Abstract: The invention relates to new benzhydrylpiperazine derivatives of the formula (I) ##STR1## wherein n is 2 or 3, and acid addition salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. More particularly, they inhibit the microsomal monooxigenase enzyme system of liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

Abstract: The invention relates to racemic or optically active E-homo-eburnane derivatives of the formula /I/, ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and acid addition salts thereof.The new compounds are pharmaceutically active, for example their certain representatives, in particular from the cis-series, show antidepressive activity, while others, especially the compounds of the trans-series, are potent anthypoxial agents. The compounds of the formula /I/ and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions.

Abstract: A tranquillo-sedative substituted 1,3,4,5-tetrahydro-2H-1,4-benzodiazepine-2-one of the formula (I), ##STR1## wherein R.sub.1 is halogen or nitro,R.sub.2 is hydrogen or methyl,R.sub.3 is --CONH.sub.2 or --CONHCH.sub.3, andR.sub.6 is phenyl or halophenyl.

Abstract: The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),X--Y--W--NH.sub.2 (I)whereinX is L-pyroglutamyl, D-pyroglutamyl, L-2-keto-imidazolidine-4-carbonyl, L-6-keto-pipecolyl, L-thiazolidine-4-carbonyl, L-prolyl or orotyl group,Y is L-leucyl, L-norvalyl or L-histidyl group, andW is L-prolyl, D-prolyl, L-thiazolidine-4-carbonyl, L-pipecolyl, L-homoprolyl, L-leucyl, L-isoleucyl, L-methionyl or D-pipecolyl group, orthe W-NH.sub.2 group stands for pyrrolidyl or piperidyl group, with the proviso that if X is L-pyroglutamyl and Y is L-histidyl group, W is other than L-prolyl group, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.

Abstract: The invention relates to new tetrahydro-1,2,4-oxadiazin-5-one derivatives having a CNS activity. More particularly, the invention concerns new N.sup.4 -substituted tetrahydro-1,2,4-oxadiazin-5-ones of the formula (1) ##STR1## wherein R.sup.2 is benzyloxycarbonyl or alkylcarbonyl containing 1 to 4 carbon atoms in the alkyl moiety, preferably acetyl;R.sup.3 is phenyl optionally substituted with 1 to 3 lower alkoxy groups; andR.sup.4 is an aliphatic or cyclic alkyl group having 1 to 11 carbon atoms, hydroxymethyl, halomethyl or acyloxymethyl.According to another aspect of the invention there are provided processes for the preparation of compounds of formula (1). Still another aspect of the invention is a pharmaceutical composition which comprises as active ingredient a compound of formula (1).

Abstract: A tranquillo-sedative substituted 1,3,4,5-tetrahydro-2H-1,4-benzodiazepine-2-one of the formula (I), ##STR1## wherein R.sub.1 is halogen or nitro,R.sub.2 is hydrogen or C.sub.1 to C.sub.6 alkyl,R.sub.3 is --CONH.sub.2, andR.sub.6 is phenyl or halophenyl.

Abstract: The invention relates to new optically active or racemic 5-phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen, halogen, trifluoromethyl or a nitro group;R.sup.2 stands for hydrogen or alkyl having 1 to 6 carbon atoms;R.sup.3 represents a group conventionally attached to the --CH(NH.sub.2)--COOH group of the known optically active or racemic .alpha.-amino-acids, preferably an optionally substituted lower alkyl group;R.sup.4 is hydrogen, chlorocarbonyl or carbamoyl; andX is hydrogen, halogen or trifluoromethyl, with the proviso that if in the racemic compounds R.sup.4 stands for hydrogen R.sup.3 is other than alkyl having 1 to 6 carbon atoms, in which the centers of asymmetry in the 3- and 5-positions have the same absolute configuration, and pharmaceutically acceptable acid addition salts thereof, and a process for their preparation.

Abstract: The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),Glp--X--Y--NH--A (I)whereinX is L-norleucyl, L-leucyl, L-norvalyl, D-leucyl, L-prolyl, L-2-aminobutyryl, L-valyl, L-threonyl, L-isoleucyl, L-2-aminodecanoyl, L-cyclohexylalanyl or L-tert.-butyl-seryl group andY is L-prolyl group, orX is L-histidyl group andY is L-homoprolyl or D-pipecolyl group, furthermoreA is hydrogen, a C.sub.1-10 alkyl group or a C.sub.1-3 alkyl group having a dimethylamino substituent,with the proviso that if X is L-leucyl group, A is other than hydrogen, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.

