Abstract: The invention relates to (+) and (-)-8-halogen-6-hydroxy-octanoic acid enantiomers wherein the halogen is Cl, Br, or I, and their respective preparatory processes.

Abstract: Anticonvulsive compounds and compositions, of the formula ##STR1## in which X is a C.sub.1-4 -alkyl, trifluoromethyl, or halogen residue, Y is hydrogen or halogen, n is 0 or 1, and m is 0 or a cardinal number from 1 to 4, and its pharmacologically acceptable acid addition salts.

Abstract: 1,3,5-trisubstituted indazole derivatives of the formula ##STR1## wherein R1 is H, (b) a C.sub.1-6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C.sub.3-7 cycloalkyl residue, (d) an unsustituted or substituted phenyl, naphthyl, anthranyl, or fluorenyl residue, (e) a quinolin-2-ylmethoxy, or pyridin-2-ylmethoxy residue; X is O, or a --NH, --NH--(C.dbd.O)--NH--, --NH--(C.dbd.O)--O--, --NH--(C.dbd.O)--, or --NH--CH.sub.2 --(C.dbd.O)-- residue; Y is O, or S; R.sub.2 is H; Z is a SO, SO.sub.2, --(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --O--, --O--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--, --(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--NH--, --NH--(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CHOH--, --CHOH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CH.dbd.CH--, or --CH.dbd.CH--(CH.sub.2).sub.

Abstract: The synthesis of pure enantiomers of 8-chloro-6-sulfonyloxy-octanoic acids and their alkyl esters and of pure enantiomers of 6,8-dichloro-octanoic acid and its alkyl esters as intermediates for the synthesis of the enantiomers of .alpha.-liponic acid as well as a method for converting the two enantiomers of 8-chloro-6-hydroxy-octanoic acid into an enantiomer of .alpha.-liponic acid.

Abstract: The invention is directed to 3-aminopyrroles of formula I, which are largely new, to methods for the preparation and to their use as medicinal agents and preparations, as well as to anti-convulsive or analgesic preparations containing these 3-aminopyrroles.Disubstituted and monosubstituted amino groups are claimed as 3-amino substituents.The invention pursues the objective of developing largely new 3-aminopyrroles, which have CNS activity, particularly ones which anti-convulsive or analgesic properties, as well as methods for their preparation and their use as medicinal preparations.Pursuant to the invention, the synthesis is carried out by cyclizing open-chain precursors, such as aminoacrylic acid derivative, or by modifying pyrroles.

Abstract: A process for determining the concentration of cyclosporine in a sample, which comprises adding to the sample a predetermined amount of an isomerase which isomerizes N-terminal peptide to proline, then measuring the enzyme-catalyzed inhibition of the isomerization of a proline-containing substrate, and determining the concentration or cyclosporine from a calibration curve.

Abstract: The invention is directed to N-acetyl-4-phenyl-pyrrolidin-2-ones, which, because of their pronounced cerebroprotective effect in human medicine, can be used for the prophylaxis and treatment of cerebral functional disorders. Pursuant to the invention, these compounds are synthesized by reacting 4-phenyl-pyrrolidin-2-ones with a reactive derivative of a carboxylic acid, or by cyclizing N-acylaminobutyric acid derivatives.

Abstract: A prophylactic pretreatment for nerve gas and pesticide poisons which can be administered orally and which comprises the following agents, in combination: a. Pyridostigmine (pyridostigmine bromide) b. Diazepam c. N-methyl-4-pipyridinyl phenylcyclopentanecarboxylateThese agents may be administered in the form of a capsule which contains, for example, tablets, one a normal release dosage form and one or two in a slow release dosage form.

Abstract: A process for producing pharmacologically active 1-unsubstituted 3-aminopyrroles of the formula ##STR1## by ring transformation of a corresponding 1,2-thiazolium pyrrole in a single step, without producing harmful byproducts.

Abstract: A method for preparing high bulk density crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine which comprises precipitating a high bulk density crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine from a starting material that is(a) a solution in an inorganic or organic acid, and precipitating with a base, or(b) a solution in a chlorinated hydrocarbon, and precipitating with an aliphatic hydrocarbon, or(c) from an aliphatic ester of an aliphatic carboxylic acid and an aliphatic alcohol.The compact, crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine, so obtained, has a bulk density of from about 220 to about 360 g/l and is most suitable for pharmaceutical preparations.

Abstract: 5-(w-Aminoacyl)-5,10-dihydro-11H-dibenzo(b,e)(1,4)-diazepine-11-ones, and their preparation are disclosed for treatment of antiarrhythmia and as an anticholinergic drug.

Abstract: A method for preparing high bulk density crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine which comprises precipitating a high bulk density crystaline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine from a starting material that is(a) a solution in an inorganic or organic acid, and precipitating with a base, or(b) a solution in a chlorinated hydrocarbon, and precipitating with an aliphatic hydrocarbon, or(c) from an aliphatic ester of an aliphatic carboxylic acid and an aliphatic alcohol.The compact, crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine, so obtained, has a bulk density of from about 220 to about 360 g/l and is most suitable for pharmaceutical preparations.

