Abstract: The subject invention provides compounds having the structure: 1

Abstract: Methods of treating a fungal or yeast infection and of killing or inhibiting fungi or yeast are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.

Abstract: A compound having the structure: 1

Abstract: A method of isolating terpene trilactones from Ginkgo biloba plant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.

Abstract: The present invention concerns a process for the preparation of 2-halopyridine N-oxide by reaction of 2-halopyridine with hydrogen peroxide in aqueous solution in the presence of an acid anhydride as catalyst in which, according to the invention, as catalyst there is used an anhydride of the formula I whereby the aromatic rings can be substituted by alkyl groups or halogens or can be anellated with a further aromatic ring.

Abstract: Compounds which are prodrugs of triptolide or its derivatives, containing an amino acid or oligopeptide moiety, are used for anticancer or immunosuppressive treatment.

Abstract: Agents for inducing apoptosis comprising a tetrocarcin derivative represented by the following formula (I) or a salt thereof as an active ingredient (---- represents a single bond or a double bond; j and k represent 0 or 1; R1 to R3, R7 to R10 and R14 represent a hydrogen atom, a lower alkyl group and the like; R4, R11, R12, R13 and R15 to R18 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like; R5 and R6 represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a group represented by the following formula (B) (R32 represents a formyl group and the like, R33 to R35 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like); R19 represents a hydroxyl group, a lower alkoxyl group, a lower alkanoyloxy group and the like). The agents are useful as medicaments for preventive and/or therapeutic treatment of diseases resulting from increased expression of Bcl-2 family proteins, for example, cancers, AIDS and the like.

Abstract: Compounds which are prodrugs of triptolide or its derivatives, containing an amino acid or oligopeptide moiety, are used for anticancer or immunosuppressive treatment.

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: The present invention relates to a novel process for preparing compounds of the formula (I) by reacting compounds of the formula (II) with a base and compounds of the formula (III) in which X, Y, Z, n, G, A, B, R1, R8 and Hal are each as defined above.

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: Compounds useful in immunosuppressive and anti-inflammatory treatment are described. The compounds are hydrolyzable triptolide analogs with improved water solubility and generally lower toxicity than the parent compound.

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: Processes for preparing spirolaxine and spirolaxine methyl ether, the compounds of formulas (I) and (II) respectively, ##STR1## comprising fermenting fungi selected from the group consisting of Sporotrichum pruinosum FD 29585, ATCC 74327; Sporotrichum pruinosum FD 29454, ATCC 74329; Sporotrichun pruinosum FD 29586, ATCC 74328; and Phanerochaete chrysosporiun LN 3576, ATCC 74326. This invention also relates to a process for preparing spirolaxine comprising fermenting Sporotrichum pruinosum FD 29458, ATCC 74330.

Abstract: The present invention relates to novel triptolide derivatives and a method of treating a patient suffering from an autoimmune disease comprising administering to a patient an effective amount of the novel triptolide derivatives.

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

Abstract: The present invention relates to novel triptolide derivatives and a method of treating a patient suffering from an autoimmune disease comprising administering to a patient an effective amount of the novel triptolide derivatives.

Abstract: The present invention relates to chrolactomycin compound represented by the following formula (I): ##STR1## or pharmaceutically acceptable salts thereof having antibacterial and antitumor activities.

Abstract: Trehalose is oxidized to give oxidized trehalose which then is hydrolyzed to produce D-glucuronolactone which is thereafter recovered to realize high-yield and low-cost production of D-glucuronolactone.

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: The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.

Abstract: Compounds and methods for use in immunosuppressive and anti-inflammatory treatment are described. The compounds are triptolide analogs with improved water solubility and low toxicity.

