Abstract: Substantially pure preparations of phosphosesquiterpenes are described. The compounds inhibit farnesyl-protein transferase activity and are useful for the treatment of cancer. Methods for inhibiting farnesyl-protein transferase activity are also described.

Abstract: This invention relates to the use of EP2 receptor subtype selective prostaglandin E2 agonists to augment bone mass including the prevention and treatment of skeletal disorders in mammals, including humans.

Abstract: Provided is a process for producing an isocoumarin-3-yl-acetic acid derivative, characterized by reacting a homophthalic acid derivative represented by a formula: (wherein Rc, R2 and R are mainly protecting groups) with a malonic acid derivating represented by a formula: (wherein R is an organic group including a lower alkyl group; R3 is a protecting group for a carboxyl group; and X is a halogen atom or a —OM group (wherein M is alkaline metal or alkaline earth metal)). According to the above process, various isocoumarin-3-yl-acetic acid derivatives can efficiently be provided.

Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, X, Y and the dashed line are as defined in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use as psychotherapeutic agents.

Abstract: A method and composition for preserving or enhancing the beneficial effects of interleukin-2 (IL-2) while simultaneously mitigating the adverse effects of IL-2 on a subject is disclosed. The method involves administering an amount of a leukotriene B4 (LTB4) antagonist, preferably a LTB4 receptor antagonistic, to a subject exhibiting adverse pharmacological effects due to exogenous IL-2, where the amount administered to the subject is sufficient to decrease the IL-2 induces adverse effects. Also disclosed is an article of manufacturing comprising a composition of the leukotriene B4 antagonist in combination with labeling instructions for treatment. Also disclosed is a method for preparing a pharmaceutical composition. Generally the LTB4 antagonist will reduce the IL-2-induced adverse effects while preserving or enhancing the antitumor, antiviral, or immunostimulatory effects of IL-2, thereby improving the therapeutic index of IL-2.

Abstract: A method for making a vinyl carbonate represented by the formula (I): CH2═CHOC(O)X1R1  (I) wherein X1 is oxygen or sulfur and R1 is a substituted or an unsubstituted aliphatic alkyl, aryl, aryl alkyl, olefinic, vinyl, or cycloaliphatic group comprises: (a) reacting a compound represented by the formula (II): X2C(O)X1R1  (II)  wherein X2 is a halogen other than fluorine, with a compound represented by the formula (III): M1-F  (III)  wherein M1 is selected from a Group IA metal, in the presence of a first phase transfer catalyst and a first organic solvent, to form a compound represented by the formula (IV): FC(O)X1R1;  (IV)  and (b) reacting a compound represented by the formula (IV) with a compound represented by the formula (V): CH2═CHOSi(R2)3  (V)  wherein R2 is a substituted or an unsubstituted aliphatic alkyl, aryl, aryl alkyl, olefinic, vinyl, or cycloaliphatic group, or any combination thereof, in the presence of

Abstract: Disclosed and claimed are cocoa extracts, compounds, combinations thereof and compositions containing the same, such as polyphenols or procyanidins, methods for preparing such extracts, compounds and compositions, as well as uses for them, especially a polymeric compound of the formula An, wherein A is a monomer of the formula: wherein n is an integer from 2 to 18, such that there is at least one terminal monomeric unit A, and one or a plurality of additional monomeric units; R is 3-(&agr;)-OH, 3-(&bgr;)-OH, 3-(&agr;)-O-sugar, or 3-(&bgr;)-O-sugar.

Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.

Abstract: A compound of the formula: or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined above are useful as ORL1-receptor agonists, and useful as analgesics or the like in mammalian subjects.

Abstract: A process for preparing compounds of the formula IIb  where R is C6-C30-alkyl or C6-C30-alkenyl, which may additionally have upto 5 hydroxyl groups, formyl groups, C1-C4-alkoxy groups, phenoxy groups or C1-C4-alkoxycarbonyl groups as substituents and may be interrupted by upto 5 nonadjacent oxygen atoms, or alkoxylate groups of the formula —(CH2)k—O—(A1O)m—(A2O)n—Y where A1 and A2 are, independently of one another, 1,2-alkylene groups having 2 to 4 carbon atoms, Y is hydrogen, C1-C12-alkyl, phenyl or C1-C4-alkoxycarbonyl, and k is 1, 2 or 3, and m and n are each numbers from 0 to 50, and the total of m+n must be at least 4, by reacting iminodiacetonitrile with aldehydes of the formula R—CHO and HCN or alkali metal cyanides, the process being carried out a) in the absence of an organic solvent and in the presence of a Lewis or Brönsted acid, or b) in the presence or absence of an organic solvent and in the presence of an emulsifier, or c)

Abstract: L-Ascorbic acid 2-phosphate zinc salt and a salt hydrate thereof having excellent solubility and exhibiting good stability even under weakly acidic conditions. Also disclosed is a process of manufacturing L-ascorbic acid 2-phosphate zinc salt by displacing a cation of a salt of an L-ascorbic acid 2-phosphate other than a zinc salt with a zinc cation. Further disclosed is a composition containing L-ascorbic acid 2-phosphate zinc salt or a salt hydrate thereof as an active ingredient.

Abstract: This invention provides processes for the preparation of a compound of Formula I: Y—C(═O)—C(R1)(R2)—CH2—S(O)nR3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R1 is hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R3 is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.

Abstract: New phosphonamide compounds and methods of forming those compounds are provided. In one embodiment, the inventive methods comprise subjecting an opened-ring phosphonamide template to a ring-closing metathesis reaction in the presence of a ring-closing catalyst (e.g., a Grubbs catalyst) to yield a phosphonamide. In another embodiment, the inventive methods comprise reacting a template structure with a phosphorus (III) compound to yield the phosphonamide. Advantageously, in either embodiment, the template structures can be provided with a wide array of functional groups (e.g., amino acid side chains, peptides) chosen to provide particular properties to the compound.

Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7- substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

Abstract: Process for the preparation of compounds of formula (I), wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula (V), wherein the general symbols are as defined in claim 1, with carbon monoxide in the presence of a catalyst.

Abstract: This invention relates to a process for the preparation of tocopherol concentrates from a material containing tocopherols and free fatty acids. The free fatty acids in the tocopherol-containing material are converted to the alkali metal salts thereof in a specific organic solvent that can not, practically, dissolve the alkali metal salts of fatty acids. The free fatty acids are removed as a precipitate of their alkali salts, and the tocopherols are recovered from the supernatant by removing the solvent. The said specific organic solvents include acetone, ethyl acetate, dimethylformamide, acetonitrile and their mixtures. The alkali salts are preferably sodium and potassium salts.

Abstract: An integrated method is disclosed for removing and recovering a substantially water-soluble solvent and at least one metal from an organic reaction mixture comprising at least about 35% by weight aromatic hydroxy compound, which comprises the steps of: (i) contacting a reaction mixture at least once with aqueous acid, (ii) mixing the organic and aqueous phases in the presence of an oxygen source, (iii) separating the organic and aqueous phases wherein said solvent remains substantially in the organic phase; (iv) recovering metal species from the aqueous phase; and (v) recovering said solvent from the organic phase.

Abstract: The invention provides a method of producing &agr;-tocopherol and &agr;-tocopheryl esters. The method comprises using a biological system to produce farnesol or geranylgeraniol. Then, the farnesol or geranylgernaiol is chemically converted into &agr;-tocopherol or an &agr;-tocopheryl ester.

Abstract: The present invention relates to novel cycloalkylalkane-carboxamides of the formula I where the substituents have the following meanings: A is C3-C6-cycloalkyl; R1 is C1-C6-alkyl or C2-C6-alkenyl; R2, R3 and R4 are hydrogen or, independently of this meaning, have one of the meanings of the radical R1; n is 0 or 1; Y is cyano or halogen; w is phenyl, naphthyl or heteroaryl.

Abstract: An object of the present invention is to provide the tocopherol derivatives represented by the following formula (I), and their salts: Wherein, R1, R2 and R3 are H or methyl group, and at least one positions selected from group consisting of the R1, R2 and R3 positions are methyl group; and, A is CH2—CH(CH3)— or CH═C(CH3)— The other object of the present invention is to provide a method for preparing the above tocopherol derivatives. The tocopherol derivatives is prepared by reacting tocopherol with phosphorous oxychloride in an equivalent ratio of 1:1˜1.3, in presence of an organic base, in an organic solvent; reacting the tocopherol dichlorophosphate produced by the above reaction with 3-aminopropanol in presence of an organic base, in an organic solvent; and, hydrolyzing the above products.