Abstract: Compounds of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 each is saturated or unsaturated, straight-chained or branched alkyl phenyl, alkylphenyl or saturated or unsaturated cycloalkyl;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), ##STR2## wherein X is halogen, with a secondary amine of the formula (III),R.sub.1 --NH--R.sub.2 (III)The new compounds of the formula (I), as well as their pharmaceutically acceptable acid addition salts are active primarily in the induction of liver microsomal enzyme, but also possess antipyretic activity.

Abstract: New compounds of the formula (I) ##STR1## wherein R.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 forms a 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.1-18 carboxylic acid. The compounds are prepared by reducing the corresponding nitro compounds of the formula (II) ##STR2## and optionally acylating the obtained product. The compounds of the formula (I) and their acid addition salts and quaternary ammonium salts are active primarily in the induction of liver microsomal enzymes, but they also possess valuable antipyretic activity and a yohimbine lethality increasing effect characteristic of antidepressants.

Abstract: Ulcer production in animals is prevented during prolonged antiphlogistic treatment with ulcerogenic quantities of indomethacin by using it in a composition of 1 part of indomethacin to 7.5 to 25 parts, preferably 10 parts by weight of a salicylate. Indomethacin is the most potent ulcerating compound among approved non-steroid antiinflammatory agents.

Abstract: New 2-amino-cyclopent-1-ene-thiocarboxylic acid-disulfides of the general formula (I), ##STR1## wherein R is hydrogen, a C.sub.1-6 alkyl group having optionally a C.sub.1-4 alkoxy, hydroxy, carboxy and/or amino substituent, a C.sub.2-4 alkenyl group, a C.sub.3-8 cycloalkyl group or phenyl group, are prepared by oxidizing the respective 2-amino-cyclopent-1-ene-dithiocarboxylic acids of the general formula (II), ##STR2## wherein R is as defined above. The new compounds of the general formula (I) and their salts exert dopamine-.beta.-hydroxylase inhibiting effects and can be applied in the therapy.

Abstract: A method of treating mammalian noradrenaline malfunctions or dysfunction or effecting dopamine-.beta.-hydroxylase inhibition comprises administering an effective dose of an acid derivative of the formula (I), ##STR1## wherein R is C.sub.2-4 alkenyl, C.sub.3-8 cycloalkyl, benzyl or C.sub.1-6 alkyl which has a C.sub.1-4 alkoxy or a hydroxy substituent, or C.sub.2-6 alkyl with a carboxy and/or amino substituent, or C.sub.5 - or C.sub.6 -unsubtituted alkyl.

Abstract: Ulcer production in animals is prevented during prolonged antiphlogistic treatment with ulcerogenic quantities of phenylbutazone by using it in a composition of 1 part of antiphlogistic to 0.2 to 50 parts by weight of alkali metal salicylate.

Abstract: New 2-amino-cyclopent-1-ene-thiocarboxylic acid-disulfides of the formula, ##STR1## wherein R is a C.sub.1-6 alkyl group having optionally a C.sub.1-4 alkoxy, hydroxy, carboxy and/or amino substituent, a C.sub.2-4 alkenyl group, or a C.sub.3-8 cycloalkyl group, are prepared by oxidizing the respective 2-amino-cyclopent-1-ene-dithiocarboxylic acids of the formula, ##STR2## wherein R is as defined above. The compounds of the formula (I) exert dopamine-.beta.-hydroxylase inhibiting effects and can be applied in therapy.

Abstract: 2-Amino-cyclopent-1-ene-1-dithiocarboxylic acid derivatives of the formula, ##STR1## wherein R is C.sub.2-4 alkenyl, or C.sub.1-6 alkyl group having optionally a C.sub.1-4 alkoxy, hydroxy, carboxy and/or amino substituent, with the proviso that if R is an unsubstituted alkyl group, this group contains at least 5 carbon atoms, are prepared by reacting 2-amino-cyclopent-1-ene-1-dithiocarboxylic acid or a salt thereof with an amine of the formula,R--NH.sub.2 (II)wherein R is as defined above. The new compounds of the invention exert dopamine-.beta.-hydroxylase inhibiting effects.

Abstract: Apovincaminol ester of formula ##STR1## wherein R is an alkylcarbonyl group having 3 to 12 carbon atoms, or a pharmaceutically acceptable acid addition salt thereof.

Abstract: The invention relates to new .alpha.

Abstract: The invention is directed to a new substituted derivative of .alpha.-ethylnyl-benzophenone, namely, the 3-iodo-.alpha.-ethynyl-benzhydrol which has high antifungal activity.

Abstract: The new compound 3,4,5-trimethoxy-.alpha.-ethynyl benzhydrol which has been found to be an effective fungicide.