Abstract: The present invention relates to new lipopeptides and in particular to compounds of either of the formulae ##STR1## wherein R.sub.1 and R.sub.2 each represent a saturated or unsaturated aliphatic or mixed aliphatic-cycloaliphatic hydrocarbon radical which has 11-21 C atoms and which is also optionally substituted by oxygen functions, R.sub.3 represents hydrogen or the radical R.sub.1 --CO--O--CH.sub.2 --, where R.sub.1 has the same meaning, R.sub.1 ' is a saturated or unsaturated aliphatic hydrocarbon radical of at least 9 C atoms, which is optionally substituted at one of the C atoms non adjacent to the sulfur atom by a free hydroxyl group or a hydroxyl group esterified with a monobasic carboxylic acid and which is optionally interrupted in the C atoms chain by one or more oxygen atoms, and which hydrocarbon is optionally substituted by a maximum of 2 cycloaliphatic hydrocarbon radicals having 5-8 ring C atoms, or R.sub.1 ' is the radical --CO--R.sub.1 ", wherein R.sub.

Abstract: Subject of the present invention are compounds of the formula ##STR1## which can be used as intermediates, wherein R represents hydrogen or R.sub.a, which represents an organic radical bonded to the ring carbon atom via a carbon atom,each of the radicalsR.sub.b and R.sub.c represents hydrogen or an organic radical bonded to the ring carbon atom via a carbon atom, it being possible for the two radicals to be bonded to one another,A represents a lower alkylene radical having 2 or 3 carbon atoms between the two hetero atoms, andn represents 0 or 2,the stereoisomers thereof and mixtures of these stereoisomers and also processes for the manufacture of such compounds of the formula I.From compounds of the formula I it is possible to manufacture 6-R.sub.a -2-penem-4-carboxylic acid compounds having antibiotic properties.

Abstract: The invention relates to a novel advantageous process for the production of compounds of the formula ##STR1## wherein n is 1, R.sub.1.sup.a is hydrogen or an amino protective group R.sub.1.sup.A, R.sub.1.sup.b is hydrogen or an acyl group Ac, or R.sub.1.sup.a and R.sub.1.sup.b together are a bivalent amino protective group, R.sub.2 is hydroxyl or a radical which, together with the carbonyl grouping --C(.dbd.O)--, forms a protected carboxyl group, and the group of the formula --N(R.sub.3.sup.a) (R.sub.3.sup.b) is a secondary or tertiary amino group, or a salt thereof with salt-forming groups. The process comprises reaction of the corresponding 3-amino compounds with borohydrides in the presence of acids.

Abstract: The invention relates to a novel and technically advanced process for producing 5-cyano-5H-dibenz[b,f]azepine by reacting 5H-dibenz[b,f]azepine with a halocyanogen in the presence of strongly polar substances. 5-Cyano-5H-dibenz[b,f]azepine can be used as starting material for producing 5-carbamyl-10(11)-oxo-10,11-dihydro-5H-dibenz[b,f]azepine, which is known to have central-depressant, anticonvulsive and central-muscle-relaxing activity.

Abstract: The present invention relates to novel pharmaceutical compositions having antiepileptic and antineuraglic action and containing (a) at least one anticonvulsive compound of the general formula I ##STR1## wherein X.sub.1 is hydrogen, halogen having an atomic number up to 35, or is cyano, and X.sub.2 and Y together are an additional bond, or X.sub.1 and X.sub.2 together are the oxo radical, or X.sub.1 is hydroxy, X.sub.2 is hydrogen and Y is also hydrogen, and (b) at least one nootropic compound of the vincamine type which has the general formula II ##STR2## wherein Z.sub.1 is lower alkoxycarbonyl, Z.sub.2 is hydroxy and Z.sub.3 is hydrogen, or Z.sub.2 and Z.sub.3 together are an additional bond, or one of Z.sub.1 and Z.sub.2 is hydroxy and the other is hydrogen and Z.sub.3 is also hydrogen, in particular vincamine (DCI rec.), in which Z.sub.1 is methoxycarbonyl, Z.sub.2 is hydroxy and Z.sub.3 is hydrogen, and also e.g., vinpocetin (DCI rec.), in which Z.sub.1 is ethoxycarbonyl and Z.sub.2 and Z.sub.