Abstract: Novel platinum(II) complexes represented by the general formula ##STR1## in which R.sub.1 represents a lower hydrocarbon radical of 1 to 3 carbon atoms, R.sub.2 and R.sub.3 each independently represent a hydrogen atom or a lower hydrocarbon radical of 1 to 3 carbon atoms, or R.sub.2 and R.sub.3 together may form --(CH.sub.2).sub.4 --or --(CH.sub.2).sub.5 --, Y and Z each independently represent an ammonia molecule or a monodentate amine of 1 to 7 carbon atoms or X and Y together may form a bidentate diamine of 2 to 10 carbon atoms, and X.sup.- represents an inorganic acid anion or an organic carboxylate anion, and agents for treating malignant tumors which contain them as effective components. The compounds are effective against cisplatin-resistant tumors, are soluble enough for intravenous administration, are stable in aqueous solution, and have excellent antitumor activity.

Abstract: A two-step process for converting ginkgolide C into ginkgolide B is disclosed. In the first step, ginkgolide C is reacted with a sulfonic anhydride to obtain a C-7 sulfonate of ginkgolide C. In the second step, the C-7 sulfonate of ginkgolide C is reacted with a borohydride, and this reaction eliminates the C-7 radical of the C-7 sulfonate of ginkgolide C, thus producing ginkgolide B.

Abstract: Compounds having formula (3), wherein R.sup.1 is hydrogen, straight or branched alkyl with 1-10 carbon atoms, straight or branched alkenyl with 2-10 carbon atoms, straight or branched alkynyl with 2-10 carbon atoms, benzyl or aryl, optionally mono- or plurisubstituted with straight or branched alkyl with 1-10 carbon atoms, hydroxy, alkoxy, halogen, an amino or a nitro group; and when R.sup.1 is H salts thereof, or R.sup.1 is acyl (R.sup.1 =--COR.sup.2) wherein R.sup.2 is straight or branched alkyl with 1-10 carbon atoms, alkenyl with 2-10 carbon atoms, alkynyl with 2-10 carbon atoms, or aryl, optionally mono- or plurisubstituted with alkyl with 1-10 carbon atoms, hydroxy, alkoxy, halogen, an amino or a nitro group. Compounds of formula (3) have interesting antifungal activities and may, accordingly, be used as active ingredients in fungicidal compositions.

Abstract: A Tripterygium wilfordii Hook F preparation having an improved LD.sub.50 in mice, an improved therapeutic activity:toxic index ratio and a lower amount of triptolide as compared to previous preparations is disclosed. The LD.sub.50 in mice of the T. wilfordii preparation is greater than about 860 mg/kg, the therapeutic activity:toxic index ratio is greater than about 2.6.times.10.sup.-3, and the amount of triptolide is less than about 1.3 .mu.g/mg. The preparation is useful for immunosuppression, in particular, the suppression of primary antibody response and suppression of autoimmune disease and for the treatment of rheumatoid arthritis.

Abstract: The present invention is directed to new ginkgolide derivatives, which may be used for the prevention or treatment of various PAF-induced diseases, and the pharmaceutical uses of these derivatives. The present invention is also directed to a process for preparing these ginkgolide derivatives.

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.

Abstract: The invention provides methods of preparing a male antifertility agent composed of a diterpene lactone compound obtained from plants of the genus Tripterygium, the diterpene lactone compounds obtained from that method, and the use of the compounds as an antifertility agent.

Abstract: Novel macrocyclic lactone antibacterials isolated from a culture containing the microorganism S. aerocolongenes sub sp. antibiotica SCC 1886, ATTC 55003 and their use for treating and/or preventing antibacterial infections, especially Chlamydia infections are disclosed.

