Abstract: Nitroderivatives of prostaglandin amides having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.

Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.

Abstract: Provided herein are catalysts useful in enabling and promoting the insertion of alkylene oxides into ester linkages. The esters employed as a substrate to be alkoxylated include esters of fatty acids, such as methyl esters of C14 to C22 fatty acids, and mono-, di-, and tri-esters of glycerine, including vegetable oils, animal fats, and plant oils. A catalyst according to the invention includes at least two alkaline earth compounds, which may include any known stable compounds of the alkaline earths, and optionally contains one or more additional materials such as a carboxylic acid or a polyalkylene glycol having a molecular weight between about 100 and 1500 or a C1-C10 alkyl-capped polyalkylene glycol having molecular weight between about 100 and 1500, which has been acidified with a strong mineral acid. The preferred alkaline earths employed are salts and compounds of magnesium and calcium.

Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6alkyl or C1-C6alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R8 and R9 are each independently hydrogen atom, C1-C6alkyl, —CON(R18)(R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

Abstract: Compounds of the formula I or I?, where the radicals R1 are each, independently of one another, a hydrogen atom or C1-C4-alkyl and R?1, is C1-C4-alkyl; X1 and X2 are each, independently of one another, a sec-phosphino group; R2 is hydrogen, R01R02R03Si— is halogen-, hydroxyl-, C1-C8-alkoxy- or R04R05N-substituted C1-C18-acyl or is R06—X01—C(O)—; R01, R02 and R03 are each, independently of one another, C1-C12-alkyl, unsubstituted or C1-C4-alkyl- or C1-C4-alkoxy-substituted C6-C10-aryl or C7-C12-aralkyl; R04 and R05 are each, independently of one another, hydrogen, C1-C12-alkyl, C3-C8-cycloalkyl, C6-C10-aryl or C7-C12-aralkyl, or R04 and R05 together are trimethylene, tetramethylene, pentamethylene or 3-oxapentylene; R06 is C1-C18-alkyl, unsubstituted or C1-C4-alkyl- or C1-C4-alkoxy-substituted C3-C8-cycloalkyl, C6-C10-aryl or C7-C12-aralkyl; X01 is —O— or —NH—; T is C-bonded C3-C20-heteroarylene; v is 0 or an integer from 1 to 4; X1 in the heteroring of the heteroarylene is bound in the ortho position relative

Abstract: Disclosed are methods for identifying individuals suffering from a CNS disorder (including Alzheimer's Disease, behavioral disorders, and the like) that could be treated with a CNS drug with greater therapeutic efficacy and lower side effects and the compounds useful for such treatment. Also disclosed are methods for predicting the efficacy of a drug candidate for the treatment of a CNS disorder. The technology is also applicable to drug discovery for use in animal models of neurodegenerative diseases.

Abstract: Disclosed herein are compounds of the formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present application provides intermediates for preparing prostaglandin analogues and processes for preparing prostaglandin analogues and intermediates thereof. The intermediates include: A compound of formula (6): R1 represents H, C1-C5-alkyl, or benzyl, in particular isopropyl.

Abstract: A transesterification process for the preparation of tetrakis [3-(3,5-di-tert-butyl-4-hydroxy phenyl)propionyl oxymethyl] methane by the reaction of methyl-(3,5-di-tert-butyl-4-hydroxy phenyl)propionate ester with pentaerythritol wherein the reaction takes place in the presence of an ester exchange catalyst combination consisting of (a) at least one basic or neutral catalyst and (b) at least one metal compound capable of behaving as a Lewis acid and wherein the reaction is conducted through a first stage in which only basic or neutral catalyst is present in the reaction mixture followed by a second stage which commences with the addition of Lewis acid catalyst to the reaction mixture when the amount of di-substituted intermediate product contained within the reaction mixture is less than 20 area % analyzed by HPLC. The preferred basic catalysts are lithium hydroxide and lithium hydroxide monohydrate. The preferred Lewis acid catalyst is zinc octanoate.

Abstract: A herbicidal compound and composition comprising at least one compound of formula I wherein R is independently selected from hydrogen, and the group (CH2)mOR4; m, q, t and v are independently zero or one; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen, lower alkyl (preferably C1 to C4 alkyl) and lower acyl (preferably C2 to C4 acyl) and the group of formula II wherein the compound of formula I comprises at least one group R1, R2, R3 and R4 which is of formula II wherein A is N or CH; X is selected from the group consisting of chloro, amino, methyl and methoxy; X1 is selected from the group consisting of hydrogen, chloro and methyl; X2 is hydrogen or chloro; R1 is selected from hydrogen and methyl; Y is oxygen or a bond; and n is from 0 to 3.

Abstract: Compounds of general formula I: wherein: R1 and R2 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, optionally substituted —CO—(C1-10alkyl), optionally substituted C3-10cycloalkyl, optionally substituted —CO—(C3-10cycloalkyl), optionally substituted C2-10alkenyl, optionally substituted —CO—(C2-10alkenyl), optionally substituted aryl, and optionally substituted —CO-aryl, or R1 and R2 together represent an optionally substituted saturated or unsaturated C1-10alkylidene group, or an optionally substituted saturated or unsaturated C3-10cycloalkylidene group, or R1 and R2 together with the carbon atom to which they are attached represent an optionally substituted saturated or unsaturated organic ring containing 3, 4, 5, 6, 7 or 8 ring carbon atoms and optionally 1, 2 or 3 ring heteroatoms selected from O, N and S; R3, which may be the same as, or different from, either of R1 and R2, is selected from optionally substituted C1-10alkyl, optionally substituted C3-10cycl

Abstract: The present invention relates to novel compounds of formula (I) and to the salts, solvates and prodrugs thereof, wherein the meanings of the various substituents are as disclosed in the description. Said compounds are useful for the treatment or prevention of psoriasis and other immune diseases.

Abstract: Aspirin (ASA) triggers a switch in the biosynthesis of lipid mediators, inhibiting prostanoid production and initiating 15-epi-lipoxin generation, through the acetylation of cyclooxygenase II.

Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6alkyl or C1-C6alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R8 and R9 are each independently hydrogen atom, C1-C6alkyl, —CON(R18)(R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

Abstract: The present invention relates to an improved process for the preparation of phenolic carboxylic acid derivatives catalysed by biocatalytic esterification, transesterification or amidation of a corresponding lower alkyl ester. Biocatalysis is performed in the presence of suitable enzymes, e.g. hydrolases, especially esterases, amidases, lipases and proteases.

Abstract: The present invention concerns a method for preparation of fispemifene by use of ospemifene as a starting material.

Abstract: The invention relates to novel spirocyclic 3?-alkoxytetramic acids and -tetronic acids of the formula (I), in which A, B, D, Q1, Q2, G, W, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides, and also to selective herbicidal compositions comprising firstly the spirocyclic 3?-alkoxytetramic acids and -tetronic acids and secondly at least one compound which improves crop plant tolerance.

Abstract: Disclosed are Compounds of formula I And methods of use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes.

Abstract: Carbonyl compounds of the formula (II), wherein R1 and R2 are as defined herein, react in the presence of an amine with carboxylic acid derivatives of the formula (II), wherein R3 and EWG are also as defined herein, to give ?,?-unsaturated compounds of the formula (I) according to the following scheme: It is possible under mild reaction conditions to obtain unsaturated esters with high (E) stereoselectivity. The reaction typically proceeds at room temperature or lower without particular requirements such as inert gas, exclusion of moisture, heat, etc., being made. The only by-products obtained are CO2 and water.

Abstract: The present compound represented by formula(I) CH2?CR1—COO—(L)k-E1-E2-E3-(E4)m-(E5)n-R2??(1) provided that the symbols in the formula have the following meanings: R1: a hydrogen atom or a methyl group; R2: a C1-8 alkyl group; L: —(CH2)pO—, —(CH2)q—, -Cy-COO— (Cy is a trans-1,4-cyclohexylene group), -Cy-OCO—, -E6-(CH2)2—, -E7-CH2O— or -E8-O— (wherein each of p and q which are independent of each other, is an integer of from 2 to 8); E1, E2, E3 E4, E5, E6, E7, E8: each independently a 1,4-pheneylene group or a trans-1,4-cyclohexylene group (provided that at least one of E1, E2 and E3 is a trans-1,4-cyclohexylene group, and in a case where L is -Cy-OCO—, E1 is a trans-1,4-cyclohexylene group),and k, m, n: each independently 0 or 1, provided that when k is 1 and L is -Cy-COO—, -Cy-OCO—, -E6-(CH2)2—, -E7-CH2O— or -E8-O—, at least one of m and n is 0. The present compound is useful for liquid crystal composition and optical element.

Abstract: The present invention relates to compounds of the general formula I in which the variables are each defined as follows: Z1, Z2 are each independently hydrogen, optionally substituted C1-C20-alkyl in which the carbon chain may be interrupted by oxygen atoms in ether function, sulfur atoms in thioether function or by nonadjacent imino or C1-C4-alkylimino groups, or reactive radicals by means of which polymerization can be brought about, A1, A2 are each independently spacers having from 1 to 30 carbon atoms, in which the carbon chain may be interrupted by oxygen atoms in ether function, sulfur atoms in thioether function or by nonadjacent imino or C1-C4-alkylimino groups, Y1, Y2 are each independently a chemical single bond, oxygen, sulfur, —CO—, —O—CO—, —CO—O—, —S—CO—, —CO—S—, —NR—CO— or —CO—NR—, Y3, Y4 are each independently a chemical single bond, oxygen, sulfur, —CR?CR—, —C?C—, —CR?CR—CO—O—, —O—CO—CR?CR—, —C?C—O—, —O—C?C—, —CH2—CH2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, —CO—, —O—CO—, —CO—O—, —S—CO—, —C

Abstract: Compounds of the formula (I): in which R1, R2, R3, R?3 and R4 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, the pharmaceutical compositions comprising them, and the processes for the preparation of these compounds.

Abstract: The present invention relates to a method of preparing a phenoxy alkanoic, alkenoic, or alkynoic acid or a salt thereof from a phenoxy containing compound via a dicarboxylate intermediate. The phenoxy alkanoic, alkenoic, and alkynoic acids and salts thereof prepared by this method are suitable for use in composition for delivering active agents via oral or other routes of administration to animals. Furthermore, the present invention relates to phenoxy dicarboxylic acids and their salts for delivering active agents, such as biologically or chemically active agents, to a target.

Abstract: The invention relates to substituted para-trifluoromethyl phenyl ether compounds and its preparation and use thereof especially. The substituted para-trifluoromethyl phenyl ether compounds of the invention having general formula (I): The substitutes see Description. The compounds of present invention have broad-spectrum activity, and may be used to control diseases in all sorts of plants caused by oomycete, basidiomycete, ascomycete pathogens and deuteromycete, and it may also provide good control efficacy at very low dosage because of the high activity. The compounds of the invention have good insecticidal activity and have good activity against many pests, especially for Carmine spider mite. The compounds are fit for synthetical control against many kinds of pests.

Abstract: Novel derivatives of fumagalone have the general formula (I): and are useful angiogenes is inhibitors; these can be formulated into pharmaceutical compositions suited for human or veterinary medicine, or can be formulated into cosmetic compositions.

Abstract: The invention relates to a process for the preparation of ferutinine (Ia) from Ferula spp extracts comprising basic hydrolysis of the extracts and treatment with p-pivaloyloxybenzoic acid.

Abstract: The invention relates to new chemical compounds that inhibit the various enzymes in the arachidonic acid pathway implicated in inflammatory disease conditions.

Abstract: The compound represented by the following formula (1): wherein A, B, R1, R2, R3 and Z are as defined in the specification is analogous to shogaol and gingerol useful in the fields of foods, medicines, quasi-drugs, cosmetics, etc., and more highly active in tyrosinase activity inhibition, etc. than shogaol and gingerol.

Abstract: The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, for use in the treatment or prophylaxis of condition mediated by an androgen receptor.

Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.

Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.

Abstract: The invention provides a process for preparing R-(+)-2-(4-hydroxyphenoxy)-2-methyl-butyric acid methyl ester of the formula (I): Various embodiments and variants are provided. The invention also provides a process for preparing S-(?)-2-(4-hydroxyphenoxy)-2-methyl-butyric acid methyl ester of the formula (II) Various embodiments and variants are provided.

Abstract: A compound represented by formula I is used as a marker for organic products. wherein Ar1 and Ar2 each independently represent a substituted or unsubstituted phenylene group or a substituted or unsubstituted naphthylene group; R1 represents a straight or branched chain alkyl group having 1 to 22 carbon atoms; R2 represents a hydrogen atom or a group of the formula C(O)R4 where R4 is a hydrogen atom or a straight or branched chain alkyl group having 1 to 22 carbon atoms; and R3 represents a hydrogen atom, a straight or branched chain alkyl group having 1 to 12 carbon atoms, a straight or branched chain alkoxy group having 1 to 12 carbon atoms, a hydroxyl group, or a substituted or unsubstituted phenyl group or a substituted or unsubstituted naphthyl group; and Z represents a hydrogen atom or a group of atoms that combine with Ar2 or R3 to form a lactone ring.

Abstract: A retardation plate having a high film strength and having an optical property is provided by using a biaxial liquid crystal compound, in which the direction having a minimum refractive index of the optically anisotropic thin layer almost coincides with the normal direction in the film plane of the retardation plate, and the retardation plate comprises a transparent support and at least one optically anisotropic layer containing a liquid crystal compound capable of expressing a biaxial liquid crystal phase, wherein the liquid crystal compound is a polymerizable compound and/or a polymer compound.

Abstract: Methyl (R)-2-(R1OSO2)-2-(2-chlorophenyl)acetates useful as intermediates in the preparation of methyl (S)-2(2-chlorophenyl)-2-(4,5,6,7-tetrahydrothieno[3,2-c]-5-pyridyl)acetate.

Abstract: A method of increasing helical twisting power (HTP) in an optically active compound used in a liquid crystal material is provided. An optically active compound which exhibits a large HTP value is also provided. Furthermore, a liquid crystal composition which exhibits a high upper temperature limit of the liquid crystal after the addition of the optically active compound, and a liquid crystal display device using the same are provided. In a method, an HTP of a compound having a partial structure represented by formula (A), which has an asymmetric carbon atom, is increased by replacing the partial structure represented by formula (A) by a partial structure represented by formula (B) (wherein * represents the position of an asymmetric carbon atom, Y1 represents a substituent such as an alkyl group and a halogen).

Abstract: The present invention provides a method of preparing a phosphonium salt of the formula [R1R2R3P—CR4R5R6]X, comprising ball-milling a phosphine of the formula R1R2R3P with a compound of the formula XCR4R5R6; a method of preparing a phosphorus ylide of the formula R1R2R3P?CR4R5, comprising ball-milling a phosphonium salt of the formula [R1R2R3P—HCR4R5]X in the presence of a base; and a method of preparing an olefin of the formula R4R5C?CR7H or R4R5C?CR7R8, comprising ball-milling a phosphorus ylide of the formula R1R2R3P?CR4R5 with a compound of the formula R7C(O)H or R7C(O)R8. The inventive method produces phosphonium salts and phosphorus ylides by mechanical processing solid reagents under solvent-free conditions.

Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?

Abstract: Demethylation of 3?, 4?-dimethoxy or 3?, 4?, 5?-trimethoxy benzoic ester of a phenol is carried out in the presence of an excess of aluminum halide in an organic solvent to get 4?-Hydroxy, 3?-methoxy or 4? hydroxy, 3?, 5?-dimethoxy benzoic acid ester of a phenol. The reaction is also applicable to 3?, 4?, 5?-trimethoxy diaryl ketone and some natural products like reserpine.

