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: The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a -CH.sub.2 -O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl,provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl, R.sup.4 is other than ethyl.

Abstract: The invention relates to a process for the extraction of solids from liquids containing solids granulated by heat effect and/or solids the moisture content of which is reducible by heat effect, especially from colloidal solutions with protein content, suspensions and slurries for reducing the fat content of the solid material, in the course of this process grains are formed in the liquid with heat effect, or the moisture content of the grains is reduced, then they are removed from the liquids and dried. The equipment for implementation of the process is also subject of the invention.The process is characterized by heating the liquid to 50.degree.-125.degree. C. temperature with heat transfer ("instant heating") for a short period, maximum for 2 minutes, then the heated material is kept at 50.degree.-125.degree. C. temperature for at least 2, preferably for 5-15 minutes. This is followed by separation of the grains from the liquid phase with filtration in a space containing vapor of 50.degree.-125.degree. C.

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 concerns a new process for the preparation of apovincaminic acid ester derivatives of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and pharmaceutically acceptable salts thereof.According to the invention the apovincaminic acid ester derivatives of the general formula (I) are prepared by reacting the corresponding 9- and/or 10- and/or 11-halo-14-oxo-15-hydroxyimino-E-homo-eburnane derivatives with an alkanol of the general formula R.sup.1 --OH, wherein R.sup.1 is as defined above, and with a dehydrating concentrated acid, and subsequently reducing the 9- and/or 10- and/or 11-halo-apovincaminic acid esters obtained, selectively on the aromatic ring. Alternatively, the 9- and/or 10- and/or 11-halo-apovincaminic acid esters can also be used as starting materials.

Abstract: The invention relates to a new enantioselective synthesis for the preparation of optically active 14-oxo-E-homo-eburnane derivatives of the formula (Ia) ##STR1## wherein R.sup.1 is alkyl having from 1 to 4 carbon atom. In the synthesis optically active 6-alkoxycarbonylhexahydroindoloquinolizinium salts are employed as starting materials, which contain a center of chirality at the site of attachment of the carboxyl group. This center of chirality preserves the optical activity of the optically active tryptophan ester from which this compound has been prepared until a new center of chirality is formed in the molecule in a configuration corresponding to the desired end product. The carboxyl group, which is not needed in the end product and only serves to preserving the optical activity can then be eliminated.Compounds of the formula (Ia) are known in the art and may be used in the synthesis of (+)-vincamine and (+)-apovincaminic acid ethylester.

Abstract: The invention relates to a new method for controlling the level and distribution of alkaloids produced by Claviceps purpurea variant strains capable of producing primarily ergocornine, .alpha.-ergocryptine and .beta.-ergocryptine under saprophytic conditions. According to the invention a compound of the biosynthesis path of isoleucine or a compound which promotes the formation of isoleucine by biochemical control is added to the fermentation broth. In other respects fermentation is performed under conditions known per se.By the method of the invention the ratio of .alpha.- and .beta.-ergocryptine formed in the fermentation broth can be adjusted to the optimum value.

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 a process for the preparation of a biologically active substance, which can be isolated from normal white blood cells and is capable of inhibiting the proliferation of normal and leukemic myeloid cells selectively.The substance obtained is a peptide, which has an amino acid composition of Tau.sub.1, Asx.sub.1, Ser.sub.2, Thr.sub.1, Glx.sub.3, Gly.sub.2, Ala.sub.1, (PO.sub.4).sub.1.sup.2-, a negative charge at pH 6.5, an electrophoretic mobility of -0.55 to -0.65 related to aspartic acid, has no charge at pH 1.9, has a mobility of about 0.26 related to .epsilon.-DNP-lysine and gives a positive chloro-toluidine reaction.

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: The invention relates to a new process for the preparation of ergot alkaloids, primarily ergocornine and .beta.-ergocryptine, by subjecting a Claviceps purpurea strain to fermentation under aerobic conditions in a culture medium which contains carbon and nitrogen sources, mineral salts and optionally other additives, too. According to the invention a Claviceps purpurea variant strain deposited under No. MNG 00186 is applied as alkaloid-producing strain.

Abstract: An apparatus for crystallization which utilizes a treating device for the formation of a crystal slurry having a prismatic drum at the inlet end of the device and a zigzag body eccentrically connected to the wide end of the drum and formed by ducts which have their axes intersecting the axis of the drum, the final duct section terminating at a ring which is coaxial with the drum. The duct walls are planar as well. The entire system is closed and includes a filter having a prismatic drum and duct arrangement but with walls which are perforated.

Abstract: The invention relates to new halovincamone derivatives of the general formula (I), ##STR1## wherein R is a C.sub.1-6 alkyl group and X is halogen, and pharmaceutically acceptable acid addition salts and optically active isomers thereof. These compounds possess valuable vasodilating effect, and can be applied to advantage in the therapy.The new compounds defined above are prepared according to the invention so that a single epimer or an epimeric mixture of a racemic or optically active halogenated 14-oxo-15-hydroxy-E-homoeburnane derivative of the general formula (II), ##STR2## wherein R and X are as defined above, or an acid addition salt thereof is treated with an oxidizing agent, and, if desired, the resulting compound of the general formula (I) is converted into its pharmaceutically acceptable acid addition salt and/or resolved.

Abstract: A rotary sieve comprises, in an elongated housing, a body which is rotatable about a substantially horizontal axis and has, at one end, a frustopyramidal drum widening in the direction of the other end and a zigzag tube communicating eccentrically with the drum. The planar walls of the drum and the tube are perforated sieves and the material is introduced by a worm centrally into the drum and is progressively advanced through the body to be discharged generally centrally from the tube through a discharge drum of the body which is peripherally open so that the material can be collected by a pipe underlying the discharge drum.

Abstract: Anti-coagulants of the formula X-Pro-Agm(HB) (.sub.n) whereinX is an alpha-amino acid moiety of the configuration having a phenyl, phenyl-(lower)-alkyl or phenyl-(heteroatom-containing) lower alkyl side chain,Agm is an agmatine group (1-amino-4-guanidino-butane),B is an acid residue, andn is an integer from 0-2, are disclosed.

Abstract: The invention relates to new hydroxyamino-eburnane derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group, as well as to pharmaceutically acceptable acid addition salts and optically active isomers of these compounds.These new compounds can be applied as peripheral vasodilatating agents or can be converted into other compounds, e.g. vincamine and apovincamine derivatives of valuable therapeutical effects.The compounds of the general formula (I) are prepared according to the invention by reacting a hexahydro-indoloquinolisinium derivative of the general formula (II), ##STR2## wherein R.sup.2 is as defined above and X stands for an acid residue, with a methylenemalonic acid diester derivative of the general formula (III), ##STR3## wherein R.sup.

Abstract: A parenteral solvent suitable for injectable solutions of eburnamenines and dihydroeburnamenines is disclosed, said solvent containing a buffer having the ability to buffer the injectable solutions at given pH values, at least one stabilizing agent which includes parenterally acceptable aliphatic alcohols containing one or more hydroxy groups or water-miscible ethers thereof, 30 to 70% by weight water and optional preservatives, anaesthetics, and antioxidants.

Abstract: The invention relates to new, racemic or optically active, halogenated 15-hydroxy-E-homoeburnane derivatives of the formulae (Ia) and/or (Ib), ##STR1## wherein R is a C.sub.1-6 alkyl group and X is halogen, and acid addition salts thereof. These compounds are biologically active, furthermore they can be applied as intermediates in the synthesis of other pharmaceutically active substances.