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: One embodiment of the invention comprises an ion exchange composition formed by reacting unsaturated carbon to carbon moieties pendant from derivatized ion binding cryptands with a support substrate under free radical activation conditions to form a covalent bond therebetween. In another embodiment, a cryptand ion exchange composition is made by covalently bonding unsaturated carbon to carbon moieties pendant from a derivatized ion binding cryptands with unsaturated carbon to carbon moieties pendant from a support substrate under free radical activation conditions to form covalent bond.

Abstract: This invention relates resiniferatoxin derivatives useful in a vanilloid receptor binding assay and methods for production thereof.

Abstract: This invention comprises compositions containing dihydroartemisinin and dihydroartemisitene dimers with activity as anticancer agents and anti-protozal, including anti-malarial and anti-leishmanial properties. This invention also describes methods of preparation of these compositions and methods of use of such compositions for the treatment of cancer, and protozoal infections, including malaria, or leishmaniasis. The compounds of this invention represent a potential new class of anti-tumor agents, one that has shown promising activity against solid tumors, and with a pattern of selectivity that suggests a possible new mechanism of action.

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 stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

Abstract: A calixarene dimer of the general formula (I-G), comprising a first calixarene moiety I and a second calixarene moiety G, wherein: L is [—CH2—] or [—O—CH2—O—] and is the same or different between each aryl group; R5 is H, NO2, halogen, or C1-C10 aliphatic hydrocarbyl group, C6-C20 aryl group, C6-C20 hydrocarbylaryl group, any of which is optionally substituted by one or more halo or oxo groups or interrupted by one or more oxo or amide groups, and R5 is the same or different on each aryl group; R1 comprises a carboxy group which is or is not protonated or protected; two groups out of R2, R3 and R4 are H; the one group out of R2, R3 and R4 not being H comprises at least one atom of one or more of O and S, the said at least one atom being capable of causing the calixarene to be adsorbed onto the surface of the substrate; and the one group out of R2, R3 and R4 not being H being conjugated to the second calixarene moiety G. The calixarene dimers may be incorporated into sensors.

Abstract: The invention relates to a process for the preparation of cyclic carboxylic acid orthoester fluorides in which a) at least one bis(alkylthio)carbenium salt is reacted with at least one organic compound containing at least two hydroxyl groups in the presence of at least one base, b) and subsequently, preferably in situ, the resultant thioorthoester is subjected to oxidative fluorodesulfurisation using a fluorinating agent and an oxidant to give the cyclic carboxylic acid orthoester fluoride.

Abstract: One embodiment of the invention comprises an ion exchange composition formed by reacting unsaturated carbon to carbon moieties pendant from derivatized ion binding cryptands with a support substrate under free radical activation conditions to form a covalent bond therebetween. In another embodiment, a cryptand ion exchange composition is made by covalently bonding unsaturated carbon to carbon moieties pendant from a derivatized ion binding cryptands with unsaturated carbon to carbon moieties pendant from a support substrate under free radical activation conditions to form covalent bond.

Abstract: The present invention relates to a process for the transformation of tricyclopentabenzene to 12-hydroxy-16-oxatetracyclo[10.3.1.01,5.

Abstract: This invention comprises compositions containing dihydroartemisinin and dihydroartemisitene dimers with activity as anticancer agents and anti-protozal, including anti-malarial and anti-leishmanial properties. This invention also describes methods of preparation of these compositions and methods of use of such compositions for the treatment of cancer, and protozoal infections, including malaria, or leishmaniasis. The compounds of this invention represent a potential new class of anti-tumor agents, one that has shown promising activity against solid tumors, and with a pattern of selectivity that suggests a possible new mechanism of action.

Abstract: The present invention provides a method for the preparation of arteether from artemisinin in one pot in just about 4 hours comprising reduction of artemisinin into dihydroartemisinin by less quantity of sodium borohydride in ethanol at room temperature in the presence of a novel polyhydroxy catalyst, acylation of dihydroartemisinin in the presence of an acid catalyst, extraction of arteether from an aqueous reaction mixture using 1% ethyl acetate in n-hexane followed by workup and purification of the impure arteether to yield 80-86% (w/w) pure alpha, beta arteether.

