Abstract: A process for the manufacture of agomelatine and its intermediate N-[2-(7-methoxy-1-naphthyl)ethyl]phthalimide is provided and includes reacting 7-methoxy-1-naphthyl ethanol (III) with benzenesulfonyl chloride to obtain 7-methoxy-1-naphthylethyl benzene sulfonate (IV), which is reacted with potassium phthalimide to produce N-[2-(7-methoxy-1-naphthyl)ethyl]phthalimide (II); and subjecting N-[2-(7-methoxy-1-naphthyl)ethyl]phthalimide (II) to alkaline hydrolysis and acetylation, to obtain agomelatine.

Abstract: The present invention relates to a process for preparing betamimetics of formula 1, wherein n denotes 1 or 2; R1 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R2 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R3 denotes hydrogen, C1-4-alkyl, OH, halogen, O—C1-4-alkyl, O—C1-4-alkylene-COOH, O—C1-4-alkylene-COO—C1-4-alkyl.

Abstract: Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, X represents a group N—OR2 wherein R2 represents a hydrogen atom or an alkyl group. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.

Abstract: Crystalline form III of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.

Abstract: The present invention relates to phenyloxyaniline derivatives, to methods of their production and to uses thereof.

Abstract: Crystalline form IV of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.

Abstract: Disclosed is a kit for use in the production of a molecular probe for PET drug screening for the purpose of producing a compound containing a short-lived radionuclide for PET applications. Specifically disclosed is a kit comprising a compound represented by the formula (I), (II) or (III) or a salt thereof. In the formulae, X1, X2, X3, X4, X5 and X6 are as defined in the description.

Abstract: A method for the production of optically active ?-alkylcarbonyl compounds with retention of the stereo information of the starting compound. The starting compound used here is a carbonyl compound which has, in the ?-position, a leaving group which is substituted by an alkyl group with inversion of the configuration. The substitution of the leaving group is effected with the use of an alkylmagnesium Grignard and a zinc (II) salt or a zinc organyl. The method permits the production of optically active ?-alkylcarbonyl compounds at very mild temperatures (for example 0° C.) with the use of starting compounds which are easy to prepare and economical and nontoxic catalysts, it also being possible to achieve a very high yield.

Abstract: The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.

Abstract: This invention relates to an improved method for crystallizing 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”), an intermediate in the industrial preparation of non-ionic X-ray contrast agents. In particular, the present invention provides an industrial process for crystallization of Compound A by evaporating methanol and water from the mother liquor after an initial crystallization of Compound A following the acetylation reaction. Specifically, the mother liquor is maintained at more than about 75% (v/v) of water and less than about 25% (v/v) of alcoholic solvent.

Abstract: Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, R2 represents a fluorine atom or an alkyl group substituted by one or more fluorine atoms. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.

Abstract: Process for the industrial synthesis of the compound of formula (I) Application of such process in the synthesis of agomelatine.

Abstract: Process for obtaining the crystalline form V of the compound of formula (I):

Abstract: Crystalline form IV of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.

Abstract: This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual melatoninergic agonist and serotoninergic antagonist.

Abstract: Crystalline form III of the compound of formula (I): characterized by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.

Abstract: The invention provides methods and reagents for the metathesis of secondary amides via a transacylation mechanism employing catalytic quantities of an imide initiator and a Brønsted base. Equilibrium-controlled exchange between various amide reactant pairs is demonstrated for substrates bearing a variety of N-alkyl and N-aryl substituents.

Abstract: This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual melatoninergic agonist and serotoninergic antagonist.

Abstract: The present invention relates to aniline derivatives of the general formula I or salts thereof, described therein, and their use.

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract: Crystalline form VI of the compound of formula (I): characterised by its X-ray powder diffraction diagram. Medicinal products containing the same which are useful in treating melatoninergic disorders.

Abstract: The present invention relates to a novel process for the industrial manufacture of substituted 7-allyl-6-hydroxy-indanes of formula (I) wherein R is a straight or branched (C1-C6)alkyl group and X is a halogen and enantiomers thereof.

Abstract: A compound selected from those of formula (I): Medicinal products containing the same which are useful in the treatment of disorders of the melatoninergic system.

Abstract: Disclosed herein are substituted naphthalene-based melatonin (MT) receptor modulators and/or 5-HT receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual melatoninergic agonist and serotoninergic antagonist.

