Patents by Inventor Gyorgy Kalaus

Gyorgy Kalaus has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4329350
    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.
    Type: Grant
    Filed: May 21, 1979
    Date of Patent: May 11, 1982
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
  • Patent number: 4314939
    Abstract: A process for the preparation of 15-hydroxyimino-E-homoeburnane derivatives of the formula (I), ##STR1## wherein X.sup.1 stands for hydrogen or halogen andR is a C.sub.1-6 alkyl group,or acid addition salts and optically active derivatives thereof. These compounds are valuable intermediates of the synthesis of compounds with outstanding biological effects. According to the invention a racemic or optically active 15-hydroxy-E-homoeburnane derivative of the formula (II), ##STR2## is treated, optionally after separating the 15-epimers and/or resolution, with a halogenating agent. The resulting 15-halo-E-homoeburnane derivative of the formula (III), ##STR3## wherein X.sup.2 stands for halogen, is reacted, optionally after separating the 15 epimers and/or resolution, with an alkali nitrite in the presence of an acid, and, if desired, the resulting 15-hydroxyimino-E-homoeburnane derivative of the formula (I) is converted into its acid addition salt and/or resolved.
    Type: Grant
    Filed: July 14, 1980
    Date of Patent: February 9, 1982
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Lajos Dancsi, Tibor Keve, Ferenc Drexler
  • Patent number: 4285950
    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
  • Patent number: 4285865
    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
  • Patent number: 4283401
    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
  • Patent number: 4278682
    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
  • Patent number: 4173642
    Abstract: New pharmacologically active 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 are prepared by reacting 2,3,4,6,7,12-hexahydro-indolo[2,3-a]quinolizine with a compound of the formula CH.sub.2 .dbd.
    Type: Grant
    Filed: December 29, 1977
    Date of Patent: November 6, 1979
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
  • Patent number: 4089856
    Abstract: Racemic and optically active 1-alkyl-1,2,3,4,6,7,12,12b-octahydro-indolo[2,3-a]quinolizines of vasodilatory and haemodynamic effect are disclosed.
    Type: Grant
    Filed: June 23, 1976
    Date of Patent: May 16, 1978
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
  • Patent number: 4057550
    Abstract: New compounds of the general formula (I) ##STR1## wherein R.sub.1 stands for alkyl and R.sub.2 stands for carboxy, a functional carboxy derivative or a group convertible into carboxy group or a functional derivative thereof, have been prepared by reducing a compound of the general formula ##STR2## wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- represents an anion derived from an acid, and optionally subjecting the obtained compound to hydrolysis. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.
    Type: Grant
    Filed: September 17, 1975
    Date of Patent: November 8, 1977
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
  • Patent number: 4057551
    Abstract: New compounds of the general formula (I) ##STR1## wherein R stands for an alkyl group, have been prepared by reducing a compound of the general formula (II) ##STR2## wherein R stands for alkyl, B stands for H.sub.2 O or an X.sup.- anion derived from an acid, and if B is an X.sup.- anion, A represents hydrogen, whereas if B is H.sub.2 O, A represents an electron pair. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.
    Type: Grant
    Filed: September 17, 1975
    Date of Patent: November 8, 1977
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
  • Patent number: 4054571
    Abstract: The invention relates to new eburnamenine derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for an alkyl group,R.sub.2 stands for a carboxy group, a functional carboxy derivative (preferably an ester group) or a group convertable into carboxy group or a functional derivative thereof (preferably cyano group), andX.sup.- is an anion derived from an acid,And the corresponding free bases.These compounds are valuable intermediates of the preparation of eburnamenine derivatives with advantageous therapeutical effects.The above compounds are prepared as follows: a compound of the general formula (II), ##STR2## wherein R.sub.1 has the same meanings as defined above, is reacted with a compound of the general formula (III), ##STR3## wherein R.sub.2 has the same meanings as defined above and Y is halogen, and, if desired, a thus-obtained compound of the general formula (I), wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.
    Type: Grant
    Filed: September 17, 1975
    Date of Patent: October 18, 1977
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajor Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
  • Patent number: 4052404
    Abstract: The invention relates to new indolo-quinolizidine derivatives of the general formula (I) or salts or optically active isomers thereof, ##STR1## wherein R stands for an alkyl group, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AS WELL AS TO A PROCESS FOR THE PREPARATION THEREOF.The new compounds according to the invention possess vasodilatating and hypotensive effects and can be used in the therapy as medicines. The new compounds according to the invention are completely devoid of harmful side-effects.
    Type: Grant
    Filed: November 25, 1975
    Date of Patent: October 4, 1977
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
  • Patent number: 4044012
    Abstract: New compounds of the formula ##STR1## are provided wherein R.sub.1 is hydrogen, and R.sub.2 stands for an alkyl group and optically active enanthiomers and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 25, 1976
    Date of Patent: August 23, 1977
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
  • Patent number: 4036841
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 stands for hydrogen or an acyl group, andR.sub.2 stands for an alkyl group are disclosed.A process for making the above compounds is also disclosed. The compounds are useful as vasodilatating agents for example.
    Type: Grant
    Filed: May 6, 1975
    Date of Patent: July 19, 1977
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny