Abstract: The invention relates to new 10-halo-E-homoeburnane derivatives of the general formula (I), ##STR1## wherein R.sup.2 is a C.sub.1-6 alkyl group and X is halogen, and epimers, optically active derivatives and pharmaceutically acceptable acid addition salts thereof. These substances exert vasodilating effects and can be applied to advantage in the therapy.The new compounds are prepared so that a racemic or optically active 9-halo-octahydroindoloquinolisine derivative of the general formula (II), ##STR2## wherein R.sup.2 and X are as defined above and R.sup.1 is a C.sub.1-6 alkyl group, or an acid addition salt thereof is treated with a strong base, and, if desired, the 15-epimers of the resulting compound having the general formula (I) are separated from each other, and/or, if desired, the resulting substance is converted into its pharmaceutically acceptable acid addition salt and/or resolved.
Type:
Grant
Filed:
August 5, 1980
Date of Patent:
August 25, 1981
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt
Inventors:
Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Lajos Dancsi, Tibor Keve, Ferenc Drexler
Abstract: The invention relates to new, racemic or optically active, halogenated 15-hydroxy-E-homoeburnane derivatives of the general formula (Ia) and/or (Ib), ##STR1## wherin 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.The compounds of the general formulae (Ia) and (Ib) are prepared by halogenating the respective racemic or optically active 15-hydroxy-E-homoeburnane derivative of the general formula (II), wherein R is as defined above.
Type:
Grant
Filed:
August 5, 1980
Date of Patent:
August 25, 1981
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt
Inventors:
Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Lajos Dancsi, Tibor Keve, Ferenc Drexler
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.
Type:
Grant
Filed:
July 11, 1979
Date of Patent:
August 11, 1981
Assignee:
Richter Gedeon Vegyeszeti Gyar RT
Inventors:
Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Lajos Dancsi, Tibor Keve, Egon Karpati, Laszlo Szporny
Abstract: A filtering and washing device has a filter body mounted in a housing for rotation about a horizontal axis and comprising a first portion in the form of a truncated cone or pyramid having a base plate with an eccentrically positioned polygonal orifice and a second portion in the form of a sawtooth-shaped tube rigidly connected at one end to the orifice and at an opposite end to a cylindrical drive shaft rotatably journaled in the housing and operationally connected to a motor, the tube in turn being formed from a multiplicity of hollow prisms or truncated pyramids. The first and second portions have surfaces provided with respective filter means. A pipe fixed to the housing traverses an end plate of the first portion opposite the base plate for rotatably supporting the filter body at one end and for feeding to the first portion material to be filtered or cleaned, while the tube is provided with an opening spaced from the base plate of the first portion for dispensing treated material.
Type:
Grant
Filed:
November 28, 1979
Date of Patent:
August 4, 1981
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt
Inventors:
Istvan Takacs, Gyula Bosits, Endre Vereczkey, Gyorgy Kerey
Abstract: Vasodilating octahydro-indolo[2,3-a]quinolizine derivatives of the formula ##STR1## wherein Q is hydrogen or an A--CH.sub.2 --CH.sub.2 -- group and A is cyano or --COOR, wherein R is C.sub.1-6 alkyl.
Type:
Grant
Filed:
April 2, 1979
Date of Patent:
July 14, 1981
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
Abstract: A drier, especially for viscous materials, comprises a double-wall cylindrical vessel which is heated and to which the material to be dried is fed at one end with the dried material being removed at the opposite end. A drying gas inlet is connected to the drying chamber to pass the drying gas in counterflow or uniflow with the material and a shaft is rotatable along the axis of the chamber and carries adjustable disks with alternately inner and outer openings so that the material path through the vessel is deflected toward and away from the axis as the material passes successively through adjustable-length cells between these disks. All of the disks carry blades which scrape the material from the heated wall from the vessel and at least some of the disks carry rollers of predetermined spacing from this wall to adjust the particle size of the dried product.
Type:
Grant
Filed:
November 28, 1979
Date of Patent:
July 7, 1981
Assignee:
Richter Gedeon Vegyeszeti Gyar RT
Inventors:
Istvan Takacs, Peter Rudolf, Bela Szabo, Gyorgy Kerey
Abstract: The packing of a tower or column for heat exchange, material exchange, contacting of two fluids with one another and chemical reaction consisting of a stack of elongated members having two walls inclined to one another and joined at a third wall, the first two walls being each formed with elongated vibratile elements interdigitated with vibratile elements of another packing member so that when the body of packing is traversed by one or more fluids, the vibratile elements are set into vibration.
Abstract: A coating ensuring the controlled release of a biological active ingredient, which can be incorporated in the coating or is surrounded thereby, consists of a varnish-forming polymer selected from the group which consists of cellulose triacetate containing polyethylene glycol as an emollient and vinyl chloride-vinyl acetate copolymer with glycerol as an emollient, and an aqueous phase dispersed in the polymer and consisting of particles of a diameter up to 20 microns, the aqueous phase making up 2% to 30% of the volume of the coating. The active ingredient is preferably a pharmaceutical agent affecting the circulatory system or a psychotropic agent.
Type:
Grant
Filed:
September 19, 1977
Date of Patent:
May 12, 1981
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Janos Dobo, Erzsebet Takacs, Gyozo Hortobagyi, Marianne Skvorecz nee Hajnoczy, Ilona Kolbe, Katalin Hoffmann nee Vas
Abstract: There are disclosed pharmaceutical compositions comprising at least one cytostatic agent and N.sup..epsilon. -trimethylthyllysin or a pharmaceutically acceptable salt thereof, optionally in association with conventional pharmaceutical carriers and other additives.The new compositions possess a reduced toxicity compared with the cytostatic agents administered alone.
Type:
Grant
Filed:
October 12, 1978
Date of Patent:
April 7, 1981
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Karoly Lapis, Bela Szende, Andreas Jeney, Laszlo Kopper, Karoly Simon, Erno Tyihak, Lajos Kisfaludy, Lajos Kovacs, Gyorgy Dobo
Abstract: Pyridazinylhydrazones capable of lowering blood pressure having the formula ##STR1## wherein R.sup.1 is hydrogen, chlorine, alkyl having from 1 to 4 carbon atoms, methoxy, hydroxyl, carbamoyl or cyano;R.sup.2 is morpholino; andK is a group having the formula ##STR2## wherein one of R.sup.3, R.sup.4, R.sup.5 or R.sup.6 is carboxyl or alkoxycarbonyl.
Abstract: 3-(1-Pyrazolyl)-pyridazine derivatives of the formula I, or pharmaceutically acceptable acid addition salts thereof, which decrease high blood pressure and inhibit catabolism or prostaglandins, ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl,R.sup.2 is hydrogen, cyano, carboxyl, carbamoyl, carbaxoyl or C.sub.1-4 alkoxycarbonyl,R.sup.3 is hydrogen or chlorine or --NR.sup.4 NHR.sup.5 or NR.sup.6 R.sup.7, wherein R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl, wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-5 alkyl, C.sub.1-5 hydroxyalkyl, C.sub.3-7 cycloalkyl, phenyl or benzyl, or benzyl or phenylethyl substituted with one or two chlorine atoms or methoxy groups, or a furylmethyl, pyridylmethyl, pyrrolidine or piperazine ring, or when R.sup.7 is hydrogen, R.sup.6 is --(CH.sub.2).sub.n --NR.sup.4 R.sup.5 wherein n is an integer from 1 to 3.
Abstract: The invention relates to novel sulfonamidobenzoic acid derivatives having the general formula ##STR1## wherein R.sup.1 denotes a C.sub.1-4 alkoxy group or a hydrazino group or an NR.sup.4 R.sup.5 group, wherein R.sup.4 and R.sup.5 denote each a hydrogen atom or an identical or different C.sub.1-4 alkyl group; furthermore R.sup.4 may denote an aralkyl or substituted aralkyl group provided that R.sup.5 denotes a hydrogen atom; furthermore NR.sup.4 R.sup.5 may denote a morpholine or piperazine ring;R.sup.2 and R.sup.3 may denote each a hydrogen atom or an identical or different C.sub.1-4 aliphatic group; furthermore R.sup.2 may denote a cycloaliphatic, aralkyl, substituted aralkyl or amino group provided that R.sup.3 denotes a hydrogen atom; furthermore R.sup.2 and R.sup.3 may denote together with the adjacent nitrogen atom a morpholino ring, an unsubstituted piperazine ring or a substituted piperazine ring,and to their pharmaceutically acceptable acid addition salts.
Abstract: The invention relates to bis(nitrosoureido)-polyol derivatives of general formula IB.sub.1 --A--B.sub.2 (I)whereinA stands for an open chain polyol comprising 4 to 6 carbon atoms or a six-membered cyclic polyol, andB.sub.1 and B.sub.2 being attached to two different carbon atoms of the chain A, are identical or different, and stand for a group of general formula II ##STR1## wherein X stands for a halogen atom andY and Z stand for a hydrogen atom or a nitroso group, with the restriction, that in B.sub.1 and B.sub.2 Y and Z must be different.The above compounds possess valuable cytostatic activity.
