Abstract: Roflumilast and new key intermediates therefor are prepared by processes involving use of carbonylation technology. Good overall yields can be achieved using available starting materials. The starting material for the process can be catechol, an o-R1-phenol, an o-R1-p-X-phenol, or a 1-X-3-R1-4-R2-benzene, where R1, is a C1-6 alkoxy, C3-7 cycloalkoxy, C3-7 cycloalkylmethoxy, or benzyloxy group, or a C1-4 alkoxy group which is completely or partially substituted by fluorine; R2 is a C1-4 alkoxy group which is completely or partially substituted by fluorine; and X is Cl, Br, or I.

Abstract: A prostaglandin derivative represented by the formula: wherein X is a halogen atom, R1 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 0 to 5, and Y is a group represented by the formula: wherein R2 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C1-4 alkyl group substituted with C3-10 cycloalkyl group(s), a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group or a bridged cyclic hydrocarbon group, or a group represented by the formula: wherein n is an integer of 1 to 8; a pharmaceutically acceptable salt thereof or a hydrate thereof.

Abstract: A subject of the present invention is a process for preparation of fluorinated ketones corresponding to general formula (I) R1—CO—R2 in which R1 and R2 are as defined in claim 1, characterized in that it consists of reacting two carboxylic acids of Formula (II), R1—COOH and Formula (III), R2—COOH, in the gaseous phase and in the presence of a catalyst comprising at least one oxide of an element chosen from the rare earths, thorium, titanium and aluminum.

Abstract: The invention relates to a method for producing (meth)acrylic acid esters by transesterification of the (meth)acrylic acid with a higher alkanol in the presence of an acid catalyst, at least one polymerization inhibitor and one organic solvent that forms an azeotropic mixture with water. The reaction mixture is heated to the boiling point of the mixture in a reactor that comprises a distillation unit with a column and a condenser. The content of the reactor is recirculated via an external evaporator and heated to the boiling point, and the azeotropic mixture is distilled off. The organic solvent forms a reflux and at least a part of the solvent reflux is recirculated between the reactor and the evaporator. The inventive method allows for the production of higher (meth)acrylic acid esters in a reactor with a circulation evaporator without using copper salts as the polymerization inhibitors.

Abstract: The present invention is directed to a novel 4-sulfanylalkyl-3,5-dinitro benzyl alcohol compound and its preparation method, more specifically, derivatives of 4-sulfanylalkyl-3,5-dinitro benzyl alcohol compound having the following formula 1 and its preparation method: wherein, R is hydrogen, alkyl group, or acetyl group, and n is an integer of 1 to 25. The organic compound of the present invention can be used as a material for molecular electronic device.

Abstract: The invention provides substituted phenol compounds and pharmaceutical compositions containing substituted phenol compounds which are useful for inducing or maintaining anesthesia or sedation in a mammal. This invention also provides methods for inducing or maintaining anesthesia or sedation in a mammal using substituted phenol compounds.

Abstract: This invention relates to a process for synthesis and method of use of an effective amount of a 3-hydroxy-3-methylbutyrate (HMB) amino acid salt for the regulation athletic function in humans.

Abstract: The invention relates to a method for producing derivatives of 3,3-diarylpropylamines of general formula (I) and sterically highly pure, stable intermediate products, and to their use for producing pharmaceutical compositions.

Abstract: The invention relates to novel diphenylmethane derivatives, processes for their preparation and their use in medicaments, in particular for the indications of arteriosclerosis and hypercholesterolaemia.

Abstract: A caged non-steroidal ecdysome memetic (NSE) compound and a method for producing free NSE by subjecting the charged NSE to UV irradiation.

Abstract: Isocyanates are produced in the gas phase in a manner such that temperature fluctuations over time and temperature distribution asymmetry are prevented. In this improved process, performance of the reaction in tubular reactors is accomplished by flow-related measures such as homogenization and centering of the educt streams. The formation of polymeric secondary products, which result in baked-on deposits in the reactor and a reduction in reactor service life, is consequently prevented.

Abstract: Described are new crystalline anhydrous forms of gabapentin formed from gabapentin monohydrate. The new crystalline forms provide advantages in the manufacture of the therapeutic agent.

Abstract: Polymers and compounds including a diphenylmethylene or a 9H-fluorene moiety; and sunscreen compositions including a mixture of a photoactive compound and any one of the foregoing derivatives are disclosed herein. Also disclosed are methods for stabilizing a sunscreen composition by the addition of one or more of the foregoing derivatives, methods of filtering out ultra-violet light from a substrate by the use of one or more such derivatives, and methods for terminating a polymerization reaction by the addition of derivatives of diphenylmethylene and/or 9H-fluorene.

Abstract: The phosphorus-containing compound of the present invention is represented by the following formula (I), (II) or (III): wherein Z1, Z2 and Z3 each represents a cycloalkane, a cycloalkene, a polycyclic aliphatic hydrocarbon or an aromatic hydrocarbon rings which may have a substituent; R represents a halogen atom, a hydroxyl, a carboxyl, a halocarboxyl(haloformyl), an alkyl, an alkoxy, an alkenyl or an aryl groups; A represents a polyvalent group corresponding to an alkane; Y1, Y2 and Y3 each represents —O—, —S— or —NR1—, wherein R1 represents a hydrogen atom or an alkyl group; k is an integer of 1 to 6; m is an integer of 0 to 2; n is an integer of not less than 1; q is an integer of 0 to 5; r is 0 or 1; and S is an integer of 1 to 4. The phosphorus-containing compound is excellent in heat resistance and is useful as flame retardants, plasticizers, or stabilizers.

Abstract: Process for the preparation of ethers of hydroxybenzoic acid having general formula (I), which comprises reacting a hydroxybenzoic acid, optionally substituted, with a halide XR1, wherein X is a halogen such as chlorine, in a basic environment and in an aqueous or aqueous/organic biphasic solvent.

Abstract: An organic single-crystalline film useful as a functional film in various devices is produced by selecting a liquid crystal material having a good molecular alignment regularity, disposing the liquid crystal material between a pair of boundaries exerting a thickness regulating force and solidifying the liquid crystal material while imparting a molecular alignment order by phase transition from a liquid crystal phase. The liquid crystal material may preferably be a smectic liquid crystal material which provides a uniform molecular alignment inclusive of the direction of the molecular long axis in a smectic phase.

Abstract: The present invention is directed to methods and compositions for treating upper respiratory indications, such as the treatment, management or mitigation of cough, cold, cold-like symtoms, symtoms related to upper respiratory infections, influenza symptoms and allergic rhinitis, perennial rhinitis, nasal and Eustachian tube congestion in an animal by administration of tannate compositions comprising single agent formulations or combinations of at least one or more agents into a single administrative dose.

Abstract: A process for purifying pravastatin sodium comprising the steps of: a. clarifying a fermentation broth containing pravastatin sodium to obtain a clear solution; and adjusting the clear solution to be basic having pH value ranging from pH 10˜13; b. adsorbing the pravastatin sodium with non-ionic resin; eluting the pravastatin sodium by water-soluble organic solvent; and forming a concentrate of pravastatin sodium; c. treating the concentrate with water-soluble anti-solvent or inorganic salt to form a precipitate of pravastatin sodium; and d. recrystallizing the precipitate for making pravastatin sodium crystal with high purity and high yield.

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: Process for the preparation of 3-aminoalkanoic acid esters of the general formula: in which R is C1-6-alkyl and R1 is hydrogen, C1-6-alkyl or phenyl, or their salts, by catalytic hydrogenation of the corresponding 3-amino-2-alkenoic acid esters of the general formula: in which R and R1 have the above mentioned meanings. The hydrogenation is carried out in the presence of a strong acid and the salt of the 3-aminoalkanoic acid ester (I) and the strong acid formed is optionally converted into the free 3-aminoalkanoic acid ester (I) or into another salt in a manner known per se.