Abstract: A compound with anti-drug resistant bacteria activity having the following formula is disclosed. A method of preparing the compound of formula (I) is also disclosed.

Abstract: The present invention relates to Form IV of fenofibrate and its preparation methods thereof. Its X-ray powder diffraction pattern expressed as 2? angle has characteristic peaks at 14.15±0.2°, 15.94±0.2°, 16.49±0.2°, 17.45±0.2°, 20.21±0.2°, and 22.87±0.2°. The present invention also provides preparation methods of Form IV. The preparation methods are simple, easy to operate, short, and have good repeatability. The methods are also non-toxic and non-polluting by using water as a medium and using a pharmaceutically accepted excipient, such as polyvinylpyrrolidone or polyvinyl alcohol as an inducer. The results of stability experiments (light exposure, high humidity and grinding) and solubility tests show that Form IV is stable and has a higher solubility than the prior art crystal form.

Abstract: Provided herein are curcumin analogues that are able to interact with amyloid beta (A?) and to attenuate the copper-induced crosslinking of A?. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

Abstract: The subject invention pertains to myricanol derivatives, therapeutic compositions, and methods for treatment of neurodegenerative diseases, in particular, neurodegenerative diseases associated with abnormal accumulation of protein tau.

Abstract: Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.

Abstract: There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.

Abstract: Disclosed herein are compounds, compositions and methods for preventing and treating diseases such as intracerebral hemorrhage, cancer, or conditions associated with damaged cells, activated lymphocytes, or microbial products. The disclosed compounds are curcumin analogs. The curcumin analogs possess anti-inflammatory and antioxidant properties, which in part, reduce AP-1 and NF-?B activity.

Abstract: In order to provide a novel method for producing a cyclopentanone compound, the present invention is a method for producing a cyclopentanone compound represented by the formula (I). The method includes the steps of: substituting the group represented by Y by a hydrogen atom by allowing a compound represented by the formula (III) or an intermediate compound obtained from the compound represented by the formula (III) to react with a catalyst or a halogenating agent; and substituting, by hydrogen atoms, (i) the group or the atom represented by Z1 and (ii) the group or the atom represented by Z2, by reducing the compound represented by the formula (III) or the intermediate compound obtained from the compound represented by the formula (III).

Abstract: Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: wherein R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.

Abstract: The presently disclosed subject matter provides methods of preparing synthetic prostacyclin analogues, including Beraprost, either as racemic mixtures or as single stereoisomers. Also provided are novel synthetic intermediates for use in these methods.

Abstract: According to the invention there is provided a compound of formula (I): wherein R1, R2, R3 and n have meanings given in the description, or a pharmaceutically acceptable solvate, salt or prodrug thereof for use in the treatment of osteoporosis and/or osteopenia.

Abstract: Substituted phenacyl molecules are provided and employed to create molecules and polymers/copolymers that exhibit photoresponsiveness. In some instances, the substituted phenacyl molecule is incorporated into the polymer/copolymer backbone, and photoirradiation of the polymer/copolymer causes the substituted phenacyl group to break down and the polymer/copolymer to undergo degradation. In other instances, the substituted phenacyl molecules extend as a side chain from the polymer/copolymer backbone. In yet other instances the substituted phenacyl molecules extend as a side chain from the polymer/copolymer backbone, and a drug or polymer additive is linked to the photoresponsive substituted phenacyl group such that photoirradiation releases the drug or additive. In yet other embodiments the substituted phenacyl molecules extend as a side chain from the polymer/copolymer backbone, and serve to link the polymer/copolymer to another polymer/copolymer backbone, and photoirradiation breaks the links.

Abstract: The present invention relates to a novel process for the preparation of a compound of formula (I) wherein R is a methyl or methoxy group; to certain novel intermediates prepared in such a process and their use.

Abstract: The invention provides an acid addition salt of a compound of the formula (1). Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogues thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analogue.

Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

Abstract: An azole derivative according to the invention is represented by Formula (I), wherein each of Ra and Rb denotes a hydrogen atom, or a C1-C6 alkyl group, a C2-C6 alkenyl group or a C2-C6 alkynyl group; Ra and Rb may be substituted with Xa or Xb which is a halogen atom; each of na and nb denotes 0 or the number of Xa- or Xb-substituted hydrogen atoms among the hydrogen atoms in Ra or Rb; each Y denotes a halogen atom, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy group, a C1-C4 haloalkoxy group, a phenyl group, a cyano group or a nitro group; m denotes 0 to 5; and A denotes a nitrogen atom or a methyne group. As a result, an azole derivative contained as an active ingredient in an agro-horticultural agent having an excellent controlling effect on diseases can be provided.

Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract: An azole derivative according to the invention is represented by Formula (I), wherein each of Ra and Rb denotes a hydrogen atom, or a C1-C6 alkyl group, a C2-C6 alkenyl group or a C2-C6 alkynyl group; Ra and Rb may be substituted with Xa or Xb which is a halogen atom; each of na and nb denotes 0 or the number of Xa- or Xb-substituted hydrogen atoms among the hydrogen atoms in Ra or Rb; each Y denotes a halogen atom, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy group, a C1-C4 haloalkoxy group, a phenyl group, a cyano group or a nitro group; m denotes 0 to 5; and A denotes a nitrogen atom or a methyne group. As a result, an azole derivative contained as an active ingredient in an agro-horticultural agent having an excellent controlling effect on diseases can be provided.

Abstract: A method for synthesizing (phenylalkyloxy)phenyl-oxobutanoic acid compounds is described. The corresponding (phenylalkyloxy)acylphenyl compound is halogenated, giving the alpha haloketone. The halide is displaced by the anion of a di-alkyl malonate to give a substituted malonic ester. Hydrolysis of the ester and decarboxylation of the diacid gives the desired product.

Abstract: In order to provide a novel method for producing a cyclopentanone compound, the present invention is a method for producing a cyclopentanone compound represented by the formula (I). The method includes the steps of: substituting the group represented by Y by a hydrogen atom by allowing a compound represented by the formula (III) or an intermediate compound obtained from the compound represented by the formula (III) to react with a catalyst or a halogenating agent; and substituting, by hydrogen atoms, (i) the group or the atom represented by Z1 and (ii) the group or the atom represented by Z2, by reducing the compound represented by the formula (III) or the intermediate compound obtained from the compound represented by the formula (III).

Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.

Abstract: The present invention provides efficient, economical and environmental friendly methods for synthesis of prostaglandin analogs including tafluprost and intermediates thereof. The invention involves a selective oxidation using in situ boronate ester protection and a unique crystallization method to remove the undesired isomers of fluorinated intermediates.

Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

Abstract: An inhibitor of endothelin action or a skin-whitening agent, comprising a compound represented by Formula (1) or a salt thereof as an active ingredient. wherein in Formula (1), R1 represents a formyl group or an alkyl group having 1 to 4 carbon atom(s), and R2 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atom(s).

Abstract: Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.

Abstract: The invention provides novel phenylglyoxylic acid derivatives, which may be useful as intermediates for preparing stereoisomerically enriched drug compounds. The invention also provides methods of making phenylglyoxylic acid derivatives, and uses of phenylglyoxylic acid derivatives.

Abstract: Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents —CHO, —C(?O)R5, —COOR5 (wherein R5 represents a C1-7 alkyl group), —CH2OH or —COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I or a pharmaceutically acceptable salt thereof. In Formula I m is 0, 1, 2, 3 or 4; n is 0 or 1; m+n is not more than 4; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R6 is hydrogen, methyl or ethyl and R12 is hydrogen or methyl, or R6 is hydroxy and R12 is hydrogen, or R6 is O and R12 is absent, or R6 and R12 together are —CH2CH2—. R7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R8 and R9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R11) wherein R11 is hydrogen or alkyl having from 1 to 3 carbon atoms.

Abstract: A polymerizable photoinitiator is represented by Formula (I): wherein R1, R2 and R3 are independently selected from the group consisting of a hydrogen, an optionally substituted alkyl group and an optionally substituted aryl group or R1 and R3 represent the necessary atoms to form a five to eight membered ring; p, w, y and z are all integers with y representing a value 1 to 6; p representing the sum of w and z; p representing a value of 1 to 6; w=1 to (p?z) and z=0 to (p?w); L represents an optionally substituted (p+y)-valent linking group comprising 1 to 14 carbon atoms; A represents a radically polymerizable group selected from the group consisting of an acrylate group, a methacrylate group, a styrene group, an acryl amide group, a methacryl amide group, a maleate group, a fumarate group, an itaconate group, a vinyl ether group, an allyl ether group, an allyl ester group and a vinyl ester group; and X represents a photoinitiating moiety including at least one group capable of initiating a free radical p

Abstract: The invention relates to methods for producing chalcone (1,3-diphenylprop-2-en-1-one) derivatives that have multiple substitutions on a phenyl ring. Intermediate chalcone derivatives are modified by Phase Transfer Catalysis (PTC) for introducing a substituted alkyl group that is provided by a sulfonic acid derivative on a phenyl ring already containing substituent groups on one or two carbon atoms adjacent to the carbon atom where a substituent group is being introduced. The methods of the invention allow producing efficiently, by either S-alkylation or O-alkylation, chalcones derivatives that are characterized for their biological activities that are intermediate compounds for producing molecules having such activities, or that can be used for generating libraries of compounds to be screened by means of in vitro and/or in vivo assays and establishing structure-activity relationships.

Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

Abstract: According to the invention there is provided a compound of formula (I): wherein R1, R2, R3 and n have meanings given in the description, or a pharmaceutically acceptable solvate, salt or prodrug thereof for use in the treatment of osteoporosis and/or osteopenia.

Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.

Abstract: Esters of 4,5-disubstituted-oxy-2-methyl-3,6-dioxo-cyclohexa-1,4-dienyl alkyl acids were prepared chemically and/or enzymatically. Depending upon the ester, improved melanocyte cytotoxicity was achieved. Improved cytotoxicity characteristics are consistent with ester analogs being more physiologically compatible and less irritating to skin than their corresponding acids.

Abstract: A bis(formylphenyl) compound expressed by general formula (2) is useful as a photo-sensitive resist material:

Abstract: A benzophenone compound is represented by the following formula (I): (A)n-X—(B)m??(I) wherein X is an organic moiety having (n+m) valence, (n+m) being an integer ranging from 1 to 4; A is B is R is H or a methyl group; n is the number of A bonded to X and is an integer ranging from 1 to 4; and m is the number of B bonded to X and is an integer ranging from 0 to 3.

Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.

Abstract: Disclosed is the use of benzotropolone derivatives of formula (1), wherein R1, R2 and R7 independently from each other are hydrogen; C1-C3alkyl; or COR8; R3 is hydrogen; or COOR9 R4 is hydrogen; or C1-C3alkyl; R5 is hydrogen; hydroxy; C1-C3-alkoxy; or -0-(CO)—R10; R6 is hydrogen; C1-C3alkyl; or COR8; or R5 and R6 together may form a five or six membered ring; or R6 and R7 together form a five or six membered ring; and R8, R9, R10 independently of each other are C1-C30alkyl; for protecting body-care and household products from photolytic and oxidative degradation.

Abstract: An azole derivative according to the invention is represented by Formula (I), wherein each of Ra and Rb denotes a hydrogen atom, or a C1-C6 alkyl group, a C2-C6 alkenyl group or a C2-C6 alkynyl group; Ra and Rb may be substituted with Xa or Xb which is a halogen atom; each of na and nb denotes 0 or the number of Xa- or Xb-substituted hydrogen atoms among the hydrogen atoms in Ra or Rb; each Y denotes a halogen atom, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy group, a C1-C4 haloalkoxy group, a phenyl group, a cyano group or a nitro group; m denotes 0 to 5; and A denotes a nitrogen atom or a methyne group. As a result, an azole derivative contained as an active ingredient in an agro-horticultural agent having an excellent controlling effect on diseases can be provided.

Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.

Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.

Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: A method for synthesis of secondary alcohols is provided for pharmaceutical secondary alcohol by addition of organoboronic acids with aldehydes in presence of the cobalt ion and bidentate ligands as the catalyst. In addition, an enantioselective synthesis method for secondary alcohols is also herein provided in the present invention. The present invention has advantages in using less expensive cobalt ion and commercially available chiral ligands as the catalyst, wide scope of organoboronic acids and aldehydes compatible with this catalytic reaction and achieving excellent yields and/or enantiomeric excess.

Abstract: A trifluoromethylthiophenium derivative salt useful as synthetic intermediates for pharmaceuticals and agrochemicals, a method for producing the same, and a method for producing trifluoromethyl-containing compounds using the same are provided. An S-(trifluoromethyl)-benzo[b]thiophenium derivative salt is represented by the following general formula (1): wherein R1, R2, R3, and R4 are each independently a hydrogen atom, a methyl group, an ethyl group, a linear, branched, or cyclic alkyl group having 3 to 10 carbon atoms, a methoxy group, an ethoxy group, a linear, branched, or cyclic alkyloxy group having 3 to 10 carbon atoms, a fluorine atom, a chlorine atom, a bromine atom, a nitro group, or a cyano group, R5 is a methyl group, an ethyl group, a linear, branched, or cyclic alkyl group having 3 to 10 carbon atoms, a phenyl group, or a substituted phenyl group, and X? represents an anion.

Abstract: This invention relates to caffeic acid derivatives and improving viability of neuronal cells by contacting neuronal cells by caffeic acid derivatives as shown in the specification.

Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract: The present invention relates to a process for preparing a prostaglandin derivative and an intermediate therefor. In accordance with the present invention, the prostaglandin F (PGF) derivative can be efficiently prepared with high purity by removing the protecting group of a protected prostaglandin E (PGE) derivative obtained from conjugate addition and then stereoselectively reducing the ketone group on the cyclopentanone ring of the PGE derivative.

Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.

Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.