Abstract: Subject of the present invention are compounds of the formula ##STR1## which can be used as intermediates, wherein R represents hydrogen or R.sub.a, which represents an organic radical bonded to the ring carbon atom via a carbon atom,each of the radicalsR.sub.b and R.sub.c represents hydrogen or an organic radical bonded to the ring carbon atom via a carbon atom, it being possible for the two radicals to be bonded to one another,A represents a lower alkylene radical having 2 or 3 carbon atoms between the two hetero atoms, andn represents 0 or 2,the stereoisomers thereof and mixtures of these stereoisomers and also processes for the manufacture of such compounds of the formula I.From compounds of the formula I it is possible to manufacture 6-R.sub.a -2-penem-4-carboxylic acid compounds having antibiotic properties.

Abstract: The invention concerns 7-amino-ceph-3-em-4-carboxylic acid compounds of the formula ##STR1## wherein R.sub.1.sup.a represents hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.b represent hydrogen or an acyl group Ac, or R.sub.1.sup.A and R.sub.1.sup.b together denote a bivalent amino protective group, and R.sub.2 represents hydrogen or an organic radical R.sub.2.sup.A which together with the --C(.dbd.O)--O-- grouping forms a protected carboxyl group, or salts such compounds which possess salt-forming groups; these compounds have antibiotic properties.

Abstract: The present invention relates to a novel general process for synthesizing a .alpha.- or .beta.-oriented hydroxyacetyl side chain of steroids of the pregnane type, which comprises treating a corresponding steroid carbaldehyde in succession with formaldehyde dimethylmercaptal-S-oxide in the form of an alkali metal salt thereof, and with a strongly acid hydrolysing agent.Preferred final products are compounds of the formula ##STR1## wherein n is 1 or 2, R.sup.2 represents methyl or difluoromethyl, and R.sup.1 represents hydroxymethyl, methoxymethyl, acetoxymethyl or hydrogen, and, if n is 2 and/or R.sup.2 is difluoromethyl, R.sup.1 also represents methyl. These compounds act as agonists or antagonists of natural steroid hormones. The antigestagenic 19,21-dihydroxy-17.alpha.-pregn-4-ene-3,20-dione and its 6,7-dehydro derivatives and diacetates are of particular interest.

Abstract: There are described hexopyranose compounds of the formula I and salts thereof having immunomodulatory action, which can be used, for example, in the form of pharmaceutical preparations, and also together with antibiotics, and processes for their manufacture. ##STR1## The variables are as described in the disclosure. The invention relates to the above-mentioned compounds as immunomodulators, especially as immunostimulants, their use as pharmacologically active substances, especially their use as immunomodulators, particularly as immunostimulants, and their use for the manufacture of pharmaceutical preparations, and to pharmaceutical preparations containing these compounds.

Abstract: The invention relates to novel benzodioxole derivatives of the formula I ##STR1## in which R.sub.1 represents an unsubstituted or substituted, aromatic or heteroaromatic radical, alk represents an alkylene or alkylidene radical having a maximum of 5 carbon atoms, n represents 0 or 1, R.sub.2 and R.sub.3 each represents, independently of the other, hydrogen, lower alkyl, lower alkoxy or halogen, and A represents the radical O--R.sub.4, wherein R.sub.4 represents hydrogen or an unsubstituted or substituted, aliphatic or araliphatic hydrocarbon radical, or A represents the radical ##STR2## in which either R.sub.5 and R.sub.6 each represents, independently of the other, hydrogen or lower alkyl, or R.sub.5 and R.sub.6 are bonded to one another and, together with the adjacent nitrogen atom, represent unsubstituted or lower alkyl-substituted tetra- or hexa-methyleneimino or 4-morpholinyl, to salts of compounds of the formula I in which A represents OR.sub.4 wherein R.sub.