Abstract: The invention relates to a process for the preparation of ginkgolide B from ginkgolide C and to ginkgolide B thus obtained, the process comprising the following succession of four steps:protecting the 10-hydroxy group of ginkgolide C by conversion to an alkyl ester, the reaction being effected in dimethylformamide at a temperature of from 15.degree. to 50.degree. C. for from 4 to 10 hours;activating the 7-hydroxy group of the resultant 10-protected ginkgolide C by conversion to a (R)thiocarbonyl ester, the activation being effected in basic conditions at a temperature of from 0.degree. to 40.degree. C. for from 1 to 24 hours;deoxygenating the 7-activated group in the resultant 10-protected 7-activated ginkgolide C by treating it with tributyltin hydride or tris-(trimethylsilyl)silane, in an aprotic solvent, in the presence of a free-radical generator, the reaction being effected at a temperature of from 70.degree. to 110.degree. C.

Abstract: The primary hydroxy group of Corey lactone diols is optically selectively acylated to obtain the desired optically active ester and/or diol. The mixture of Corey lactone diols of formulae (Ia) and (Ib): ##STR1## is reacted with an acylating agent optically selectively in the presence of an enzyme and/or a microorganism thereby to acylate, isolate and purify the primary alcohol.

Abstract: 13-alkyl-11.beta.-phenyl-gonanes of general formula I ##STR1## wherein A and B together stand for an oxygen atom, a CH.sub.2 group or a second bond between carbon atoms 9 and 10,X is an oxygen atom or the hydroxyimino grouping N.about.OH,R.sub.1 is a straight-chained or branched, saturated or unsaturated alkyl radical with up to 8 carbon atoms, which contains the grouping ##STR2## with X as described above, R.sub.2 is a methyl or ethyl radical in the .alpha. or .beta. position,R.sub.9, R.sub.10, R.sub.11 and R.sub.12 each stand for a hydrogen atom, a hydroxy, alkyl, alkoxy or acyloxy group with 1 to 4 carbon atoms respectively or a halogen atom and R.sub.3 and R.sub.4 have a variety of meanings, have antigestagenic and antiglucocorticoid effects.

Abstract: A living tissue or living cell preservation solution comprising an effective amount of a ginkgolide to reduce reperfusion injury in living tissue which has been stored therein and a substance or mixture or substances present in an amount sufficient to produce an osmotic pressure in said solution approximately equal to the osmotic pressure or mammalian cell and a method for preventing or reducing reperfusion injury in transplanted mammalian organs, which comprises contacting an organ prior to reperfusion with an effective amount of a ginkgolide to reduce reperfusion injury in said organ.

Abstract: Synthesis and applications of fluorescent dyes which are derivatives of benzo[c]xanthenes is described. The dyes exhibit pH dependent absorption and fluorescence spectra with pKas near the normal physiological range. Unlike fluorescein, the dyes exhibit emission of different characteristic wavelengths dependent on the pH of the medium. This permits several methods of measuring the pH of the medium in contact with the indicator including measuring two emissions with one excitation, selectively exiting the acid and base forms independently and measuring their emission at either single or dual wavelengths, or measuring the characteristic pH dependent absorption or fluorescence excitation spectral. Methods are presented for making the indicators permeant to cell membranes for the measurement of intracellular pH.

Abstract: There are disclosed benzanthrone lactones of formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined in claim 1. The benzanthrone lactones of formula (1) are important intermediates for the synthesis of novel dyes which are obtained by coupling suitable diazo components to said compounds of formula (1).

Abstract: A copolymer formed from an isoimide oligomer and another compound, such as an aryl sulfone, each of which has reactive functional terminal groups, such as ethylenic or acetylenic groups. The isoimide oligomer is soluble in the other compound, unreactive with the compound below a certain temperature and forms a liquid blend therewith. Upon heating the liquid blend above that certain temperature, the terminal groups on the isoimide oligomer and the other compound react with each other to form a copolymer. The liquid blends may be used to form encapsulants, coatings, films, and resin matrices for composites to provide resins with excellent high temperature properties.

Abstract: The salt of GA.sub.4 and/or GA.sub.7 with an amine of formula R.sup.1 CH.sub.2 NHR.sup.2 wherein R.sup.1 is optionally substituted phenyl, thienyl or pyridyl and R.sup.2 is alkyl or alkynyl. The salts are useful in the preparation of GA.sub.4 /GA.sub.7 and their separation from GA.sub.3.