Abstract: Naphthyl crown ether ligand molecules containing at least two naphthyl groups that are covalently bonded to suitable solid supports and coated by hydrophobic organic solvents are disclosed. These compositions and associated methods are characterized by selectivity of desired amine or amino acid enantiomers over their counter-enantiomers and derivatives. The composition preferably has an &agr;-value greater than or equal to 4. This allows for the separation of such enantiomers with nonchromatographic resin bed separations of three separation stages or less.

Abstract: The present invention relates to a process for the isolation of artemisinin, an antimalarial agent from the herb of the Artemisia annua plant, comprising of extracting the herb with ethanol, partitioning of the extract between water and hexane, followed by evaporative crystallization of artemisinin from hexane phase to produce substantially pure artemisinin.

Abstract: The present invention relates to an improved method for the preparation of Artemether. Artemether prepared from the process is useful for the treatment of uncomplicated, severe complicated and multi drug resistant malaria.

Abstract: The present invention provides a single pot process for the preparation of artesunic acid from artemisinin involving reduction followed by esterification of the reduced product at room temperature.

Abstract: This invention relates to compounds containing a trioxane moiety, especially certain artemisinin derivatives, which have cytotoxic and antitumour activity and their use in the treatment of cancer. Some of these compounds comprise a ligand which is capable of binding to a nucleic acid and a group containing a trioxane moiety which is capable of acting as source of free radicals which are capable of chemically interacting with a nucleic acid. Processes for the preparation of such compounds and pharmaceutical compositions containing such compounds are also provided.

Abstract: The present invention relates to an improved method for the preparation of Artemether. Artemether prepared from the process is useful for the treatment of uncomplicated, severe complicated and multi drug resistant malaria.

Abstract: The present invention provides an optically active compound represented by the following general formula (1), a photoreactive chiral agent, a liquid crystal composition, a liquid crystal color filter, an optical film, and a recording medium which include the optically active compound. wherein, Ra and Rb each independently denotes a hydrogen atom, an alkyl group, an aryl group, a heterocyclic group, an alkenyl group, or an alkynyl group, Rc and Rd each independently denotes a hydrogen atom, an alkyl group, or an alkoxycarbonyl group, and L denotes a divalent group and a binaphtyl portion has an axial asymmetry of either (R) or (S).

Abstract: This invention concerns the compounds of formula (I), 1

Abstract: Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and artemisinin dimers have the following structure or diastereomers thereof, having antimalarial, and antiproliferative and antitumor activities wherein, the monomers of the present invention are formed when n is I and R is alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl. The dimers of the present invention are formed when n is 2 and R is a linker including, but not limited to, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl.

Abstract: The present invention of compounds of formula (I) 1

Abstract: A derivatized macrocyclic compound comprising the formula: 1

Abstract: The present invention is to provide calixcrown derivatives of formulae 1 to 3 requisite for the preparation of a self-assembled monolayer as well as a process for the preparation thereof. Further the present invention is to provide a self-assembled monolayer which is produced by immersing a gold substrate or related metal substrate in an organic solution containing said calixcrown derivatives of formulae 1 to 3. Still further the present invention provides a process for fixing a protein monolayer by fixing proteins having molecular weight of not less than 20,000D (20KD) on said self-assembled monolayer.

Abstract: Natural products such as certain chaetochromins are described. These compounds are useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein.

Abstract: The invention relates to an improved process for the preparation of arteether. The process comprises dissolving dihydroartemisinin in dry ethanol, adding a solid acid catalyst with trialkylorthoformate in the reaction mixture, stirring the reaction mixture at room temperature, adding H2O to the reaction mixture, extracting the reaction product with a non-polar organic solvent, and drying the solvent over anhydrous sodium sulphate and evaporating the solvent to obtain pure arteether.