Abstract: The invention relates to pharmaceutical preparations that contain an antibiotic and a muramylpeptide of the formula I or a salt thereof, to processes for their manufacture and to a method for increasing the antibiotic effectiveness of antibiotics. ##STR1## In the formula I, X represents carbonyl or carbonyloxy, R.sub.1 represents optionally substituted alkyl or aryl, R.sub.2, R.sub.3, R.sub.4 and R.sub.6 represent hydrogen or lower alkyl, R.sub.5 represents hydrogen, optionally substituted lower alkyl, cycloalkyl, aryl or nitrogen-containing heterocyclyl, or R.sub.4 and R.sub.5 together represent also C.sub.3 -C.sub.4 alkylene, R.sub.7 represents hydrogen or free, esterified or amidated carboxyl, one of the radicals A.sub.1 and A.sub.2 represents a radical of the formula II and the other of the radicals A.sub.1 and A.sub.2 represents optionally substituted or functionally modified hydroxy or amino.

Abstract: New antibiotically active compounds having the basic structure of rifamycin S, namely 3-hydroxyrifamycin S (formula A: X=>C.dbd.O; R.sup.1 =OH; R.sup.2 =H), 3,31-dihydroxy-rifamycin S (formula A: X=>C.dbd.O; R.sup.1 =R.sup.2 =OH) and 1-desoxy-1-oxarifamycin S (formula A: X=--O--; R.sup.1 =R.sup.2 =H) ##STR1## are formed by cultivating, under aerobic conditions, a strain of Nocardia mediterranei which is derived from Streptomyces mediterranei ATCC 13 685 as the parent strain and is characterized by the ability to produce at least one of the mentioned compounds. The recombinant strain Nocardia mediterranei DSM 1415 has proved suitable. The mentioned rifamycin S analogues have analogous antibiotic properties to this but have a wider range of action, especially against gram-negative bacteria.

Abstract: Phosphorylmuramyl peptides of the formula ##STR1## are immuno-potentiating. In the formula, R.sub.1 represents optionally substituted alkyl or aryl, R.sub.2, R.sub.4, R.sub.6 and R.sub.7 represent, for example, hydrogen, R.sub.3 represents hydrogen or lower alkyl, R.sub.5 represents, for example, hydrogen, lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl, or nitrogen-containing heterocyclyl or heterocyclyl-lower alkyl, and one of the radicals A.sub.1 and A.sub.2 represents a radical of the formula (II) ##STR2## In the formula (II), T represents NH or O, Y represents an optionally substituted alkylene group, which may also be interrupted by one or two oxycarbonyl and/or iminocarbonyl groups, and W represents an aliphatic radical or a cycloalkyl or cycloalkenyl radical having more than 6 carbon atoms. The other of the radicals A.sub.1 and A.sub.2 represents free or etherified hydroxy, amino, lower alkylamino or aminocarbonyl-lower alkylamino.

Abstract: The invention relates to a method of preventing or treating cerebral insufficiency, which method comprises administering to a human being in need of such treatment, orally or rectally, a prophylactic or a therapeutically effective amount of a compound of the general formula I ##STR1## wherein X.sub.1 is hydrogen, halogen having an atomic number up to 35, or is cyano, and X.sub.2 and Y together are an additional bond, or X.sub.1 and X.sub.2 together are the oxo radical and Y is hydrogen, or X.sub.1 is hydroxy and X.sub.2 and Y are hydrogen. Examples of suitable compounds are 10,11-dihyro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxamide, 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepine-5-carboxamide and, in particular, carbamazepine (5H-dibenz[b,f]azepine-5-carboxamide).

