Abstract: Process for the biotechnological preparation of L-thienylalanines in enantiomerically pure form from 2-hydroxy-3-thienylacrylic acids, and their use.L-Thienylalanines are prepared via the hydantoin or the azlactone route. The starting substances used for the biotransformation are 2-hydroxy-3-thienylacrylic acids. The innovative step consists in the transamination of the enol form of the 2-hydroxy-3-thienylacrylic acids to give L-thienylalanines with the aid of biotransformation. The transaminiation is carried out in the presence of L-aspartic acid or L-glutamic acid as amino donor.

Abstract: Process for the biotechnological preparation of L-thienylalanines in enantiomerically pure form from 2-hydroxy-3-thienylacrylic acidsL-Thienylalanines are prepared via the hydantoin or the azlactone route. The starting substances used for the biotransformation are 2-hydroxy-3-thienylacrylic acids. The innovative step consists in the transamination of the enol form of the 2-hydroxy-3-thienylacrylic acids to give L-thienylalanines with the aid of biotransformation. The transaminiation is carried out in the presence of L-aspartic acid or L-glutamic acid as amino donor.

Abstract: L-Thienylalanines are prepared via the hydantoin or the azlactone route. The starting substances used for the biotransformation are 2-hydroxy-3-thienylacrylic acids. The innovative step consists in the transamination of the enol form of the 2-hydroxy-3-thienylacrylic acids to give L-thienylalanines with the aid of biotransformation. The transaminiation is carried out in the presence of L-aspartic acid or L-glutamic acid as amino donor.

Abstract: A process for the preparation of racemic and optically active 1,2.3,4-tetrahydroisoquinoline-3-carboxylic acid is described, in which dihalo-o-xylylenes are cyclized to dicarboxylic acid esters in basic medium using dialkyl N-acylamidomalonates of the formula (CO.sub.2 R.sup.1).sub.2 CHNHCOR.sup.2, in which R.sup.1 is (C.sub.1 -C.sub.4)-alkyl and R.sup.2 is H, (C.sub.1 -C.sub.4)-alkyl or (C.sub.6 -C.sub.

Abstract: Two processes are described for the preparation of the optically pure compounds of formula 1: ##STR1## in which R.sup.1 and R.sup.2 are e.g. alkyl, R.sup.3 and R.sup.4 are e.g. hydrogen and R.sup.5 is e.g. hydrogen. Both processes include, as key steps, the enantioselective hydrogenation of a C.dbd.C double bond and the regioselective formation of a dicarboxylic acid monoamide derivative. In one process a phenylitaconic acid derivative is asymmetrically hydrogenated to give an optically active (R)-benzylsuccinic acid which is then converted to a diester, said diester being converted to the monoamide compound of formula 1. In the second process, a phenylitaconic acid derivative is converted to its anhydride, and the anhydride is then converted to a monoamide which is then asymmetrically hydrogenated to give the compound of formula 1.

Abstract: A process for the preparation of racemic and optically active 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is described, in which dihalo-o-xylylenes are cyclized to dicarboxylic acid esters in basic medium using dialkyl N-acylamidomalonates of the formula (CO.sub.2 R.sup.1).sub.2 CHNHCOR.sup.2, in which R.sup.1 is (C.sub.1 -C.sub.4)-alkyl and R.sup.2 is H, (C.sub.1 -C.sub.4)-alkyl or (C.sub.6 -C.sub.

Abstract: The invention relates to new comoounds having a cognition adjuvant action, to the use of ACE inhibitors as medicaments having a cognition adjuvant action, to agents containing them, and to the use thereof for the treatment and prophylaxis of cognitive dysfunctions.

Abstract: The invention relates to compounds of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.4 represent optionally substituted aliphatic, alicyclic, alicyclic-aliphatic, aromatic, araliphatic, heteroaromatic or heteroaromatic-aliphatic radicals, with R.sup.2, if not already covered by the above-mentioned definitions, denoting the side-chain, which is protected if necessary, of a naturally occurring .alpha.-amino acid, R.sup.4 can additionally represent ##STR2## R.sup.3 denotes an optionally substituted aliphatic, alicyclic, aromatic or araliphatic radical, or R.sup.3 and R.sup.4 form, together with the atoms carrying them, a mono-, bi- or tricyclic heterocyclic ring system,agents containing these, and the use thereof as pharmaceuticals having a psychotropic action for the prophylaxis of disorders of the central nervous system, especially having a nootropic action for the treatment of cognitive dysfunctions.

Abstract: The invention relates to amino acid esters of the formula I ##STR1## in which n is 2 and R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning indicated in the description, to a process and intermediates for the preparation thereof, to agents containing them, and the use thereof.

Abstract: A description is given of compounds I ##STR1## with R(1) equal to H, alkyl, alkoxy, Hal, NO.sub.2, OH, acetamido or amino; R(2) equal to H, alk(en)yl or phenylalkyl; R(3) equal to H, (cyclo)alk(en)yl(alkyl), phenyl or phenylalkyl; R(4) equal to H, alkyl, alkoxy, Hal CF.sub.3, NO.sub.2, OH, acetamido or amino; A equal to --C.tbd.C-- or --CH.dbd.CH--; R(5) equal to various amines; m and n equal to 1-3; and their salts. Preparation processes are also described. Compounds I are excellent calcium agonists or calcium antagonists. They also act to regulate the blood glucose.

Abstract: Compounds I ##STR1## in which R(1) and R(4) equal H, alkyl, alkoxy, Hal, CF.sub.3, NO.sub.2, OH, acetamido or amino;R(2) equals H, alk(en)yl or phenylalkyl (optionally substituted);R(3) equals H, (cyclo)alk(en)yl-(alkyl), phenyl or phenylalkyl (optionally substituted);A equal CHOH, CO, CH.dbd.CH, C.tbd.C, CH.sub.2, O or S;m equals 1 or 2;n equals 1 to 3;p equals 0 to 4;R(5) equals some amino groups, and their salts, exhibit excellent calcium-antagonistic activity.Processes for their preparation are described.

Abstract: Calcium antagonists of the formula ##STR1## with R(1), R(2), R(3) and R(4) being, inter alia, H, alkyl, alkoxy, halogen, in some cases phenyl; m being 1-4; n being 0-3; X being CH.sub.2, O, S, CO, CHOH or CR.sub.2, and R(5) being various groups containing nitrogen atoms, are described.They are obtained by reaction of compounds II which are likewise new and which contain in place of R(5) a leaving group Y (Cl, Br, I) with the appropriate (cyclic) amino compound.Another synthesis comprises reaction of the appropriate indollinone derivative IV which has a non-etherified hydroxyl group with a side chain which contains a terminal leaving group Z (Cl, Br, I) in the presence of a base.Furthermore, indolinone derivatives VI with an ether side chain with a terminal epoxide group can be reacted with (cyclic) amines to give compounds I.

Abstract: Calcium antagonists of the formula ##STR1## with R(1), R(2), R(3) and R(4) being, inter alia, H, alkyl, alkoxy, halogen, in some cases phenyl; m being 1-4; n being 0-3; X being CH.sub.2, O, S, CO, CHOH or CR.sub.2, and R(5) being various groups containing nitrogen atoms, are described.They are obtained by reaction of compounds II which are likewise new and which contain in place of R(5) a leaving group Y (Cl, Br, I) with the appropriate (cyclic) amino compound.Another synthesis comprises reaction of the appropriate indolinone derivative IV which has a non-etherified hydroxyl group with a side chain which contains a terminal leaving group Z (Cl, Br, I) in the presence of a base.Furthermore, indolinone derivatives VI with an ether side chain with a terminal epoxide group can be reacted with (cyclic) amines to give compounds I.

Abstract: Benzothiazinone derivatives I ##STR1## with R.sup.1 and R.sup.4 being H, alkyl, alkoxy, Hal, CF.sub.3, NO.sub.2, OH, acetamido or amino,R.sup.2 being H, (cyclo)alk(en)yl, cycloalkylakyl, phenyl or phenylalkyl,A being (CH.sub.2).sub.m O(CH.sub.2).sub.n, (CH.sub.2).sub.p --CH(OH)--CH.sub.2).sub.q, (CH.sub.2).sub.p --CH(OCH.sub.3)--(CH.sub.2).sub.q, or (CH.sub.2).sub.r OCH.sub.2 --CO-- and (CH.sub.2).sub.s --CO--,R.sup.5 being NR(6)R(7) or certain cyclic amines, show a calcium-antagonistic action.They are obtained, inter alia, from II ##STR2## by reaction with III ##STR3## A and B are same or different and are lower alkylene having 1 to 6 carbon atoms; and n is 3 to 4.

Abstract: Compounds of the formula I ##STR1## where R(1), R(2), R(3), R(4) and R(5) are, inter alia, hydrogen and alkyl, m is 1-4, n is 0 or 1, p is 0-4 and R(6) is identical or different dialkylamine derivatives, and salts thereof, have a calcium-antagonistic action. They are obtained by reacting corresponding amines with a compound II which carries, on the side chain, a leaving group which can be displaced nucleophilically, or from a hydroxyphenyl-dihydroquinolin-2-one compound by reaction with a corresponding side chain compound which has a leaving group which can be displaced nucleophilically.

Abstract: The invention relates to a process for resolving racemic mixtures of bicyclic imino-.alpha.-carboxylic acid esters into the components of the formula Ia and Ib ##STR1## in which R.sup.1 stands for an aliphatic, cycloaliphatic, aromatic or araliphatic radical,A denotes hydrogen and B and C together form a carbon chain or C denotes hydrogen and A and B together form a carbon chain, by crystallizing diastereoisomeric salts, which comprises preparing the salts of the racemic esters with optically active O,O-diacyltartaric acids in a suitable solvent in which only one of the two diastereoisomeric salts crystallizes in optically pure form, if desired purifying the diastereoisomeric salt by recrystallization, reprecipitation or trituration, and finally adding basec to the salt to cleave it into the pure enantiomer of the formula Ia or Ib.The invention also relates to diastereoisomeric salts of an ester of the formula Ia or Ib and a diacyltartaric acid.

Abstract: The winder shaft for a sewing machine, fashioned as a support for a thread bobbin, is positioned directly on the shaft of a low-voltage motor, independent of the drive motor for the sewing mechanism of the sewing machine. An on/off switch for this motor is operable by means of a three-armed switching lever, with the first arm being adapted to scan the package of wound thread forming on the bobbin. A trigger cam disposed on the third arm slides, during this operation, over a first surface of a spring-biased dual ramp. Once the thread bobbin is full, the trigger cam surpasses the apex of the dual ramp, and the switching lever flips into a disconnect position and cuts off the motor by way of a switching cam disposed on the second arm. All of the elements of the spooling device are mounted to a common support so that the spooling device, which is independent of the drive mechanism of the sewing machine, can be attached as a composite unit at any desired location on the sewing machine.

Abstract: Benzothiazine derivatives of the formula I ##STR1## with (R(1), R(1)', R(1)", R(4) and R(4)' equal to hydrogen, alkyl, alkoxy, halogen, nitro, hydroxyl, acetamido or amino; R(2) equal to hydrogen, alkyl, alkenyl, phenyl; R(3) equal to hydrogen, alkyl, alkenyl, phenyl; R(5) equal to hydrogen or (C.sub.1 -C.sub.

Abstract: What is disclosed are prostacyclin analogs of the general formula I ##STR1## which have a more specific action and/or a longer action than the naturally occurring prostacyclin PGI.sub.2, as well as intermediate products for their preparation and a process for their preparation. The compounds of formula I are distinguished by inhibitory action on thrombocyte aggregation and by relaxation of the vascular walls, in particular of the coronary arteries. They can thus be used as medicaments.

Abstract: The invention relates to new prostaglandin derivatives of the 6-keto-PGE.sub.1 series, to processes and intermediates for their manufacture and to their use as medicaments.