Abstract: New .DELTA..sup.1,3,5 -3-chloro-pregnane derivatives of the general formula (I), ##STR1## wherein X is hydrogen atom, acetyl group or a chloroacetyl group, andY and Z represent hydrogen atom or a halogen atom, with the proviso that at least one of them is other than hydrogen,are prepared by reacting a .DELTA..sup.1,4 -3-oxo-pregnane derivative of the general formula (II), ##STR2## wherein X' is acetyl group or a chloroacetyl group and Y and Z are as defined above, with a chloromethyleneiminium salt of the general formula (III), ##STR3## wherein A.sup.(-) is a salt-forming anion, in an aprotic solvent in the presence of a tertiary base, and, if desired, subjecting the resulting product to hydrolysis.The compounds of the general formula (I) exert antiphlogistic effects and can be used in the therapy for the treatment of inflammations.

Abstract: New bicyclic compounds of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent a C.sub.1-6 alkyl group, andR.sup.3 is an etherified hydroxy group of the formula --CR.sup.4, wherein R.sup.4 is benzyl group, benzhydryl group or a phenyl group bearing optionally a phenyl or a trihalomethyl substituent or one or more halogen substituent(s), orR.sup.3 is an esterified hydroxy group of the formula --OCO--R.sup.5, which representsa phenyl-(C.sub.1-5 alkyl)-carbonyloxy group,a cinnamoyloxy group having optionally a halogen or one or more C.sub.1-4 alkoxy substituent(s),a benzoyloxy group having optionally a C.sub.1-4 alkyl, phenyl or trihalomethyl substituent or one or more C.sub.

Abstract: The invention relates to new polycyclic compounds substituted on the A-ring. More particularly, the invention concerns new polycyclic compounds of the formula (I) ##STR1## wherein R.sup.1 is methoxy or halogen andR.sup.2 is hydrogen; orR.sup.1 is hydrogen andR.sup.2 is halogen and acid addition salts thereof.

Abstract: A novel process for preparing 10-bromo-vincaminic acid esters and homologous compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group is disclosed.All the intermediate products are new and exhibit valuable therapeutical effect on the blood circulation.

Abstract: Peptides affecting the immune regulation selected from the following group:Arg-Lys-AspArg-Lys-Asp-ValArg-Lys-Asn-ValArg-Lys-Asu-ValArg-Lys-Ala-ValArg-Lys-Asp-AlaArg-Lys-Asp-IleArg-Lys-Glu-ValArg-Ala-Asp-ValArg-Asp-Lys-ValAla-Lys-Asp-ValLys-Arg-Asp-ValGlp-Arg-Lys-AspGlp-Arg-Lys-Asp-ValGlp-Arg-Lys-Asp-Val-Tyr and salts, amides lower alkyl esters and protected derivatives thereof.

Abstract: The invention relates to the new 17,18-dehydro-apovincaminol-3',4',5'-trimethoxy-benzoate of formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of these new compounds. Still another aspect of the invention is a pharmaceutical composition for treating psoriasis.

Abstract: The invention relates to the new apovincaminol-3',4',5'-trimethoxy-benzoate and acid addition salts thereof.The new compound may be prepared by reacting apovincaminol or an acid addition salt thereof with 3,4,5-trimethoxy benzoic acid or a reactive derivative thereof capable of acylation and if desired converting the compound thus obtained into an acid addition salt.The new compound of the present invention can be used in therapy in the treatment of skin diseases attached to pathological cell proliferation and in the propylaxis of such diseases.

Abstract: The present invention relates to the compounds of the Formulae 1a and 1b and pharmaceutically acceptable acid addition salts thereof.The new 9-nitro-apovincaminol-3',4',5'-trimethoxybenzoate of the Formula 1a ##STR1## and the 11-nitro-apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 1b ##STR2## and pharmaceutically acceptable acid addition salts thereof can be prepared by nitrating the apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 11, ##STR3## if desired separating the mixture of the compounds of the Formulae 1a and 1b thus obtained into its components, if desired converting a compound of the Formula 1a or 1b thus obtained into pharmaceutically acceptable acid addition salts thereof.The new compounds of the present invention can be used in therapy in the treatment of psoriasis.

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: New octapeptides of the general formula (I),X--Arg--Val--Tyr--Ile--His--Pro--Y--OA (I)whereinX stands for the acyl group of an N-methylamino acid or the acyl group of an aliphatic .alpha.-hydroxy- or .alpha.-aminooxycarboxylic acid,Y is the residue of an aliphatic amino acid, andA is a C.sub.1-5 alkyl group, are prepared so that the protecting groups of a protected octapeptide derivative of the general formula (II),B--X--Arg(C)--Val--Tyr(D)--Ile--His(E)--Pro--Y--OA (II)whereinB is a group removable by acidolysis or catalytic hydrogenation,C is a group for the temporary protection of the guanidino group on the Arg moiety,D is a group for the temporary protection of the aromatic hydroxy group on the Tyr moiety,E is a group for the temporary protection of the imidazole group on the His moiety, andA, X and Y are as defined above,are removed either stepwise or in a single step. If desired, a compound of the general formula (I) is converted into its acid addition salt or pharmaceutically acceptable complex.

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: New angiotensin-II analogues of the general formula (I),X-Arg-Val-Tyr-Ile-His-Pro-Y-OA (I)whereinX stands for the acyl group of an N-methylamino acid, or the acyl group of an aliphatic .alpha.-aminooxy- or .alpha.-hydroxycarboxylic acid,Y is the residue of an aliphatic .alpha.-hydroxycarboxylic acid, andA is hydrogen or a C.sub.

Abstract: Compounds of the formula: ##STR1## wherein R is alkyl having 1 to 6 carbon atoms;A is substituted or unsubstituted alkyl having 1 to 6 carbon atoms, aralkyl having 7 to 16 carbon atoms wherein the alkyl or aralkyl groups are unbranched in the 1-position or an acyl group derived from an aliphatic or aromatic carboxylic acid;B is hydrogen; orA and B together form an optionally substituted alkylidene having 2 to 8 carbon atoms or an aralkylidene group having 7 to 18 carbon atoms where the alkylidene and aralkylidene groups are unbranched in the 1-position or pharmaceutically acceptable salts thereof are disclosed. The compounds have vasodilating properties.

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: Skin diseases such as psoriasis in a human patient can be treated by topically or parenterally administering a dermatological composition containing a compound of the formula: ##STR1## wherein R.sub.1 is hydrogen andR.sub.2 is the group --COOCH.sub.3, --CONH.sub.2 or --CONHNH.sub.2 ; orR.sub.1 is methoxy andR.sub.

Abstract: The invention is directed to 1-alkyl-9-bromohexagydro indoloquinolizium salts and a method for their use to increase blood circulation and decrease in blood vessel resistance.

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: A novel process for preparing 11-bromo-vincaminic acid esters of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand independently from each other for a C.sub.1-6 alkyl group, comprising the steps of treating a 1-alkyl-1-alkoxycarbonylethyl-octahydroindolo-quinolisine of the general formula ##STR2## wherein R.sup.2 is as defined above and R.sup.3 stands for a C.sub.1-6 alkyl group, with a brominating agent and treating the resulting isomeric mixture of the bromo-derivatives with an alkaline agent or treating the corresponding 14-oxo-E-homo-eburnane being unsubstituted in ring A with a brominating agent and nitrosating the resulting 11-bromo-14-oxo-E-homo-eburnane of the general formula ##STR3## wherein R.sup.2 is as defined above, then subjecting the resulting 11-bromo-14-oxo-15-hydroxyimino-E-homoeburnanes to deoxyimination and treating the 14,15-dioxo-derivatives obtained with a base in an alcohol of the general formula R.sup.1 OH, wherein R.sup.1 is as defined above.