coordinating group and one phosphino coordinating group, in hydrogenation processes for the reduction of esters or lactones into the corresponding alcohol or diol respectively.

Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me

Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required a-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Abstract: Synthetic compounds of 1,2-naphthalein moelcules (I) having specific inhibitory properties of the enzymatic activity of thymidylate synthases of bacterial species, their preparation, their pharmaceutical composition and use in the treatment and prophylaxis of infectious pathologies are disclosed.

Abstract: The present invention relates to concentricolide and its derivatives, a method for the preparation of the compound and its derivatives, a pharmaceutical composition containing concentricolide and its derivatives, and use of the compound and its derivatives for the treatment and prevention of infection caused by human immunodeficiency virus (HIV).

Abstract: The invention provides a process for the production of a substance or composition for the treatment, by therapy or prophylaxis, of parasitic infections, in particular malarial infections such as Plasmodium falciparum infections, of the human or animal body. The process comprises extracting the substance or composition from roots of the plant species Dicoma anomala, by an extraction using an organic solvent to obtain a liquid extract containing the substance or composition and removing the solvent from the liquid extract to leave a dried extract containing the substance or composition. The invention extends also to the use of the substance or composition in the manufacture of a medicament or preparation for such treatment of infections; to a substance or composition for use in such treatment of said infections; to compounds for use in such treatment of said infections; and to a method of treating said infections using such compounds.

Abstract: The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer.

Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.

Abstract: The present invention relates to industrially useful production processes in which (±)-3a,6,6,9a-tetramethyldecahydronaphtho[2,1-b]furan-2(1H)-ones and further (±)-3a,6,6,9a-tetramethyldo decahydronaphtho[2,1-b]furans are produced from raw materials which are readily available at low costs, through short steps and in a simple manner.

Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.

Abstract: 4-O esters of podophyllotoxin and 4?-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4?-demethylepipodophyllotoxin. The compounds are useful for treating cancer.

Abstract: The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer.

Abstract: The present invention relates to extracts and compounds which are isolated from Calomeria amaranthoides, and to derivatives and analogues of such compounds, which demonstrate cytotoxic activity against a variety of cell types exhibiting hyperproliferative cell division.

Abstract: Compounds of the formula having anti-tumor activity, wherein R1 and R2 are as described herein

Abstract: A method for the identification of a composition useful in the treatment of an overweight or obese person to reduce the person's body mass index is provided which comprises obtaining an extract of an ethnobotanical plant, and evaluating the activity of the extract in an assay selected from the group consisting of a lipolysis assay, an assay that measures the amount of glycerol introduced by a cell into a suspension medium of the cell, an adipocyte differentiation assay, an assay that measures the level of the enzyme glycerol-3-phosphate dehydrogenase, an assay that measures the inhibition of differentiation of preadipocytes to adipocytes, an assay that measures the accumulation of lipid in an adipocyte, an assay that measures the de-differentiation of adipocytes into preadipocytes, and combinations thereof.

Abstract: Purification of poly-amino acid-tagged recombinant proteins has been improved by the use of a carboxymethylated aspartate ligand complexed with a third-block transition metal having an oxidation state of 2+ and a coordination number of 6. A method for synthesizing the metal ion-CM-Asp complex is also described. Further, the metal ion-CM-Asp complex can be used for screening protein function.

Abstract: The present invention relates to the field of organic synthesis and more particularly to a new process for the optical resolution of a precursor of sclareolide. This process includes the reaction of [(1RS,2RS,4aSR,8aSR)-2-hydroxy-2,5,5,8a-tetramethyldecahydronaphthalen-1-yl]acetic acid, or an alkaline salt thereof, with an enantiomer of the 2-(methylamino)-1-phenyl-1-propanol, or an ammonium salt thereof respectively, which is used as resolving agent.

Abstract: Process for the preparation of compounds of formula I wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula V wherein the general symbols are as defined in claim 1, with carbon monoxide in the presence of a catalyst.

Abstract: A method for producing an optically active lactone compound by Baeyer-Villiger oxidation of a cyclic ketone compound with at least one kind of oxidants selected from the group consisting of hydrogen peroxide and urine-hydrogen peroxide adduct (UHP) using a cobalt(salen) complex having a cis-&bgr; structure expressed by the following formula (I) or (II) as a catalyst. in which X and Y independently denote H, a t-butyl group or an electron-withdrawing substituting group and W is a halogen element. in which X and Y independently denote H, a t-butyl group or an electron-withdrawing substituting group and Z− is a monovalent anion. The optically active lactone compounds can be used for the synthesis of medicines and argochemicals.

Abstract: The invention relates to compounds of formula (I): wherein R1 represents an alkyl or ureido group, R2 represents an alkyl group or a hydrogen atom, or R1 and R2 together form a 5- or 6-membered ring, R3 represents a group CN, NO2, NRaR′a, NRaSO2,R′aCZR5 or CZNRaR′a, R4 represents a hydrogen atom or a group R3.

Abstract: Heterocyclic-substituted tricyclics of the formula 1

Abstract: Fluorescent dye compounds of formula (I) are disclosed. These compounds are useful as they interact with organic compounds in a manner such that excitation with certain wavelengths of light results in fluorescent emmission. Detection and/or monitoring of the fluorescence provides a means for the detection or quantification of organic compounds when bound to these fluorescent dye compounds. Formula (I), wherein: each of R, R′ and R″ is a hydrogen atom, halogen atom or a straight or branched chain (C1-20alkyl, alkenyl or alkynyl group optionally substituted with one or more halogen, hydroxy and/or oxy group: rings A, B and C optionally include one or more double bonds; rings B and C are optionally substituted with one or more halogen atoms.

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediate by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutic compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of formula (1) as defined herein.

Abstract: Provided are, among other things, lipid-lowering or glucose-lowering methods and compounds, particularly lipid-lowering or glucose-lowering compounds, with an A-B ring structure as follows: wherein the dotted line between carbons 5 and 6, the dotted line between carbon 4 and R2, and the dotted line between carbon 11 and R3 each independently represent an optional double bond from the respective numbered carbon to a linked carbon, and wherein X is hydroxy or, together with Y is oxy linking carbon 8 and carbon 12.

Abstract: Colorants comprising a chromophore having two methine moieties attached to a benzodifuranone backbone, wherein said moieties optionally have at least one poly(oxyalkylene) chain, preferably at least two such chains attached thereto are provided. Such colorants exhibit excellent thermal stability, effective colorations, excellent low extraction rates, and effective lightfastness levels, particularly when incorporated within certain media and/or on the surface of certain substrates, particularly polyesters. The optional poly(oxyalkylene) chains also increase the solubility in different solvents or resins thereby permitting the introduction of such excellent coloring chromophores within diverse media and/or on diverse substrates as well as provides a liquid colorant which facilitates handling. Compositions and articles comprising such colorants are provided as are methods for producing such inventive colorants.

Abstract: A purification method for obtaining high-purity PMDA. The method controls temperatures of cyclone separators in a series to separate PMDA and other by-products of different sublimation temperatures. High-purity PMDA is collected in the first cyclone separator, and no other purification steps are needed.

Abstract: The present invention refers to a polycyclic dye of the formula (I) wherein each of R1, R2, R4 and R5, independently, is hydrogen, alkyl or alkoxy; R3 is hydrogen, alkyl, optionally substituted alkoxy or amino; and Y is a straight or branched chain C1-8 alkylene group, methods for its preparation and a method for coloring synthetic fibre material or fibre blend thereof using such polycyclic dye.

Abstract: Substantially pure preparations of phosphosesquiterpenes are described. The compounds inhibit farnesyl-protein transferase activity and are useful for the treatment of cancer. Methods for inhibiting farnesyl-protein transferase activity are also described.

Abstract: Process for the preparation of compounds of formula (I), wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula (V), wherein the general symbols are as defined in claim 1, with carbon monoxide in the presence of a catalyst.

Abstract: The present invention refers to a polycyclic dye of the formula (I) 1

Abstract: Intermediates for the preparation of himbacine exhibiting muscarinic M2 receptor antagonism, which are hydronaphtho[2,3-c]furan derivatives represented by general formula (1) or intermediates for the preparation thereof: wherein R1 is lower alkyl or aralky; R2 is hydrogen, lower alkyl or aralkyl; R3 and R4 together represent oxygen or methylene, or alternatively R4 is hydroxyl, lower alkoxy, aralkyloxy or lower acyloxy, with R3 being hydrogen; R5 and R6 together represent oxygen, or alternatively R6 is hydroxyl, lower alkxy, aralkyloxy or lower acyloxy, with R5 being hydrogen; and either of the broken lines is a single bond and the other thereof is a double bond, or alternatively both are single bonds.

Abstract: A process for purifying statin compounds from a fermentation broth by extraction and crystallization is disclosed. A fermentation broth is subjected to a pretreatment procedure which involves an alkaline pretreatment and an alkaline purification. Following the pretreatment procedure, the statin compound is extracted under acidic conditions into a hydrophobic solvent and purified by crystallization. The organic extraction solvent is concentrated and then extracted with a mild base. The statin compound is then purified by crystallization.

Abstract: The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their regioisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: Provided are, among other things, lipid-lowering or glucose-lowering methods and compounds, particularly lipid-lowering or glucose-lowering compounds, with an A-B ring structure as follows: wherein the dotted line between carbons 5 and 6, the dotted line between carbon 4 and R2, and the dotted line between carbon 11 and R3 each independently represent an optional double bond from the respective numbered carbon to a linked carbon, and wherein X is hydroxy or, together with Y is oxy linking carbon 8 and carbon 12.

Abstract: Substantially pure preparations of phosphosesquiterpenes are described. The compounds inhibit farnesyl-protein transferase activity and are useful for the treatment of cancer. Methods for inhibiting fanesyl-protein transferase activity are also described.

Abstract: Compounds represented by the following formula (I) and pharmaceutically acceptable salts thereof are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as abortifacients, oral contraceptive pills, carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for endometriosis, meningioma, and myeloma, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance.

Abstract: The use of a calcium intracellular store inactivator for inhibiting cell growth is disclosed; for example, thapsigargin or a derivative may be used to inhibit intraocular lens cell growth. Formulations include an emulsion of the compound for coating an IOL, either ex vivo or in vivo.

Abstract: A compound, 3-phenyl-7-[4-(tetrahydrofurfuryloxy)phenyl]-1,5-dioxa-s-indacene-2,6-dione, which has a structure of crystals exhibiting the strongest peak at an angle of diffraction, 2&thgr;, of 4.7°, among peaks appearing within the range of not smaller than 3° of 2&thgr;, in an X-ray diffraction using a Cu-K&agr;-ray. The compound gives dyed or printed products having deep and brilliant tint of colors with excellent fastnesses, when applied to hydrophobic fiber materials, particularly, polyester fiber materials.

Abstract: The invention provides various derivatives of arglabin, a sesquiterpene lactone isolated from Artemisia glabella. These compounds are effective for suppressing tumor growth in mammals. A method of suppressing tumor growth in humans is also described.

Abstract: A compound selected from those of formula (I): ##STR1## in which A, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the Specification, and pharmaceutical compositions containing the same, which are useful for treating a mammal afflicted with a disorder of the melatoninergic system.

Abstract: Substantially pure preparations of phosphosesquiterpenes are described. The compounds inhibit farnesyl-protein transferase activity and are useful for the treatment of cancer. Methods for inhibiting farnesyl-protein transferase activity are also described.

Abstract: The invention provides various derivatives of arglabin, a sesquiterpene lactone isolated from Artemisia glabella. These compounds are effective for suppressing tumor growth in mammals. A method of suppressing tumor growth in humans is also described.

Abstract: A process for the preparation of a polycyclic dye of Formula (1) which comprises steps: i) reaction of a compound of formula (2) with a compound of formula (3) or a derivative thereof to form an intermediate of formula (4) and ii) reaction of the intermediate of formula (4) with an aromatic compound of formula (5): B--H optionally in the presence of an oxidizing agent, wherein: A and B each independently is optionally substituted aryl; and X.sup.1 and X.sup.2 each independently is --H, halo, alkyl, or alkoxy.

Abstract: The present invention is directed to novel seco-cholestane derivatives, as well as to pharmaceutical compositions thereof, and methods of making the same. More particularly, the invention relates to C5- and C8-substituted seco-cholestane derivatives. The compounds of the invention can exhibit CDC25 phosphatase inhibition properties and anti-cancer activity.

Abstract: The present invention is directed to a process for preparing a condensation product of a glyoxylic reactant and a hydrocarbyl-substituted aromatic compound having at least one hydroxy functionality, which includes (a) providing the glyoxylic reactant in the form of a compound represented by the formula ##STR1## or its reactive equivalent, wherein R.sup.1 and R.sup.3 independently are hydrogen or hydrocarbyl group of 1 to about 4 carbon atoms; and R.sup.2 and R.sup.4 independently are hydrocarbyl groups of 1 to about 4 carbon atoms; (b) mixing the aromatic compound with the glyoxylic reactant; and (c) heating the mixture to a temperature of about 50.degree. C. to about 200.degree. C. in the presence of an acid catalyst for a sufficient time to form the condensation product.