Abstract: An object of present invention is to provide a diamine and an acid dianhydride having photoreactivity and thermoreactivity and a polyimide composition containing the diamine and the acid dianhydride as monomer components, and specifically to synthesize a diamine and an acid dianhydride having a photoreactive and thermoreactive group containing a double bond or triple bond such as cinnamic acid, chalcone, benzalacetophenone, stilbene, coumarin, pyrone, allyl, propargyl, and acetylene or a derivative skeleton thereof so as to exhibit photoreactivity and thermoreactivity specific to the reactive group, thereby providing a polyimide composition containing the diamine and the acid dianhydride.

Abstract: Ibuprofen-aspirin compounds useful in treating aspirin or ibuprofen-treatable conditions, hydroxymethylacylfulvene analogs useful as antitumor drugs, and L-sugar illudin analogs useful as antitumor drugs.

Abstract: The first aspect of the present invention relates to a photo-activated pro-accord conjugate having the formula: wherein [PHOTO] is a photo-labile unit which upon exposure to electromagnetic radiation is capable of releasing a pro-accord unit; X is selected from oxygen, nitrogen, sulfur; R1 and R2 are moieties when taken together comprise an aldehyde or a ketone fragrance raw material, and R3 comprises hydrogen, a fragrance raw material alcohol, an amine, or a thio compound.

Abstract: The present invention discloses reworkable epoxy compositions suitable for encapsulation of and underfill for electronic components including (a) the epoxidized reaction product of a multifunctional 1-alkenyl ether or 1-cycloalkenyl ether and an alkenyl carboxylic acid, the epoxidized reaction product having two or more thermally labile alpha-alkoxy ester linkages; and (b) a curing agent for the epoxy component. The epoxy composition, when cured, provides a composition which is thermally reworkable, the weak ?-alkoxy ester linkages providing for the reworkable aspect of the invention.

Abstract: Methyl (R)-2-(R1OSO2)-2-(2-chlorophenyl)acetates useful as intermediates in the preparation of methyl (S)-2(2-chlorophenyl)-2-(4,5,6,7-tetrahydrothieno[3,2-c]-5-pyridyl)acetate.

Abstract: A ferulic acid derivative represented by the general formula (1); a process for preparing a ferulic acid derivative represented by the general formula (1), comprising reacting ferulic acid or an ester thereof represented by the general formula (2) with a dihalomethane represented by the general formula CH2X2, wherein X is a halogen atom; and an ultraviolet light-absorbent composition comprising the ferulic acid derivative. Since the ultraviolet light absorbent composition is not only excellent in the ultraviolet light absorption but also very stable against heat, the ultraviolet light absorbent composition can be suitably used as cosmetics which especially require long-term stability.

Abstract: Compounds of formula (I), wherein R1 and R2 are, independently of one another, H,C1-C6alkyl, C1-C6halogenalkyl, C1-C6alkoxyl, C1-C6alkoxy-C1-C6alkyl, or C1-C6alkoxy-C1-C6alkyloxy, and R3 is C1-C6alkyl, are obtainable in high yiedls by stereoselective addition of R3-substituted propionic acid esters to R1- and R2-substituted benzaldehydes of formula R—CHO to form corresponding 3-R-3-hydroxy-2-R3-propionic acid esters, conversion of the OH group to a leaving group, subsequent regioselective elimination to form 3-R-2-R3-propenic acid esters, and reduction to corresponding 3-R-2-R3-allyl alcohols and their enantioselective hydrogenation, wherein R is (a).

Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.

Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-? by adipose tissue.

Abstract: A novel norbornene derivative represented by a general formula (1m) shown below is provided. By conducting a ring opening polymerization of this norbornene derivative, or by performing a subsequent hydrogenation following the ring opening polymerization, a ring opening polymer or a hydrogenated product thereof with an excellent low birefringence can be obtained. [wherein, at least one of R1 to R4 is a group selected from the group consisting of groups represented by a general formula (1-1) shown below and groups represented by a general formula (1-2) shown below] [wherein, at least one of RA, RB and Z is a group represented by the formula —C(O)O—].