Abstract: Processes for the preparation of 1,2-dihydro-3-hydroxy gibberellin acids of general formula (1) from precursor gibberellin acids that employs conditions which (a) do not require prior protection of the free carboxylic acid group; (b) preserve the .DELTA.(16)-olefinic bond and the lactone; and (c) enable the stereochemistry of the hydroxyl moiety at position 3 to be controlled, enabling access to the individual stereoisomers of the 1,2-dihydro-3-hydroxy gibberellin acids; said processes comprising the reaction of either a 3-keto gibberellin of general formula (2), or of the general formula (3), or a mixture thereof, in the presence or absence of a proton source depending on the particular precursor gibberellin acid, with a compound of general formula (4):M.sup.+ (alkyl).sub.3 BH.sup.- (4)wherein M.sup.30 represents a monovalent cation.______________________________________ ##STR1## R.sup.1 R.sup.2 R.sup.3 R.sup.

Abstract: Processes for forming a class of relatively low molecular-weight oligomers containing at least one isoimide group and terminal groups capable of undergoing an addition polymerization reaction are provided. These oligomers are characterized by excellent solubility in common solvents and a melting temperature considerably lower than their cure temperature, thus enabling the oligomers to be formed into cured polymers more slowly and at lower temperatures, all without the evolution of deleterious gases. The process for forming these oligomers includes the formation of a polyamic acid and dehydration thereof under specified conditions to effect cyclization of the polyamic acid to form the isoimide-containing oligomer, without the formation of undesired side-reaction products.

Abstract: A class of relatively low molecular-weight oligomers containing at least one isoimide group and terminal groups capable of undergoing an addition polymerization reaction are provided. These oligomers are characterized by excellent solubility in common solvents and a melting temperature considerably lower than their cure temperature, thus enabling the oligomers to be formed into cured polymers more slowly and at lower temperatures, all without the evolution of deleterious gases. The oligomers of the present invention may be formed by reacting an aromatic dianhydride with an aromatic diamine, followed by reaction with a monoanhydride. The resulting product is dehydrated to form the isoimide-containing oligomer.

Abstract: A class of relatively low molecular-weight oligomers containing at least one isoimide group and terminal groups capable of undergoing an addition polymerization reaction are provided. These oligomers are characterized by excellent solubility in common solvents and a melting temperature considerably lower than their cure temperature, thus enabling the oligomers to be formed into cured polymers more slowly and at lower temperatures, all without the evolution of deleterious gases. The oligomers of the present invention may be formed by reacting an aromatic dianhydride with an aromatic diamine, followed by reaction with a functional mono-amine. The resulting product is then dehydrated to form the isoimide-containing oligomer.

Abstract: A class of relatively low molecular-weight oligomers containing at least one isoimide group and terminal groups capable of undergoing an addition polymerization reaction. The oligomers of the present invention are characterized by excellent solubility in common solvents and a melting temperature considerably lower than their cure temperature, thus enabling the oligomers to be formed into cured polymers more slowly and at lower temperatures, all without the evolution of deletrious gases.

Abstract: Is the objective of the invention to develop a process for the production of tagged gibberellin-(7)-aldehydes which is of general applicability. As per the invention a gibberellin-(7)-aldehyde is converted into the gibberellin-(7)-aldehyde tagged at the C-15 position of the basic gibberellin skeleton under the influences of ultraviolet radiation, in given cases after the isolation of a developing 7-Hydroxy-7,15-cyclo butane derivative, and in the presence of compounds with tritium or deuterium donor properties respectively. The process is of particular suitability for the tagging of alkali-sensitive gibberellin-(7)-aldehydes. The tagged gibberellin-(7)-aldehydes produced by the process as per invention, are of importance for instance as primary materials for the obtaining of tagged natural gibberellins and their derivatives.