Abstract: The invention relates to pharmaceutical preparations for topical application which contain salts of alkanecarboxylic acids, in particular compounds of the formula ##STR1## wherein R.sub.1 is a group of the formula ##STR2## wherein X.sub.1 and X.sub.2 are hydrogen and X.sub.3 is isobutyl, or X.sub.1 and X.sub.3 are hydrogen and X.sub.2 is benzoyl, or X.sub.1 is hydrogen, X.sub.2 is chlorine, and X.sub.3 is 3-pyrrolin-1-yl, or X.sub.1 is hydrogen, X.sub.2 is a group of the formula --CH.dbd.CH--C(OCH.sub.3).dbd.CH--X.sub.4, and X.sub.3 together with X.sub.4 are a bond, and R.sub.2 is methyl, or X.sub.2 and X.sub.3 are hydrogen and X.sub.1 is 2,6-dichloroanilino, and R.sub.2 is hydrogen, or R.sub.1 is a group of the formula ##STR3## wherein X.sub.5 is the common bond with the methine group in formula I, X.sub.6 and X.sub.7 are hydrogen, X.sub.8 is p-methylbenzoyl, Y is a nitrogen atom, and X.sub.9 is a methyl group, or X.sub.5 is a methyl group, X.sub.6 is a common bond with the methine group in formula I, X.sub.

Abstract: The invention relates especially to 2-(3'-hydroxypyrid-2'-yl)-2-thiazoline-4-carboxylic acid derivatives of the formula (I) and salts and also certain metal complexes of these compounds, processes for their manufacture, pharmaceutical agents containing such compounds and the use of these compounds. ##STR1## In the formula, R.sup.1 represents free, etherified or esterified hydroxy, R.sup.2 represents hydrogen or an aliphatic, carbocyclic or carbocyclic-aliphatic radical having 1-12 carbon atoms, and R.sup.3 represents hydrogen or an unsubstituted aliphatic radical having 1-7 carbon atoms.The compounds of the formula (I) can be used, for example, for the abstraction of heavy metals from the organism of warm-blooded animals and/or they have an antibiotic action.

Abstract: Described are derivatives of pyranoses of the formula I, manufacturing processes and intermediates, and their use as medicaments. ##STR1## The pyranose moiety in the compounds of the formula I is derived especially from D-glucose, but alternatively from D-galactose or D-mannose.Characteristic of the compounds of the formula I is the lower alkyl or phenyl-lower alkyl radical R.sub.8, which carries an oxycarbonyl, mercaptocarbonyl or aminocarbonyl group, which is bonded to an aliphatic, cycloaliphaticaliphatic, cycloaliphatic or aromatic hydrocarbon radical R.sub.0, each of which is optionally substituted and which may be interrupted by oxycarbonyl, mercaptocarbonyl and/or iminocarbonyl and which, like the remaining radicals of the formula I, is defined in patent claim 1.

Abstract: The invention relates to muramyl peptide compounds, especially of the formula ##STR1## in which R.sub.1 represents, for example, alkyl or phenyl,R.sub.3 represents, for example, hydrogen or methyl andR.sub.5 represents, for example, hydrogen or lower alkyl optionally substituted, for example, by hydroxy, mercapto, or methylthio,and in which one of the radicalsA.sub.1 and A.sub.2 represents a group of the formula ##STR2## in which T represents the group of the formula -NH or -O, andY represents an alkylene radical optionally interrupted by a radical of the formula -CO-O- or -CO-NH-,and in whichW represents hydrogen andZ represents a hydroxy-substituted ethyl group, wherein at least one hydroxy group is esterified by a long-chained acyl radical orW and Z represent hydroxymethyl, wherein hydroxy is esterified by a long-chained acyl radical,and the other of the radicals A.sub.1 and A.sub.2 represents optionally etherified hydroxy or optionally substituted amino.

Abstract: A novel method of diagnosis of atherosclerosis comprises comparing the migration of endothelial cells or of cells of endothelium-like morphology in vitro, in the presence of serum from the person being examined, with the migration of identical cells in the presence of serum from healthy persons or of other standard sera, and interpreting a reduced migration in the presence of serum of the person being examined as being an indication of the possible existance of atherosclerosis in this person. The cell migration is measured for example on monolayer cell cultures of pig aorta endothelial cells or of Balb/c 3T3-A31 cells, in which cultures a portion of the cellular layer has been removed. An outfit for carrying out the method contains the materials and devices necessary for the purpose.

Abstract: Rheumatoid arthritic and like diseases involving joint inflammation are treated by administering desferrioxamine in a therapeutically effective dosage over a prolonged period.