Abstract: The invention relates to fused heterocyclic compounds with ring junction nitrogen atom of the formula: ##STR1## wherein Q stands for 2-indolizinyl, 2-imidazo[1,2-a]pyridinyl, 2-imidazo[1,2-a]pyrimidinyl, 6-(2,3-dihydroimidazo[2,1-b]thiazol)-yl or 6-imidazo[2,1-b]thiazolyl group; and n is an integer from 2 to 4, as well as therapeutically useful salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions. The compounds of formula (I) exhibit mainly antipsychotic effects so the invention relates also to a method of treatment of schizophrenia, organic mental disorders, affective disorders, anxiety and personality disorders.

Abstract: The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), ##STR1## wherein R means hydrogen or a group (a), wherein Z stands for C.sub.1-4 alkyl, optionally substituted aryl, aralkyl, heteroaryl or 14-eburnameninyl group; and n is an integer of 2, 3 or 4, as well as therapeutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions, and in addition, to a method of treatment. The novel compounds of Formula (I) exhibit particularly antioxidant, antiischemic as well as antiamnesic effects and are useful for inhibiting lipid peroxidation and for protection from or treatment of ischemia and amnesia as well as for treating various degenerative neurological diseases, e.g. Alzheimer's disease.

Abstract: Anti-Fungal compounds are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is C.sub.1 to C.sub.10 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.6 alkyl, and the phenyl moiety of the two latter groups may carry at least one substituent selected from the group consisting of a halogen atom,C.sub.1 to C.sub.6 alkoxy group, phenyl group, phenoxy group, and trifluorome thyl group;R.sup.2 is a hydrogen atom, a C.sub.1 to C.sub.10 alkyl group or a phenyl group;R.sup.3 and R.sup.4 are independently from each other a C.sub.1 to C.sub.10 alkyl group or a phenyl group;X is a hydrogen atom, halogen atom or a group of the formula (A) ##STR2## and in this formula Y.sup.1 and Y.sup.2 are independently from each other, a --N.dbd. atom or a group of the formula --CH.dbd., or an optical antipode thereof.

Abstract: The invention relates to novel N-hydroxy-substituted 1,2,3,6-tetrahydropyridine and piperidine derivatives of the formula ##STR1## wherein A, B, D, E, G, I and R are as defined in the specification, m is 0, 1 or 2, with the proviso that:m is 0 or 2, or both G and I are hydrogen, when A is benzyl or halogen-monosubstituted benzyl group; andm is 1, when A is 2-picolyl, as well as their pharmaceutically acceptable acid addition salts. The compounds of formula (I) are useful for enhancing the tolerance of mammals (including man) against hypoxic and/or ischaemic states as well as for treating the degenerative and functional disturbances arising from hypoxic and/or ischaemic results.

Abstract: The invention relates to novel 17.beta.-substituted 4-azaandrostane derivatives of general formula (I), ##STR1## wherein R means hydrogen or a C.sub.1-3 alkyl group;R.sup.1 and R.sup.2 are the same or different and stand for hydrogen or a C.sub.1-4 alkyl group with the proviso that both can mean hydrogen only in the case when n is higher than 5; orR.sup.1 and R.sup.2 together means an .alpha.,.omega.-alkylene group containing 5 to 7 carbon atoms, the terminal carbon atoms of said alkylene group being bound to the same ring carbon atom;n is 4, 5, 6 or 7; and--- bond line represents a single or double bond.Furthermore, the invention relates to pharmaceutical composition containing these compounds as well as a process for the preparation of the compounds of general formula (I).The compounds of general formula (I) exert a 5.alpha.

Abstract: The invention relates to novel 4-azaandrostene intermediates of formula (I), ##STR1## wherein R is hydrogen or a C.sub.1-3 alkyl group;X is chlorine, bromine or iodine; and the---- bond line is a single or double bond.

Abstract: An intermediate compound is disclosed that is useful in the preparation of a lipid-peroxidation inhibiting substance and that is selected from the group consisting of:2,4-bis[1-adamantylamino]-6-(1-piperazinyl)pyrimidine; and4,6-bis(1-adamantylamino)-2-(1-piperazinyl)pyrimidine;or a pharmaceutically acceptable acid addition salt thereof.

Abstract: Novel, therapeutically active 21-aminosteroids of formula (I) ##STR1## with pregnane skeleton, are disclosed wherein two of X, Y and Z are a nitrogen atom each and the third one is a methine group; R.sup.1 and R.sup.2 are independently from each other, a primary amino group bearing as substituent a branched-chain C.sub.4-8 alkyl -alkenyl or -alkynyl group, or a C.sub.4-10 cycloalkyl group comprising 1 to 3 ring(s) and being optionally substituted by at least one C.sub.1-3 alkyl group; or R.sup.1 and R.sup.2 are each a spiro-heterocyclic secondary amino group containing at most 10 carbon atoms and optionally at least one oxygen atom as additional heteroatom; or one of R.sup.1 and R.sup.2 is an unsubstituted heterocyclic secondary amino group containing 4 to 7 carbon atoms and the other one is an above-identified primary amino group, an above-identified spiro-heterocyclic secondary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by at least one C.sub.

Abstract: The invention relates to novel eburnamenine derivatives of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 as well as R.sup.3 and R.sup.4, independently from each other, stand for hydrogen, C.sub.2-6 alkyl group, C.sub.2-6 alkenyl group; or a C.sub.3-10 alicyclic group involving 1 to 3 rings, and this latter group may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, together with the adjacent nitrogen atom and optionally with an additional oxygen or nitrogen atom, form a 4- to 6-membered, saturated or unsaturated cyclic group which may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; two of X, Y and Z are nitrogen whereas the third of them means a methine group; n is 1 or 2; W means oxygen or two hydrogen atoms; and the wavy line means .alpha.-/.alpha.-, .alpha.-/.beta.- or .beta.-/.alpha.- steric position, as well as their acid addition salts and solvates.

Abstract: New compounds with the ability to inhibit calcium uptake in the brains of mammals are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.4 alkyl;one of R.sup.2 and R.sup.3 is C.sub.1 to C.sub.4 alkoxy and the other one is phenyl-C.sub.1 to C.sub.4 alkoxy optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus; andR.sup.4 is phenyl optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus, or their solvates, individual optically active and geometric isomers, mixtures of such isomers, as well as pharmaceutically acceptable acid addition salts thereof. The compounds of the Formula (I) are capable of inhibiting calcium uptake to brain cells and have a protective effect on hypobaric hypoxia.

Abstract: The invention relates to carbazolone derivatives of the formula ##STR1## wherein A stands for a group of formula--CH.sub.2 --R (V),wherein R means a hydroxyl or 2-methyl-1H-imidazol-1-yl group;B represents a group of formula ##STR2## wherein R.sub.1 means hydrogen or a methyl or ethyl group; or A and B together form a group of formula ##STR3## wherein R.sub.2 means a methyl or ethyl group; or A and B together form a group of formula ##STR4## The above compounds are useful intermediates in the synthesis of ondansetron of formula ##STR5## chemically 9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-1,2,3,9-tetrahydro-4H-carba zol-4-one.The invention further relates to a novel process for the preparation of compounds of the formula (I) , wherein A and B are the same as in formula (I) but B may be also hydrogen. Thus, this novel process is suitable for the preparation of ondansetron itself.

Abstract: Complexes of deprotonated hyaluronic acid with 3d metal ions of the 4th period of the Periodic Table and compositions containing these complexes as active ingredients or carriers. A process for the preparation of the complexes and compositions (pharmaceutical and cosmetic compositions) containing these complexes as active ingredients are disclosed in which zinc or cobalt (II) hyaluronate is preferably used as active ingredient.

Abstract: A mixing device, especially for a fermenter, capable of dispersing gas in a broth therein, in which a number of propeller mixers are provided on a vertically extending shaft. The lower propeller mixer is a gas dispersing mixer having a hollow hub and open channels on the blades extending from this hub and tapering outwardly. At least one intermediate propeller mixer has some blades shorter than others and of reverse flow direction, some blades having baffle bars on trail edges thereof. The upper propeller mixer has the longer blades without channels and flow modifying elements.

Abstract: New monoquaternary and diquaternary 5-alpha-hydroxy-3,16-diaminoandrostane salts are disclosed with curare-like muscle relaxant activity. The new salts are characterized by a surprisingly rapid onset time.

Abstract: The invention relates to novel, parenterally useful, stable aqueous pharmaceutical compositions, mainly injectable solutions containing a bis-indole alkaloid. The compositions contain the zinc complex of a bis-indole alkaloid, preferably vincristine, vinblastine or 5'-nor-dihydrovinblastine together with a bivalent metal gluconate and a preserving agent dissolved in a mono- or polyhydric alcohol.The invention further relates to a process for the preparation of the above compositions.The composition according to the invention can be utilized for the parenteral administration of bis-indole alkaloids in the cancer chemotherapy.

Abstract: A method of treating a mammalian subject for Parkinson's disease or to provide a central muscle relaxant effect, which comprises the step of administering to the mammalian subject in need of the treatment, a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein m is 1,2 or 3;R.sub.1 and R.sub.2 each independently stand for hydrogen, C.sub.1 to C.sub.4 straight or branched chain alkyl, C.sub.1 to C.sub.4 alkoxy, C.sub.5 to C.sub.7 cycloalkyl, or halogen; andB is a 5- or 6-membered saturated or unsaturated heterocyclic group containing a nitrogen heteroatom, the heterocyclic group being bound through its heterocyclic nitrogen atom to the remainder of the compound, and which can contain one or two additional heteroatoms selected from the group consisting of an oxygen heteroatom, a sulfur heteroatom, and one or two additional nitrogen heteroatoms, which may be as an .dbd.N--, --NH-- or --NR-- group, where R is a C.sub.1 to C.sub.5 alkyl or C.sub.1 to C.sub.

Abstract: The present invention relates to novel peptides of formulaeXaa Glu Asp Cys Lys (SEQ I.D. No: 1),andGlu Asp Cys Lys (SEQ I.D. No: 2)wherein the Cys sulfur is bonded to an acetamidomethyl group, and Xaa is pyro-Glu, the acid addition salts thereof, the pharmaceutical compositions comprising the same and a process for the preparation of the novel peptides and compositions.The novel peptides selectively inhibit the proliferation of hemopoietic cells.The invention also covers the treatment of mammals (including human beings) with the said peptides and compositions for selectively inhibiting the proliferation of hemopoietic cells.The advantage of the novel compounds is that they are almost completely harmless, they do not have any side-effect in therapeutic dose-range, in addition they significantly inhibit the damaging effects of drugs and radiation used for the therapy of tumorous diseases or the dose of drug or radiation can be increased when they are administered.

Abstract: Complex mixing system with stages consisting of propeller mixers of high diameter ratio, where the blades are provided with flow modifying elements, whereby the energy proportions spent on dispersion of the amount of gas injected into the reactor, homogenization of the multi-phase mixtures, suspension of solid particles, etc. and the properties corresponding to the rheological properties of the gas-liquid mixtures and to the special requirements of the processes can be ensured even in extreme cases. Open channels (5) opposite to the direction of rotation are on the blades (4) of the dispersing stage (2a) of the propeller mixers (2) fixed to a common shaft, where the channels (5) are interconnected with gas inlet (7). The angle of incidence of a certain part of the blades (4) of mixing stages (2b, 2d) used for homogenization and suspension is of opposite direction and the length is shorter and/or the angle of incidence is smaller than those of the other blades.

Abstract: The invention relates to acaricidal compositions containing as active ingredient: the fermentation broth or cell-free fermentation broth, of a concentrate of the fermentation broth or cell-free fermentation broth, or a solidified form of the fermentation broth or cell-free fermentation broth of one or two bacterium strains deposited at the National Collection of Agricultural and Industrial Microorganisms, Budapest, Hungary under the identification Nos. 001083 and 001086 or of their mixed micropopulation, if desired, in a sterilized state, optionally together with the metabolism products arising during the fermentation and inutilized nutriments, as well as one or more solid and/or liquid carrier(s) (preferably sugar or a grist of natural minerals), or an inert solvent (e.g. water) and, if desired, with surface active (preferably anionic or nonionic emulsifying or dispersing) agents.

Abstract: The invention relates to a novel process for the resolution of an acid mixture (hereinafter: threo acid mixture) containing (+)-threo-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)-propionic acid [hereinafter: (+)-threo acid]and (-)-threo-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)-propionic acid [hereinafter: (-)-threo acid].