Abstract: The invention relates to a process for the preparation of a compound of the formula (I) by reacting a compound of the formula (II) with a compound of the formula (III) characterized by dissolving the compounds of the formula (II) and formula (III) in a water-inmiscible organic solvent in the presence of a phase transfer catalyst, reacting with a.) an aqeuos solution of a base, or b.) a base in solid form directly and if desired transforming the compound of formula (I) thus obtained into its salt.

Abstract: The invention relates to the crystalline and amorphous forms of the desmotrope of general formula IB and its salts and solvates, and their preparation.

Abstract: The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2?[1?H]-one derivatives of the general formula I wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of the general formula II wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group—with an acrylic acid C1-4ester, cyclizing the resulting compound of the general formula IV wherein R1, R2 and A are as defined above, R3 stands for C1-4 alkyl grou

Abstract: The invention relates to a process for the preparation of a compound of the formula (I) by reacting a compound of the formula (II) with a compound of the formula (III) characterised by dissolving the compounds of the formula (II) and formula (III) in a water-inmiscible organic solvent in the presence of a phase transfer catalyst, reacting with a.) an aqeuos solution of a base, or b.) a base in solid form directly and if desired transforming the compound of formula (I) thus obtained into its salt.

Abstract: Process for the preparation of a compound of the general formula (I) and pharmaceutically acceptable salts and solvates thereof, (I) characterised by reacting an N-(amino-tioxo-methyl)-1H-indole-2-carboxamide of the general formula (II), with an &agr;-halogen-ketone of the general formula (III), wherein X stands for halogen.

Abstract: New process for the preparation of 1,5-disubstituted-3-amino-1,2,4-triazoles of the general formula (I), wherein the meaning of R is C1-5alkyl group; C3-13cycloalkyl-C0-4alkyl group, optionally substituted by one or more C1-3alkyl group; phenyl-C0-2alkyl-, (CH2)n-morpholino-, piperidino-, pyrrolidino- or piperazino-group, optionally substituted by one or more halogen atom, C1-3alkyl group, C1-3alkoxy group, n is 1-5, R1, R2, R3, and R4 stand independently for hydrogen, halogen, C1-6alkyl group, C1-3alkoxy group or trifuluoromethyl group, with the proviso that of the substituents R1, R2, R3, and R4 at least one stands for hydrogen.

Abstract: The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of the general formula I 1

Abstract: New salts of the general formula (I), their solvates, polymorphs and pseudo polymorphs wherein X stands for ethanolamine, diethanolamine or diethylamine.

Abstract: The invention relates to a process for the preparation of a compound of formula (I) and the salts thereof by reacting the compound of formula (II) with the compound of formula (III), which comprises carrying out the reaction in dimethyl sulfoxide, at a temperature between 10° C. and 40° C., preferably at room temperature and transforming the resulting base of formula (I), if desired, into its salt by a method known per se.

Abstract: Orally active compounds of general formula (I) wherein R1 is methyl, ethyl or 2-morpholino-ethyl group, R2 is piperidino, morpholino or 4-methyl-piperazinyl group, n is 2 or 3 and their salts, solvates and hydrates.

Abstract: The invention relates to a process for the preparation of spiro [(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of general formula I—wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of general formula II—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group—with acrylic acid C1-4ester; cyclizing the resulting compound of general formula IV—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of formula III thus obtained,—wherein R1 and R2 are as defined abo

Abstract: The invention relates to a process for the preparation of 2-methoxy-4-(N-t-butylaminocarbonyl)benzenesulfonyl chloride by sulfonating m-hydroxybenzoic acid, methylating the hydroxy group of the resulting sulfonic acid or its salt, transforming the carboxylic acid group and the sulfonic acid group to acid chloride groups and reacting the 4-chlorosulfonyl-3-methoxy-benzoyl chloride with t-butylamine, which comprises carrying out the sulfonation of the 3-methoxy-benzoic acid of general formula (II) with 96% sulfuric acid, separating the resulting 3-hydroxy-4-sulfobenzoic acid of general formula (III) in the form of its salt of general formula (IV), wherein Z stands for alkali metal or ammonium group, methylating the compound of general formula (IV) in the presence of a phase transfer catalyst at a pH value of about 11.

Abstract: The invention relates to a process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3H]indol]-2′[1′H]-one derivatives of the formula (I) wherein R1 and R2 are as defined herein, by reduction of a dispiro[(1,3-dioxolane)-2,4′-cyclohexane-1′3′-[3H]indol]-2″[1″H]-one derivative of general formula (II), wherein R1 and R2 are as defined herein, which comprises carrying out the reduction (a) with sodium cyanoborohydride in the presence of a Lewis acid, or (b) with sodium borohydride in the presence of a strong acid.

Abstract: The invention relates to a process for the preparation of Fumagillin by liberation from its salt characterized by reacting Fumagillin dicyclohexylamine salt with an organic acid in alcoholic medium.

Abstract: A process for the preparation of &agr;,&bgr;-unsaturated alcohols of general formula (I), wherein R means an alkyl group of 1-4 carbon atoms, or benzoyloxy group optionally substituted with a phenyl group; R1 means a hydrogen atom or an alkyl group of 1-4 carbon atoms, R2 means a hydrogen atom or an alkyl group of 1-4 carbon atoms; R3 means an alkyl group of 1-6 carbon atoms optionally substituted by phenyl group or cycloalkyl group of 5-7 carbon atoms; or a phenoxy group optionally substituted by a halogen atom, or a cycloalkyl group of 5-7 carbon atoms; R4 means a hydrogen atom or a halogen atom whereby at &agr;,&bgr;-unsaturated ketones of general formula (II) wherein the meanings of R, R1, R2, R3, and R4 are as given above—is diastereoselectively reduced with a borohydride type compound in an aprotic solvent, in the presence of an inorganic substance dissolublein the reaction mixture and having particle size from 0.

Abstract: The present invention relates to new prolylendopeptidase inhibitors of general formula (I).

Abstract: New process for the preparation of prostaglandin E1 of formula (I) starting from the compound of formula (II).

Abstract: The invention relates to two phase pharmaceutical compositions comprising as active ingredient a MAO inhibitor and an uptake inhibitor together with usual pharmaceutical auxiliaries. The compositions can be used for the treatment of neurodegenerative diseases. As active ingredient optionally N-(1-phenyl-isopropyl)-N-methyl-propinylamine or N-(4-fluoro-phenyl)-isoprop-1-yl-N-methyl-propinylamine or their salts, optically active isomers or metabolites are used both as MAO inhibitor and as uptake inhibitor.

Abstract: 4-oxo-4H-pyrido[1,2-a]-pyrimidines are disclosed of the formula ##STR1## wherein R is a C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl, --(CH.sub.2).sub.n --COOR.sup.3 wherein R.sup.3 is C.sub.1 to C.sub.4 alkyl and n is 0 or 1 or a C.sub.7-8 aralkyl group, optionally substituted by one or more halogen atom(s), or by a nitro-group, R.sup.1 is a hydrogen atom or a C.sub.1-4 alkyl group, and salts thereof, as well as a process for their preparation, and pharmaceutical compositions containing them. These compounds are therapeutically useful as gastroprotectives in the treatment and prevention of ulcer.

Abstract: The invention relates to a novel process for the preparation of 13,14-dihydro-15 (R)-17-phenyl-18,19,20-trinor-PGF.sub.2.alpha. isopropyl ester of the formula (I)--wherein R stands for saturated or unsaturated straight, branched or cyclic C.sub.