Abstract: Vasodilatory eburnamine-type alkaloid esters of the formula (I) ##STR1## and salts and quaternary derivatives thereof, wherein X.about.Y REPRESENTS A =CH=CH- or ##STR2## R represents a C.sub.1-6 alkoxycarbonyl group optionally substituted with a hydroxy group or with a halogen atom, further an alkenyloxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl group or an acylated primary alcohol group, especially apovincaninic acid ethyl ester, have been prepared by various methods of esterification.

Abstract: New benzodiazepine derivatives of the formula (I), ##STR1## wherein R.sub.1 stands for halogen, trifluoromethyl, nitro or amino,R.sub.2 stands for hydrogen or alkyl, andR.sub.3 stands for nitroso, amino, alkylideneamino, substituted alkylideneamino, aralkylideneamino, substituted aralkylideneamino, acylamido or substituted acylamido.The new compounds possess remarkable enzyme-inducing effects and exert only moderate central nervous activities.

Abstract: New tricyclic fused imidazole derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##STR2## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a=C-- group, orA stands for a group of the general formula (III), ##STR3## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##STR4## wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##STR5## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(ch.sub.2).sub.m --X VI.in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen.

Abstract: New compounds of the general formula (I) ##SPC1##whereinR.sub.1 and R.sub.2 each is a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form substituted or unsubstituted heterocyclic group with or without a further oxygen or nitrogen heteroatom, andR.sub.3 is hydrogen or an acyl group derived from a C.sub.1.sub.-18 carboxylic acid.The compounds are prepared by reducing the corresponding nitro compounds of the general formula (II) ##SPC2##and optionally acylating the obtained product.The compounds of the general formula (I) and their acid addition salts and quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess valuable antipyretic activity and a yohimbine lethality increasing effect characteristic of antidepressants.

Abstract: Pharmaceutically active steroids of the formula (I) ##SPC1##whereinX.sub.1 and X.sub.2 each is hydrogen, mercapto or acetylthio andX.sub.3 and X.sub.4 each is hydrogen or acetylthio orX.sub.3 and X.sub.4 form together a valence bond, with the proviso that at least one of X.sub.1 to X.sub.4 is selected from the group consisting of mercapto and acetylthio. The compounds are prepared as follows: a compound of the formula (III) ##SPC2##wherein Z.sub.1 is hydrogen and Z.sub.2 is hydrogen or acetylthio or Z.sub.1 and Z.sub.2 form together a valence bond, is brominated, the thus-obtained compound of the formula ##SPC3##Wherein Y.sub.1 and Y.sub.2 each is hydrogen or bromine, Y.sub.3 is bromine, Y.sub.4 is hydrogen or acetylthio or Y.sub.3 and Y.sub.4 form together a valence bond, is reacted with an alkali methal thioacetate or with an alkali metal hydrosulphide. Thioacetic acid can be coupled onto the obtained product, and/or optionally the obtained thioacetyl compound can be subjected to alcoholysis.

Abstract: New compounds of the general formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form an optionally substituted heterocyclic group optionally containing a further oxygen or nitrogen hetero atom,But if R.sub.1 stands for methyl, R.sub.2 may only stand for a group other than methyl,Are prepared by reacting a compound of the general formula (II), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2 (iii)wherein R.sub.1 and R.sub.2 each have the same meanings as defined above.The new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.

Abstract: The invention is a new process for the preparation of .alpha.-ethynyl-benzohydrols and of ring-substituted derivatives thereof by reacting the starting benzophenone or a ring-substituted derivative thereof with acetylene in a solvent delivering no protons, in the presence of an alkali metal tertiary alcoholate, preferably potassium-tert.-butylate or potassium-tert.-amylate. Also new substituted derivatives of .alpha.-ethynyl-benzhydrol are prepared by the invention.

Abstract: New compounds of the formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straightchained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom form a substituted or unsubstituted heterocyclic group which can contain a further oxygen or nitrogen hetero atom,But when R.sub.1 is methyl, R.sub.2 is a group other than methyl, are prepared by reacting a compound of the formula (II), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2. (iii)the new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.

Abstract: The invention relates to the preparation of biologically active polypeptides containing the aspartyl group, particularly an aspartyl-glycine moiety, using the active-ester technique.According to the method of the invention, human adrenocorticotropic hormone and its fragments characteristic to the individual species, as well as the blocked derivatives of such compounds are prepared by the pentafluorophenol method, i.e., the carboxy group of the acylating component is activated by converting it into pentafluorophenyl ester in the coupling reaction carried out with blocked peptides containing the aspartyl group or an aspartylglycine moiety. The acylation is carried out preferably using equimolar quantities of the respective reactants. The free peptides obtained after removing the blocking groups can be converted into their acid addition salts or pharmaceutically acceptable complexes or condensates.Human adrenocorticotropic hormone and its derivatives are valuable substances of therapeutical activity.

Abstract: New tricyclic fused imidazole derivatives of the general formula (I), ##SPC1##whereinR.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##EQU1## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a =C-- group, orA stands for a group of the general formula (III), ##EQU2## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##SPC2##wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##EQU3## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(CH.sub.2).sub.m --X (VI)in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen.