Abstract: The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.

Abstract: The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.

Abstract: The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.

Abstract: Described herein are novel metal complexes, especially ruthenium complexes, represented by the formula (1): wherein L1 is a N-heterocyclic carbene ligand, L2 is a neutral phosphine ligand, preferably tricyclohexyl-phosphine, and process of catalyzing olefin metathesis reactions, especially tetra-substituted olefin metathesis reactions.

Abstract: Described is pentamycin in a purity exceeding 95%, certain polymorphs and solvates of pentamycin, processes for their manufacture, and a method for decreasing the rate of degradation of pentamycin.

Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.

Abstract: The present invention relates to (meth)acrylated compounds (A) prepared from (a) at least one cyclic ether polyol, (b) at least one linking compound (b1) and/or (b2), wherein the linking compound (b1) is selected from cyclic compounds (b11) containing at least one (I) group in the cycle where X=O or NH, from hydroxy acids (b12) and/or from alkylene oxides (b13) containing from 2 to 4 carbon atoms and the linking compound (b2) is selected from epihalohydrins or polyisocyanates, (c) a (meth)acrylating compound; and to their use in radiation curable compositions for the coatings, inks, overprint varnishes, adhesives and composites.

Abstract: The present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material. Furthermore, the present invention relates to the use of the sorbent according to the invention for the purification of organic molecules, in particular pharmaceutically active compounds, preferably in chromatographic application.

Abstract: The present invention provides a resist composition giving a resist pattern excellent in CD uniformity and focus margin. A chemically amplified photoresist composition comprises a resin (A) and an acid generator (B), and the resin (A) contains, as a part or an entirety thereof, a copolymer (A1) which is obtained by polymerizing at least: a (meth)acrylic monomer (a1) having C5-20 alicyclic hydrocarbon group which becomes soluble in an aqueous alkali solution by the action of an acid; a (meth)acrylic monomer (a2) having a hydroxy group-containing adamantyl group; and a (meth)acrylic monomer (a3) having a lactone ring, and the copolymer (A1) has a weight-average molecular weight of 2500 or more and 5000 or less, and a content of the copolymer (A1) is not less than 50 parts by mass with respect to 100 parts by mass of the resin (A).

Abstract: The present invention relates to a new use of a known medicament. Specifically, the invention relates to methods and compositions for enhancing the therapeutic efficacy of a therapeutic agent by increasing the uptake of the therapeutic agent by target cells, and in particular relates to a pharmaceutical composition comprising a regulating agent of lipid raft/caveolae-dependent endocytic pathway and some therapeutic agents, such as anti-tumor agents. The invention also relates to a method for screening a regulating agent of lipid raft/caveolae-dependent endocytic pathway capable of enhancing the therapeutic efficacy of anti-tumor agents.

Abstract: The present invention provides a resist composition giving a resist pattern excellent in CD uniformity and focus margin. A chemically amplified photoresist composition comprises a resin (A) and an acid generator (B), and the resin (A) contains, as a part or an entirety thereof, a copolymer (A1) which is obtained by polymerizing at least: a (meth)acrylic monomer (a1) having C5-20 alicyclic hydrocarbon group which becomes soluble in an aqueous alkali solution by the action of an acid; a (meth)acrylic monomer (a2) having a hydroxy group-containing adamantyl group; and a (meth)acrylic monomer (a3) having a lactone ring, and the copolymer (A1) has a weight-average molecular weight of 2500 or more and 5000 or less, and a content of the copolymer (A1) is not less than 50 parts by mass with respect to 100 parts by mass of the resin (A).

Abstract: The present invention is related to variants of mycolactones of formula (I), processes for the preparation thereof, pharmaceutical compositions thereof and their use in modulating inflammation, immunity and pain. Y—O—W (I), wherein Y and W are as defined in claim 1.

Abstract: The invention refers to primycin or a primycin component or a combination of primycin components, for use in the treatment or prevention of infections caused by Gram-positive bacteria resistant to methicillin and/or vancomycin and/or mupirocin or by penicillin-resistant streptococci. The invention also covers antibiotic compositions containing these active agents.

Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.

Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

Abstract: The present invention concerns groups of compounds derived from tunicates of the Synoicum species, as well as to pharmaceutical compositions comprising these compounds, and uses thereof. Extracts from tunicates show selective toxicity against several different cancer cell lines in the NCI 60 cell line panel. These compounds are useful in the effective treatment of cancers, particularly malignant melanomas, colon cancer, and renal cancer cell lines.

Abstract: The present invention relates to a new use of a known medicament. Specifically, the invention relates to methods and compositions for enhancing the therapeutic efficacy of a therapeutic agent by increasing the uptake of the therapeutic agent by target cells, and in particular relates to a pharmaceutical composition comprising a regulating agent of lipid raft/caveolae-dependent endocytic pathway and some therapeutic agents, such as anti-tumor agents. The invention also relates to a method for screening a regulating agent of lipid raft/caveolae-dependent endocytic pathway capable of enhancing the therapeutic efficacy of anti-tumor agents.

