Abstract: The present invention relates to a process for preparing an intermediate for the preparation of eribulin mesylate with high yields, and an intermediate therefor.

Abstract: Provided is an EP2 agonist having excellent safety. A compound represented by general formula (I) (wherein all symbols are as defined in the description), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has an EP2 agonist activity and is highly safe, and is therefore useful as a medicine, particularly a therapeutic agent for diseases associated with EP2 receptors, such as immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases and cartilage injury.

Abstract: Disclosed is a method of preparing an oxa-bicycloalkene via the reaction of a cycloalkanone and an allyl alcohol compound in the presence of an organic acid, a manganese catalyst, and oxygen at a predetermined temperature.

Abstract: A compound represented by general formula (I) wherein all symbols are as defined in the specification, a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has a selective EP2 agonist activity and is highly safe, and is therefore useful as a drug, especially as a therapeutic agent for EP2 receptor-related diseases including immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases, cartilage injury and others.

Abstract: This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.

Abstract: Provided are novel ligand, a chiral metal complex including the same, and a use of the chiral metal complex for analyzing the chirality of a charged compound by 1H NMR spectroscopy. The chiral metal complex of the present invention may be used as the chiral solvating agent to conveniently analyze the optical purity of charged compounds such as various amine derivatives, carboxylic acid derivatives, cyanohydrin derivatives and charged metal complexes by 1H NMR spectroscopy.

Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.

Abstract: Intermediates of the following formulae for the preparation of lubiprostone:

Abstract: Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS.

Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.

Abstract: Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.

Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds of formula (I), which are suitable for use as herbicides.

Abstract: The present application relates to amine salts of prostaglandin analogs and their uses for the preparation of substantially pure prostaglandin analogs. Specific embodiments relate to amine salts of tafluprost and their uses for the preparation of substantially pure tafluprost.

Abstract: A method for suppressing tumorigenicity of stem cells in a mammalian subject, which comprises administering an effective amount of a fatty acid derivative and a method for suppressing tumorigenicity of stem cells of a mammalian subject, which comprises contacting said stem cell with an effective amount of a fatty acid derivative, are provided.

Abstract: Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.

Abstract: There is provided a crystalline form of Lubiprostone, termed APO-II and methods for making APO-II. APO-II is a polymorphic form of Lubiprostone.

Abstract: The present invention relates to a lubiprostone crystal, the method for the preparation thereof, and a pharmaceutical composition or kit comprising the same, as well as the use of said crystal in the preparation of a medicament for the treatment of gastrointestinal tract diseases, especially constipation. The X-ray powder diffraction pattern of said crystal comprises characteristic peaks measured at the following 2? reflection angles: 14.6±0.2°, 17.0±0.2° and 19.6±0.2°. As compared to amorphous lubiprostone, the crystal of the present invention has the advantages of relative high purity, stable properties and easy-for-storage and use.

Abstract: The object is to develop an antiprotozoal remedy having a novel mechanism of action. Provided is a compound represented by a chemical formula (1), a prodrug or a pharmaceutically acceptable salt thereof, wherein within the formula (1), R1 represents R10— of formula (4) or R20— of formula (5); R2 represents CHO—, etc.; R3 represents a hydrogen atom, CH3—C(?O)—, etc.; R4 represents a hydrogen atom, CH3—C(?O)—, etc.; each of R11 and R12 independently represents a hydrogen atom, a methyl group, etc.; R13 represents —CH2—, —CH(—OH)— or —C(?O)—; each of R21 and R22 independently represents a hydrogen atom, a methyl group, etc.; R23 represents —CH2—, —CH(—OH)— or —C(?0)—; and R24 represents a hydrogen atom, a hydroxyl group, a methyl group, etc.

Abstract: The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II): wherein, R1, R2, R3, R4, R5, R6, R7, R8, , , , R1?, R2?, R3?, and R4? are defined the same as the specification.

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: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.

Abstract: Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein.

Abstract: Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.

Abstract: New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed.

Abstract: A positive resist composition comprising (A) a compound capable of generating an acid upon irradiation with an actinic ray or radiation, (B) a resin capable of increasing the solubility in an alkali developer by the action of an acid, and (C) a compound having a specific structure, which decomposes by the action of an acid to generate an acid, a pattern forming method using the positive resist composition, and a compound for use in the positive resist composition are provided as a positive resist composition exhibiting good performance in terms of pattern profile, line edge roughness, pattern collapse, sensitivity and resolution in normal exposure (dry exposure), immersion exposure and double exposure, a pattern forming method using the positive resist composition and a compound for use in the positive resist composition.

Abstract: Provided is a method for producing a gardenia blue pigment resistant to discoloration which may occur in colored sugar-coated food or pharmaceutical products. The method for producing such a gardenia blue pigment comprises performing membrane separation using a membrane (for example, an ultrafiltration membrane) with a molecular weight cut-off of 3000 Da or larger for removal of low-molecular compounds from a solution resulting from ?-glucosidase treatment of an iridoid glycoside (for example, geniposide etc.) in the presence of a protein hydrolysate (for example, a casein protein hydrolysate), the iridoid glycoside being obtainable by extraction from fruits of Gardenia jasminoides (Rubiaceae). Also provided is a sugar-coated food or pharmaceutical product (for example, a sugar-coated tablet, a sugar-coated chewing gum, etc.) having a sugar-coating layer colored with the gardenia blue pigment obtainable by the above-described method.

Abstract: Compounds that inhibit proteolytic enzymes of Human Immunodeficiency Virus (HIV) are described. Preparation of the inhibitors, pharmaceutical compositions containing them, and uses of the compounds or compositions for the treatment of HIV infections are also described.

Abstract: Aspects of the present application relate to process for the preparation of lubiprostone.

Abstract: A method of preparing genipin-rich materials from the fruit of Genipa americana fruit for their use as a cross-linking agent and as a raw material to produce colors is disclosed. The genipin-rich materials can be used in a broad range of applications including personal care, cosmetics, dietary supplements, packaging, textiles, beverages, foodstuffs, drugs, and animal feeds.

Abstract: There is provided a crystalline form of Lubiprostone, termed APO-II and methods for making APO-II. APO-II is a polymorphic form of Lubiprostone.

Abstract: The present invention relates to a process for the preparation of cyclic enol ethers.

Abstract: Radiolabeled tracers for sulfotransferases (SULTs), their synthesis, and their use are provided. Included are substituted phenols, naphthols, coumarins, and flavones radiolabeled with 18F, 123I, 124I, 125I, or 11C. Also provided are in vivo techniques for using these and other tracers as analytical and diagnostic tools to study sulfotransferase distribution and activity, in health and disease, and to evaluate therapeutic interventions.

Abstract: The object is to develop an antiprotozoal remedy having a novel mechanism of action. Provided is a compound represented by a chemical formula (1), a prodrug or a pharmaceutically acceptable salt thereof, wherein within the formula (1), R1 represents R10— of formula (4) or R20— of formula (5); R2 represents CHO—, etc.; R3 represents a hydrogen atom, CH3—C(?O)—, etc.; R4 represents a hydrogen atom, CH3—C(?O)—, etc.; each of R11 and R12 independently represents each a hydrogen atom, a methyl group, etc.; R13 represents —CH2—, —CH(—OH)— or —C(?O)—; each of R21 and R22 independently represents eaeh a hydrogen atom, a methyl group, etc.; R23 represents —CH2—, —CH(—OH)— or —C(?0)—; and R24 represents a hydrogen atom, a hydroxyl group, a methyl group, etc.

Abstract: The present invention relates to a process for the preparation of cyclic enol ethers.

Abstract: There is provided processes for purification of Lubiprostone by formation of amine salts. Also provided are compounds of the Lubiprostone amine salt. Also provided are compositions comprising Lubiprostone and amines.

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: The disclosure describes fungal organisms and preparations useful for inhibiting infection by Xylella sp. and in the treatment of Pierce's Disease.

Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.

Abstract: It is possible to produce oseltamivir safely and stably in large quantities by using as a starting material tartaric acid, mannitol or arabinose, via dihydroxyhexenoic acid ester of the formula (4c).

Abstract: Compounds of formulas I-IV: (I), (II), (III) (IV), wherein: R1 and R4-R23 are independently selected from H and 1-3 carbon lower alkyl; and R2 and R3 are independently selected from H, 1-3 carbon lower O II alkyl, and —C—Ra, wherein Ra is 1-3 carbon lower alkyl. Pharmaceutical compositions, which include any of Compounds I-IV and a pharmaceutically acceptable carrier, methods of inducing tumor cell apoptosis by administering to a patient in need thereof an effective amount of any of Compounds I-IV, and methods for obtaining any of Compounds I-IV by extracting the compound from coral are also provided.

Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.

Abstract: The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer, and intermediates for the synthesis of such compositions.

Abstract: There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds.

Abstract: Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.

Abstract: The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II): wherein, R1, R2, R3, R4, R5, R6, R7, R8, R1?, R2?, R3?, and R4? are defined the same as the specification.

Abstract: Compounds of the general formula (formula I) in which the meanings of the substituents R1 to R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.

Abstract: The present invention provides high throughput assays for TRPM7 activity. The present invention encompasses methods and compositions for screening a sample for inhibitors of TRPM7, including methods and compositions for competitive high throughput assays.

Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.

Abstract: A positive resist composition comprising (A) a compound capable of generating an acid upon irradiation with an actinic ray or radiation, (B) a resin capable of increasing the solubility in an alkali developer by the action of an acid, and (C) a compound having a specific structure, which decomposes by the action of an acid to generate an acid, a pattern forming method using the positive resist composition, and a compound for use in the positive resist composition are provided as a positive resist composition exhibiting good performance in terms of pattern profile, line edge roughness, pattern collapse, sensitivity and resolution in normal exposure (dry exposure), immersion exposure and double exposure, a pattern forming method using the positive resist composition and a compound for use in the positive resist composition.