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)- 1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract: Compounds of the formula (I) wherein R is phenyl, or phenyl substituted by Cl, Br, C1-C4alkyl or CF3; R1 is H or methyl or ethyl; R2 is H or methyl or acyl; R3 is H or methyl; R?4 is —CH3 or ?CH2; may be obtained in high enantiopurity by hydrogenation of a compound of the formula (II) wherein R and R3 are as in formula (I); A is acyl; and R4 is —CH3 or ?CH2; in the presence of a chiral Rhodium or Ruthenium catalyst. Residues R1 as methyl or ethyl and/or R2 as H or methyl may subsequently be introduced without racemization by deacylation and optional alkylation.

Abstract: A compound selected from those of formula (I): Medicinal products containing the same which are useful in the treatment of disorders of the melatoninergic system.

Abstract: A compound selected from those of formula (I): wherein: R1 represents a group R4 or NHR4, wherein R4 is as defined in the description; R2 represents a substituted linear or branched (C1-C6)alkyl group; R3 represents a hydrogen or halogen atom or a linear or branched (C1-C6)alkyl or linear or branched (C2-C6)alkenyl group. Medicinal products containing the same which are useful in the treatment of disorders of the melatoninergic system.

Abstract: A compound selected from those of formula (I): Medicinal products containing the same which are useful in the treatment of disorders of the melatoninergic system.

Abstract: The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.

Abstract: A process for preparing indanylamine and aminotetralin derivatives from indanone or tetralone oximes by acylating the oximes with an organic anhydride, followed by catalytic hydrogenation in the presence of an organic anhydride with subsequent hydrolysis is described. The process is commercially feasible providing indanylamine and aminotetralin derivatives in high yield that are useful as intermediates in the production of therapeutically active compounds. Also described are novel intermediates, 1-indanone O-acetyl oximes and 1-tetralone O-acetyl oximes.

Abstract: Disclosed is a method of manipulating the carboxamide functionality in a catalytic manner. The method includes the steps of reacting amides with or without amines in the presence of various types of metal catalysts, at a temperature of about 250° C. or less.

Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:

Abstract: New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, CN, halogen, C(?O)H, C(?O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form ?O; Y is NR1, OR1, PR1, SR1, or halogen, wherein the number of substituents R1 is selected to suit the valency and each R1 is independently selected of H, OH, C(?O)R?, P(?O)R?R?, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHC(O)R?, CN, halogen, C(?O

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract: A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16. (in the formula, X is an aliphatic alkyl group, desirably is an aliphatic alkyl group having 7 to 15 carbon atoms).

Abstract: A phenyloxyaniline derivative useful as a ligand for peripheral benzodiazepine receptor having a strong affinity and a high selectivity, which is represented by formula (1): wherein X1 and X2 are same or different and each is hydrogen atom or halogen atom; R1 and R2 are same or different and each is hydrogen atom, an alkyl group having 1 to 10 carbon(s) or a halogen-substituted alkyl group having 1 to 10 carbon(s); and R3 is a halogen-substituted alkyl group having 1 to 5 carbon(s), or a radioisotope thereof.

Abstract: A novel process for producing an optically active amide excellent in chemical selectivity and enantioselectivity by asymmetric hydrogenation of an ?,?-unsaturated amide and also allowing the reaction to proceed efficiently even when a trace amount of a catalyst is used relative to the substrate as compared with the amount in a conventional process. An optically active amide is produced by asymmetric hydrogenation of an ?,?-unsaturated amide derivative in the presence of a transition metal complex containing a specific phosphine-phosphorane compound.

Abstract: The invention provides a novel &bgr;2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel &bgr;2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.

Abstract: The invention relates to bisaryl derivatives of the formula I, 1

Abstract: A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16.

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B  (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.

Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: The invention relates to compounds of formula (I): and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.

Abstract: The invention relates to compounds of for a (I): wherein: R represents ORa, SRa or Ra or a cyclic group A is a cyclic structure G1 and G2 represent an alkylene chain or a single bond B represents —NR1aC(Q)R2a, —NR1aC(Q)NR2aR3a or C(Q)NR1aR2a p and q are such that 1≦p+q≦4, and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.

Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:

Abstract: The present invention relates to a method for producing a compound of the formula [71] wherein R1 is an optionally substituted cycloalkyl group, an optionally substituted aryl group or an optionally substituted heterocyclic group, R2 is a lower alkyl or a halogenated lower alkyl and R3 is a halogen atom or a hydrogen atom. The method of the present invention includes reacting compound [1] with thionyl chloride to give compound [2] and obtaining the objective compound [7] at a high yield via intermediate [5], and is utilizable for industrial production.