Abstract: The invention discloses a method for the production of a macrocyclic lactone represented by a formula (2), which comprises subjecting a hydroxycarboxylic acid ester represented by a formula (1) to intramolecular esterification reaction. In the formulae (1) and (2), m is an integer of from 5 to 10, n is an integer wherein m+n becomes from 11 to 16, X represents —CH2—, —CH═CH—, —O—, —S— or —NH—, and R represents a hydrocarbon group having from (m+n+2) to 40 carbon atoms or a group represented by —(AO)pR1 wherein AO represents an alkyleneoxy group having from 2 to 4 carbon atoms, p is average addition mole number of alkylene oxide and R1 represents a hydrocarbon group having a specified number of carbon atoms so that the total number of carbon atoms of the —(AO)pR1 group becomes from (m+n+2) to 40.

Abstract: The invention relates to novel epothilone derivatives of general formula (I), wherein R8 means a halogen atom, especially a fluorine or chlorine atom, and the remaining substituents have the meanings given in the description. The novel compounds are suitable for producing medicaments.

Abstract: The present invention describes the use of cationic vinylidene, allenylidene and higher cumulenylidene complexes of ruthenium or osmium as catalysts or catalyst precursors for olefin metathesis reactions of all types, as well as to new cationic allenylidene complexes of ruthenium and osmium which can be used as metathesis catalysts with preferred embodiment. These catalysts or catalyst precursors are easy to prepare from well accessible, stable and essentially non toxic starting materials, can be isolated and stored, they exhibit a high catalytic activity, a good compatibility with functional groups, solvents, water and additives, and they need not to be activated by any additive.

Abstract: This invention is an improvement upon the known process for polymerization of polytrimethylene terephthalate by esterification of terephthalic acid or dimethyl terephthalate with 1,3-propane diol, precondensation of the esterification product to produce a precondensation product, and polycondensation of the precondensation product to produce polytrimethylene terephthalate and, optionally, solid stating of this product to produce higher intrinsic viscosity polytrimethylene terephthalate. The cyclic dimer of terephthalic acid and 1,3-propane diol is produced as a byproduct of the above process and the improvement comprises (a) recovering the cyclic dimer from the polymerization, (b) reacting from 0.5 to 25 percent by weight of the cyclic dimer in 1,3-propane diol in the presence of from 0.1 to 10 percent by weight of the cyclic dimer of a basic catalyst for five minutes to 24 hours at 50 to 210° C.

Abstract: The present invention relates to novel macrocyclic compounds, and to their preparation and use in perfumes. Specifically, the present invention relates to novel 1,4-dioxacycloalkan-2ones and 1,4-dioxzcycloaken-2-ones.

Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.

Abstract: Cyclic ester oligomers (CEOs) are manufactured from linear polyesters or their precursors by a continuous reactive extraction in which the linear polyesters are converted to the CEOs and the CEOs selectively removed from the mixture by extraction with a fluid. The fluid may be a liquid or a gas. The CEOs produced are useful as monomers, for example in a reaction injection molding process to rapidly form polyesters from low viscosity liquids.

Abstract: The present invention relates to derivatives of 3-deoxy desmycosin of the formula I, wherein, starting from triply protected desmycosin, there are performed an oxidation at C-3 in the first step and then, optionally, a hydrogenation of double bonds and an epoxidation followed by a reductive opening of the oxirane ring. The present invention also relates to derivatives of 3-deoxy-desmycosin of the formula II, wherein in the first step triacetyl desmycosin is hydrogenated and then, via an intermediate mesylate, it is converted to a 2,3-didehydro derivative; or 2,3-didehydro-desmycosin is subjected to epoxidation reactions followed by a reductive opening of the oxirane ring.

Abstract: This invention relates to a bioactive compound and to compositions which contain it. The invention further relates to methods of microtubule stabilization. In particular, it relates to a compound which has cytotoxic properties and which therefore has utility in inter alia anti-tumor treatments.

Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as modulators of SK Ca, IK Ca and BK Ca channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, for methods of therapy, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.

Abstract: Michael addition conducted in the presence of a zinc-amine complex and additional amounts of the amine component results in product with high diastereomeric excess.

Abstract: Macrocyclic ester compounds can be prepared from oligoesters by thermal cleavage in the presence of a thermostable benzene derivative.

Abstract: 3′-Des-dimethylamino-9-oxyimino macrolides of formula (I) endowed with anti-inflammatory activity and their pharmaceutical use are described.

Abstract: Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.

Abstract: Macrocyclic ester compounds can be prepared from oligoesters by thermal cleavage in the presence of a thermostable benzene derivative.

Abstract: Genetic engineering of the erythromycin polyketide synthase genes to effect combinatorial alterations of catalytic activities in the biosynthetic pathway can be used to generate a library of macrolides impractical to produce by chemical methods. The library includes examples of analogs with one, two and three altered carbon centers of the polyketide products.

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: A compound having the following formula: wherein R3 and M are defined herein, and processes therewith.

Abstract: A purified salt of &bgr;-hydroxyethoxy acetic acid of formula (1) having a fusion peak-top temperature detected by differential scanning calorimetry (DSC) and a purified 2-p-dioxanone of formula (2) derived from the purified salt of &bgr;-hydroxyethoxy acetic acid of formula (1).

Abstract: The present invention relates to the use of known efomycins and elaiophylins for the treatment of autoimmune disorders, to new natural substances efomycins M and T, and processes for their preparation; in particular to their use as medicaments in psoriasis therapy.

Abstract: Compositions comprising ketone bodies and/or their metabolic precursors are provided that are suitable for administration to humans and animals and which have the properties of, inter alia, (i) increasing cardiac efficiency, particularly efficiency in use of glucose, (ii) for providing energy source, particularly in diabetes and insulin resistant states and (iii) treating disorders caused by damage to brain cells, particularly by retarding or preventing brain damage in memory associated brain areas such as found in Alzheimer's and similar conditions.

Abstract: The present invention relates to the use of known efomycins and elaiophylins for the treatment of autoimmune disorders, to new natural substances efomycins M and T, and processes for their preparation; in particular to their use as medicaments in psoriasis therapy.

Abstract: The invention relates to a process for the preparation of a macrocyclic ester of the general formula: in which m is an integer from 6 to 14 and n is an integer from 2 to 12.

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: Intermediates for the preparation of compounds selected from the group consisting of a compound of the formula ##STR1## wherein R is ##STR2## n is an integer from 3 to 5, Ar is an optionally substituted heterocyclic selected from the group consisting of

Abstract: Disclosed are modified bryostatins and their use as anticancer drugs.

Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the polyacetate-, diaminobenzyl alcohol-, diacylglycerol- and bryostatin-classes.

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: Disclosed are odorant compounds having 14- to 17-membered 4-methyl substituted 1,7-dioxacycloalkan-8-ones and 14- to 16-membered 1,7-dioxacycloalkan-8-ones with 4,4-dimethyl substitution. Also disclosed are methods of odorizing a substance using at least one of the above mentioned compounds, as well as an economical process for their manufacture.

Abstract: Compositions having anti-inflammatory, antiviral and other activities are disclosed. The compositions are derived from phorboids of the polyacetate- and bryostatin-classes.

Abstract: Compounds of formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, unsubstituted lower alkyl or lower alkyl substituted by lower alkoxy or lower alkyl thio, or acyl which is unsubstituted or substituted by one or more of lower alkyl, lower alkyl substituted by halogen, and lower alkoxy;X is CO or CHOH;Y is CO or CH.sub.2 ; andZ is O or NH, and epimers and enantiomers thereof,or the physiologically usable salts thereof are useful as anti-tumor agents. They can be prepared by fermentation of Aspergillus sp. and, optionally, subsequent modification of functional groups.

Abstract: Methods for effecting epoxidation of olefinic compounds using cyclic ketone catalysts is provided. In particular, catalytic asymmetric epoxidation of unfunctionalized olefins, e.g., trans-olefins and trisubstituted olefins using novel cyclic ketones possessing C.sub.2 symmetric chiral elements is provided.

Abstract: Novel macrolide compounds, including Lasonolide A and Lasonolide B, have been isolated from a marine sponge. These compounds, analogs, derivatives, or isomers of these compounds, and compositions comprising the compounds or its derivatives, are useful as antitumor agents and as biochemical tools.

Abstract: Compound of the Formula 1 ##STR1## wherein: R.sup.1 and R.sup.2 are independently selected from the group comprising hydrogen, C.sub.1 to C.sub.6alkyl, C.sub.1 to C.sub.6 haloalkyl, phenyl, and substituted phenyl;X is selected from the group comprising sulfur, sulphone, disulfide;Y is selected from oxygen, carbon, N--H, N-alkyl, N-aryl, or sulfur; andZ is any linking functionality.The compounds represent a new class of ring opening monomers.

Abstract: The practicality of known depolymerization reactions in which there is a danger of building up adherent residues on heat transfer surfaces is greatly improved by performing the process under conditions that provide a driving force which assures that none of the feed material and none of any liquid or solid residue produced during the depolymerization of the feed material remains in contact with any heat transfer surface for a time sufficiently long to form any adherent solid residue on the surface. A preferred apparatus for achieving such a driving force includes a horizontal thin film evaporator, a controlled continuous input of liquid feed material, and continuous collection of desired reaction product and any residue that remains condensed throughout its passage through the reaction zone.

Abstract: The invention is directed to compounds having general formula (I) or general formula (II). Compounds of formulae (I) or (II) have interesting antifungal activities and may, accordingly, be used as active ingredients in fungicidal compositions.

Abstract: Lactones of formula ##STR1## and their pharmacologically acceptable salts endowed with antioxiding and hypolipidaemic properties and that show the capability to prevent and/or to delay the oxidative modification of the lipoproteins by competing with the chain of propagation of the lipidic peroxidation by means of an effective scavenging of the peroxylic radicals. The compounds object of the present invention are useful in the treatment of the atherosclerosis and of many correlated vascular pathologies, like ischaemic cardiopathies (angina pectoris and myocardial infarction), cerebral thrombosis and peripheral arteriopathies, because the high plasma levels of lipids and the oxidative modifications of the low density lipoproteins (LDL) represent crucial events in the pathogenesis of the atherosclerosis.

Abstract: Macrocylic lactam compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the invention, as well as compositions containing the same and methods for their use in stimulating contractile motion of the gastrointestinal tract.

Abstract: Macrocylic lactam compounds of formula (i) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the invention, as well as compositions containing the same and methods for their use in stimulating contractile motion of the gastrointestinal tract.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: Compound (1), isolated from a marine dinoflagellate, is a novel macrolide which has potent in vitro cytotoxicity against human colon carcinoma cell line HCT116 (IC.sub.50 =1.6 nM) and a multiple drug resistant subline. In addition, this compound has good in vivo antitumor activity against a P388 mouse leukemia (150% T/C).

Abstract: A novel macrolide compound, lasonolide A, has been isolated from a marine sponge. This compound, derivatives of the compound, and compositions comprising the compound or its derivatives, are useful as antitumor agents and as biochemical tools.

Abstract: Fluorine-containing, chiral liquid crystal compounds comprise (a) an aliphatic fluorocarbon terminal portion containing at least two catenary ether oxygen atoms; (b) a chiral, aliphatic hydrocarbon terminal portion; and (c) a central core connecting the terminal portions. The compounds have smectic mesophases or latent smectic mesophases and are useful, for example, in liquid crystal display devices.

Abstract: Novel scytophycin compounds and compositions are disclosed, along with methods of making and using the new compounds. Methods for preparing the new scytophycin compounds from new strains of the blue-green algae Scytonema ocellatum, Scytonema burmanicum and purified cultures of the algae are also provided. The scytophycins are useful as anti-cancer agents, antifungal agents and for cell research purposes.

Abstract: An Eastern Indian Ocean marine sponge in the genus Spongia was located in the Republic of the Maldives and found to contain a structurally unprecedented macrocyclic lactone named spongistatin 1. The new perhydropyran-containing structure, as shown below, was found to be remarkably potent and specific, log molar TCI.sub.50 to <-10, against twenty human cancer cell lines in the U.S. National Cancer Institute's panel of sixty.

Abstract: An intensive long-term investigation of marine organisms as sources of new anticancer drugs has led to the isolation and structural elucidation (primarily by high field NMR and mass spectrometry) of halistatin 1, a new polyether macrolide of the halipyran-type, from the Western Indian Ocean sponge Phakellia carteri. Halistatin 1 (8.8.times.10.sup.-7 % yield) caused the accumulation of cells arrested in mitosis, inhibited tubulin polymerization, and inhibited the binding of radiolabeled vinblastine and GTP to tubulin.

Abstract: A Southwest Indian Ocean marine sponge Spirastrella spinispirulifera (bri colored reds and purples) has been found to contain new and exceptionally active cell (human cancer) growth inhibitors spongistatin 5, spongistatin 7, spongistatin 8 and spongistatin 9. These compositions are related to spongistatin 1, which was found in a black Spongia sp. in the Porifera family. A method of treating human cancer cells with spongistatin 5 and spongistatin 7 is also disclosed.

Abstract: An optically active oligomer obtained by polycondensation of an (R)-3-hydroxyalkanoic acid alkyl ester and at least one of a diol, a diamine and an amino alcohol and an optically active polymer obtained by copolymerization of said oligomer and a monomer selected from diisocyanic acid esters, dicarboxylic acid derivatives, and dichlorosilanes are disclosed. Novel functional polymers with biodegradability and hydrolyzability are produced with industrial advantage.

Abstract: Unguinol is a well-known metabolite of the fungi Aspergillus unguis and Aspergillus nidulans. Unguinol has been found to be an active growth permittant and promotant in animals, in particular, monogastric animals such as chickens. In addition, the fermentation broth also produced the additional known unguinol derivatives of folipastatin and 2-chloro unguinol as well as the novel 4-methyl derivative. All of these compounds are active animal growth permittants. Compositions containing such unguinol derivatives for use as growth permittants and promotants are also disclosed.

Abstract: Novel chemical compounds that can be used to synthesize halichondrin B and norhalichondrin B, and related derivatives, are described. The synthesis of halichondrin B and norhalichondrin B from these compounds also is described.