Abstract: The invention relates to a process for the preparation of cyclopropyl benzyl ketone compounds of formula (II) wherein R1 represents fluorine or chlorine atom or C1-4 alkoxy group, by the reaction of a Grignard reagent, obtained from the reaction of compound of formula (V), wherein X represents chlorine or fluorine atom, with the compound of formula (IV), wherein R2 represents C1-4 alkyl group, having a straight or branched chain. The process can be applied preferably on industrial scale. Compound of formula (II), wherein R represents a fluorine atom in position 2 is an intermediate of the preparation process of prasugrel, which is a platelet inhibitor used in the therapy.

Abstract: The object of the present invention is a one-pot process for preparing the 2-acetoxy-5-(2-fluoro-?-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]-pyridine (prasugrel) of the formula (I) by reacting the 5,6,7,7a-tetrahydro-4H-tieno[3,2-c]-pyridine-2-on of the formula (II) with 2-bromo-1-cyclopropyl-2-(2-fluorophenyl)-etanone of the formula (III) or with 2-chloro-1-cyclopropyl-2-(2-fluorphenyl)-etanone of the formula (IIIa) and acetylating of the formed compound of the formula (IV), wherein the reaction is carried out in the presence of an organic base with an acetylation agent without isolating the compound of the formula (IV). The coupling and acetylation are carried out in the presence of the same organic base such as triethylamine, N,N-diisopropyl-ethylamine or pyridine. At the end of the process the prasugrel of the formula (I) is purified by recrystallization from an organic solvent or a mixture of solvents.

Abstract: The object of the present invention is a process for preparing the 2-acetoxy-5-(2-fluor-?-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]pyridine (prasugrel) of the formula (I). The process starts form crystalline 5-trityl-4,5,6,7-tetrahydro-tieno[3,2-c]pyridine of the formula (VI). Further objects of the present invention are two novel crystalline forms of 5-trityl-4,5,6,7-tetrahydro-tieno[3,2-c]pyridine of the formula (VI) and the use thereof for preparing the compound of the formula (V) and process preparing thereof.

Abstract: The invention relates the use of 4-chloro-5-{2-[4-(6-fluoro-1,2-benz[d]isoxazole-3-yl)piperidin-1-yl]ethyl-amino}-2-methyl-3-(2H)pyridazinone of the Formula (I) or pharmaceutically acceptable salts thereof for the preparation of medicaments suitable for the improvement of cognitive function or obtaining neuroprotective effect. The medicaments containing 4-chloro-5-{2-[4-(6-fluoro-1,2-benz[d]isoxazol-3-yl)piperidin-1-yl]ethyl-amino}-2-methyl-3-(2H)pyridazinone of the Formula (I) or therapeutically acceptable salt thereof can be used for the treatment or prevention of neuronal death, mental decline, sclerosis multiplex, Creuzfeld-Jacobs disease, Huntington-syndrome, amyotrophic lateral sclerosis, Parkinson-disease, memory disturbance, loss of memory, amnesia, stroke or for the improvement of memory function or learning ability.

Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or an alkyl group; R2 represents an alkyl group; R3 represents an aryl or heteroaryl group. Medicinal products containing the same which are useful in the treatment or prevention of psychiatric and neurological disorders characterised by cognitive deficits.

Abstract: According to the present invention, 2-chloroethoxy-acetic acid-N,N-dimethylamide of the Formula (I) is prepared by reacting 2-hydroxyethoxy-acetic acid-N,N-dimethylamide of the Formula (II) in a solvent optionally in the presence of a catalyst with thionyl chloride and removing the solvent by distillation.

Abstract: The invention relates to an apparatus and method for testing transdermal medicaments, wherein the sample tested in a membrane penetration cell resides in the open sample compartment of said cell and is exposed to environmental factors such as temperature, air flow, light and air humidity during testing the absorption and penetration.

Abstract: The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.

Abstract: The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium sait monohydrate is produced. Said sait is subsequently treated with mineral or organic acid to yield high-purity meloxicam.

Abstract: The invention relates to a process for the preparation of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno-[2,3-b][1,5]benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno[2,3-b][1/5]benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1,3-dimethyl-2-imidazolidinone. The invention also encompasses new 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b] [1,5]benzodiazepine dihydrochloride trihydrate of the formula (IB), the preparation thereof and pharmaceutical compositions comprising said new compound.

Abstract: The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I), wherein R stands for a lower alkyl group or a group of the general formula —NH—R?, wherein R? stands for a lower alkyl or a lower cycloalkyl group), and pharmaceutically acceptable acid addition salts thereof. The invention also encompasses a process for the preparation of said compounds, pharmaceutical compositions containing them and new intermediates useful for the preparation of the new 8-chloro-2,3-benzodiazepine derivatives. The compounds according to the invention possess AMPA/kainate receptor inhibiting activity.

Abstract: The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.

Abstract: The present invention is concerned with new indol-2-one derivatives of Formula (I), which have favorable activity profile for the prophylaxis and treatment of disorders in the central nervous or in the cadiovascular system.

Abstract: The present invention is related to 1-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.

Abstract: The present invention is concerned with new 3,3-disubstituted indol-2-one derivatives of the general Formula (I), wherein R1 stands for hydrogen, halogen, alkyl having 1-7 carbon atom(s) or sulfonamido; R2 represents hydrogen or halogen; R3 denotes hydrogen, alkyl having 1-7 carbon atom(s) optionally carrying an aryl substituent or aryl optionally carrying one or two halogen substituent(s); R4 stands for alkyl having 1-7 carbon atom(s); R5 represents a group of the general Formula (II a) or (II b), wherein Q and W each represents nitrogen or CH; R6, R7 and R8 each stands for hydrogen, halogen, trifluoromethyl, alkyl or alkoxy having 1-7 carbon atom(s), or R6 and R7 together represent ethylenedioxy; m is 0, 1, or 2; a is a single, double or triple bond; n is 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof which are useful in the treatment or prophylaxis of diseases of the central nervous system, the gastrointestinal system and the cardiovascular system.

Abstract: The present invention is related to new 3,4-dihydroberizo[1,2,3]thiadiazine-1,1-dioxide derivatives of the Formula (I), medicaments containing said new compounds, process for the preparation thereof and the use of said derivatives in the medicine. The compounds according to the present invention are suitable for the treatment or prevention of disorders of the central nervous system.

Abstract: The present invention provides for new salts of aripiprazole of the general formula (II) formed with dibasic organic acids, camphorsulfonic acid, phosphoric acid, and processes for their preparation. Further objects of the present invention are pharmaceutical compositions containing said new aripiprazole salts. Aripiprazole salts according to present invention can be prepared by the reaction of aripiprazole base and suitable acid compounds in a molar ratio 0.5-3 based on the molar amount of aripiprazole in a suitable organic solvent.

Abstract: The present invention relates to a new method of preparation of the polymorph form 1 of methyl (S)-(+)-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyridine-5-yl-acetate hydrogensulfate of the formula (I)

Abstract: The present invention is concerned with new indol-2-one derivatives of Formula (I), which have favourable activity profile for the prophylaxis and treatment of disorders in the central nervous or in the cadiovascular system.

Abstract: The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent.