Abstract: The invention relates to a method for the preparation of an enantiomerically pure imidazolyl compound of the general formula ##STR1## wherein n is 0 or 1; m is 1 or 2;R.sub.

Abstract: The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group.The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate.

Abstract: An automatic injector for the separate storage of a solid and a solvent for this solid. The injector comprises a discharge mechanism, a cartridge assembly and a front cover which is connected to a front portion of the cartridge assembly and provided at its front with a pierceable central area. The cartridge assembly comprises a hollow barrel, a pierceable stopper connected to the front portion of the barrel and constituting a compartment in front of said stopper for accommodating the solid, a piston slidably accommodated in the backward portion of the barrel and constituting a compartment for liquid in the barrel, an injection needle longitudinally extending in the liquid compartment, and means for centering the distal end of the needle in order to position the needle tip towards the pierceable stopper. The front cover is capable of rotational movement relative to the outer sleeve to allow the liquid in the barrel to reach the solid compartment through the needle.

Abstract: The invention relates to a method of preparing an optically active cyanohydrin carboxylic acid ester from an optically active cyanohydrin of opposite configuration, wherein said starting cyanohydrin is converted with a carboxylic acid in the presence of a dialkyl azodicarboxylate and a triarylphosphine.The invention also relates to a method of preparing an optically active cyanohydrin of opposite configuration by a subsequent solvolysis of the ester obtained under conservation of the configuration.

Abstract: The present invention is concerned with the separation of organic compounds in a mixture using their tendency of binding a weak acid by applying electrodialysis to a mixture of at least one of said organic compounds and said weak acid, while preferably an ionexchange resin is present in the electrodialysis cell.

Abstract: The present invention is concerned with compounds having 5-HT1A antagonistic activity useful in treating CNS disorders and having formula 2 ##STR1## wherein R.sub.1 is halogen, lower alkyl or alkoxy, hydroxy, trifluotomethyl or cyano,m has the value 1 or 2 and n has the value 0 or 1,A represents an alkylene chain containing 2-6 C-atoms which may be substituted with one or more lower alkyl groups or a monocyclic (hetero)aryl group, andB is methylene, ethylene, carbonyl, sulfinyl, sulfonyl or sulfur, and salts thereof.

Abstract: The present invention is concerned with a method for the preparation of a compound of the general formula 2 ##STR1## by reaction of a compound of the formula 3Ar--Y (3)with a compound of the general formula 4 ##STR2## wherein Ar means a (hetero)aryl group, preferably selected from phenyl, naphtyl, furyl, thienyl, pyridyl, bicylic heteroaryl and tricyclic heteroaryl, which (hetero)aryl group is optionally sustituted with one to five non-strongly-electron-withdrawing substituents;M is a metal from the groups I or II of the periodic table;R.sub.12 is an electronegative group; andis 0 or 1.The invention also relates to compounds prepared according to this method and to new substituted aryl(homo)piperazines.

Abstract: The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;R.sub.3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;R.sub.4 is a sec. or tert. (C.sub.3 -C.sub.6)alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.

Abstract: The invention relates to a process for the production of an acid addition salt of a dobutamine compound of the general formula ##STR1## wherein R is a hydrogen atom or a methyl group, and n is 1 or 2,by reacting a mineral acid--addition salt of a dopamine compound of the general formula ##STR2## with a ketone of the general formula ##STR3## under the influence of a catalytic amount of a base, and in the presence of hydrogen and a hydrogenation catalyst, after which the pH of the reaction mixture is adjusted to approx. 6 at most and the product is isolated.

Abstract: The invention relates to new compositions with pyschotropic activity which comprise a compound of formula 1 of the formula sheet as the active substance. The compounds of formula 1 are for the greater part new compounds. The invention therefore also relates to these new compounds and to the preparation thereof in a manner known for the synthesis of analogous compounds.

Abstract: The invention relates to a method of preparing solid forms of administration of lactulose by evaporating lactulose syrup to a water content of at most 10%, preferably 2 to 6%, cooling the thick, evaporated syrup, grinding and sieving, or breaking the solid product.

Abstract: The present invention is concerned with the preparation of N-substituted vicinal aminoalcohol derivatives from the corresponding hydroxyl-protected cyanohydrin derivatives by successive partial reduction, transimination using a primary amine, reduction of the resulting imine and optional removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the starting cyanohydrin derivatives.The present invention is also concerned with certain new enantiomerically pure hydroxyl-protected vicinal aminoalcohols.

Abstract: The invention relates to a tablet dispenser, including a dispenser housing, a replaceable tablet package to be accommodated in the housing, an adjustable periodicity indicator and a single tablet dispensing aperture in the dispenser cover. The tablet package includes a cover, rotatably connected to the bottom portion of the package and provided with an opening which, upon use of the dispenser, is in alignment with the tablet dispensing aperture. The dispenser further includes a locking device to compel joint rotational movement of periodicity indicator and package bottom portion, and an operating member to effect stepwise rotation of the package bottom portion relative to said package cover.

Abstract: The invention relates to a group of new 3,4-dehydropiperidine derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1-3 carbon atoms;Y is a group of the general formula 2 ##STR2## wherein R.sub.2 is a group of the formula --(CH.sub.2).sub.n --C(.dbd.X)--NR.sub.3 R.sub.4, --(CH.sub.2).sub.n --SO.sub.2 --NR.sub.3 R.sub.4, --(CH.sub.2).sub.n --NR.sub.5 --C(.dbd.X)--R.sub.6 or --(CH.sub.2).sub.n --NR.sub.5 --SO.sub.2 --R.sub.6, wherein R.sub.3, R.sub.4 and R.sub.5 independent of each other represent hydrogen or alkyl (1-3C), R.sub.6 is alkyl (1-3C), X represents O or S; n is 0-4, andR is hydrogen or alkyl (1-3C).These compounds have interesting serotonin-1-like (partial) agonistic activity and can be used for the treatment of migraine.

Abstract: The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group.The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate.

Abstract: The invention relates to a method of preparing a compound having an alkyl or alkoxyalkyl side-chain with a terminal 2-hydroxyprop-2-yl group, by oxidizing a compound having a terminal isopropyl group in its side-chain with a dioxirane as the oxidant.

Abstract: The invention relates to a pre-filled injection device, comprising (i) a barrel which is open at each end in which, before using the device, a liquid diazepam formulation is accommodated in a sealed manner and which comprises at least one rubber sealing member to seal the said formulation, and (ii) an injection needle or a needle connection at the front end of the barrel, said sealing member being manufactured at least substantially from bromobutyl rubber.

Abstract: The present invention is concerned with vaccine for combating Treponema hyodysenteriae infection in swine containing proteins or polypeptides typical of the hemolysin protein of Treponema hyodysenteriae or containing recombinant polynucleotides having as part thereof a polynucleotide coding for said protein or polypeptide, and also is concerned with the preparation of said proteins, polypeptides and polynucleotides.

Abstract: The invention relates to a method of preparing an optically active cyanohydrin by addition of hydrogen cyanide to a carbonyl compound, selected from aldehydes and ketones, in the presence of hydroxynitrile lyase, in a biphasic solvent system, comprising a homogeneous aqueous solution of said enzyme, and a suitable organic solvent which is at least substantially immiscible with water. Said method is performed in that said homogeneous aqueous solution is buffered with an acetate buffer having a buffer concentration of between 0.005 and 0.1 mole per liter or with a non-acetate buffer, that the volume ratio organic phase:aqueous phase is between approx. 5:1 and approx. 1:5, and that a solution of hydrogen cyanide and said carbonyl compound in said organic solvent is properly mixed during the reaction period with said homogeneous aqueous solution of hydroxynitrile lyase.

Abstract: The present invention is concerned with the preparation of erythro N-substituted vicinal aminoalcohol derivatives from hydroxyl-protected cyanohydrin derivatives by successive Grignard reaction, transimination using a primary amine, reduction of the resulting imine and removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the cyanohydrin derivatives.