Abstract: New 3-carbalkoxyamino-5-(alpha-aminopropionyl)-5H-dibenz[b,f]azepines of formula I and their pharmaceutically acceptable salts were found to be suitable actives for the treatment of cardiac arrhythmia. Previously unknown 3-carbalkoxyamino-5-(alpha-halogenpropionyl)-5H-dibenz[b,f]azepines are obtained from 3-carbalkoxyamino-5H-dibenz[b,f]azepines by reaction with alpha-halogenpropionyl halides. Through their reaction with ammonia, primary amines or secondary amines, the new 3-carbalkoxyamino-5-(alpha-aminopropionyl)-5H-dibenz[b,f]azepines are obtained, which can be optionally converted into their pharmaceutically acceptable acid addition salts.

Abstract: A process for producing carbamazepine ##STR1## by (i) optionally purifying a solution of CCDA ##STR2## in an anhydrous, aromatic solvent; (ii) if required distilling off water in the solution; (iii) diluting the water-free solution with an additional amount of the anhydrous, aromatic solvent; (iv) in a reactor aminating the diluted solution at from about 70.degree. C. to about 105.degree. C.

Abstract: The substituted 5-(phenoxyalkanoylamino)-uracil compounds have the following formula I: ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen; a branched or linear alkyl group having 1 to 6 carbon atoms; a branched or straight chain alkenyl or alkynyl group having 1 to 6 carbons atoms; a cycloalkyl group having from 3 to 7 carbon atoms or a cycloalkylmethyl group having a cycloalkyl residue of 3 to 7 carbon atoms; or a phenylalkyl group having an alkyl residue having from 1 to 3 carbon atoms and a phenyl residue, the phenyl residue being unsubstituted or having a halogen, methoxy, methyl or trifluoromethyl substituent; R.sub.3 is a hydrogen, methyl or amino groups; R.sub.4 is halogen, methoxy or methyl groups, and n is 1 or 2.

Abstract: A 3-cyano-5,4'-bipyridine-1'-oxide of the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R is an amino, alkoxy, oxyalkoxy or chloro residue, have heart stimulating cardiotonic and vasodiolatory properties. They can be preparaed by (a) converting an R-substituted-3-cyano-bipyridine to its corresponding N-oxide, or (b) by substituting an R-residue or an R-unsubstituted precursor of the conpound of fomula (i), and if required, converting the product into its pharmaceutically acceptable acid addition salt.

Abstract: New 3-carbalkoxyamino-5-aminoacyl-5H-dibenz[b,f]azepines and their pharmaceutically acceptable acid addition salts, and methods for their synthesis are described. These compounds are useful as antiarrhythmic agents in the treatment of heart disorders. The new compounds are made by reacting a 3-carbalkoxyamino-5-halogenacyl-5H-dibenz[b,f]azepines with an amine to form the desired target product, which can be optionally converted into its pharmaceutically acceptable acid addition salt.

Abstract: The invention is directed to a process for the synthesis of 5-chlorocarbonyl-5H-dibenz[b,f]azepine, which is the precursor for the industrial scale synthesis of 5-carbamoyl-5H-dibenz[b,f]azepine. The latter substance is used as pharmaceutical compound. In the process phosgene is passed into a suspension of iminostilbene in an inert solvent at 20.degree. C.-60.degree. C. until the iminostilbene reacted to form an almost equimolar mixture of 5-chlorocarbonyl-5H-dibenz[b,f]azepine and iminostilbene hydrochloride, and then iminostilbene is released from the iminostilbene hydrochloride by the addition of an aqueous base. The iminostilbene so released is also made available for a complete phosgenation while an acidic reaction environment is maintained. After the iminostilbene reacted completely, the reaction mixture is heated slowly to 20.degree. C.-90.degree. C. with stirring and is detoxified by the hydrochloric acid that is formed.

Abstract: Hydroxamic acids, pharmaceutical preparations containing the same, new .omega.(2'-naphthoxy)-alkylhydroxamic acids as well as a process for their production are disclosed. The new compounds display antiasthmatic and further pharmacologically valuable characteristics. They are prepared by reacting the corresponding carboxylic acid ester or amide with hydroxylamine or its salt under the described conditions into compounds of Formula I,R--CO--NH--OH.The compounds of Formula I are useful in human and veterinary medicine as medicaments the active principal of which is the inhibition of lipoxygenase, thus as antiasthmatic, antianaphylactic, antiphlogistic, antirheumatic and antithrombotic preparations.

Abstract: A method is disclosed for production of 1-alkyl-4(1H)-oxo-cinnolin-3-carboxylic acids. Mesoxalic acid dialkylester-3,4-methylenedioxy-phenylhydrazone is saponified using 1 to 1.5 Mol alkali into the corresponding monoalkylester, which is cyclicized with a Friedel-Crafts catalyst in the presence of a carboxylic acid anhydride into 6,7-methylenedioxy-4(1H)-oxo-cinnolin-3-carboxylic acid alkylester, which is alkylated with a C.sub.1 -C.sub.4 alkyl halogenide in the presence of alkali in a suitable solvent, after which the ester is saponified. Small amounts of byproduct alkylated in the 2-position are removed by brief heating and precipitation from alkaline solution, leaving a pure 1-alkyl product. The product is useful for the treatment of urinary tract infections.