Abstract: The invention relates to a polymeric waveguide comprising a lanthanide ion-sensitizer complex, characterized in that the lanthanide ion is preferably neodymium(III) ion (Nd3+), ytterbium(III) ion (Yb3+), or erbium(III) ion (Er3+), and the sensitizer absorbs in the 400-1200 nm region, and preferably in the 600-1000 nm region. The invention also relates to an optical device comprising the same.

Abstract: 1

Abstract: A cyclic compound of formula (I) wherein Rx groups which may be the same or different are selected from —O—(CH2)n—O— where n is an integer of from 2-6; Ry and Rz groups which may be the same or different are independently selected from hydrogen, halogen or a hydrocarbyl group; Ra together with Rb of the adjacent phenyl ring and Rc together with Rd of the adjacent phenyl ring form a group of formula —(CH2)m— or —(CH2)p—O— where m and p are integers of from 1-5, and each group Ra-Rb and Rc-Rd may be the same or different; and x is an integer of 2 or more, such as 4. Compounds of formula (I) display particular selectivity for specific ions such as potassium ions. They are useful inter alia in reactions where scavenging of a specific cation is required or as ion specific electrodes.

Abstract: The invention relates to compound of the general formula (I): R—O—A  (I) wherein: R represents the radical of formula (II): A is as defined in the description, and medicinal products containing the same which are useful in treating or in preventing cancer.

Abstract: A diterpene derivative compound, having the formula I, II, or III, compositions, and therapeutic compositions containing the compounds are disclosed. Also disclosed are methods for treating an inflammatory disorder by providing an inflammatory inhibiting amount of the compound as well as methods for obtaining the compound.

Abstract: The invention provides halichondrin analogs having pharmaceutical activity, such as anticancer or antimitotic (mitosis-blocking) activity, and methods of identifying agents that induce a sustained mitotic block in a cell after transient exposure of the cell to the agents.

Abstract: A method of preparation of an artemisinin extract comprising the steps of extraction of Artemisia annua with liquid carbon dioxide and allowing the carbon dioxide to evaporate from the resultant mixture.

Abstract: The present invention provides a two-step procedure for the replacement of the pyranose anomeric 10-OH group in dihydroartemisinin by a variety of carbon nucleophiles, resulting in the novel C-10 carbon-substituted trioxanes of structure: ##STR1## wherein, when n is 1, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, acetylenics, or benzoylmethylenes, or alkanoylmethylenes; or when n is 2, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes; or when n is 3, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes.

Abstract: The present invention provides a two-step procedure for the replacement of the pyranose anomeric 10-OH group in dihydroartemisinin by a variety of carbon nucleophiles, resulting in the novel C-10 carbon-substituted trioxanes of structure: ##STR1## wherein, when n is 1, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, acetylenics, or benzoylmethylenes, or alkanoylmethylenes; or when n is 2, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes.

Abstract: Improved liquid phase process useful in the hydrocyanation of diolefinic compounds to produce nonconjugated acyclic nitriles and to the liquid phase process of isomerization of the nitrites to, among other things, 3- and/or 4-monoalkene linear nitriles. The improvement involves conducting the process in the presence of zero-valent nickel and a multidentate phosphite ligand. Novel multidentate phosphite ligands and catalyst precursor compositions made therefrom are also disclosed.

Abstract: Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N--R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub.2 OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR.sub.11 OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.

Abstract: Novel polycyclic ethyl alkylamides of formula I are active as melatonergic agents. ##STR1## wherein Z=CH (when a double bond is present) or (CH.sub.2).sub.n, wherein n is 1-4;X=O, CH.sub.2, or CH (when a double bond is present);R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or C.sub.1-3 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-4 alkoxyalkyl, C.sub.1-4 trifluoromethylalkyl, C.sub.1-6 aminoalkyl; andY=H, C.sub.1-6 alkoxy or halogen.

Abstract: The invention relates to a preparation of azadirachtin, in a dry solid powder form, having a purity upto 88%; an emulsion concentrate having upto 30% by weight of azadirachtin, and a process for preparing said azadirachtin dry powder from neem seeds/kernels, which comprising: (a) disintegrating the neem seeds/kernels into a powder; (b) subjecting the said powder to continuous extraction using methanol or aqueous methanol or ethanol (rectified spirit) or aqueous ethanol at ambient temperature; (c) concentrating the extract and stirring the concentrate with petroleumether or hexane and phase separating by conventional methods; (d) stirring the denser phase containing major quantity of azadirachtin with a water immiscible organic solvent and water as required depending on the solvent used for extraction and phase separating by conventional methods; (e) concentrating the organic phase and gradually adding the concentrate to petroleumether or hexane under stirring at ambient temperature (f), filtering under suctio

Abstract: Novel taxane derivatives and intermediates having the formula 1. ##STR1## and a process for the preparation of the compounds of the formula 1 from 14-.beta.-hydroxy-10-deacetylbaccatin III of formula 2 ##STR2## and pharmaceutically acceptable compositions containing the taxane derivatives and intermediates of formula 1.

Abstract: This invention relates to the compounds represented by general formula (I) and the processes for their preparation, wherein R is selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl unsubstituted or substituted by a halogen atom or nitro group, biphenyl unsubstituted by a halogen atom or nitro group, naphthyl unsubstituted or substituted by a halogen atom or nitro group. The compounds of this invention are used to prepare agents for prevention and treatment of AIDS and drugs against malaria and toxoplasmosis.

Abstract: Compounds of formula I ##STR1## in which Q denotes hydrogen, a hydroxy group or a C.sub.1 to C.sub.8 alkoxy group which can be substituted if desired, by carboxyl or C.sub.1 to C.sub.6 alkoxycarbonyl and eitherY and Z together form a group ##STR2## and X represents hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.2 to C.sub.6 alkenyl orY and X together form a group ##STR3## or an alkylene residue of 2-4 carbon atoms and Z represents hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.1 to C.sub.6 alkanoyl, whereR denotes hydrogen or a C.sub.1 to C.sub.6 alkyl residue as well as physiologically tolerated salts thereof, processes for their production and pharmaceutical agents containing these compounds for the treatment of inflammatory diseases and allergic diseases.

Abstract: Disclosed herein are novel artemisinin dimers of structure ##STR1## which possess anticancer activity.

Abstract: The invention relates to a polymeric optical amplifier doped with lanthanide ions, which are present in the amplifier in the form of a complex.The invention also relates to novel electrically neutral lanthanide complexes which can be applied with advantage in the above-described polymeric optical amplifiers. These complexes comprise host molecules which readily complex with the lanthanide and fully encapsulate it.

Abstract: Dihydroartemisinin hemisuccinate is prepared by acylation of dihydroartemisinin with 1.0 to 1.3 molar equivalents of succinic anhydride in the presence of 0.5 to 1.5 molar equivalents of tri(C.sub.1 -C.sub.3 -alkyl)amine in a low-boiling, neutral, water-miscible, inert organic solvent or solvent mixture and subsequent isolation of the product at pH 5-8. The product is obtained directly in crystalline form and high yield.

Abstract: A process of preparing a purified crown compound is disclosed which comprises the steps of (a) dissolving a crown compound and a salt in an organic solvent to form a solution of a complex salt of a crown compound; (b) filtering the solution to obtain a filtrate; (c) adding water to the filtrate to produce a precipitate; and (d) filtering out the produced precipitate.

Abstract: The invention relates to a polymeric optical amplifier doped with lanthanide ions, which are present in the amplifier in the form of a complex. The invention also relates to novel electrically neutral lanthanide complexes which can be applied with advantage in the above-described polymeric optical amplifiers. These complexes comprise host molecules which readily complex with the lanthanide and fully encapsulate it.

Abstract: The present invention relates to new ginkgolide derivatives of the formula (I) as below which represents PAF-antagonistic activity and the method for the preparation thereof, by that the cyclic compounds of substituted Ginkgolide B derivatives are produced by reacting the known Ginkgolide B and C mixture having the hydroxy group in 1- and 10-carbon with acid, then they are separated, and separated Ginkgolide B derivatives is hydrolyzed in acidic aqueous solution. And the present invention is related to make use it as PAF-antagonistic agent through separating the only one component of the new ginkgolide derivative by those methods.