Type:
Grant
Filed:
July 17, 1978
Date of Patent:
December 2, 1980
Assignee:
Richter Gedeon Vegyeszeti Gyar RT
Inventors:
Tibor Horvath, Endre Csanyi, Sandor Eckhardt, Emilia Kiraly nee Vida
Abstract: The invention relates to new 8.beta.-hydrazinomethyl-ergoline derivatives of the general formula (I), ##STR1## wherein x y stands for a ##STR2## or ##STR3## group, R stands for hydrogen or methyl group, andR.sub.1 stands for hydrogen, a lower acyl group, a di-(lower-alkylaminocarbonyl group, a group of the general formula (VI), ##STR4## wherein Z.sub.1, Z.sub.2 and Z.sub.3 each represent hydrogen, halogen or a trifluoromethyl group, or a group of the general formula (VII), ##STR5## wherein Y represents a lower alkyl group, allyl group or phenyl group, and acid addition salts thereof. These compounds possess valuable antiserotonine, antidepressant and hypotensive effects, furthermore they can be applied as starting substances in the preparation of other biologically active ergoline derivatives.The new compounds of the general formula (I) are prepared according to the invention by reacting the respective 6-methyl-8.beta.-mesyloxymethyl or -tosyloxymethyl-ergoline derivatives with dry hydrazine.
Abstract: The invention relates to compounds of general formula ##STR1## wherein R.sup.1 stands for a hydrogen atom or a C.sub.1-6 alkyl-, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group,R.sup.2 stands for a hydrogen, fluorine, chlorine or bromine atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a nitro or an --NR.sup.5 R.sup.6 group, wherein R.sup.5 and R.sup.6 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl or a C.sub.2-4 hydroxyalkyl group,R.sup.3 stands for a hydrogen atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group, a chlorine atom or a hydroxyl, amino or methoxy group,R.sup.4 stands for a carbamoyl, a cyano or an --NR.sup.7 --NHR.sup.8 group, wherein R.sup.7 and R.sup.8 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.1-4 alkoxycarbonyl or an --NR.sup.9 R.sup.10 group, wherein R.sup.9 and R.sup.
Abstract: Diuretic pharmaceutically active steroid-spiro-oxazolidinone compounds of the formula (I), ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is C.sub.1-4 alkyl,R.sup.3 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl,Z.sup.1 and Z.sup.2 each are hydrogen or together form a second valence bond, or Z.sup.1 is hydrogen and Z.sup.2 is R.sup.4 --S--,Z.sup.3 and Z.sup.4 each are hydrogen or together form a second valence bond, or Z.sup.3 is hydrogen and Z.sup.4 is R.sup.4 --S--, with at least one of the pairs Z.sup.1 -Z.sup.2 and Z.sup.3 -Z.sup.4 representing hydrogen and an R.sup.4 --S-- group, andR.sup.4 is hydrogen or alkyl, alkenyl, aralkyl or acyl with up to 7 carbon atoms, provided that when Z.sup.1 and Z.sup.2 together form a valence bond, or Z.sup.1 represents a hydrogen atom and Z.sup.2 and R.sup.4 --S-- group then R.sup.1 is methyl.
Type:
Grant
Filed:
March 29, 1979
Date of Patent:
August 19, 1980
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt
Inventors:
Sandor Solyom, Lajos Toldy, Katalin Szilagyi nee Farago, Inge Schafer, Eleonora Szondy, Janos Borvendeg, Ilona Hermann nee Szente
Abstract: The packing of a tower or column for heat exchange, material exchange, contacting of two fluids with one another and chemical reaction consisting of a stack of elongated members having two walls inclined to one another and joined at a third wall, the first two walls are each formed with elongated vibratile elements interdigitated with vibratile elements of another packing member so that when the body of packing is traversed by one or more fluids, the vibratile elements are set into vibration.
Abstract: Novel Angiotensin II peptides of the formula:X-Arg-Val-Tyr-Ile-His-Pio-Ywhere X is hydroxyacetyl or .alpha.-hydroxypropyl and Y is leucyl, isoleucyl, alanyl or threonyl or an acid addition salt or a complex thereof are disclosed and a process for the preparation thereof are disclosed having the ability to lower renal hypertension.
Type:
Grant
Filed:
July 11, 1978
Date of Patent:
June 24, 1980
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Lajos Kisfaludy, Gyorgyne Nyeki nee Olga Kuprina, Laszlone Szirmai nee Maria Sarkozi, Egon Karpati, Katalin Gidai, Laszlo Szporny