Abstract: Described is pentamycin in a purity exceeding 95%, certain polymorphs and solvates of pentamycin, processes for their manufacture, and a method for decreasing the rate of degradation of pentamycin.

Abstract: The present invention concerns groups of compounds derived from tunicates of the Synoicum species, as well as to pharmaceutical compositions comprising these compounds, and uses thereof. Extracts from tunicates show selective toxicity against several different cancer cell lines in the NCI 60 cell line panel. These compounds are useful in the effective treatment of cancers, particularly malignant melanomas, colon cancer, and renal cancer cell lines.

Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of various disorders including cancer, metastasis and disorders involving increased angiogenesis, wherein R1-R6, Ra-Rc, Q, Y1, Y2 and n are as defined herein.

Abstract: A method of using organic compounds and providing slow release flavoring in or for food products wherein flavor precursors are added to flavor compositions and/or food products and release flavor compounds upon consumption of the food products, and novel flavor precursor compounds. The flavor precursors can be prepared from mono- and/or diglycerides and lactone flavor compounds.

Abstract: Described is pentamycin in a purity exceeding 95%, certain polymorphs and solvates of pentamycin, processes for their manufacture, and a method for decreasing the rate of degradation of pentamycin.

Abstract: This invention is the design and synthesis of a caprolactone monomer which bears a pendant protected carboxyl group. This monomer has been copolymerized with caprolactone in varying ratios. After polymerization, the protecting group can be removed and an antibiotic can be attached as a new pendant group. The bioactivity of the antibiotic-bound poly(caprolactone) polymer is described.

Abstract: A shape-memory polymers comprising at least one monomer subunit represented by the following structural formula (1).

Abstract: The present invention relates to micelle-forming poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups on the polyester block therein. The biodegradability of these copolymers and their biocompatibilities with a large number of bioactive agents make them suitable as carriers for various bioactive agents. The bioactive agents, such as DNA, RNA, oligonucleotide, protein, peptide, drug and the like, can be coupled to the reactive groups on the polyester block of the copolymer.

Abstract: The invention relates to Iejimalides having the following formula (I) in which a, b, c, d, e, f, g, h, i, j, k, l, m, n, o, p are simple or double bonds, the continuous lines representing at least one simple bond, the dotted lines representing a possible bond. A double bond can be present but it is not necessary, and provided that a continuous line is also present, or a simple bond can be present if no other line is represented; m=0-20 and n1-n18=1, 2. The bonds can be used as chemotherapeutic agents for treating cancer.

Abstract: Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.

Abstract: The present invention relates to a polyketide molecule of the following formula (I): or a pharmaceutically acceptable salt thereof, where R1 is a hydrogen atom or a (C1-C7) alkyl group, as well as the method of preparation and use thereof, in particular as an anticancer agent.

Abstract: The present invention provides compounds represented by formula (1): wherein, R1, R2, R3 and R4 are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. The invention also relates to processes for the manufacture of compounds of formula (1) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful for the treatment of cancer. The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.

Abstract: The present invention relates to an anti-inflammatory use of macrolactin compounds such as macrolactin A, 7-O-malonyl macrolactin A and 7-O-succinyl macrolactin A, which are produced from a novel Bacillus strain of Bacillus polyfermenticus KJS-2 (KCCM10769P). The macrolactin compounds provided by the present invention were confirmed to greatly suppress the expression and formation of inducible nitric oxide synthetase (iNOS) and cyclooxygenase-2 (COX-2) which are proteins related to the formation of inflammatory mediators, and to accordingly inhibit the formation of nitric oxide (NO) and of prostaglandin E2 (PGE2) which are the metabolites of the proteins. In addition, the macrolactin compounds provided by the present invention were confirmed to have excellent effects in inhibiting the formation of tumor necrosis factor-alpha (TNF-?), interleukin-1? (IL-1?), interleukin-6 (IL-6) and granulocyte macrophage colony-stimulating factor (GM-CSF), which are pro-inflammatory cytokines.

Abstract: This invention is the design and synthesis of a caprolactone monomer which bears a pendant protected carboxyl group. This monomer has been copolymerized with caprolactone in varying ratios. After polymerization, the protecting group can be removed and an antibiotic can be attached as a new pendant group. The bioactivity of the antibiotic-bound poly(caprolactone) polymer is described.

Abstract: A positive photosensitive composition ensuring wide exposure latitude and reduced line edge roughness not only in normal exposure (dry exposure) but also in immersion exposure, a pattern forming method using the positive photosensitive composition, and a novel resin contained in the positive photosensitive composition are provided, which are a positive photosensitive composition comprising (A) a resin having a specific lactone structure in the side chain and being capable of increasing the solubility in an alkali developer by the action of an acid and (B) a compound capable of generating an acid upon irradiation with an actinic ray or radiation, a pattern forming method using the positive photosensitive composition, and a novel resin contained in the positive photosensitive composition.

Abstract: A compound of the following structure: wherein R1 is H, an alkyl group, an aryl group, an alkenyl group, an alkynyl group, or a halogen atom; R2 is H, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; Ra, Rb and Rc are independently an alkyl group or an aryl group; Rd is an alkyl group, an aryl group, an alkoxylalkyl group, —RiSiRaRbRc or a benzyl group, wherein Ri is an alkylene group; Re is an alkyl group, an allyl group, a benzyl group, an aryl group, an alkoxy group, or —NRgRh, wherein Rg and Rh are independently H, an alkyl group or an aryl group; R3 is (CH2)n where n is and integer in the range of 0 to 5, —CH2CH(CH3)—, —CH?CH—, —CH?C(CH3)—, or —C?C—; R4 ?wherein y1 and y2 are 1 and y3, y4 and y5 are independently 0 or 1, Rk1, Rk2, Rk3, Rk4 and Rk5 are independently H, CH3, or OR2a, and Rs1, Rs2, Rs3, and Rs4 are independently H or CH3, wherein R2a is H, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; and R5 is

Abstract: Described is pentamycin in a purity exceeding 95%, certain polymorphs and solvates of pentamycin, processes for their manufacture, and a method for decreasing the rate of degradation of pentamycin.

Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.

Abstract: The invention provides a compound termed Carolacton having the structure and derivatives thereof for medical use against biofilm formation by bacteria.

Abstract: The present invention relates to methods of screening for agents that bind to FBP21. In particular the present invention provides a method of identifying anti-angiogenic agents by screening for agents which are able to bind to FBP21. Compounds identified using the methods and screens of the present invention are useful in the prevention and treatment of conditions associated with angiogenesis.

Abstract: Salarines and Tulearins isolated from Fascaplysinopsis sp. sponge and synthetic derivatives thereof are provided.

Abstract: This invention relates to methods, compositions, and apparatuses for producing macrocyclic compounds. First, one or more reactants are provided in a reaction medium, which are capable of forming the macrocyclic compound through a desired reaction pathway that includes at least cyclization, and which are further capable of forming undesired oligomers through a undesired reaction pathway that includes undesirable oligomerization. Oligomerization of such reactions in the reaction medium is modulated to reduce formation of undesired oligomers and/or to reduce separation of the undesired oligomers from the reaction medium, relative to a corresponding unmodulated oligomerization reaction, thereby maximizing yields of the macrocyclic compound. The macrocyclic compound so formed is then recovered from the reaction medium. Preferably, the macrocyclic compound spontaneously separates from the reaction medium via phase separation.

Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.

Abstract: Combinatorial libraries of polyketides can be obtained by suitable manipulation of a host modular polyketide synthase gene cluster such as that which encodes the PKS for erythromycin. The combinatorial library is useful as a source of pharmaceutically active compounds. In addition, novel polyketides and antibiotics are prepared using this method.

Abstract: Disclosed are: a novel dinoflagellate alga; and a macrolide compound which can be used as a novel anticancer agent. Specifically disclosed is a macrolide compound produced by a dinoflagellate Amphidinium sp. Strain HYA002 or HYA0024. The macrolide compound has excellent proliferation-inhibiting effect against a human tumor cell and therefore can be used as a novel anticancer agent.

Abstract: An object of the present invention is to provide a method, a probe, a primer, an antibody, a reagent, and a kit for assaying an action of a pladienolide derivative to a living subject. According to the present invention, there is provided a method for assaying an action of the pladienolide derivative using a decrease in gene expression level as an index.

Abstract: The invention relates to a composition containing a particulate solid, an organic or aqueous medium, and a compound with a head group derived from phosphoric acid or sulphuric acid. The invention further relates to novel compounds, and the use of the compound as a dispersant.

Abstract: The present invention concerns compounds derived from tunicates of the species Synoicum adareanum, as well as to pharmaceutical compositions comprising these compounds and methods of use. Extracts from tunicates show selective toxicity against several different cancer cell lines in the NCI 60 cell line panel. These compounds are useful in the effective treatment of cancers, particularly malignant melanomas, colon cancer, and renal cancer cell lines.

Abstract: Novel derivatives of prostaglandin compounds of the F-series (PGF), specifically macrocyclic internal 1,15-lactones of fluprostenol and related PGF analogs, such as cloprostenol or latanoprost. The novel analogs can be formulated into ophthalmic solutions and topically applied for the treatment of the increased intraocular pressure caused by glaucoma and the reduction of ocular hypertension.

Abstract: The invention relates to Iejimalides having the following formula (I) in which a, b, c, d, e, f, g, h, i, j, k, l, m, n, o, p are simple or double bonds, the continuous lines representing at least one simple bond, the dotted lines representing a possible bond. A double bond can be present but it is not necessary, and provided that a continuous line is also present, or a simple bond can be present if no other line is represented; m=0-20 and n1-n18=1, 2. The bonds can be used as chemotherapeutic agents for treating cancer.

Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it.

Abstract: A stain inhibitor, which acts to neutralise the alkali leached to the surface of a sheet of glass in the presence of water, is disclosed. The stain inhibitor comprises a compound that reacts with the water to produce an acid. The acid acts to neutralise the alkali leached to the surface of the glass. Preferably, the compound hydrolyses to produce the acid, and is an ester.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.